Journal articles: 'Eudragit'

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Hussien, Ahmed Abbas. "Preparation and Evaluation of Oral Microsponge Drug Delivery System of Ketoconazole." Al Mustansiriyah Journal of Pharmaceutical Sciences 14, no. 1 (June 1, 2014): 1–8. http://dx.doi.org/10.32947/ajps.v14i1.119.

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In oral applications, the microsponge system has been shown to increase the rate of solubilization of poorly water-soluble drugs by entrapping such drugs in the microsponge system's pores.Because these pores are very small, the drug is in effect reduced tomicroscopic particles and increased surface area thus greatly increases the rate ofsolubilization.This investigation was done to increase solubility and then bioavialibility of poorly soluble ketoconazole (BCS class II drug) by preparing it as microsponges by quasi emulsionsolvent technique using different types of Eudragits as Eudragit E 100, Eudragit RS or Eudragi tRL. Physicochemical interaction between drug and excipients as individual one,physical mixture and prepared microsponge has been evaluated using Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) which indicates theabsence of interaction between them. The1: 0.1 ratio drug: Eudragit E 100 at stirring rate of 2000 rpm (F1b) was found to give the best production yield of 80.46±2.41, entrapment efficiency of 70.84%±1.71, and smallest particle size of 57.42±2.26 μm. Scanning electron microscopy of F1b at magnification of 1000x and 50000x shows the presence of drug as nanocrystals inside microsponge. All prepared formulas shows good flow properties indicated the possibility of capsule formulation which show significant (P<0.05) high drug release percent in 0.1 HCl compared with traditional Nizoral® oral tablet (83.15%±1.10) but Eudragit E (F1b ) shows the best drug release percent of 100±0.91 at 20 minutes. Finally, the overall obtained data revealed the feasibility of preparing fast release ketaconazole as microsponges in oral capsules dosage form.

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Ranpise, N. S., S. S. Somavanshi, R. K. Bhujbal ., and Y. M. Jagtap. "DEVELOPMENT OF SUSTAINED RELEASE TABLET OF METFORMIN HYDROCHLORIDE BY AQUEOUS COATING." INDIAN DRUGS 49, no. 02 (February 26, 2012): 26–32. http://dx.doi.org/10.53879/id.49.02.p0026.

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The aim of present work was to develop a metformin hydrochloride sustained release tablet by aqueous coating. Eudragit RL and Eudragit RS were used for coating of tablets. Eudragit RL having 10% and Eudragit RS having 5% of functional quaternary ammonium groups, which give rise to pH independent permeability of the polymer. Metformin hydrochloride uncoated tablets were prepared by wet granulation technique. Tablets were coated with blends of Eudragit RS30D and Eudragit RL30D in 5:1 and in 3:1 ratios at different coating level viz. 7%, 5%, 3%, 1.5%, 1%. Two dissolution media: pH 1.2 and pH 6.8 phosphate buffer were employed for in vitro release behaviors of metformin hydrochloride tablets. Coating with blends of Eudragit RS 30D and Eudragit RL 30D in 5:1 and in 3:1 ratio at 1% and at 3% showed sustained release effect for 12 h. The two Eudragit polymers with different features as coating materials produced the desired results.

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Moustafine, R. I., T. V. Kabanova, V. A. Kemenova, and G. Van den Mooter. "Characteristics of interpolyelectrolyte complexes of Eudragit E100 with Eudragit L100." Journal of Controlled Release 103, no. 1 (March 2005): 191–98. http://dx.doi.org/10.1016/j.jconrel.2004.11.031.

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Han, Min, Qin Yu, Xuerong Liu, Fuqiang Hu, and Hong Yuan. "Preparation and Characterization of a Novel Aqueous Dispersion for Enteric Coating of Pantoprazole Sodium Pellets." Acta Pharmaceutica 68, no. 4 (December 1, 2018): 441–55. http://dx.doi.org/10.2478/acph-2018-0035.

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Abstract The purpose of this work was to investigate a novel aqueous dispersion (Eudragit® L100-55) f or e nteric c oating o f drugs. Three different casting solutions, Eudragit® L100-55 aqueous dispersion, Eudragit® L 100-55 o rganic s olution, and Eudragit® L30D-55 aqueous dispersion, were used to prepare free films by the casting method. Drug-loaded pellets, prepared by the extrusion-spheronization method, were coated with one of these three coating solutions using the fluidized-bed spray coating technology. Properties of the free films were thoroughly investigated. Films formed by Eudragit® L100-55 aqueous dispersions showed similar properties to those formed by Eudragit® L100-55 organic solution regarding thermodynamic properties, moisture permeability, solubility and acid tolerance ability. Furthermore, the performance of the novel film was better than that formed by Eudragit® L30D-55 aqueous dispersion. Among the three enteric coating solutions, Eudragit® L100- 55 aqueous dispersion will be a promising aqueous dispersion for enteric coating and can be used in the development of enteric-coated preparations.

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Ha, Eun-Sol, Du Hyung Choi, In-hwan Baek, Heejun Park, and Min-Soo Kim. "Enhanced Oral Bioavailability of Resveratrol by Using Neutralized Eudragit E Solid Dispersion Prepared via Spray Drying." Antioxidants 10, no. 1 (January 11, 2021): 90. http://dx.doi.org/10.3390/antiox10010090.

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In this study, we designed amorphous solid dispersions based on Eudragit E/HCl (neutralized Eudragit E using hydrochloric acid) to maximize the dissolution of trans-resveratrol. Solid-state characterization of amorphous solid dispersions of trans-resveratrol was performed using powder X-ray diffraction, scanning electron microscopy, and particle size measurements. In addition, an in vitro dissolution study and an in vivo pharmacokinetic study in rats were carried out. Among the tested polymers, Eudragit E/HCl was the most effective solid dispersion for the solubilization of trans-resveratrol. Eudragit E/HCl significantly inhibited the precipitation of trans-resveratrol in a pH 1.2 dissolution medium in a dose-dependent manner. The amorphous Eudragit E/HCl solid dispersion at a trans-resveratrol/polymer ratio of 10/90 exhibited a high degree of supersaturation without trans-resveratrol precipitation for at least 48 h by the formation of Eudragit E/HCl micelles. In rats, the absolute oral bioavailability (F%) of trans-resveratrol from Eudragit E/HCl solid dispersion (10/90) was estimated to be 40%. Therefore, trans-resveratrol-loaded Eudragit E/HCl solid dispersions prepared by spray drying offer a promising formulation strategy with high oral bioavailability for developing high-quality health supplements, nutraceutical, and pharmaceutical products.

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Ha, Eun-Sol, Du Hyung Choi, In-hwan Baek, Heejun Park, and Min-Soo Kim. "Enhanced Oral Bioavailability of Resveratrol by Using Neutralized Eudragit E Solid Dispersion Prepared via Spray Drying." Antioxidants 10, no. 1 (January 11, 2021): 90. http://dx.doi.org/10.3390/antiox10010090.

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In this study, we designed amorphous solid dispersions based on Eudragit E/HCl (neutralized Eudragit E using hydrochloric acid) to maximize the dissolution of trans-resveratrol. Solid-state characterization of amorphous solid dispersions of trans-resveratrol was performed using powder X-ray diffraction, scanning electron microscopy, and particle size measurements. In addition, an in vitro dissolution study and an in vivo pharmacokinetic study in rats were carried out. Among the tested polymers, Eudragit E/HCl was the most effective solid dispersion for the solubilization of trans-resveratrol. Eudragit E/HCl significantly inhibited the precipitation of trans-resveratrol in a pH 1.2 dissolution medium in a dose-dependent manner. The amorphous Eudragit E/HCl solid dispersion at a trans-resveratrol/polymer ratio of 10/90 exhibited a high degree of supersaturation without trans-resveratrol precipitation for at least 48 h by the formation of Eudragit E/HCl micelles. In rats, the absolute oral bioavailability (F%) of trans-resveratrol from Eudragit E/HCl solid dispersion (10/90) was estimated to be 40%. Therefore, trans-resveratrol-loaded Eudragit E/HCl solid dispersions prepared by spray drying offer a promising formulation strategy with high oral bioavailability for developing high-quality health supplements, nutraceutical, and pharmaceutical products.

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dos Santos, Juliana, Guilherme Silveira da Silva, Maiara Callegaro Velho, and Ruy Carlos Ruver Beck. "Eudragit®: A Versatile Family of Polymers for Hot Melt Extrusion and 3D Printing Processes in Pharmaceutics." Pharmaceutics 13, no. 9 (September 8, 2021): 1424. http://dx.doi.org/10.3390/pharmaceutics13091424.

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Eudragit® polymers are polymethacrylates highly used in pharmaceutics for the development of modified drug delivery systems. They are widely known due to their versatility with regards to chemical composition, solubility, and swelling properties. Moreover, Eudragit polymers are thermoplastic, and their use has been boosted in some production processes, such as hot melt extrusion (HME) and fused deposition modelling 3D printing, among other 3D printing techniques. Therefore, this review covers the studies using Eudragit polymers in the development of drug delivery systems produced by HME and 3D printing techniques over the last 10 years. Eudragit E has been the most used among them, mostly to formulate immediate release systems or as a taste-masker agent. On the other hand, Eudragit RS and Eudragit L100-55 have mainly been used to produce controlled and delayed release systems, respectively. The use of Eudragit polymers in these processes has frequently been devoted to producing solid dispersions and/or to prepare filaments to be 3D printed in different dosage forms. In this review, we highlight the countless possibilities offered by Eudragit polymers in HME and 3D printing, whether alone or in blends, discussing their prominence in the development of innovative modified drug release systems.

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Thakur, Nishant, Bhupinder Kaur, Manish Goswami, and Chandan Sharma. "Compatibility studies of the Thiocolchicoside with Eudragit RLPO, Eudragit E100 and Eudragit L100 using thermal and non-thermal methods." Drug Combination Therapy 4, no. 1 (2022): 1. http://dx.doi.org/10.53388/dct2021100301.

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Jun, Hee-Sook, Gongdeuk Bae, Young Tag Ko, and Yoon Sin Oh. "Cytotoxicity and Biological Efficacy of Exendin-4-Encapsulated Solid Lipid Nanoparticles in INS-1 Cells." Journal of Nanomaterials 2015 (2015): 1–6. http://dx.doi.org/10.1155/2015/753569.

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Exendin-4 (Ex-4), a peptide of glucagon-like peptide-1 receptor agonist, is a potent insulinotropic agent and alternative drug delivery systems to increase therapeutic utility have been explored. We developed exendin-4-encapsulated solid lipid nanoparticles (Eudragit Ex-4 SLNs) and compared the effects of Eudragit Ex-4 SLNs with those of native Ex-4 on INS-1 cells. We observed no significant toxic effects of nanoparticles at concentrations from 1 nM to 100 nM. Similar to Ex-4, Eudragit Ex-4 SLNs stimulated the production of cyclic AMP at 10 nM. Moreover, unlike treatment with the vehicle, treatment with 10 nM Eudragit Ex-4 SLNs increased insulin mRNA levels and insulin secretion. These insulinotropic effects of Eudragit Ex-4 SLNs were comparable to those of Ex-4. Thus, ourin vitroresults suggest that the biological effects of Eudragit Ex-4 SLNs are similar to those of Ex-4, and furtherin vivopharmacokinetic studies are required to propose an alternative sustained release drug system.

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Quan, Ji Shan, Hu Lin Jiang, Yun Jaie Choi, Mi Kyong Yoo, and Chong Su Cho. "Thiolated Eudragit-Coated Chitosan Microspheres as an Oral Drug Delivery System." Key Engineering Materials 342-343 (July 2007): 445–48. http://dx.doi.org/10.4028/www.scientific.net/kem.342-343.445.

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The aim of this study is to prepare mucoadhesive chitosan microspheres for protein drug to deliver to intestine through oral administration. The thiolated Eudragit was synthesized by reaction between L-cysteine hydrochloride and Eudragit® L-100. About 8 mol-% of cysteine was introduced to the Eudragit-cysteine conjugate. The conjugate was used to coat bovine serum albumin (BSA)-loaded chitosan microspheres. The average particle sizes of BSA-loaded thiolated Eudragit-coated chitsoan microspheres (TECMs) were 4.06±0.74 .m and the uniform sizedistribution was shown. The in vitro release of BSA from BSA-loaded TECMs was pH-dependent. Our results indicated that thiolated Eudragit might be a good candidate as a coating material for oral delivery of protein drug owing to mucoadhesive and pH-sensitive properties.

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Cetin, Meltem, Mustafa Sinan Aktas, Imran Vural, and Murat Ozturk. "Salmon calcitonin-loaded Eudragit® and Eudragit®-PLGA nanoparticles:in vitroandin vivoevaluation." Journal of Microencapsulation 29, no. 2 (November 30, 2011): 156–66. http://dx.doi.org/10.3109/02652048.2011.635426.

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Charernsriwilaiwat, Natthan, Thapakorn Chareonying, and Praneet Opanasopit. "Electrospinning of Eudragit RS100 for Nerve Tissue Engineering Scaffold." Key Engineering Materials 859 (August 2020): 220–25. http://dx.doi.org/10.4028/www.scientific.net/kem.859.220.

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Electrospinning technique is widely investigated in medical applications such as tissue engineering scaffolds, wound dressing and drug delivery. In this study, the aligned nanofiber scaffold of Eudragit RS100 was successfully fabricated via electrospinning technique for nerve tissue engineering scaffold. The diameter distribution and degree of alignment of Eudragit RS100 nanofiber scaffold were observed by scanning electron microspore (SEM). The chemical and crystalline structure of Eudragit RS100 nanofiber scaffold were analyzed using Fourier transform infrared spectroscopy (FTIR) and Powder X-ray diffactometer (PXRD). Cell culture studies using rat Schwann cells were determined to evaluate cell proliferation cell alignment and morphology. The results implied that the diameter of fiber was in the nanometer region. The Eudragit RS100 nanofiber scaffold were in an amorphous form and its chemical structure was not destructive after the electrospinning process. The Eudragit RS100 nanofiber scaffold showed biocompatibility with rat Schwann cells and growing parallel to the aligned fibers. In conclusion, the Eudragit RS100 nanofiber scaffold may have the ability to apply to nerve tissue engineering scaffold.

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Sampaopan, Yupaporn, and Jirapornchai Suksaeree. "Mechanical Properties of Pectin/Eudragit Blend Films." Key Engineering Materials 819 (August 2019): 3–8. http://dx.doi.org/10.4028/www.scientific.net/kem.819.3.

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The aim of this study was to prepare the pectin film-based different types of Eudragit® polymer blends using glycerine as a plasticizer and to study the mechanical properties of these films. The mixing of polymer mixture was carried out using distilled water as a solvent throughout the experiment. The polymer mixture was poured into Petri dish and transferred to hot air oven for solvent evaporation. The maximum positive force and percentage of elongation at break were found at the range of 63.58-409.94 g and 74.92-145.42%, respectively for pectin film-based Eudragit® RL 30D polymer blends, 87.12-409.94 g and 74.42-145.42%, respectively for pectin film-based Eudragit® RS 30D polymer blends, 76.50-409.94 g and 72.68-145.42%, respectively for pectin film-based Eudragit® NM 30D polymer blends, and 137.12-409.94 g and 44.42-145.42%, respectively for pectin film-based Eudragit® NE 40D polymer blends. The results indicated that the mechanical properties of the pectin film decreased with inclusion of various types of Eudragit® (p < 0.05). However, it was found that the pectin film-based different types of Eudragit® polymer blends has high potential to be used in pharmaceutical applications. Further investigation related to the incorporation of drugs or herbal extracts and the in vitro evaluation are recommended.

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Noviyanty, Yuska, Elfi Sahlan Ben, and Erizal Zaini. "Studi Sistem Dispersi Padat Klaritromisin – Eudragit L100." Jurnal Sains Farmasi & Klinis 2, no. 2 (July 12, 2016): 183. http://dx.doi.org/10.29208/jsfk.2016.2.2.68.

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Telah dilakukan penelitian pembentukan sistem dispersi padat klaritromisin-Eudragit L100. Dispersi padat dibuat dengan perbandingan berat (b/b) menggunakan metode pelarutan. Analisa DTA dispersi padat diperoleh pada Eudragit L 100 mempengaruhi posisi dan ketajaman puncak. Analisa difraksi sinar-x menunjukkan bahwa dispersi padat klaritromisin – Eudragit L 100 berupa amorf dan tidak menghasilkan fase kristalin baru. Hasil analisis SEM dispersi padat menunjukkan kristal Eudragit L 100 lebih kecil (amorf) dan menempel pada permukaan kristal klaritromisin. Analisis spektrofotometer IR menunjukkan tidak ada interaksi kimia antara klaritromisin – Eudragit L 100. Penetapan kadar klaritromisin dengan KCKT fase gerak metanol dan 0,067 M KH2PO4 13:7 ditambah asam fospat pH 4,0. Hasil profil disolusi pada waktu 60 menit berturut-turut untuk klaritromisin 45,73%, CF (1:1) 49,86 %, DP (1:1) 51,53 %, DP (2:1) 55,87 % dan DP (1:2) 58,97 % Dispersi padat 1:2 (b/b) memiliki peningkatan laju disolusi jika dibandingkan dengan klaritromisin.

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Widjaja, Marsella, Jefri Gan, Joseph Talpaneni, and Raymond Tjandrawinata. "Determination of Eudragit® L100 in an Enteric-Coated Tablet Formulation Using Size-Exclusion Chromatography with Charged-Aerosol Detection." Scientia Pharmaceutica 86, no. 3 (September 12, 2018): 38. http://dx.doi.org/10.3390/scipharm86030038.

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Eudragit® L100 is a commonly used polymer in a coating layer of modified-release drug formulation to prevent drug release in the stomach. The amount of Eudragit® L100 in the formula determines the dissolution profile of drug at its release medium. Hence, its quantification in reference product will facilitate the formulation of a bioequivalent drug product. Some analytical methods including size-exclusion chromatography (SEC) have been reported for characterization of Eudragit® L100 either as single component or its conjugate with the enzyme, but none for its quantification in drug formulation. In this work, an SEC method with charged-aerosol detection (CAD) was developed for determination of Eudragit® L100 in an enteric-coated tablet formulation using Waters Ultrahydrogel 1000 and Waters Ultrahydrogel 120 columns in series. The mobile phase was a mixture of 90:10 (v/v) 44.75 mM aqueous ammonium acetate buffer, pH 6.6 and acetonitrile pumped at a constant flow rate of 0.8 mL/min in isocratic mode. The method was validated for specificity, working range, limit of detection (LOD), limit of quantification (LOQ), accuracy and precision. The method was shown to be specific for Eudragit® L100 against the diluent (mobile phase) and placebo of a coating layer for the tablet. A good correlation coefficient (r = 0.9997) of CAD response against Eudragit® L100 concentration from 0.1–1.0 mg/mL was obtained using polynomial regression. LOD and LOQ concentrations were 0.0015 and 0.0040 mg/mL, respectively. The mean recovery of Eudragit® L100 was in the range of 88.0–91.1% at three levels of working concentration: 50%, 100% and 150%. Six replicated preparations of samples showed good precision of the peak area with % relative standard deviation (RSD) 2.7. In conclusion, the method was suitable for quantification of Eudragit® L100 in an enteric-coated tablet formulation.

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Letmanski, Tomasz, Anna Kodym, Piotr Weber, Michal Lewandowski, Andrzej Wisniewski, and Tomasz Baj. "Eudragit FS 30D as a potential polymer for use in the technology of preparing matrix tablets contain metronidazole – an experimental and mathematical modeling study." Current Issues in Pharmacy and Medical Sciences 28, no. 2 (June 1, 2015): 97–104. http://dx.doi.org/10.1515/cipms-2015-0053.

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Abstract The aim of this study was to examine the usefulness of a pH-dependent copolymer - Eudragit FS - for employment in the technology of preparing modified release metronidazole matrix tablets. In addition, in our work, Eudragit RL and Eudragit RS were included in the composition of some formulations, as well as sodium lauryl sulfate and polysorbate 80. As part of the study of the dissolution test, the similarity coefficient (f2) for the obtained profiles was calculated, and mathematic models were used to estimate the kinetics and mechanism of active substance release. In our work, it was observed that the inclusion of polymer Eudragit FS alone in the tablet composition ensured a modified release of the active substance for 10 h. After this time period, the amount of metronidazole determined in the acceptor fluid was 71% - 81% of the declared dose. Modification of the composition by the addition of surfactants resulted in an increased release of the active substance of up to 98%. This effect was dependent on the type of surfactant and its quantitative ratio to the Eudragit FS. Similar release profiles were obtained for tablets containing Eudragit RS and sodium lauryl sulfate, as well as Eudragit RS and polysorbate 80. Depending on the composition of tablets, metronidazole release proceeded in accordance with either first or second-order kinetics. We calculated as well, that the differing masses of Eudragit FS in the studied formulations correlates with the order of release kinetics (p < 0.002). Such an effect was validated using the Weibull model, wherein, in all the studied formulations, the release rate was seen as a decreasing function of time. An analysis of data according to the Ritger-Peppas model and the Peppas-Sahlin model for some formulations, indicated that the mechanism of active substance release from matrix tablets is diffusion.

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Rezvani, Maryam, Maria Letizia Manca, Carla Caddeo, Elvira Escribano-Ferrer, Claudia Carbone, José Esteban Peris, Iris Usach, Octavio Diez-Sales, Anna Maria Fadda, and Maria Manconi. "Co-Loading of Ascorbic Acid and Tocopherol in Eudragit-Nutriosomes to Counteract Intestinal Oxidative Stress." Pharmaceutics 11, no. 1 (January 4, 2019): 13. http://dx.doi.org/10.3390/pharmaceutics11010013.

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The present study aimed at developing a new vesicular formulation capable of promoting the protective effect of ascorbic acid and tocopherol against intestinal oxidative stress damage, and their efficacy in intestinal wound healing upon oral administration. A pH-dependent copolymer (Eudragit® L100), a water-soluble prebiotic fibre (Nutriose® FM06), a phospholipid mixture (Lipoid S75), and two natural antioxidants (ascorbic acid and tocopherol) were combined to fabricate eudragit-nutriosomes by a simple, solvent-free procedure. The vesicles were spherical and oligolamellar, with some multicompartment structures in Eudragit-nutriosomes, small in size (~100 nm), with highly negative zeta potential. The effect of Eudragit® and Nutriose® on the stability on storage and in simulated gastrointestinal fluids were confirmed by the Turbiscan® technology and in vitro studies, respectively. Eudragit-nutriosomes exhibited a protective effect against H2O2-induced oxidative stress, and a proliferative effect in Caco-2 cells, as they provided the closure of the scratched area after 96 h of incubation.

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Thireesha, Bannaravuri, Ayya Rajendra Prasad, and Haroled Peter P L. "FORMULATION AND EVALUATION OF LORNOXICAM MICROSPONGES USING EUDRAGIT RS 100 AND EUDRAGIT RSPO." Asian Journal of Pharmaceutical and Clinical Research 11, no. 10 (October 7, 2018): 217. http://dx.doi.org/10.22159/ajpcr.2018.v11i10.26861.

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Objective: The objective of the present study was preparation and evaluation of lornoxicam microsponges to prolong their drug release up to 12 h for effective osteoarthritis, rheumatoid arthritis, and acute lumbar-sciatica therapy.Methods: Lornoxicam microsponges were prepared by the quasi-emulsion solvent diffusion technique using different concentrations of polymers such as Eudragit RS 100 and Eudragit RSPO in ethanol and dichloromethane organic solvent mixture. Microsponges were evaluated for their particle size, percentage yield, entrapment efficiency, scanning electron microscopy (SEM), and in vitro drug release studies.Results: The percentage yield, entrapment efficiency, average particle size, and in vitro drug release for optimized formulation F12 were found to be 70.23% w/w, 81.34% w/w, 172.72 μm, and 96.64% up to 8 h, respectively. From SEM, it was observed that microsponges were found to be spherical in shape with rough surface texture. The formulation F12 shows zero-order release kinetics with an r2 value of 0.961 and the value of Korsmeyer–Peppas model was found to be 0.792; it follows super case II non-Fickian diffusion. The in vitro drug release studies showed that formulations comprised varying concentrations of Eudragit RSPO in higher proportion exhibited much-retarded drug release as compared to formulations comprised a higher proportion of varying concentrations of Eudragit RS 100.Conclusion: Among all the formulations F12 shows better results, which are released more than 80% of the drug release within 8 h; hence, it is optimized. These developed microsponges are releasing the drug for a longer period, which will be effective for osteoarthritis, rheumatoid arthritis, and acute lumbar sciatica therapy.

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Rajesh, Katta, R. Deveswaran, S. Bharath, and B. V. Basavaraj. "DEVELOPMENT OF MESALAZINE MICROSPHERES FOR COLON TARGETING." International Journal of Applied Pharmaceutics 9, no. 4 (July 13, 2017): 1. http://dx.doi.org/10.22159/ijap.2017v9i4.17326.

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Objective: The present work was aimed at preparation of mesalazine microspheres by a non-aqueous solvent evaporation method using eudragit S 100 and eudragit L 100 as pH dependent polymers for colon targeting.Methods: The ratio of drug to polymer was varied and the effect of formulation variables revolutions per minute (RPM) (1000, 1500, 2000 and 2500) and concentration of span 80 (1%, 1.5%, 2% and 2.5%) were studied. Prepared microspheres were evaluated for particle size, percent drug entrapment, granular analysis, in vitro drug release studies, Fourier transformed infrared spectroscopy (FT-IR) Differential Scanning Calorimetry (DSC), X-ray diffraction (XRD) and scanning electron microscopy (SEM) studies.Results: Particle size has decreased and percent drug entrapment had increased with increase in RPM in all formulations. When the span 80 concentration increased, the particle size of the microsphere formulations increased and percent drug entrapment decreased in eudragit S 100 microspheres; whereas in eudragit L 100 microspheres, as the concentration of span 80 increased, the particle size of the microsphere formulations decreased. The prepared microspheres sustained the drug release over a period of 12 h.Conclusion: Thus eudragit S 100 and eudragit L 100 microspheres could constitute a promising approach for colon-specific and sustained delivery of mesalazine for the treatment of inflammatory bowel disease.

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Shaikh, M. S. "Double Coated Tablets of Nimesulide for Colon Targeting." International Journal of Pharmaceutical Sciences and Nanotechnology 3, no. 2 (August 31, 2010): 1000–1005. http://dx.doi.org/10.37285/ijpsn.2010.3.2.14.

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The present study was aimed at developing oral colon targeted drug delivery system for Nimesulide utilizing recently designed and patented system called CODESTM, which consisted of a lactulose containing core overcoated with both Eudragit E and Eudragit L designed to rapidly disintegrate in the colon, in order to give a new life for an existing banned drug. CODESTM tablets were prepared by tabletting Nimesulide and lactulose, followed with film coating of Eudragit. The prepared tablets were evaluated on the basis of in vitro dissolution study and in vivo disintegration study was performed by gamma scintigraphic evaluation in rats. The onset of Nimesulide release was found to dependent on the coating level of Eudragit E, and at Eudragit E coating level of 8% (coating weight gain), the onset of in vitro drug release was found to be optimum. When the same was subjected on scintigraphic evaluation for in vivo disintegration study, there was a reasonable agreement between the in vitro/in vivo data. It is concluded that Nimesulide can be targeted to hindgut by a novel approach of CODESTM.

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Mooranian, Armin, Corina Mihaela Ionescu, Daniel Walker, Melissa Jones, Susbin Raj Wagle, Bozica Kovacevic, Jacqueline Chester, et al. "Single-Cellular Biological Effects of Cholesterol-Catabolic Bile Acid-Based Nano/Micro Capsules as Anti-Inflammatory Cell Protective Systems." Biomolecules 12, no. 1 (January 4, 2022): 73. http://dx.doi.org/10.3390/biom12010073.

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Recent studies in our laboratories have shown promising effects of bile acids in ➀ drug encapsulation for oral targeted delivery (via capsule stabilization) particularly when encapsulated with Eudragit NM30D® and ➁ viable-cell encapsulation and delivery (via supporting cell viability and biological activities, postencapsulation). Accordingly, this study aimed to investigate applications of bile acid-Eudragit NM30D® capsules in viable-cell encapsulation ready for delivery. Mouse-cloned pancreatic β-cell line was cultured and cells encapsulated using bile acid-Eudragit NM30D® capsules, and capsules’ images, viability, inflammation, and bioenergetics of encapsulated cells assessed. The capsules’ thermal and chemical stability assays were also assessed to ascertain an association between capsules’ stability and cellular biological activities. Bile acid-Eudragit NM30D® capsules showed improved cell viability (e.g., F1 < F2 & F8; p < 0.05), insulin, inflammatory profile, and bioenergetics as well as thermal and chemical stability, compared with control. These effects were formulation-dependent and suggest, overall, that changes in ratios of bile acids to Eudragit NM30D® can change the microenvironment of the capsules and subsequent cellular biological activities.

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Burapapadh, Kanokporn, Napat Wattanakhejorn, Panitsupa Sukpipat, Sirapa Promchuay, Thicha Phengpinit, and Phennapha Saokham. "A Comparative Study on the Effect of Hydroxypropyl Methylcellulose F4M and Eudragit^® E PO on the Physicochemical Properties of Taste-Masking Microparticles." Key Engineering Materials 859 (August 2020): 15–20. http://dx.doi.org/10.4028/www.scientific.net/kem.859.15.

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The objective of this study was to investigate the effect of polymers and their content level on the taste-masking efficiency of spray-dried microparticles. Diclofenac sodium (DS) was used as a model drug, owing to its bitter taste. Hydroxypropyl methylcellulose F4M (HPMC F4M) and Eudragit® E PO were involved in the study as a hydrophilic and a pH-responsive polymer, respectively. The taste-masked DS microparticles with the drug:polymer ratios of 1:1, 1:2 and 1:4 were prepared by the spray-drying technique. The collapsed hollow sphere HPMC F4M based-microparticles was observed meanwhile spray-dried Eudragit® E PO based-microparticles were spherical. Loading capacity of both polymer based-microparticles decreased regarding to the increment of drug:polymer ratio. The Eudragit® E PO based-microparticle in the ratio of 1:4 provided the highest loading efficiency as 91.97%. According to the simplified dissolution testing, the taste-masking ability of HPMC F4M and Eudragit® E PO based-microparticles increased upon the increase of drug:polymer ratio. Drug release at the first 5 minutes from dissolution profiles, tested by type II dissolution apparatus, of the Eudragit® E PO based-microparticles was delayed compared to HPMC F4M based-microparticles. Therefore, it could be assumed that Eudragit® E PO was a promising taste-masking polymer for DS with a pleasant taste.

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Gong, Mingcheng, Zhenhua Chen, Liangliang Zhou, Feng Gao, Jianxin Cheng, and Wanqing Zou. "Application of Mesoscale Simulation to Explore the pH Response of Eudragit S100 Used as the Novel Colon-Targeted Powder of Pulsatilla Saponin D." Journal of Nanomaterials 2021 (December 1, 2021): 1–10. http://dx.doi.org/10.1155/2021/9556911.

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As a pH-sensitive nanomaterial, Eudragit S100 has good colon targeting. However, little research has been carried out on its mesoscopic scale. In this paper, the self-assembly behavior of Pulsatilla saponins D (PSD) and Eudragit S100, as well as the loading and release mechanism of PSD, was investigated via computer simulations. The effects of the self-assembly characteristics of PSD and Eudragit S100 in the dry powder state on the drug-carrier ratio were explored by the coarse-grained molecular dynamics (CGMD) method. According to the pH-responsive feature of Eudragit S100, the drug protection under gastric pH conditions and release in colonic pH conditions were simulated through the dissipative particle dynamics (DPD) method, which has provided insights into the microscopic morphological changes in the pH-sensitive drug delivery systems.

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Sonje, Abhijit, and Amrish Chandra. "COMPREHENSIVE REVIEW ON EUDRAGIT POLYMERS." International Research Journal of Pharmacy 4, no. 5 (May 28, 2013): 71–74. http://dx.doi.org/10.7897/2230-8407.04515.

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Thakral, Seema, Naveen K. Thakral, and Dipak K. Majumdar. "Eudragit®: a technology evaluation." Expert Opinion on Drug Delivery 10, no. 1 (October 26, 2012): 131–49. http://dx.doi.org/10.1517/17425247.2013.736962.

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Boeris, Valeria, Laura Verónica Cappella, Gisele Peres, Inés Burgos, Nádya Pesce da Silveira, Gerardo Fidelio, and Guillermo Picó. "Chymotrypsin — Eudragit® complex formation." Biotechnology and Bioprocess Engineering 18, no. 3 (June 2013): 538–45. http://dx.doi.org/10.1007/s12257-012-0553-9.

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Kriplani, Priyanka, and Kumar Guarve. "Eudragit, a Nifty Polymer for Anticancer Preparations: A Patent Review." Recent Patents on Anti-Cancer Drug Discovery 17, no. 1 (February 2022): 92–101. http://dx.doi.org/10.2174/1574892816666211013113841.

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Background: Polymers are the backbone of modern pharmaceutical formulations and drug delivery technologies. Polymers that may be natural, synthetic, or semisynthetic are used to control the release of drugs in a pre-programmed fashion. The drug delivery systems are mainly prepared to enhance the bioavailability, site-specific release, sustained release, controlled release, i.e., to modify the release of drug from dosage form may be a tablet, capsule, etc. Objective: The objective of the present study is to overview the recent patents concerning the application of eudragit in the prevention of cancer and other ailments. Eudragit polymers are polymethacrylates and may be anionic, cationic, or non-ionic polymers of methacrylic acid, dimethylaminoethyl methacrylates, and methacrylic acid esters in varying ratios. Eudragit is available in various grades with solubilities at different pH, thus helping the formulators design the preparation to have a well-defined release pattern. Method: In this review, patent applications of eudragit in various drug delivery systems employed to cure mainly cancer are covered. Results : Eudragit has proved its potential as a polymer to control the release of drugs as coating polymer and formation of the matrix in various delivery systems. It can increase the bioavailability of the drug by site-specific drug delivery and can reduce the side effects/toxicity associated with anticancer drugs. Conclusion: The potential of eudragit to carry the drug may unclutter novel ways for therapeutic intercessions in various tumors.

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Jain, Sunil Kumar, Akhlesh K. Jain, and Kuldeep Rajpoot. "Expedition of Eudragit® Polymers in the Development of Novel Drug Delivery Systems." Current Drug Delivery 17, no. 6 (August 6, 2020): 448–69. http://dx.doi.org/10.2174/1567201817666200512093639.

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Eudragit® polymer has been widely used in film-coating for enhancing the quality of products over other materials (<i>e.g</i>., shellac or sugar). Eudragit® polymers are obtained synthetically from the esters of acrylic and methacrylic acid. For the last few years, they have shown immense potential in the formulations of conventional, pH-triggered, and novel drug delivery systems for incorporating a vast range of therapeutics including proteins, vitamins, hormones, vaccines, and genes. Different grades of Eudragit® have been used for designing and delivery of therapeutics at a specific site <i>via</i> the oral route, for instance, in stomach-specific delivery, intestinal delivery, colon-specific delivery, mucosal delivery. Further, these polymers have also shown their great aptitude in topical and ophthalmic delivery. Moreover, available literature evidences the promises of distinct Eudragit® polymers for efficient targeting of incorporated drugs to the site of interest. This review summarizes some potential researches that are being conducted by eminent scientists utilizing the distinct grades of Eudragit® polymers for efficient delivery of therapeutics at various sites of interest.

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Soares, Luciana Arantes, and Eduardo Crema. "Study of a delayed-release system for hard and soft capsules coated with eudragit® s100 acrylic polymers." Acta Scientiarum. Health Sciences 42 (March 10, 2020): e48422. http://dx.doi.org/10.4025/actascihealthsci.v42i1.48422.

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The objective of this study was to evaluate a pH-dependent system of ileocolonic release of active ingredients using the polymer Eudragit® S100. A spouted bed was used in the coating process of soft capsules containing palm oil and of hard capsules containing glutamine under standardised experimental conditions. The height and diameter of the palm oil and glutamine capsules were measured using a calliper. The following variables were analysed: Eudragit® S100 dispersion amount used in the capsule coating process, nozzle air pressure, nozzle air flow rate, spray rate and temperature of the spouted bed coating process. The Eudragit® S100 dispersion formulation, trademarked as Quickstart® by Evonik Industries, was used with modifications to prepare the enteric coating. The results showed that the adequate temperature for the spouted bed coating process was 50°C and that 0.2 mL of 6.5% Eudragit® S100 coating per cm2 capsule was resistant for 60 minutes at pH 6.8. The findings demonstrate the pharmaceutical application of Eudragit® S100 in the modification of the coating and the preparation of a delayed-release system of hard and soft capsules, thus enabling ileal release of active ingredients.

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Šveikauskaitė, Indrė, and Vitalis Briedis. "Effect of Film-Forming Polymers on Release of Naftifine Hydrochloride from Nail Lacquers." International Journal of Polymer Science 2017 (2017): 1–7. http://dx.doi.org/10.1155/2017/1476270.

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The successful topical therapy of onychomycosis depends on effective drug release and penetration into nail, which can be achieved by using an adequately developed delivery system. This study evaluated and compared effect of film-forming polymers Eudragit RL100, Eudragit RS100, and ethyl cellulose on naftifine hydrochloride release from experimental nail lacquer formulations. Quality of formulations was evaluated by determining drying time and water resistance. Interactions between active pharmaceutical ingredient and excipients were investigated using microcalorimetry and FT-IR. Optimization of nail lacquer formulations was performed by naftifine hydrochloride release testing. Release of naftifine hydrochloride increased with increasing concentration of Eudragit RL100. Plasticizer triacetin affected the release of naftifine hydrochloride, when Eudragit RS100 polymer was used. Ethyl cellulose polymer was determined to be not applicable for naftifine hydrochloride nail lacquer formulations. Two compositions of nail lacquers were optimized and could be used in further development of transungual delivery systems.

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Kumar, Sahoo Sunit, Baurahari Behury, and Patil Sachinkumar. "Formulation and Evaluation of Transdermal Patch of Stavudine." Dhaka University Journal of Pharmaceutical Sciences 12, no. 1 (September 2, 2013): 63–69. http://dx.doi.org/10.3329/dujps.v12i1.16302.

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Stavudine has the half life of 1 to 1.5 hour and bioavailability in the body is 86% due to first-pass metabolism. The dose of stavudine is 40 mg two to three times daily depending on weight and gender; hence, it requires frequent dosing. Transdermal patch of stavudine was prepared to sustain the release and improve bioavailability of drug and patient compliance. Different formulations were prepared by using different concentrations of Eudragit RS 100 and Eudragit RL 100. The prepared formulations were evaluated for various parameters like weight, thickness, drug content, percentage moisture content, percentage moisture uptake, tensile strength, folding endurance, In vitro drug release and in vitro permeation studies. Also these patches were characterized by Field Emission Scanning Electron Microscopy and Fourier transforms Infrared Spectrosphotometry (FTIR). All formulations have shown 0 % constriction of the patches indicating 100% flatness of the transdermal patches. Thus, these formulations can maintain a smooth and uniform surface when they are functional onto skin. The folding endurance values of patches showed optimum flexibility of the patches. The moisture content and moisture uptake in the formulations of transdermal patch was found to be increased by increase in the concentration of Eudragit RS 100 and decreasing the concentration of Eudragit RL 100. FTIR study has shown absence of any interaction of the drug with the excipients. As concentration of Eudragit RL100 increased and subsequently the concentration of Eudragit RS100 decreased, the drug release was enhanced. Dhaka Univ. J. Pharm. Sci. 12(1): 63-69, 2013 (June) DOI: http://dx.doi.org/10.3329/dujps.v12i1.16302

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Gaware, Ravi U., Sujit T. Tambe, Shankar M. Dhobale, and Suresh L. Jadhav. "Formulation and in-vitro evaluation of theophylline sustained release tablet." Journal of Drug Delivery and Therapeutics 9, no. 1-s (February 15, 2019): 48–51. http://dx.doi.org/10.22270/jddt.v9i1-s.2252.

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The aim of present study was to prepare sustained release tablet of Theophylline so as to prolong its elimination time and at the same time to keep cost of the formulation minimum. In this study ethyl cellulose and Eudragit are used in the formulation to sustain the release of Theophylline. Ethyl cellulose and Eudragit are added at the granulation step to form a sustained release coating around each granule. Different batches were designed one after another on trial and error basis to get the optimum drug release upto 12 hours. Keywords: Theophylline, ethyl cellulose, Eudragit, sustained release, coating, tablet.

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Pyar, Hassan, and Kok-Khiang Peh. "Enteric coating of granules containing the probiotic Lactobacillus acidophilus." Acta Pharmaceutica 64, no. 2 (June 1, 2014): 247–56. http://dx.doi.org/10.2478/acph-2014-0011.

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Abstract In the present study, a capsule formulation composed of enteric coated granules of Lactobacillus acidophilus ATCC 4962 was developed using Eudragit L30D-55 as enteric polymer. Optimization of the capsule formulation was achieved with a maximum viable cell count after 2 h of incubation in acid medium and disintegration time of 1 h in buffer pH 6.8. The amount of Eudragit L30D-55 in the capsules correlated with gastric juice resistance. The best protective qualities against artificial gastric juice were observed when capsules were prepared from granules composed of L. acidophilus, corn starch, lactose monohydrate, polyvinylpyrrolidone and coated with 12.5 % (m/V) of Eudragit L30D-55. Capsule formulation of L. acidophilus in edible broth medium suspension serves as a cheap alternative to the expensive freeze-drying procedure for preparing L. acidophilus. In addition, the enteric coating using Eudragit L30D-55 could protect probiotics from the acidic gastric environment and enhance the bioactivity of probiotics along with replacement of pathogenic microbes in human intestine

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B., Baloǧlu, and Kirkaǧaçhoǧlu O. "Preparation and evaluation of tolmetin sodium conventional and sustained-release suppositories." Scientia Pharmaceutica 70, no. 1 (February 14, 2002): 77–86. http://dx.doi.org/10.3797/scipharm.aut-02-09.

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Conventional suppositories of tolmetin sodium were prepared by using two different types of Witepsol as an oily base and two different ratios of polyethylene glycol 400: polyethylene glycol 4000 as an water-soluble base. In addition, sustained- release suppositories were prepared by adding Eudragit L-100 ta the suppositories. The effects of the suppository base and the ratios of the polyethylene glycol 400: polyethylene glycols 4000 on the in vitro release characteristics were investigated. The release rate of tolmetin sodium from the conventional suppositories prepared with polyethylene glycol was slower than the other suppositories prepared with Witepsol. All of the suppositories with Eudragit L-100 showed slow-release profiles and the drug release rates clearly depended on the Eudragit L-100 content. When dissolution results were evaluated kinetically, zero order kinetic was observed with the sustained- release suppositories of tolmetin sodium prepared with polyethyleneglycol 400: polyethyleneglycol 4000 by adding Eudragit L-100.

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Nernplod, Tassanee, Prasert Akkaramongkolporn, and Pornsak Sriamornsak. "Preparation of Eudragit^® L Beads for Intragastric Floating Drug Delivery." Advanced Materials Research 1060 (December 2014): 79–82. http://dx.doi.org/10.4028/www.scientific.net/amr.1060.79.

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The aim of this study was to prepare matrix beads made of enteric polymer, Eudragit® L, metronidazole and various amounts of cetyl alcohol (0, 0.1 and 1%). Eudragit® L, metronidazole and cetyl alcohol were dissolved in acetone and then extruded into dichloromethane. The influence of amount of cetyl alcohol on floating and drug release behavior of matrix beads of Eudragit® L was investigated. The results showed that, after extruding, cetyl alcohol dissolved out from the beads already formed, resulting in a porous structure. Thus, the beads can float in simulated gastric fluid for more than 8 hours. Different amounts of cetyl alcohol had a slight effect on the drug release. However, the increased amount of cetyl alcohol in the formulations significantly sustained the drug release while the beads remained floating. The results suggest that Eudragit® L beads could be used as a carrier for intragastric floating drug delivery.

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Pandav, Satish, and Jitendra Naik. "Preparation and In Vitro Evaluation of Ethylcellulose and Polymethacrylate Resins Loaded Microparticles Containing Hydrophilic Drug." Journal of Pharmaceutics 2014 (April 10, 2014): 1–5. http://dx.doi.org/10.1155/2014/904036.

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Objective. The purpose of the recent study was to prepare and estimate sustained release of Ethylcellulose (300 cps) and Eudragit (RS 100 and RL 100) microparticles containing Propranolol hydrochloride used as a treatment of cardiovascular system, especially hypertension. Method. Propranolol hydrochloride was microencapsulated with different polymers (Ethylcellulose, Eudragit RS, and Eudragit RL) using modified hydrophobic (O/O) solvent evaporation method using 1 : 1 combination of acetone and isopropanol as the internal phase. Obtained microparticles were showing higher batch yield with higher encapsulation efficiency. Microparticles were prepared with different ratios of 1 : 1, 1 : 3, 1 : 5, and 1 : 7 (%, wt/wt) using span 80 (%, v/v) as a surfactant. Results. The influence of formulation factors like drug: polymer ratio, internal phase, and type of polymers on obtained microparticles was characterized with respect to particle size distribution, encapsulation efficiency, percentage yield, FTIR, and FE-SEM. Higher encapsulation efficiencies were obtained with various polymers like Ethylcellulose (96.63 ± 0.5) compared to Eudragit RS 100 (83.70 ± 0.6) and RL 100 (89.62 ± 0.6). The in vitro release study was characterized by initial burst. Conclusion. The result of study displays that Ethylcellulose and Eudragit loaded microparticles of Propranolol hydrochloride can be effectively prepared using modified hydrophobic emulsification solvent evaporation technique. Therefore, the modified hydrophobic emulsion technique can also be applied to the preparation of microparticles for low molecular weight and highly water soluble drugs.

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Partheniadis, Ioannis, Miltiadis Toskas, Filippos-Michail Stavras, Georgios Menexes, and Ioannis Nikolakakis. "Impact of Hot-Melt-Extrusion on Solid-State Properties of Pharmaceutical Polymers and Classification Using Hierarchical Cluster Analysis." Processes 8, no. 10 (September 25, 2020): 1208. http://dx.doi.org/10.3390/pr8101208.

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The impact of hot-melt extrusion (HME) on the solid-state properties of four methacrylic (Eudragit® L100-55, Eudragit® EPO, Eudragit® RSPO, Eudragit® RLPO) and four polyvinyl (Kollidon® VA64, Kollicoat® IR, Kollidon® SR, and Soluplus®) polymers was studied. Overall, HME decreased Tg but increased electrostatic charge and surface free energy. Packing density decreased with electrostatic charge, whereas Carr’s and Hausner indices showed a peak curve dependency. Overall, HME reduced work of compaction (Wc), deformability (expressed as Heckel PY and Kawakita 1/b model parameters and as slope S′ of derivative force/displacement curve), and tablet strength (TS) but increased elastic recovery (ER). TS showed a better correlation with S′ than PY and 1/b. Principal component analysis (PCA) organized the data of neat and extruded polymers into three principal components explaining 72.45% of the variance. The first included Wc, S′ and TS with positive loadings expressing compaction, and ER with negative loading opposing compaction; the second included PY, 1/b, and surface free energy expressing interactivity with positive loadings opposing tap density or close packing. Hierarchical cluster analysis (HCA) assembled polymers of similar solid-state properties regardless of HME treatment into a major cluster with rescaled distance Cluster Combine Index (CCI) < 5 and several other weaker clusters. Polymers in the major cluster were: neat and extruded Eudragit® RSPO, Kollicoat® IR, Kollidon® SR, Soluplus®, and extruded Eudragit® L100-55. It is suggested that PCA may be used to distinguish variables having similar or dissimilar activity, whereas HCA can be used to cluster polymers based on solid-state properties and pick exchangeable ones (e.g., for sustain release or dissolution improvement) when the need arises.

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Panomsuk, Suwannee, Karnjanolarn Jarunan, Chinpongsanond Laksika, Tachasan Sirapong, and Rungruang Adchara. "Development of In Situ Film as Skin Barrier." Applied Mechanics and Materials 378 (August 2013): 190–93. http://dx.doi.org/10.4028/www.scientific.net/amm.378.190.

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In situ film or liquid plaster, a medical product for topical use, was developed using various polymers and plasticizers. The film bases were formulated and evaluated for their physical appearances, tensile properties, integrity on porcine skin, powder x-ray diffraction (PXRD) and drug release. Formulations containing Eudragit® L100 and triethyl citrate (TEC) or PEG 400 represent good films. Benzalkonium chloride (BZCl), 0.4 % w/w, was also added in these formulations as anti-infective agents. Films containing Eudragit® L100 and TEC have revealed the most suitable properties as topically applicable plaster film: good physical appearance as well as adhesion on the porcine skin. A soft and tough film was also obtained from the formulation containing Eudragit® L100 and TEC. PXRD results have shown that drug exist in amorphous form in all formulations. The percentages of drug release among three formulations within 3 hours are between 8-12%. In conclusion, formulation containing Eudragit® L100 and TEC have revealed the most suitable properties as topically applicable plaster film.

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Mestres, Júlia, Francesca Leonardi, and Klaus Mathwig. "Amperometric Monitoring of Dissolution of pH-Responsive EUDRAGIT® Polymer Film Coatings." Micromachines 13, no. 3 (February 25, 2022): 362. http://dx.doi.org/10.3390/mi13030362.

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Electrochemical sensors are powerful tools for the detection and real-time monitoring of a wide variety of analytes. However, the long-term operation of Faradaic sensors in complex media is challenging due to fouling. The protection of the electrode surface during in vivo operation is a key element for improving the monitoring of analytes. Here, we study different EUDRAGIT® controlled release acrylate copolymers for protecting electrode surfaces. The dissolution of these polymers—namely EUDRAGIT® L 30 D-55 and EUDRAGIT® FS 30 D—is triggered by a change in pH of the environment, and it is electrochemically monitored by detecting electrode access by means of a redox probe. The full dissolution of the polymer is achieved within 30 min and the electrode response indicates a complete recovery of the original electrochemical performance. We demonstrate that amperometric sensing is a practical and straightforward technique for real-time and in situ sensing of EUDRAGIT® dissolution profiles. It will find future applications in determining the protection of polymer electrode coating in real matrices and in vivo applications.

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Iswandana, Raditya, Kurnia Sari Setio Putri, Cindy Espreancelly Sandiata, Sisilia Triani, Santi Purna Sari, and Joshita Djajadisastra. "FORMULATION OF TETRANDRINE BEADS USING IONIC GELATION METHOD CA-PECTINATE COATED PH-SENSITIVE POLYMERS AS COLON-TARGETED DOSAGE FORM." Asian Journal of Pharmaceutical and Clinical Research 10, no. 10 (September 1, 2017): 90. http://dx.doi.org/10.22159/ajpcr.2017.v10i10.19994.

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Objectives Pectin, a natural polysaccharide, can be used as colon targeted drug delivery systems. Ionotropic gelation of pectin in the presence of certain divalent cations, such as calcium ions, protects drugs by producing insoluble hydrogels that can be used as a colon-targeted drug delivery carrier. In this study, calcium pectinate beads containing tetrandrine were made and were evaluated for in-vitro drug release and in-vivo study.Methods: Calcium pectinate beads were prepared by ionic gelation method with varied calcium chloride concentration (5%, 10%, and 15%). The best formula was coated with pH sensitive polymers, i.e. Eudragit L100-55, Eudragit L100, HPMCP (Hydroxypropylmethyl Cellulose Phthalate) HP-55 or CAP (Cellulose Acetate Phthalate).Results: Characterization results showed that the beads produced were quite spherical and have yellow-brownish color. After the coating process, beads were used in in-vitro drug release and targeted test. From in-vitro release study, beads coated with Eudragit L100 10% has shown good colon targeted dosage form with percent cumulative release 57.87%. This result also confirmed with the in-vivo test. Beads which were coated by Eudragit L100 10% could be found in the rat intestine.Conclusion: Formula 1 (5% calcium chloride concentration) was chosen as the best beads characterization. Formula 1C (5% beads coated with 10% Eudragit L100) showed an optimal protection from gastric acid in the in-vitro release study and able to deliver the beads to the intestine in the in-vivo targeted test.

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Mašková, Eliška, Martina Naiserová, Kateřina Kubová, Josef Mašek, Sylvie Pavloková, Martina Urbanová, Jiří Brus, Jakub Vysloužil, and David Vetchý. "Highly Soluble Drugs Directly Granulated by Water Dispersions of Insoluble Eudragit® Polymers as a Part of Hypromellose K100M Matrix Systems." BioMed Research International 2019 (March 5, 2019): 1–13. http://dx.doi.org/10.1155/2019/8043415.

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The aim of the present study was to investigate the suitability of insoluble Eudragit® water dispersions (NE, NM, RL, and RS) for direct high-shear granulation of very soluble levetiracetam in order to decrease its burst effect from HPMC K100M matrices. The process characteristics, ss-NMR analysis, in vitro dissolution behavior, drug release mechanism and kinetics, texture profile analysis of the gel layer, and PCA analysis were explored. An application of water dispersions directly on levetiracetam was feasible only in a multistep process. All prepared formulations exhibited a 12-hour sustained release profile characterized by a reduced burst effect in a concentration-dependent manner. No effect on swelling extent of HPMC K100M was observed in the presence of Eudragit®. Contrary, higher rigidity of formed gel layer was observed using combination of HPMC and Eudragit®. Not only the type and concentration of Eudragit®, but also the presence of the surfactant in water dispersions played a key role in the dissolution characteristics. The dissolution profile close to zero-order kinetic was achieved from the sample containing levetiracetam directly granulated by the water dispersion of Eudragit® NE (5% of solid polymer per tablet) with a relatively high amount of surfactant nonoxynol 100 (1.5%). The initial burst release of drug was reduced to 8.04% in 30 min (a 64.2% decrease) while the total amount of the released drug was retained (97.02%).

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Varshosaz, Jaleh, Jaber Emami, Naser Tavakoli, Mohsen Minaiyan, Nakisa Rahmani, and Farid Dorkoosh. "Development and Evaluation of a Novel Pellet-Based Tablet System for Potential Colon Delivery of Budesonide." Journal of Drug Delivery 2012 (April 22, 2012): 1–7. http://dx.doi.org/10.1155/2012/905191.

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Budesonide, a potent glucocorticoid, is used for the treatment of inflammatory bowel diseases. Current available oral formulations of budesonide have low efficacy against ulcerative colitis because of the premature drug release in the upper part of the gastrointestinal tract. In this paper a pH- and time-controlled colon-targeted pellet-based tablet of budesonide was established. Pellet cores were prepared by extrusion-spheronization method and further coated with xanthan gum (barrier layer), Eudragit NE30D and L30D55 combination (inner layer), and Eudragit FS30 (as enteric layer) sequentially to achieve the required release profile. The coated pellets then compressed into tablets using inert tabletting granules of Cellactose or Pearlitol. Release studies, performed in simulated gastric, intestinal, and colon pH were used in sequence to mimic the gastrointestinal transit. The influence of formulation variables like barrier layer thickness, inner layer composition, and enteric coat thickness on drug release were investigated and the coated pellets that contained 12% weight gain in xanthan gum layer, Eudragit L30D55 and Eudragit NE30D with a ratio of 3 : 7 in inner layer with 30% weight gain and 25% weight gain in Eudragit FS layer were found to protect the drug release in stomach and small intestine and 83.35 ± 2.4 of budesonide was released at 24 h. The drug release from the tablets prepared using 40% Cellactose 80 as tableting excipient was found to be closely similar to that of uncompressed pellets.

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Bauer, Kurt H. "Effekte von Eudragit®- und Ethylzelluloseumhüllungen." Medizinische Klinik 94, S1 (February 1999): 12–16. http://dx.doi.org/10.1007/bf03042027.

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Patra, Ch Niranjan, Richa Priya, Suryakanta Swain, Goutam Kumar Jena, Kahnu Charan Panigrahi, and Debashish Ghose. "Pharmaceutical significance of Eudragit: A review." Future Journal of Pharmaceutical Sciences 3, no. 1 (June 2017): 33–45. http://dx.doi.org/10.1016/j.fjps.2017.02.001.

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Beten, D. B., M. Gelbcke, B. Diallo, and A. J. Moës. "Interaction between dipyridamole and Eudragit S." International Journal of Pharmaceutics 88, no. 1-3 (December 1992): 31–37. http://dx.doi.org/10.1016/0378-5173(92)90301-h.

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Rahman, Md Ataur, Nusrat Ahmed, Ikramul Hasan, and Md Selim Reza. "Formulation and in vitro Assessment of Eudragit L 100 and Eudragit S 100 Based Naproxen Microspheres." Dhaka University Journal of Pharmaceutical Sciences 15, no. 1 (August 8, 2016): 47–55. http://dx.doi.org/10.3329/dujps.v15i1.29192.

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In the present study naproxen loaded microspheres were prepared by emulsification solvent evaporation method in order to achieve targeted drug delivery. Eudragit L 100 and Eudragit S 100 were used as the rate retardant polymers in the preparations. Thirteen formulations (F1-F13) were prepared using 22 factorial design by changing the concentration of these two polymers. All the formulations were evaluated for product yield, drug content, entrapment efficiency, particle size and drug release profiles. Highest drug content and entrapment efficiency were found to be 30.17% (F4) and 91.86% (F8) respectively. The particle size was found to be 159.26-234.70 ?m for all formulations. In-vitro drug release studies were performed using USP type II (Paddle) apparatus for 8 hrs in pH 7.4 phosphate buffer. The maximum drug release after 8 hrs was found to be 60.19% for batch F4. The release kinetics of all formulations were evaluated by using zero order, first order, Higuchi, Korsmeyer-Peppas, Kopcha and Hixson Crowell model. Almost all formulations fitted best with the Kopcha kinetic model. The SEM study indicated the spherical structure of the microspheres having rough surfaces.Dhaka Univ. J. Pharm. Sci. 15(1): 47-55, 2016 (June)

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47

Cetin, Meltem, Alptug Atila, Selma Sahin, and Imran Vural. "Preparation and characterization of metformin hydrochloride loaded-Eudragit®RSPO and Eudragit®RSPO/PLGA nanoparticles." Pharmaceutical Development and Technology 18, no. 3 (August 24, 2011): 570–76. http://dx.doi.org/10.3109/10837450.2011.604783.

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48

Goto, Shigeru, Masakazu Kawata, Tatsuya Suzuki, Nak-Seo Kim, and Chikage Ito. "Preparation and Evaluation of Eudragit Gels. I: Eudragit Organogels Containing Drugs as Rectal Sustained-Release Preparations." Journal of Pharmaceutical Sciences 80, no. 10 (October 1991): 958–61. http://dx.doi.org/10.1002/jps.2600801011.

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49

Ali, Asgar, Nitin Kumar, Abdul Ahad, Mohd Aqil, and Yasmin Sultana. "Enhanced delivery of diclofenac diethylamine loaded Eudragit RL 100® transdermal system against inflammation." Journal of Polymer Engineering 35, no. 7 (September 1, 2015): 699–708. http://dx.doi.org/10.1515/polyeng-2014-0352.

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Abstract A transdermal therapeutic system (TTS) of diclofenac diethylamine (DDE) was developed to obtain a prolonged controlled drug delivery by the solvent evaporation technique. The matrix diffusion controlled systems used various combinations of hydrophilic (polyvinylpyrrolidone K30) and lipophilic (Eudragit RL 100® and Eudragit RS 100®) polymers containing dimethyl sulfoxide (DMSO) (0, 5 and 10% w/w) as a penetration enhancer. In vitro drug release was improved with an increased fraction of hydrophilic polymer. Formulation F8 containing Eudragit RL 100® and polyvinylpyrrolidone K30 in the ratio 40:60 presented the highest drug release (92.45%) and permeation rate (0.0988±0.010 mg/cm2/h) with sustained release action for 48 h. In vivo pharmacodynamic study of DDE-loaded Eudragit RL 100® transdermal system (formulation F8) showed significant higher percent inhibition of rat paw edema compared with the marketed formulation of the drug. Our results suggest that a developed formulation is an efficient system for transdermal diclofenac delivery against inflammation. The optimized formulation was found to be stable and did not show physicochemical interaction. The system is envisaged to be stable for a sufficiently long period (2.52 years) at room temperature.

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50

Hasan, Ikramul, Shovan Paul, Sharmin Akhter, Navid Jubaer Ayon, and Md Selim Reza. "Evaluation and Optimization of Influence of Permeability Property and Concentration of Polymethacrylic Polymers on Microspheres of Metformin HCl." Dhaka University Journal of Pharmaceutical Sciences 12, no. 2 (January 12, 2014): 131–41. http://dx.doi.org/10.3329/dujps.v12i2.17611.

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Metformin HCl microspheres were prepared with the aim of increasing its bioavailability and decreasing gastrointestinal side effects by means of sustained action. Eudragit RSPO and Eudragit RLPO, polymers of different permeability characteristics were used to prepare different microspheres. Emulsification solvent evaporation technique using acetone as the internal phase and liquid paraffin as the external phase was the method of choice. Six formulations were prepared using two polymers. The effect of drug loading and polymeric property on the surface morphology, entrapment efficiency, particle size and release characteristics of the microspheres were examined. FTIR and DSC studies established compatibility of the drug with the polymers. SEM studies clearly revealed the effect of drug loading and polymeric nature on the surface morphology of the microspheres. Entrapment efficiencies were within 77.09-97.11% and particle size of all the batches were in the acceptable range. Release data were treated with different mathematical kinetic models. The drug release profile showed that Eudragit RSPO and Eudragit RLPO have opposite effect on drug release. On the other hand, increase in drug loading results in increased drug release. Kinetic modeling of in vitro dissolution profiles revealed that the drug release mechanism varies from diffusion controlled to anomalous type. Dhaka Univ. J. Pharm. Sci. 12(2): 131-141, 2013 (December) DOI: http://dx.doi.org/10.3329/dujps.v12i2.17611

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Journal articles on the topic 'Eudragit'

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