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Bron, J., C. A. M. van Egmond, A. P. de Jong, A. Pullen, and S. W. de Jong. "Modified release dosage form of isosorbide-5-mononitrate." European Journal of Pharmaceutical Sciences 4 (September 1996): S156. http://dx.doi.org/10.1016/s0928-0987(97)86477-9.
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Murugesan, Senthilkumar, Byran Gowramma, Kaviarasan Lakshmanan, Veera Venkata Satyanarayana Reddy Karri, and Arun Radhakrishnan. "Oral Modified Drug Release Solid Dosage Form with Special Reference to Design; An Overview." Current Drug Research Reviews 12, no. 1 (2020): 16–25. http://dx.doi.org/10.2174/2589977511666191121094520.
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Oral drug delivery is the most widely utilized route of administration among all the routes that have been explored for systemic delivery of drugs via pharmaceutical products of different dosage form and this oral route provides maximum active surface area among all drug delivery system for administration of various drugs. The attractiveness of these dosage forms is due to awareness of toxicity and ineffectiveness of drugs when administered by oral conventional method in the form of tablets and capsules. Usually, conventional dosage form produces wide range of fluctuation in drug concentration in the bloodstream and tissues with consequent undesirable toxicity and poor efficiency. The maintenance of concentration of drug in plasma within therapeutic index is very critical for effective treatment. These factors as well as factors such as repetitive dosing and unpredictable absorption lead to the concept of oral modified drug delivery systems like Sustained release, prolonged release, modified release, extended release. These formulations are used to identify drug delivery systems that are designed to achieve or extend therapeutic effect by continuously releasing medication over an extended period of time after administration of a single dose. This review describes the basic information regarding modified release dosage form like designed to release their medication in controlled manner, criteria for selecting modified release dosage form and factors influencing the dosage and release pattern.
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Lee, Jaemin, Chanwoo Song, Inhwan Noh, Sangbyeong Song, and Yun-Seok Rhee. "Hot-Melt 3D Extrusion for the Fabrication of Customizable Modified-Release Solid Dosage Forms." Pharmaceutics 12, no. 8 (2020): 738. http://dx.doi.org/10.3390/pharmaceutics12080738.
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In this work, modified-release solid dosage forms were fabricated by adjusting geometrical properties of solid dosage forms through hot-melt 3D extrusion (3D HME). Using a 3D printer with air pressure driving HME system, solid dosage forms containing ibuprofen (IBF), polyvinyl pyrrolidone (PVP), and polyethylene glycol (PEG) were printed by simultaneous HME and 3D deposition. Printed solid dosage forms were evaluated for their physicochemical properties, dissolution rates, and floatable behavior. Results revealed that IBF content in the solid dosage form could be individualized by adjusting the volume of solid dosage form. IBF was dispersed as amorphous state with enhanced solubility and dissolution rate in a polymer solid dosage form matrix. Due to absence of a disintegrant, sustained release of IBF from printed solid dosage forms was observed in phosphate buffer at pH 6.8. The dissolution rate of IBF was dependent on geometric properties of the solid dosage form. The dissolution rate of IBF could be modified by merging two different geometries into one solid dosage form. In this study, the 3D HME process showed high reproducibility and accuracy for preparing dosage forms. API dosage and release profile were found to be customizable by modifying or combining 3D modeling.
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Shah, Hiten J., Gunta Subbaiah, Dasharath M. Patel, and Chhagan N. Patel. "In vitro-in vivocorrelation of modified release dosage form of lamotrigine." Biopharmaceutics & Drug Disposition 30, no. 9 (2009): 524–31. http://dx.doi.org/10.1002/bdd.688.
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Pund, Atul, Atishkumar Mundada, Manoj Magar, and Abhijeet Kadam. "Recent Patents on Modified Release Oral Dosage Forms." Journal of Drug Delivery and Therapeutics 11, no. 4-S (2021): 195–211. http://dx.doi.org/10.22270/jddt.v11i4-s.4973.
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Background: Conventional oral dosage forms have limited bioavailability and frequent dosing of the drug is needed to maintain the effective therapeutic concentration in the body. This results in poor patient compliance and fluctuations in the plasma drug levels, especially in the chronic diseases and disorders.
 Objective: To overcome such problems and to enhance the efficiency and bioavailability of the drug, modified drug delivery systems such as extended release delivery systems (controlled release; sustained release) and delayed release delivery systems are developed which can prolong the release and hence action of the drug in the body.
 Methods: Through this review, we throw the light on recent patents and patent applications on modified release systems pertaining to oral dosage forms. The various free patent search databases were used to collect and analyze the information on modified release delivery systems.
 Results: Modified release systems such as extended release and delayed release delivery systems have been found to be of great significance due to their advantages over immediate release dosage forms. These systems are formulated using various approaches, different types of release controlling polymers such as natural, semisynthetic and synthetic polymers and found to avoid the limitations of conventional oral dosage forms.
 Conclusion: Modified drug release systems have potential especially, in case of the chronic diseases, mental health disorders and lifestyle diseases and disorders. These systems have unique commercial advantages which will sustain the interest of both the researchers and the pharmaceutical companies.
 Keywords: Modified release systems, extended release systems, controlled release systems, sustained release systems, delayed release systems, oral dosage forms, multilayer dosage form, multilayered tablets
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Keraliya, Rajesh A., Chirag Patel, Pranav Patel, et al. "Osmotic Drug Delivery System as a Part of Modified Release Dosage Form." ISRN Pharmaceutics 2012 (July 17, 2012): 1–9. http://dx.doi.org/10.5402/2012/528079.
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Conventional drug delivery systems are known to provide an immediate release of drug, in which one can not control the release of the drug and can not maintain effective concentration at the target site for longer time. Controlled drug delivery systems offer spatial control over the drug release. Osmotic pumps are most promising systems for controlled drug delivery. These systems are used for both oral administration and implantation. Osmotic pumps consist of an inner core containing drug and osmogens, coated with a semipermeable membrane. As the core absorbs water, it expands in volume, which pushes the drug solution out through the delivery ports. Osmotic pumps release drug at a rate that is independent of the pH and hydrodynamics of the dissolution medium. The historical development of osmotic systems includes development of the Rose-Nelson pump, the Higuchi-Leeper pumps, the Alzet and Osmet systems, the elementary osmotic pump, and the push-pull system. Recent advances include development of the controlled porosity osmotic pump, and systems based on asymmetric membranes. This paper highlights the principle of osmosis, materials used for fabrication of pumps, types of pumps, advantages, disadvantages, and marketed products of this system.
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DEVI, GAYATRI, MALKIET KAUR, MANJU NAGPAL, et al. "Advanced Dosage Form Design: Role of Modified Natural Gums." Asian Journal of Chemistry 33, no. 1 (2020): 1–9. http://dx.doi.org/10.14233/ajchem.2021.22937.
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Gums are naturally occurring segments in plants, which are cheap and abundant. Natural gums and their derivatives are widely used in a pharmaceutical dosage form. These natural materials possess several advantages over synthetic ones being chemically inert, non-toxic, low cost and biodegradable. However, quick degradation in the body, poor mechanical properties and low solubility are few disadvantages. To overcome these disadvantages, natural gums are modified by applying different chemical modification procedures. The modification of gums is done via various methods such as changing functional groups of gum, cross-linking with ions, grafting with polymers, sulfation, phosphorylation and thiolation. Modification of gums results in some superior properties which can be used in drug delivery applications. For example, change in crystallinity, improved solubility, stability, and improved mechanical properties are of use in development of modified drug delivery systems. Modified gums help to achieve pH dependent delivery and sustained delivery along with improved release kinetics of the drug. Current review covers various types of modifications in general and research literature on various medications of different gums (locust bean gum, cashew gum, moringa gum, xanthan gum, etc.). The modified natural gums and their derivatives can be the prospective carriers in the controlled drug delivery of drugs.
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Babu, P. "In vitro–In vivo Correlation Studies of Modified Release Solifenacin Tablet Dosage Form." Journal of Scientific Research and Reports 3, no. 14 (2014): 1905–15. http://dx.doi.org/10.9734/jsrr/2014/9951.
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Ritschel, Wolfgang A., and Mukul A. Agrawal. "Physiologically based novel peroral modified release drug delivery system: Self-destructing hydrogel piston-pump." Ciencia e Investigación 6, no. 2 (2003): 24–29. http://dx.doi.org/10.15381/ci.v6i2.3439.
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Peroral modified drug delivery systems on the market release fue drug by either 0-order, 1º-order, square root oftime or mixed rate. This means that the drugis released mto the gastrointestinallumenin amounts being either constantper unit of time or decreasingwith time. However, physiologically absorption from the GI lumen gets slower and more difficult past the small intestme. A novel drug delivery system is described far 24 horus drug delivery which follows approximate 0-orden release throughout the small intestine, but releases increasing amounts of drug once in the colon ta compensate for increasingly more difficult absorption. Nearly constant steady state drug plasma concentrations are achieved . The novel drug delivery system is a two layered dosage form with an immediate release layer and a modified release layer. The latter ene is a hydrogel piston pump comprised of a drug core layer and a hydrogel swelling layer, embedded into a semipermeable shell by compression coating. The upper site of the shell has a release channel in the center.
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Mahaparale, PareshRamesh, and BhanudasShankarrao Kuchekar. "Development and evaluation of modified release wax matrix tablet dosage form for tramadol hydrochloride." Asian Journal of Pharmaceutics 9, no. 2 (2015): 102. http://dx.doi.org/10.4103/0973-8398.154701.
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Romodanovsky, D. P., N. N. Eremenko, and D. V. Goryachev. "Regulatory Requirements of the European Medicines Agency for Evaluation of Bioequivalence of Modified-release Medicinal Products." Bulletin of the Scientific Centre for Expert Evaluation of Medicinal Products 9, no. 1 (2019): 28–33. http://dx.doi.org/10.30895/1991-2919-2019-9-1-28-33.
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There are no specific requirements and recommendations in the Russian Federation for evaluation of bioequivalence of modified-release medicinal products. Until recently, modified-release products were regulated in a similar manner as immediate-release products, which is unacceptable considering the active ingredient release profile and its pharmacokinetics. The modified release characteristics require a more complex approach to the assessment of equivalence of generic medicines as compared with the reference product. The number of parameters to be assessed and the scope of testing depend on many factors (release mechanism, specific features of the dosage form, linearity of pharmacokinetics, potential for ingredient accumulation, dependence on food intake, dose-dumping effects, and the number of dosage strengths to be registered). The aim of this paper was to develop recommendations for the national procedure of modified-release products authorisation based on the analysis of international regulatory experience in this field. The paper reviews the current European Medicines Agency (EMA) guidelines on evaluation of bioequivalence of generic modified-release dosage forms for oral use that were taken as a basis for the development of Eurasian Economic Union regulations on bioequivalence assessment. The analysis of the above-mentioned documents made it possible to develop recommendations for the national procedure of modified-release products authorisation. In the case of modified-release products for oral use it is recommended to perform bioequivalence studies by comparing the test product with the reference product. The authors developed a procedural algorithm for bioequivalence studies of modified-release medicinal products.
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Ostrowski, Michał, Ewa Wilkowska, and Tomasz Bączek. "Impact of pharmaceutical dosage form on stability and dissolution of roxithromycin." Open Medicine 5, no. 1 (2010): 83–90. http://dx.doi.org/10.2478/s11536-009-0113-7.
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AbstractThe behavior of dispersible tablets containing enteric-coated pellets and oral suspension, both containing roxithromycin, was investigated using dissolution tests in different media. The dissolution test was performed under different pH conditions. For both dosage forms investigated, the test was conducted at pH 1.2, 4.5, and 6.8. Additionally, for dispersible tablets, the test involving increasing pH was performed at pH 1.2 (acid stage) and afterwards at pH 6.8 (buffer stage). The extent of dissolution was measured using high-performance liquid chromatography (HPLC). In all cases tested, roxithromycin underwent rapid degradation at pH 1.2. Dispersible tablets displayed the features of modified release preparations with a non-complete dissolution during the test times in all media. Conversely, the oral suspension behaved as an immediate release preparation, with degradation at pH 1.2. However, the dissolution of the oral suspension at pH 4.5 and 6.8 was rapid and complete. The role of enteric-coated pellets is to mask the bitter taste of the active substance upon administration. However, the coating showed lack of resistance to media at pH 1.2. Therefore, dispersible tablets containing enteric-coated pellets are not pharmaceutically equivalent to the immediate-release oral suspension.
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Almeida, Nilsa Maria Galvão, Renata Lima, Thaís Francine Ribeiro Alves, Márcia de Araújo Rebelo, Patrícia Severino, and Marco Vinícius Chaud. "A novel dosage form for buccal administration of bupropion." Brazilian Journal of Pharmaceutical Sciences 51, no. 1 (2015): 91–100. http://dx.doi.org/10.1590/s1984-82502015000100010.
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Bupropion is an antidepressant used in the treatment of smoking. The purpose of this study was to prepare controlled-release hydrogel films for buccal administration of bupropion and investigate its physicochemical and cytotoxic properties. The films were prepared from ultrapure sodium carboxymethylcellulose, hydroxypropylmethylcellulose K4M, and medium-viscosity chitosan. Evaluation of film physicochemical characteristics was based on scanning electron microscopy, bupropion content, mechanical strength (burst strength, relaxation, resilience, and traction), and cytotoxicity. Bupropion content in bilayer films was 121 mg per 9 cm2. The presence of bupropion modified film mechanical strength, but did not compromise the use of this pharmaceutical form. As shown by the cytotoxicity results, films containing bupropion did not cause cellular damage. Bupropion administration in the form of hydrogel films is a potentially useful alternative in the treatment of smoking.
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Al-Hashimi, Nihad, Nazish Begg, Raid Alany, Hany Hassanin, and Amr Elshaer. "Oral Modified Release Multiple-Unit Particulate Systems: Compressed Pellets, Microparticles and Nanoparticles." Pharmaceutics 10, no. 4 (2018): 176. http://dx.doi.org/10.3390/pharmaceutics10040176.
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Oral modified-release multiparticulate dosage forms, which are also referred to as oral multiple-unit particulate systems, are becoming increasingly popular for oral drug delivery applications. The compaction of polymer-coated multiparticulates into tablets to produce a sustained-release dosage form is preferred over hard gelatin capsules. Moreover, multiparticulate tablets are a promising solution to chronic conditions, patients’ adherence, and swallowing difficulties if incorporated into orodispersible matrices. Nonetheless, the compaction of multiparticulates often damages the functional polymer coat, which results in a rapid release of the drug substance and the subsequent loss of sustained-release properties. This review brings to the forefront key formulation variables that are likely to influence the compaction of coated multiparticulates into sustained-release tablets. It focusses on the tabletting of coated drug-loaded pellets, microparticles, and nanoparticles with a designated section on each. Furthermore, it explores the various approaches that are used to evaluate the compaction behaviour of particulate systems.
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Babu, P., S. Parveen, K. Chandrasekar, and B. Challa. "In vitro- In vivo Correlation Studies of Modified Release Tolterodine Tablet Dosage form in Rabbits." British Journal of Pharmaceutical Research 4, no. 15 (2014): 1861–72. http://dx.doi.org/10.9734/bjpr/2014/9950.
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Manyarara, Tapiwa E., Star Khoza, Admire Dube, and Chiedza C. Maponga. "Formulation and characterization of a paediatric nanoemulsion dosage form with modified oral drug delivery system for improved dissolution rate of nevirapine." MRS Advances 3, no. 37 (2018): 2203–19. http://dx.doi.org/10.1557/adv.2018.320.
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ABSTRACTBackground: The development of appropriate dosage forms for paediatric antiretroviral therapy is key for improved therapeutic outcomes in children. The focus of this study was to improve solubility, dissolution rate, drug release and maintain high drug permeability.Methodology: A nanoemulsion was prepared using emulsion inversion point and evaluated. The nanoemulsion had nevirapine (3% w/w). In vitro drug release studies were performed using dialysis membrane. Permeability studies using the Caco-2 cell model were performed for the formulation.Results: The optimized nevirapine nanoemulsion had a mean droplet size of 36.09±12.27nm, low pdI of 0.598 and zeta potential of -7.87±4.35mV. At pH 2, the nanoemulsion released 76 ± 2 % of nevirapine within 2 h, while at pH 6.4 value representing the small intestine, amount of nevirapine released was 41.6± 4 %. The permeability rate of the nevirapine nanoemulsion was 30.02 x 10-6cm/s and higher than that of propranolol. Efflux ratio was 0.02 indicating low chance of drug efflux occurring.Conclusion: The results showed that a modified liquid drug release formulations of nevirapine could improve rate of dissolution and maintain high permeability and low drug efflux improving bioavailability of nevirapine in vivo.
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Mahboob, Muhammad Bilal Hassan, Tehseen Riaz, Muhammad Jamshaid, Irfan Bashir, and Saqiba Zulfiqar. "Oral Films: A Comprehensive Review." International Current Pharmaceutical Journal 5, no. 12 (2016): 111–17. http://dx.doi.org/10.3329/icpj.v5i12.30413.
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In the late 1970s, rapid disintegrating drug delivery system was developed as an alternative to capsules, tablets and syrups for geriatric and pediatric patients having problems in swallowing. To overcome the need, number of orally disintegrating tablets which disintegrate within one minute in mouth without chewing or drinking water were commercialized. Then later, oral drug delivery technology had been improved from conventional dosage form to modified release dosage form and developed recently rapid disintegrating films rather than oral disintegrating tablets. Oral disintegrating film or strips containing water dissolving polymer retain the dosage form to be quickly hydrated by saliva, adhere to mucosa, and disintegrate within a few seconds, dissolve and releases medication for oro-mucosal absorption when placed in mouth. Oral film technology is the alternative route with first pass metabolism. This review give a comprehensive detail of materials used in ODF, manufacturing process, evaluation tests and marketed products.Mahboob et al., International Current Pharmaceutical Journal, November 2016, 5(12): 111-117http://www.icpjonline.com/documents/Vol5Issue12/03.pdf
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Joshi, Sameer, Rajnish Sahu, Vida A. Dennis, and Shree R. Singh. "Nanofiller-Enhanced Soft Non-Gelatin Alginate Capsules for Modified Drug Delivery." Pharmaceuticals 14, no. 4 (2021): 355. http://dx.doi.org/10.3390/ph14040355.
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Capsules are one of the major solid dosage forms available in a variety of compositions and shapes. Developments in this dosage form are not new, but the production of non-gelatin capsules is a recent trend. In pharmaceutical as well as other biomedical research, alginate has great versatility. On the other hand, the use of inorganic material to enhance material strength is a common research topic in tissue engineering. The research presented here is a combination of qualities of alginate and montmorillonite (MMT). These two materials were used in this research to produce a soft non-gelatin modified-release capsule. Moreover, the research describes a facile benchtop production of these capsules. The produced capsules were critically analyzed for their appearance confirming resemblance with marketed capsules, functionality in terms of drug encapsulation, as well as release and durability.
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Herman, Barry K., Thomas R. King, Judith C. Kando, and Antonio Pardo. "31 A Modified-Release Drug Delivery Technology Containing Amphetamine-Ion Exchange Complexes." CNS Spectrums 24, no. 1 (2019): 191. http://dx.doi.org/10.1017/s1092852919000257.
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AbstractThe proprietary, immediate and extended drug delivery technologyLiquiXR® utilizes an ion-exchange resin that complexes with amphetamine or any active moiety that can be protonated and is water-soluble. The active ingredient of the drug product forms a complex with an ion exchange polymer of the resin resulting in micron-sized particles. A portion of these particles is then coated with an aqueous, pH-independent polymer designed to provide sustained release of drug product. The polymer coating applied to the ion-exchange resin particles is of varying thickness, allowing for extended release of active drug while uncoated particles provide for immediate release of drug.The micron-sized particles lend themselves to being formulated into an appropriate dosage form: solid/chewable tablet, liquid suspension, orally disintegrating tablet, film, or capsules. Active ingredient of drug product is subsequently released from the dosage form in millions of particles, with release driven by a combination of ion exchange and diffusion. After drug release, the ion-exchange resin particles are excreted in the feces.The release characteristics of LiquiXR allow for customized, sustained release of active drug ∼24hours post dose. Mechanistically, drug particles enter the gastrointestinal (GI) tract. As positively-charged ions from GI fluids diffuse across the coating, it displaces drug ions from product and they diffuse through the coating and into the GI fluids for absorption. As the coating is of variable thickness, some drug product takes longer to diffuse and absorb, providing for the delayed drug release characteristics.The LiquiXR drug delivery technology has already been successfully utilized in the development of treatment options (liquid suspension and chewable tablet) that offer rapid absorption and sustained plasma levels after once-daily dosing. LiquiXR is utilized in Dyanavel® XR (amphetamine extended-release oral suspension; AMPH EROS), which is indicated for treatment of ADHD. It comprises 2.5mg/mL amphetamine base and uses LiquiXR technology to provide an immediate release component followed by an extended-release profile.Efficacy of AMPH EROS was established in children 6 to 12 yr in a Phase 3, placebo-controlled laboratory classroom study. In that study, ADHD symptoms in children on an individually optimized dose of amphetamine (range 10–20mg/day) were statistically significantly improved compared with symptoms in children treated with placebo. For children treated with AMPH EROS, onset of effect was demonstrated at 1hour after dosing, and efficacy was observed through 13hr post-dose. The effect size (ES) was comparable to ES demonstrated for other psychostimulants tested in studies using a similar design. The efficacy data reported for AMPH EROS provides an excellent example of the potential utility and clinical application for other active drug products requiring an immediate and extended release profile.Funding Acknowledgements: Support provided by Tris Pharma, Inc.
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Ilić, Marija, Ivan Kovačević, and Jelena Parojčić. "Deciphering nifedipine in vivo delivery from modified release dosage forms: Identification of food effect." Acta Pharmaceutica 65, no. 4 (2015): 427–41. http://dx.doi.org/10.1515/acph-2015-0039.
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Abstract With the increased reliance on in vitro dissolution testing as an indicator of in vivo drug behavior and the trend towards the in silico modeling of dosage form performance, the need for bioperformance dissolution methodology development has been enhanced. Determination of the in vivo drug delivery profile is essential for the bioperformance dissolution test development and in vitro/in vivo correlation modeling, as well as the understanding of absorption mechanisms. The aim of this study was to compare different methods in terms of their usefulness and applicability in deciphering in vivo delivery of nifedipine administered in modified release dosage forms. A detailed survey of publications on nifedipine pharmacokinetics was done and used to identify the magnitude of food effect. In vitro dissolution testing was performed under various experimental conditions. Obtained results indicate the potential for using the developed in silico model coupled with discriminative in vitro dissolution data for identification of the in vivo drug product behavior
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Herman, Barry K., Thomas R. King, Judith C. Kando, and Antonio Pardo. "89 A Novel, Modified-Release Drug Delivery Technology Containing Amphetamine-Ion Exchange Complexes." CNS Spectrums 24, no. 1 (2019): 220. http://dx.doi.org/10.1017/s1092852919000671.
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AbstractThe proprietary immediate and extended drug delivery technology LiquiXR™ utilizes an ion-exchange resin that complexes with amphetamine or any other active moiety that can be protonated and is water-soluble. The active drug product forms a complex with ion-exchange polymers contained in the resin, which is then formed into micron-sized particles. Some of these particles are coated with an aqueous, pH-independent polymer designed to provide immediate or sustained release of active drug product. The polymer coating applied to the ion-exchange resin particles is of varying thickness, allowing for programmed, extended release of active drug product. Solid, coating-free particles provide for immediate release of active drug product.The micron-sized particles are formulated into an appropriate dosage form (solid or chewable tablet, liquid suspension, orally disintegrating tablet, film, or capsules). Active drug product is subsequently released from the dosage form in millions of particles, with the release driven by a combination of ion exchange and diffusion. After drug release, the ion-exchange resin is excreted in the feces.The release characteristics of LiquiXR™ are programmable and allow for a customized, sustained release of active drug product for up to 24hours post-dose. Mechanistically, drug particles enter the gastrointestinal tract. As positively-charged ions from gastrointestinal (GI) fluids diffuse across the coating, ionically-charged drug product diffuses through the coating and into the GI fluids for absorption. As the coating is of variable thickness, some drug product takes longer to diffuse and absorb, providing for the programmable delayed drug release characteristic.The LiquiXR™ drug delivery technology is utilized in Dyanavel® XR (amphetamine extended-release oral suspension; AMPH EROS), which is indicated for the treatment of attention-deficit hyperactivity disorder. It comprises 2.5mg/mL amphetamine base complexed with LiquiXR technology to provide an immediate release component followed by an extended-release profile. The efficacy of AMPH EROS was established in children ages 6 to 12 years in a Phase 3, placebo-controlled laboratory classroom study. In that study, attention-deficit/hyperactivity disorder (ADHD) symptoms in children on an individually optimized dose of amphetamine (range 10–20mg/day) were statistically significantly improved compared with symptoms in children treated with placebo. For children treated with AMPH EROS, onset of effect was demonstrated at 1hour after dosing, and efficacy was observed through 13hours post-dose. The effect size was comparable to effect sizes demonstrated for other psychostimulants tested in studies using a similar design. The efficacy data reported for AMPH EROS provides an excellent example of the potential utility and clinical application for other active drug products requiring an immediate release and extended release profile.Funding Acknowledgements: This work was funded by Tris Pharma, Inc.
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Dong, QianQian, Xiao Zheng, MiaoMiao Zhou, et al. "Engineering Size and Structure of Particles in Novel Modified-Release Delivery Systems." Journal of Pharmacy & Pharmaceutical Sciences 22 (April 24, 2019): 150–70. http://dx.doi.org/10.18433/jpps30253.
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Particle engineering has become a hot topic in the field of modified-release delivery systems during last decades. It has a wide range of pharmaceutical applications and is a bridge linking between drugs and drug delivery systems. Particles are an important part of many dosage forms and viewed as a carrier of drugs. Their size, shape, crystalline form, and structure directly affect the stability and releasing pattern of drugs. Engineering size or modifying particles by forming porous, core-shell, or skeleton structures can realize the development and utilization of functionally modified release systems (including fast-release systems, sustained-release systems, and targeted-release systems). However, there are certain problems in the practical application, such as bitter taste and coating damage. Combining with some polymer or lipid materials to form core-shell or embedded structures is considered as the key to taste masking. And, using cushioning agents is proven to be effective in preserving the integrity of the functional coating film of multiparticulates during tableting. To sum up, this review, from a particle engineering point, expounds the influence of different factors on the functionality of particles and offers some useful comments and suggestions for industry personnel.
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Gupta, Brahma Prakash, Navneet Thakur, Nishi P. Jain, Jitendra Banweer, and Surendra Jain. "Osmotically Controlled Drug Delivery System with Associated Drugs." Journal of Pharmacy & Pharmaceutical Sciences 13, no. 4 (2010): 571. http://dx.doi.org/10.18433/j38w25.
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Conventional drug delivery systems have slight control over their drug release and almost no control over the effective concentration at the target site. This kind of dosing pattern may result in constantly changing, unpredictable plasma concentrations. Drugs can be delivered in a controlled pattern over a long period of time by the controlled or modified release drug delivery systems. They include dosage forms for oral and transdermal administration as well as injectable and implantable systems. For most of drugs, oral route remains as the most acceptable route of administration. Certain molecules may have low oral bioavailability because of solubility or permeability limitations. Development of an extended release dosage form also requires reasonable absorption throughout the gastro-intestinal tract (GIT). Among the available techniques to improve the bioavailability of these drugs fabrication of osmotic drug delivery system is the most appropriate one. Osmotic drug delivery systems release the drug with the zero order kinetics which does not depend on the initial concentration and the physiological factors of GIT. This review brings out new technologies, fabrication and recent clinical research in osmotic drug delivery.
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Uekama, Kaneto, Kazutaka Matsubara, Kentaro Abe, Yasuhide Horiuchi, Fumitoshi Hirayama та Nobuo Suzuki. "Design and In Vitro Evaluation of Slow-Release Dosage Form of Pretanide: Utility of β-Cyclodextrin:Cellulose Derivative Combination as a Modified-Release Drug Carrier". Journal of Pharmaceutical Sciences 79, № 3 (1990): 244–48. http://dx.doi.org/10.1002/jps.2600790314.
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Shah, Sunil, Dilip Shukla, and Harish Pandey. "Formulation Optimization of Polyox Based Modified Release Drug Delivery System." Journal of Drug Delivery and Therapeutics 9, no. 4-s (2019): 551–61. http://dx.doi.org/10.22270/jddt.v9i4-s.3383.
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Polyethylene Oxide (PEOs) offer specific advantages to be used in pharmaceutical products as release modifiers by forming a hydrogel around the dosage form in aqueous environment causing the drug to follow a diffusional path before releasing into the media. The strength of the hydrogel governs the release retardation capacity of the PEO system. The objective of this dissertation work was to use the Design of Experiments methodology to develop and optimize a PEO based modified release formulation of a highly water-soluble drug like Metoprolol succinate. The effect of the different viscosity grade PEOs, their concentration with respect to the drug, combination of two different viscosity grades, % drug content in the formulation and the use of water soluble / insoluble fillers on the dissolution of metoprolol succinate was studied. The critical formulation parameters namely PEO concentration and % drug content were chosen as input factors and dissolution at 1, 4, 8 and 20 hours was recorded as responses to carry out optimization using the DOE approach. The results obtained after statistical treatment of data provided a design space that can be used for achieving the desired formulation profile. The model has been validated to predict the effect of the input factors (PEO type and concentration and % drug content) on the responses (in vitro dissolution).
 Keywords: Polyethylene Oxide, Modified Release Drug Delivery System, Metoprolol
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Nesterenko, V. G., R. N. Bolgarin, B. A. Rudoy, et al. "Development of a Gastro-retentive Dosage Form of a New Promising Anti-tuberculosis Drug Macozinone." Drug development & registration 10, no. 3 (2021): 55–69. http://dx.doi.org/10.33380/2305-2066-2021-10-3-55-69.
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Introduction. Due to increase in the frequency of detecting cases of tuberculosis caused by strains of mycobacteria with resistance not only to traditional, but also recently introduced into clinical circulation anti-tuberculosis drugs, it is urgent to search for and develop new drugs that can be effective against multidrug-resistant (MDR-TB) and extensively drug resistant (XDR-TB) strains. One of the most promising classes of such compounds are fluorine derivatives of benzothiazinones, and particularly compound PBTZ169 (INN macozinone). This antibiotic has a high specificity against mycobacteria tuberculosis (M. tuberculosis), inhibiting one of the key enzymes of cell wall synthesis. However, macozinone as an active pharmaceutical ingredient has significant features of physical and chemical properties that hinder the development of oral dosage forms based on it. It is classified as class IV by BCS and is characterized by a very low solubility and lipophilicity, a pronounced dependence of dissolution rate on the pH of the medium, and very low bioavailability when taken orally.Aim. To substantiate the target profile, critical quality attributes and to develop a prototype of an oral dosage form with modified release of macozinone, allowing to maximize its pharmacological activity.Materials and methods. Using pharmaceutical substance macozinone hydrochloride and various excipients, experimental tablets with a dosage of 500 mg macozinone were developed. The influence of the composition of the media and the added excipients on the solubility of macozinone in various biorelevant media, the degree of swelling in the liquid and the degree of mucoadhesion of the experimental tablets to the mucus of the pig stomach were evaluated. The HPLC method was used to evaluate the kinetics of the release of the active substance.Results and discussion. In this work, the expediency of creating macozinone-containing gastro-retentive dosage forms with a slow release of the active substance, the delay mechanism of which is provided by swelling and increased adhesion to the gastric mucosa, has been substantiated. Various tablet samples were experimentally tested in which the modification of the release of the active substance and the degree of swelling and mucoadhesion were varied by introducing various excipients into the formulations, including known swelling and bioadhesive matrix agents.Conclusion. According to the results of the experiments, samples of high-dose (500 mg) swellable and mucoadhesive tablets created by the technology of two-stage granulation with the inclusion of macozinone - hydroxypropyl-beta-cyclodextrin mixtures in the primary granules and introduction of combinations of soluble and insoluble hydrophilic matrix agents into the intergranular space were recognized as the most promising for subsequent pharmacokinetic studies.
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Fukuhara, Yoshiki, Yshihiro Ohzuno, Takayuki Takei, and Masahiro Yoshida. "Effect of Alkyl Chain Length on Adsorption and Release of Hydrophobic Drug to/from Hydrophobically-modified Gelatin Hydrogel." MATEC Web of Conferences 333 (2021): 11008. http://dx.doi.org/10.1051/matecconf/202133311008.
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Hydrogels have become popular as drug carriers. Controlled release of the drugs from hydrogels can reduce dosage, inducing prevention of side effects. However, the hydrophilicity of hydrogels interferes with controlled release of hydrophobic drugs such as anticancer agents or antibiotics. In this study, we developed hydrophobically-modified gelatin (HMG) hydrogel, which was cross-linked only by hydrophobic interaction. HMG does not require toxic chemical cross-linkers to form hydrogel. In addition, the HMG hydrogel has hydrophobic chambers in its structure which hydrophobic drugs can adsorb to and desorb from. In order to control the amount of hydrophobic drugs adsorbed into the hydrogel, hydrophobic alkyl chains with different lengths (C4-C12) were incorporated into gelatin molecules. Uranine was used as a model for hydrophobic drugs. The adsorption test exhibited that the amount of uranine adsorbed in HMG hydrogels could be controlled by varying hydrophobic alkyl chain length and that the drug could be released in a controlled manner. These results show that HMG hydrogels are promising carriers of hydrophobic drugs.
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Fukuhara, Yoshiki, Yshihiro Ohzuno, Takayuki Takei, and Masahiro Yoshida. "Effect of Alkyl Chain Length on Adsorption and Release of Hydrophobic Drug to/from Hydrophobically-modified Gelatin Hydrogel." MATEC Web of Conferences 333 (2021): 11008. http://dx.doi.org/10.1051/matecconf/202133311008.
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Hydrogels have become popular as drug carriers. Controlled release of the drugs from hydrogels can reduce dosage, inducing prevention of side effects. However, the hydrophilicity of hydrogels interferes with controlled release of hydrophobic drugs such as anticancer agents or antibiotics. In this study, we developed hydrophobically-modified gelatin (HMG) hydrogel, which was cross-linked only by hydrophobic interaction. HMG does not require toxic chemical cross-linkers to form hydrogel. In addition, the HMG hydrogel has hydrophobic chambers in its structure which hydrophobic drugs can adsorb to and desorb from. In order to control the amount of hydrophobic drugs adsorbed into the hydrogel, hydrophobic alkyl chains with different lengths (C4-C12) were incorporated into gelatin molecules. Uranine was used as a model for hydrophobic drugs. The adsorption test exhibited that the amount of uranine adsorbed in HMG hydrogels could be controlled by varying hydrophobic alkyl chain length and that the drug could be released in a controlled manner. These results show that HMG hydrogels are promising carriers of hydrophobic drugs.
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Haznar-Garbacz, Dorota, Ewa Kaminska, Daniel Zakowiecki, et al. "Melts of Octaacetyl Sucrose as Oral-Modified Release Dosage Forms for Delivery of Poorly Soluble Compound in Stable Amorphous Form." AAPS PharmSciTech 19, no. 2 (2017): 951–60. http://dx.doi.org/10.1208/s12249-017-0912-0.
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Boateng-Marfo, Yaa, Yuancai Dong, Wai Kiong Ng, and Hai-Shu Lin. "Artemether-Loaded Zein Nanoparticles: An Innovative Intravenous Dosage Form for the Management of Severe Malaria." International Journal of Molecular Sciences 22, no. 3 (2021): 1141. http://dx.doi.org/10.3390/ijms22031141.
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Artemether, an artemisinin derivative, is used in the management of life-threatening severe malaria. This study aimed to develop an intravenous dosage form of artemether using nanotechnology. Artemether-loaded zein nanoparticles were prepared by modified antisolvent precipitation using sodium caseinate as a stabilizer. Subsequently, the physicochemical properties of the nanoparticles were characterized; the in vitro hemolytic property was examined with red blood cells, while the pharmacokinetic profile was evaluated in Sprague–Dawley rats after intravenous administration. The artemether-loaded zein nanoparticles were found to display good encapsulation efficiency, excellent physical stability and offer an in vitro extended-release property. Interestingly, encapsulation of artemether into zein nanoparticles substantially suppressed hemolysis, a common clinical phenomenon occurring after artemisinin-based antimalarial therapy. Upon intravenous administration, artemether-loaded zein nanoparticles extended the mean residence time of artemether by ~80% in comparison to the free artemether formulation (82.9 ± 15.2 versus 45.6 ± 16.4 min, p < 0.01), suggesting that the nanoparticles may prolong the therapeutic duration and reduce the dosing frequency in a clinical setting. In conclusion, intravenous delivery of artemether by artemether-loaded zein nanoparticles appears to be a promising therapeutic option for severe malaria.
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Sai Chebrolu, Tejasvini, Lalit Kumar, and Ruchi Verma. "Lacidipine: review of analytical methods developed for pharmaceutical dosage forms and biological fluids." Bioanalysis 13, no. 12 (2021): 1011–24. http://dx.doi.org/10.4155/bio-2021-0024.
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Lacidipine (LAC) is a calcium antagonist used in the treatment of hypertension. It is a lipophilic drug containing dihydropyridine ring that is responsible for the activity. This review article gives an overview of various analytical techniques proposed for the determination of LAC in pharmaceutical dosage forms, in pure form, in biological fluids and to determine characteristics of LAC in modified release dosage forms. Ultra violet/visible spectrophotometric, spectroflourimetric, high performance liquid chromatography, high performance thin layer chromatography, electro-analytical, bioanalytical and miscellaneous methods such as microbiological assay, X-ray diffraction, differential scanning calorimetry, were discussed. Various parameters such as system suitability, selectivity, linearity, precision, accuracy, limit of detection, limit of quantification and robustness have been discussed for the employed methods.
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Jain, Abhishek K., and Geeta K. Patel. "FORMULATION AND EVALUATION OF MODIFIED RELEASE TRI-LAYERED TABLET USING A FIXED DOSE COMBINATION OF METFORMIN HCL AND VILDAGLIPTIN." International Research Journal of Pharmacy 11, no. 11 (2020): 54–67. http://dx.doi.org/10.7897/2230-8407.111198.
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The aim of present investigation is to formulate the tri-layered tablet of an Anti-Hyperglycaemic drug comprising Metformin HCl as sustained release layer and Vildagliptin as an immediate release layer in a fixed dose combination along with a fast dissolving intermediate layer or barrier layer in between the two layers just like a sandwich. Vildagliptin is well-known for its instability in presence of Metformin HCl. Hence, Vildagliptin degrades in formulation of single unit dosage form. The in vitro release layer of Metformin HCl was prepared using combination of sustained release polymer HPMC K100M & HPMC K4M and binder used in formulation is Povidone K90 which was prolonged up to 10 - 12 hours. The In-vitro release of Vildagliptin is rapid from tablet and showed highest drug release of more than 90% in 30 Minutes. Final formulation was tested for accelerated stability study. Intermediate barrier layer was optimised using Lactose Monohydrate and Microcrystalline cellulose as a diluents and Croscarmellose sodium as a disintegrant. The disintegration time of tablet into two halves for final formulation was 51 seconds. Combination of lactose monohydrate and microcrystalline cellulose as well as thickness of the intermediate layer was found important to achieve quick disintegration.
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Aleksovski, Aleksandar, Chris Vervaet, and Rok Dreu. "Hot-melt extrusion and prilling as contemporary and promising techniques in the solvent free production of solid oral dosage forms, based on solid dispersions." Macedonian Pharmaceutical Bulletin 62, no. 1 (2016): 3–24. http://dx.doi.org/10.33320/maced.pharm.bull.2016.62.01.001.
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Hot melt extrusion and prilling are gaining importance as solvent free and continuous techniques in the production of solid oral dosage forms with added value, by incorporating active compound in a molten carrier which is further solidified to form solid dispersion. This article reviews these two techniques in terms of understanding process basics, equipment characteristics, required properties of processed materials and application of the processes for development of solid oral dosage forms. Studies revealed that both hot-melt extrusion and prilling are regarded as simple, robust and continuous methods for processing different types of materials and production of solid dosage forms based on solid matrices. However, understanding of their concepts and requirements together with careful material selection is crucial for stable material processing and obtaining stable products of high-quality. Hot-melt extrusion proved to be a suitable method for production of modified release dosage forms, taste masked dosage forms and dosage forms offering improved drug dissolution rate and solubility. Prilling till now has been successfully applied just in the production of multiple unit drug delivery systems for immediate and sustained drug delivery. Further studies on product development and process understanding are required for full implementation of prilling in the pharmaceutical field.
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Mandpe, Pankaj, Bala Prabhakar, and Pravin Shende. "Potential of Mirabegron and its Extended-release Formulations for the Treatment of Overactive Bladder Syndrome." Current Drug Metabolism 21, no. 2 (2020): 79–88. http://dx.doi.org/10.2174/1389200221666200425211139.
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Background: Overactive bladder syndrome is a broadly occurring urological disorder with a distressing impact on the quality of life. The commonly used antimuscarinic drugs show poor patient compliance because of unsatisfactory potency, tolerability and high occurrence of adverse effects such as dry mouth, blurred vision, constipation, dizziness etc. Mirabegron is the first approved β3-adrenoreceptor agonist, used as mono or in combination therapies for overactive bladder syndrome. Objective: The present review provides an insight into the mechanism, pharmacokinetics, toxicokinetics, clinical trials and the development of various conventional and modified-release dosage forms of mirabegron for the treatment of overactive bladder syndrome. Results: The clinical trials of phase II and phase III of mirabegron demonstrated symptomatic relief from the overactive bladder without disturbing the micturition cycle. To date, mirabegron showed promising results for safety, tolerability and efficacy in patients with overactive bladder syndrome. The modified-release tablet dosage form of mirabegron appear to be a proficient and suitable replacement for antimuscarinics and revealed the tremendous potential to overcome the adverse effects of conventional antimuscarinic drugs like Oxybutyline chloride ER, Detrol LA, VESIcare, etc. Conclusion: Mirabegron shows a distinct mode of action, i.e., targeting β3-adrenoreceptors and improving bladder storage without altering void contractions. The limited side effects, high safety, efficacy and tolerability of mirabegron present an adequate substitute to antimuscarinics. However, long-term analysis and clinical studies are prerequisites for assessing the safety, tolerability and efficacy profile of mirabegron.
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Santosh Kumar, Rada, and K. P. R. Chowdary. "Formulation and optimization of carbamazepine floating tablets by 23 - factorial design employing Starch-Urea-Borate: A new floating polymer." Journal of Drug Delivery and Therapeutics 9, no. 2 (2019): 285–95. http://dx.doi.org/10.22270/jddt.v9i2.2576.
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Several approaches are currently used to retain the dosage form in the stomach. These include bioadhesive systems, swelling and expanding systems, floating systems and other delayed gastric emptying devices. The principle of floating tablets offers a simple and practical approach to achieve increased gastric residence time to enhance the bioavailability and to obtain controlled release. Floating tablets are designed based on gas generating principle. Design of floating tablets needs a strong matrix forming polymer. Though several polymers are available for floating tablets, there is a continued need to develop new, effective and efficient polymers for controlled release floating tablets. The major objective of the investigation is to evaluate starch-urea-borate, a new modified starch as a floating matrix former in the design of controlled release floating tablets.
 Keywords: Optimisation, Carbamazepine, Starch-Urea-Borate, Floating Tablets
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WANG, ZHENG, TAKASHI HORIKAWA, FUMITOSHI HIRAYAMA та KANETO UEKAMA. "Design and In-vitro Evaluation of a Modified-release Oral Dosage Form of Nifedipine by Hybridization of Hydroxypropyl-β-cyclodextrin and Hydroxypropylcellulose". Journal of Pharmacy and Pharmacology 45, № 11 (1993): 942–46. http://dx.doi.org/10.1111/j.2042-7158.1993.tb05631.x.
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Venkateswara Rao, Korlapati, and V. V. Venkatachalam. "Recent Advances in Gastro-Retentive Drug Delivery Systems." International Journal of Pharmaceutical Sciences and Nanotechnology 9, no. 3 (2016): 3221–54. http://dx.doi.org/10.37285/ijpsn.2016.9.3.1.
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Controlled gastric retention of solid dosage form may be achieved by the mechanisms of floatation, muco-adhesion, sedimentation, expansion or by a modified shaped system. The purpose of this paper is to review the recent literature and current technology used in the development of gastroretentive drug delivery systems. Oral sustained release gastroretentive dosage forms offer many advantages for drugs having absorption from upper gastrointestinal tract and improve the bioavailability of medications that are characterized by a narrow absorption window. Gastroretention would also facilitate local drug delivery to the stomach and proximal small intestine. So, gastroretention could help to provide greater availability of new products and consequently improved therapeutic activity and required benefits to patients. The purpose of writing the article was to compile the recent literature with special focus on various gastroretentive approaches that have recently become leading methodologies in the field of site-specific orally administered controlled release drug delivery. In particular, bioadhesive, size-increasing and floating drug delivery systems are presented and their major advantages and shortcomings are critically discussed in this review. Thus, gastroretention could help to provide greater availability of new products and consequently improved therapeutic activity and substantial benefits to patients
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Li, Hai-yan, Xiang-yong Cui, Feng Gao, et al. "Characterization and mapping of the multi-component release kinetics of a Traditional Chinese Medicine dosage form using a modified LC/MS/MS method and chemomic release kinetic theory." Acta Pharmaceutica Sinica B 1, no. 2 (2011): 106–14. http://dx.doi.org/10.1016/j.apsb.2011.06.007.
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Sharma, Shyam Bihari, Suman Jain, and K. Ganesan. "Preformulation Studies of Pralidoxime Chloride for Formulation Development of Microspheres." Journal of Drug Delivery and Therapeutics 9, no. 4-s (2019): 338–42. http://dx.doi.org/10.22270/jddt.v9i4-s.3336.
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Microspheres are one of the novel drug delivery system which possess several applications and are made up of assorted polymers. Microspheres can be defined as solid, approximately spherical particles ranging in size from 1 to 1000 μm range in diameter having a core of drug and entirely outer layers of polymers as coating material. They are made up of polymeric, waxy or other protective materials i.e. biodegradable synthetic polymer and modified natural products such as starches, gums, proteins, fats and waxes. Preformulation is a group of studies that focus on the physicochemical properties of a new drug candidate that could affect the drug performance and the development of a dosage form. This couldprovide important information for formulation design or support the need for molecular modification. Every drug has intrinsic chemical and physical properties which has been consider before development of pharmaceutical formulation. This property provides the framework for drugs combination with pharmaceutical ingredients in the fabrication of dosage form. Objective of preformulation study is to develop the elegant, stable, effective and safe dosage form by establishing kinetic rate profile, compatibility with the other ingredients and establish Physico-chemical parameter of new drug substances. The purpose of the present study was to systematically investigate some of the important physicochemical properties of pralidoxime chloride for preparation of microspheres. The physicochemical properties such as solubility, pKa, dissolution, melting point, assay development, excipient compatibility etc. of pralidoxime chloride was carried out. Before selection of excipients, the Preformulation study of drug pralidoxime is completed for successful formulation of microspheres. The result of Preformulation studies shows good flow properties, excipient compatibility, solubility efficiency and melting point. From this study we concluded that pralidoximewith HPMC and EC can be used to formulate pralidoxime microspheres for modified release.
 Keywords: Microspheres, Preformulation, Pralidoxime chloride, Physico-chemical parameter.
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Jantratid, Ekarat, Vincenzo De Maio, Emanuela Ronda, Valentina Mattavelli, Maria Vertzoni, and Jennifer B. Dressman. "Application of biorelevant dissolution tests to the prediction of in vivo performance of diclofenac sodium from an oral modified-release pellet dosage form." European Journal of Pharmaceutical Sciences 37, no. 3-4 (2009): 434–41. http://dx.doi.org/10.1016/j.ejps.2009.03.015.
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Vlachou, Marilena, Angeliki Siamidi, and Yannis Dotsikas. "Utilization of a Single Experimental Design for the Optimization of Furosemide Modified-Release Tablet Formulations." Current Drug Delivery 16, no. 10 (2019): 931–39. http://dx.doi.org/10.2174/1567201816666191029130324.
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Background: The loop diuretic drug furosemide is widely used for the treatment of edema in various conditions, such as pulmonary, cardiac and hepatic edema, as well as cardiac infarction. Furosemide, due to its poor water solubility and low bioavailability after oral administration of conventional dosage form, is categorized as class IV in the biopharmaceutical classification system. Objective: In the case of furosemide, this release profile is responsible for various physiological problems, acute diuresis being the most serious. This adverse effect can be circumvented by the modified release of furosemide from tablet formulations compared to those forms designed for immediate release. Method: In this report, a D-optimal combined experimental design was applied for the development of furosemide containing bilayer and compression coated tablets, aiming at lowering the drug’s burst release in the acidic environment of the stomach. A D-optimal combined design was selected in order to include all requirements in one design with many levels for the factors examined. The following responses were selected as the ones reflecting better criteria for the desired drug release: dissolution at 120 min (30-40%), 300 min (60-70%) and 480 min >95%. The new formulations, suggested by the Doptimal combined design, incorporated different grades of Eudragit ® polymers (Eudragit® E100 and Eudragit® L100-55), lactose monohydrate and HPMC K15M. The dissolution profile of furosemide from these systems was probed via in vitro dissolution experiments in buffer solutions simulating the pH of the gastrointestinal tract. Results: The results indicate that the use of Eudragit® E100 in conjunction with lactose monohydrate led to 21.32-40.85 % drug release, in the gastric medium, in both compression-coated and bilayer tablets. This is lower than the release of the mainstream drug Lasix® (t=120 min, 44.5% drug release), implying longer gastric retention and drug waste minimization. Conclusion: Furosemide’s release in the intestinal environment, from compression coated tablets incorporating Eudragit® L100-55 and HPMC K15M in the inner core or one of the two layers of the bilayer tablets, was delayed, compared to Lasix®
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Algahtani, Mohammed S., Abdul Aleem Mohammed, Javed Ahmad, and Ehab Saleh. "Development of a 3D Printed Coating Shell to Control the Drug Release of Encapsulated Immediate-Release Tablets." Polymers 12, no. 6 (2020): 1395. http://dx.doi.org/10.3390/polym12061395.
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The use of 3D printing techniques to control drug release has flourished in the past decade, although there is no generic solution that can be applied to the full range of drugs or solid dosage forms. The present study provides a new concept, using the 3D printing technique to print a coating system in the form of shells with various designs to control/modify drug release in immediate-release tablets. A coating system of cellulose acetate in the form of an encapsulating shell was printed through extrusion-based 3D printing technology, where an immediate-release propranolol HCl tablet was placed inside to achieve a sustained drug release profile. The current work investigated the influence of shell composition by using different excipients and also by exploring the impact of shell size on the drug release from the encapsulated tablet. Three-dimensional printed shells with different ratios of rate-controlling polymer (cellulose acetate) and pore-forming agent (D-mannitol) showed the ability to control the amount and the rate of propranolol HCl release from the encapsulated tablet model. The shell-print approach also showed that space/gap available for drug dissolution between the shell wall and the enclosed tablet significantly influenced the release of propranolol HCl. The modified release profile of propranolol HCl achieved through enclosing the tablet in a 3D printed controlled-release shell followed Korsmeyer–Peppas kinetics with non-Fickian diffusion. This approach could be utilized to tailor the release profile of a Biopharmaceutics Classification System (BCS) class I drug tablet (characterized by high solubility and high permeability) to improve patient compliance and promote personalized medicine.
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Devi Thamizhanban, Gampa Tulja Rani, and Kathiresan krishnasamy. "Development of bio-relevant dissolution method for prognosis of In-vivo performance of Dipyridamole from modified release capsules." International Journal of Research in Pharmaceutical Sciences 11, no. 2 (2020): 2340–49. http://dx.doi.org/10.26452/ijrps.v11i2.2211.
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In-vitro biorelevant dissolution test method was developed for Dipyridamole in modified release multi-particulate dosage form, to simulate the product drug release after oral administration to human. The Dipyridamole concentration in blood plasma achieved after oral administration under pre-prandial (fasting) condition were used for deriving the target dissolution profile deconvoluting the plasma concentration using numerical deconvolution technique. The fraction of drug absorbed was considered as the target dissolution profile. The drug product was tested by using the dissolution method recommended by office of generic drugs, and the dissolution results observed are not comparable with the target dissolution profile. Dissolution method was developed using reciprocating cylinder, Bio-Dis (apparatus -3 as per USP), by simulating the pre-prandial conditions. A full factorial design of experiment was carried out to achieve the target dissolution profile. Media volume and dips per minute (DPM) are considered as main factors, in design of experiment. The dissolution results achieved with media volume 250ml and 10DPM were found to be comparable with target dissolution profile and observed with the F2 value (similarity factor) of 92%. The developed dissolution method demonstrates a very good in-vitro/in-vivo correlation under pre-prandial condition, and shall be used as a predictive in-vitro tool for evaluation Dipyridamole extended release capsules.
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Hopkins, Sean P., and Megan C. Frost. "S-Nitroso-N-Acetyl-D-Penicillamine Modified Hyperbranched Polyamidoamine for High-Capacity Nitric Oxide Storage and Release." Bioengineering 7, no. 1 (2020): 9. http://dx.doi.org/10.3390/bioengineering7010009.
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Synthetic nitric oxide (NO)-donating materials have been shown to have many beneficial effects when incorporated into biomedical materials. When released in the correct dosage, NO has been shown to increase the biocompatibility of blood and tissue contacting materials, but materials are often limited in the amount of NO that can be administered over a period of time. To address this, hyperbranched polyamidoamine (HPAMAM) was modified with the S-nitrosothiol, S-nitroso-N-acetyl-D-penicillamine, and nitrosated to form a controlled, high-capacity NO-donating compound (SNAP-HPAMAM). This compound has the potential of modifying polymers to release NO over long periods of time by being blended into a variety of base polymers. Nitric oxide release was triggered by photoinitiation and through passive ion-mediated release seen under physiological conditions. A material that delivers the beneficial dose of NO over a long period of time would be able to greatly increase the biocompatibility of long-term implantable devices. Structural analysis of a generation 2 HPAMAM molecule was done through Fourier transform infrared spectroscopy (FTIR), 1H nuclear magnetic resonance spectroscopy (NMR), and matrix assisted laser desorption ionization, time of flight (MALDI-TOF) mass spectrometry. The NO capacity of the finalized generation 2 SNAP-HPAMAM compound was approximately 1.90 ± 0.116 µmol NO/mg. Quantification of the functional groups in the compound proved that an average of 6.40 ± 0.309 reactive primary amine sites were present compared to the 8 reactive sites on a perfectly synthesized generation 2 dendrimer. There is a substantial advantage of using the hyper-branched HPAMAM over purified dendrimers in terms of reduced labor and expense while still providing a high-capacity NO donor that can be blended into different polymer matrices.
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Stanojević, Gordana, Djordje Medarević, Ivana Adamov, Nikola Pešić, Jovana Kovačević, and Svetlana Ibrić. "Tailoring Atomoxetine Release Rate from DLP 3D-Printed Tablets Using Artificial Neural Networks: Influence of Tablet Thickness and Drug Loading." Molecules 26, no. 1 (2020): 111. http://dx.doi.org/10.3390/molecules26010111.
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Various three-dimensional printing (3DP) technologies have been investigated so far in relation to their potential to produce customizable medicines and medical devices. The aim of this study was to examine the possibility of tailoring drug release rates from immediate to prolonged release by varying the tablet thickness and the drug loading, as well as to develop artificial neural network (ANN) predictive models for atomoxetine (ATH) release rate from DLP 3D-printed tablets. Photoreactive mixtures were comprised of poly(ethylene glycol) diacrylate (PEGDA) and poly(ethylene glycol) 400 in a constant ratio of 3:1, water, photoinitiator and ATH as a model drug whose content was varied from 5% to 20% (w/w). Designed 3D models of cylindrical shape tablets were of constant diameter, but different thickness. A series of tablets with doses ranging from 2.06 mg to 37.48 mg, exhibiting immediate- and modified-release profiles were successfully fabricated, confirming the potential of this technology in manufacturing dosage forms on demand, with the possibility to adjust the dose and release behavior by varying drug loading and dimensions of tablets. DSC (differential scanning calorimetry), XRPD (X-ray powder diffraction) and microscopic analysis showed that ATH remained in a crystalline form in tablets, while FTIR spectroscopy confirmed that no interactions occurred between ATH and polymers.
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WANG, ZHENG, FUMITOSHI HIRAYAMA та KANETO UEKAMA. "In-vivo and in-vitro evaluations of a modified-release oral dosage form of nifedipine by hybridization of hydroxypropyl-β-cyclodextrin and hydroxypropylcelluloses in dogs". Journal of Pharmacy and Pharmacology 46, № 6 (1994): 505–7. http://dx.doi.org/10.1111/j.2042-7158.1994.tb03836.x.
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Dahima, Rashmi. "Formulation and Evaluation of Pseudoephedrine Hydrochloride Loaded Alginate Microbeads." Journal of Drug Delivery and Therapeutics 10, no. 3 (2020): 137–41. http://dx.doi.org/10.22270/jddt.v10i3.4094.
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Multiple unit dosage forms such as microbeads have increased acceptance because of added even spreading of the drug in the gastrointestinal tract, unvarying drug absorption, abridged local irritation and removal of undesirable intestinal retaining of polymeric material, when compared to non-disintegrating single unit dosage form. The purpose of the presented research is to develop microbeads of pseudoephedrine hydrochloride utilizing sodium alginate as the hydrophilic carrier in combination with HPMC as drug release modifier to lessen the dosing frequency and thereby advance the patient compliance. The microbeads were formulated by varying concentrations of HPMC and calcium chloride. The optimum formulation was chosen based upon in vitro drug release studies and further evaluated. The compatibility of drug-polymer was studied using FTIR analysis. The prepared formulation underwent evaluation for various parameters like drug entrapment, microbeads size, swelling index, mucoadhesive property and stability. No significant drug-polymer interactions were observed in compatibility studies and the formulation was found to be stable on 45 days storage. The formulations exhibited an extended drug release pattern which was the ultimate aim of the study. The microbeads represented good yield, high drug entrapment, low microbeads size and appropriate swelling property. The in vitro wash-off test indicated that the sodium alginate microbeads represent decent mucoadhesive properties. Henceforth, the formulated HPMC coated sodium alginate beads can be utilized as a substitute and cost-effective carrier for the oral controlled delivery of pseudoephedrine hydrochloride.
 Keywords: microbeads, pseudoephedrine hydrochloride, sodium alginate, drug release
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Desai, Hetal, Mohamed Y. Mahmoud, Jinlian Tan, Farnaz Minooei, Donald R. Demuth, and Jill M. Steinbach-Rankins. "Assessment of CafA Targeted BAR-Encapsulated Nanoparticles against Oral Biofilms." Pharmaceutics 12, no. 9 (2020): 835. http://dx.doi.org/10.3390/pharmaceutics12090835.
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Porphyromonas gingivalis adherence to Streptococcus gordonii is a crucial initial event that facilitates the colonization of P. gingivalis, a key pathogen in periodontal disease. As such, blocking these early interactions may present a potential avenue to limit P. gingivalis colonization. Nanoparticles encapsulating a synthetic peptide BAR (BAR-encapsulated NPs) inhibit P. gingivalis/S. gordonii biofilm formation 1.8-fold more potently relative to free BAR. However, BAR-encapsulated NPs, like many orally delivered formulations, may benefit from a strategy that improves their retention in an open flow environment. Here, we sought to enhance the efficacy of BAR-encapsulated NPs by modifying their surfaces with coaggregation factor A (CafA), a fimbrial protein expressed by the early colonizer, Actinomyces oris. We demonstrate that the targeting moiety, CafA, enhances NP binding and exhibits specificity of adherence to S. gordonii, relative to other oral bacterial species. Furthermore, CafA-modified NPs release inhibitory concentrations of BAR for 12 h, a time frame relevant to oral dosage form delivery. Lastly, CafA-modified NPs potently inhibit P. gingivalis/S. gordonii biofilm formation for up to 12 h and are non-toxic at therapeutically-relevant concentrations. These results suggest that CafA-modified NPs represent a novel and efficacious delivery vehicle for localized, targeted delivery of BAR to P. gingivalis preferred niches.
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Gupta, Ankita, Gaurav Tiwari, Ruchi Tiwari, Rishabh Srivastava, and A. K. Rai. "Enteric coated HPMC capsules plugged with 5-FU loaded microsponges: a potential approach for treatment of colon cancer." Brazilian Journal of Pharmaceutical Sciences 51, no. 3 (2015): 591–605. http://dx.doi.org/10.1590/s1984-82502015000300011.
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The work was aimed at developing novel enteric coated HPMC capsules (ECHC) plugged with 5 Florouracil (5-FU) loaded Microsponges in combination with calcium pectinate beads. Modified quasi-emulsion solvent diffusion method was used to formulate microsponges based on 32 factorial design and the effects of independent variables (volume of organic solvent and Eudragit RS100 content) on the dependent variables (Particle size, %EE & % CDR) were determined. The optimized microsponges (F4) were characterized by SEM, PXRD, TGA and were plugged along with calcium pectinate beads in HPMC capsules and the HPMC capsules were further coated with enteric polymer Eudragit L 100 (Ed-L100) and/ or Eudrgit S 100 (Ed-S 100) in different proportions. In vitro release study of ECHC was performed in various release media sequentially SGF for 2 h, followed by SIF for the next 6 h and then in SCF (in the presence and absence of pectinase enzyme for further 16 h). Drug release was retarded on coating with EdS-100 in comparison to blend of EdS-100: EdL-100 coating. The percentage of 5-FU released at the end of 24 h from ECHC 3 was 97.83 ± 0.12% in the presence of pectinase whereas in control study it was 40.08 ± 0.02% drug. The optimized formulation was subjected to in vivo Roentgenographic studies in New Zealand white rabbits to analyze the in vivo behavior of the developed colon targeted capsules. Pharmacokinetic studies in New Zealand white rabbits were conducted to determine the extent of systemic exposure provided by the developed formulation in comparison to 5-FU aqueous solutions. Thus, enteric coated HPMC capsules plugged with 5-FU loaded microsponges and calcium pectinate beads proved to be promising dosage form for colon targeted drug delivery to treat colorectal cancer.
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Hiral, Chavda D., Sonpal N. Rakshit, Paresh Prajapati A, and Madhabhai M. Patel. "Formulation and Evaluation of Modified Pulsincap as Pulsatile Drug Delivery System for Treatment of Rheumatoid Arthritis." International Journal of Pharmaceutical Sciences and Nanotechnology 9, no. 5 (2016): 3476–87. http://dx.doi.org/10.37285/ijpsn.2016.9.5.5.
Full textAbstract:
The aim of the present study was to design and evaluate a modified pulsincap pulsatile drug delivery system of etodolac for treatment of rheumatoid arthritis. Capsule body was made water insoluble by cross linking with formaldehyde vapour. It was filled with drug, osmogen NaCl and super disintegrant sodium starch glycolate to expel the drug after predetermined lag time. A hydro gel plug made of HPMC K4M was placed in the capsule body to achieve desired drug release after lag time for chronotherapy of rheumatoid arthritis. Untreated cap was then fitted to the treated body was sealed. Entire unit was coated with 5% Eudragit S-100 to prevent variable gastric emptying. A 32 full factorial design was used for optimization in which concentration ratio of NaCl and SSG (X1), and the weight of hydrogel plug (X2) were selected as independent variables while lag time and t90% were taken as dependent variables. FTIR and DSC studies confirmed drug excipient compatibility. Developed formulation was evaluated for in-vitro drug release in pH 1.2, phosphate buffer pH 6.8 and phosphate buffer pH 7.4. Statistical analysis confirmed the significance of selected independent variables. Response surface plot and contour plot indicate augmentation of the line toward the weight of hydrogel plug factor indicating greater significance. Formulation with highest desirability containing 34.4 mg of SSG, 137.6 mg of NaCl and 48 mg of HPMC K4M plug was selected as an optimized formulation as it provided the desired lag time of 6 hours and t90% of about 477 mins. Accelerated stability study performed on optimized formulation suggested stable and viable formulation. A stable, efficient formulation modified pulsincap of Etodolac as a pulsatile drug delivery system was developed with proposed increased patient compliance and improved dosage form efficiency.