Journal articles: 'Pharmaceutical excipient'

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Bin, Liew Kai, Anand Gaurav, and Uttam Kumar Mandal. "A REVIEW ON CO-PROCESSED EXCIPIENTS: CURRENT AND FUTURE TREND OF EXCIPIENT TECHNOLOGY." International Journal of Pharmacy and Pharmaceutical Sciences 11, no. 1 (January 1, 2019): 1. http://dx.doi.org/10.22159/ijpps.2019v11i1.29265.

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There is no single-component excipient fulfills all the requisite performance to allow an active pharmaceutical ingredient to be formulated into a specific dosage form. Co-processed excipient has received much more attention in the formulation development of various dosage forms, specially for tablet preparation by direct compression method. The objective of this review is to discuss the emergence of co-processed excipients as a current and future trend of excipient technology in pharmaceutical manufacturing. Co-processing is a novel concept of combining two or more excipients that possess specific advantages that cannot be achieved using a physical admixture of the same combination of excipients. This review article discusses the advantages of co-processing, the need of co-processed excipient, general steps in developing co-processed excipient, limitation of co-processed excipient, technologies used in developing co-processing excipients, co-processed excipients in the literature, marketed products and future trends. With advantages offered by the upcoming newer combination of excipients and newer methods of co-processing, co-processed excipients are for sure going to gain attraction both from academia and pharmaceutical industry. Furthermore, it opens the opportunity for development and use of single multifunctional excipient rather than multiple excipients in the formulation.

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Patel, Rahul, James Barker, and Amr ElShaer. "Pharmaceutical Excipients and Drug Metabolism: A Mini-Review." International Journal of Molecular Sciences 21, no. 21 (November 3, 2020): 8224. http://dx.doi.org/10.3390/ijms21218224.

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Conclusions from previously reported articles have revealed that many commonly used pharmaceutical excipients, known to be pharmacologically inert, show effects on drug transporters and/or metabolic enzymes. Thus, the pharmacokinetics (absorption, distribution, metabolism and elimination) of active pharmaceutical ingredients are possibly altered because of their transport and metabolism modulation from the incorporated excipients. The aim of this review is to present studies on the interaction of various commonly-used excipients on pre-systemic metabolism by CYP450 enzymes. Excipients such as surfactants, polymers, fatty acids and solvents are discussed. Based on all the reported outcomes, the most potent inhibitors were found to be surfactants and the least effective were organic solvents. However, there are many factors that can influence the inhibition of CYP450, for instance type of excipient, concentration of excipient, type of CYP450 isoenzyme, incubation condition, etc. Such evidence will be very useful in dosage form design, so that the right formulation can be designed to maximize drug bioavailability, especially for poorly bioavailable drugs.

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Tita, Ioana Cristina, Lavinia Lupa, Bogdan Tita, Roxana Liana Stan, and Laura Vicas. "Compatibility Studies of Valsartan with Different Pharmaceutical Excipients." Revista de Chimie 70, no. 7 (August 15, 2019): 2590–600. http://dx.doi.org/10.37358/rc.19.7.7386.

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Compatibility studies between active drugs and excipients are substantial in the pharmaceutical technology. Thermal analysis has been extensively used to obtain information about drug-excipient interactions and to perform pre-formulation studies of pharmaceutical dosage forms. The objective of the present study was to evaluate the compatibility of the valsartan (VALS) with pharmaceutical excipients of common use including diluents, binders, disintegrants, lubricants and solubilising agents. Thermogravimetry (TG), derivative thermogravimetry (DTG), but especially differential scanning calorimetry (DSC) were used for a first screening to find small variations in peak temperature and/or their associated enthalpy for six drug/excipient mixtures (starch, cross caramelose sodique, microcrystalline cellulose 102, povidone K30, lactose monohydrate and magnesium stearate), which indicate some degree of interaction. Additional methods using Fourier transformed infrared spectroscopy (FT-IR) and X-ray powder diffraction (XRPD) confirmed the incompatibility of VALS with starch, povidone K30, lactose monohydrate and magnesium stearate. Those excipients should be avoided in the development of solid dosage forms.

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Santos, Ana, Francisco Veiga, and Ana Figueiras. "Dendrimers as Pharmaceutical Excipients: Synthesis, Properties, Toxicity and Biomedical Applications." Materials 13, no. 1 (December 21, 2019): 65. http://dx.doi.org/10.3390/ma13010065.

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The European Medicines Agency (EMA) and the Current Good Manufacturing Practices (cGMP) in the United States of America, define excipient as the constituents of the pharmaceutical form other than the active ingredient, i.e., any component that is intended to furnish pharmacological activity. Although dendrimers do not have a pharmacopoeia monograph and, therefore, cannot be recognized as a pharmaceutical excipient, these nanostructures have received enormous attention from researchers. Due to their unique properties, like the nanoscale uniform size, a high degree of branching, polyvalency, aqueous solubility, internal cavities, and biocompatibility, dendrimers are ideal as active excipients, enhancing the solubility of poorly water-soluble drugs. The fact that the dendrimer’s properties are controllable during their synthesis render them promising agents for drug-delivery applications in several pharmaceutical formulations. Additionally, dendrimers can be used for reducing the drug toxicity and for the enhancement of the drug efficacy. This review aims to discuss the properties that turn dendrimers into pharmaceutical excipients and their potential applications in the pharmaceutical and biomedical fields.

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Sopyan, Iyan, and Rizka Guntina Khairunisa. "Mini Review : Sedem System as a Tool to Characterize Excipients in Solid Dosage Form." Indonesian Journal of Pharmaceutics 3, no. 1 (March 20, 2021): 20. http://dx.doi.org/10.24198/idjp.v3i1.34038.

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SeDem System is a new system that can be applied in solid dosage form preformulation studies of medicines. It have parameters to evaluates critical quality attributes of materials that have an impact on final drug product’s quality. SeDeM studies could be used as a method for identifying the best excipient and calculating the maximum amount of excipient required for formulation. SeDeM method can , providing formulation with the lowest amount of excipients as it combines the Active Pharmaceutical Ingredients (API) with only one excipient and the standard formula of lubricants, thus avoiding the used of unnecessary excipients, such as diluents, binders and agglutinants. The information given by the SeDeM system contributes to a quality by drug design development.Keywords: SeDeM System, Excipients

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Patel, Jalpa, and Dhaval Mori. "Application of 32 Full Factorial Design and Desirability Function for Optimizing The Manufacturing Process for Directly Compressible Multi-Functional Co-Processed Excipient." Current Drug Delivery 17, no. 6 (August 6, 2020): 523–39. http://dx.doi.org/10.2174/1567201817666200508094743.

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Background: Developing a new excipient and obtaining its market approval is an expensive, time-consuming and complex process. Compared to that, the co-processing of already approved excipients has emerged as a more attractive option for bringing better characteristic excipients to the market. The application of the Design of Experiments (DoE) approach for developing co-processed excipient can make the entire process cost-effective and rapid. Objective: The aim of the present investigation was to demonstrate the applicability of the DoE approach, especially 32 full factorial design, to develop a multi-functional co-processed excipient for the direct compression of model drug - cefixime trihydrate using spray drying technique. Methods: The preliminary studies proved the significant effect of atomization pressure (X1) and polymer ratio (microcrystalline cellulose: mannitol - X2) on critical product characteristics, so they were selected as independent variables. The angle of repose, Carr’s index, Hausner’s ratio, tensile strength and Kuno’s constant were selected as response variables. Result: The statistical analysis proved a significant effect of both independent variables on all response variables with a significant p-value < 0.05. The desirability function available in Design Expert 11® software was used to prepare and select the optimized batch. The prepared co-processed excipient had better compressibility than individual excipients and their physical mixture and was able to accommodate more than 40 percent drug without compromising the flow property and compressibility. Conclusion: The present investigation successfully proved the applicability of 32 full factorial design as an effective tool for optimizing the spray drying process to prepare a multi-functional co-processed excipient.

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Viera-Herrera, Camila, Javier Santamaría-Aguirre, Karla Vizuete, Alexis Debut, Daniel C. Whitehead, and Frank Alexis. "Microcrystalline Cellulose Extracted from Native Plants as an Excipient for Solid Dosage Formulations in Drug Delivery." Nanomaterials 10, no. 5 (May 19, 2020): 975. http://dx.doi.org/10.3390/nano10050975.

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Excipients represent the complement of the active principle in any pharmaceutical form. Their function is to provide stability, protection, and to ensure absorption of the drug and acceptability in patients. Cellulose is a conventional excipient in many pharmaceutical solid dosage products. Most of the sources used to extract microcrystalline cellulose come from cotton or wood, which are expensive and in high demand from other industries. As plants are considered the main source of excipient production, we have taken advantage of the biodiversity of Ecuador to evaluate microcrystalline cellulose extracted from borojó (Alibertia patinoi), a native plant, as an excipient for solid dosage formulations. The method of choice for tablet manufacturing was direct compression since it is a conventional fabrication method in the pharmaceutical industry. First, we performed scanning electron microscopy (SEM), Fourier-transform infrared (FTIR) spectroscopy, and X-ray diffraction (XRD) in order to compare the structure and characteristics of the extracted cellulose with two reference commercial cellulose materials. Second, we performed quality tests to evaluate the use of the isolate as an excipient including fluidity, hardness, friability, and disintegration. Compared with commercial and microcrystalline cellulose, the extracted cellulose from the native plant showed comparable characteristics and is consequently a potential excipient that could be used in the pharmaceutical industry. Last, we performed a dissolution test in which we concluded that all tablets have a short release time of active principle.

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Pituanan, Baginda Sati, and Silvia Surini. "FAST-DISINTEGRATING TABLET FORMULATION OF GINGER (ZINGIBER OFFICINALE ROSC.) EXTRACT USING COPROCESSED EXCIPIENT OF PRE-GELATINIZED CASSAVA STARCH-ACACIA GUM." International Journal of Applied Pharmaceutics 9 (October 30, 2017): 154. http://dx.doi.org/10.22159/ijap.2017.v9s1.77_84.

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Objective: Fast-disintegrating tablets (FDTs) are tablets that disintegrate and/or dissolve rapidly in the mouth, thereby helping patients who havedifficulty in swallowing tablets. Ginger extract contains gingerol and is generally known for its antiemetic property. This study aimed to obtain anduse coprocessed excipients of pre-gelatinized cassava starch (PCS) with acacia gum (AG) in FDT formulations of ginger extract.Materials and Methods: In this research, five types of PCS-AG coprocessed excipients (Co-PCS-AG) were prepared by mixed PCS and AG with thefollowing ratios mass of PCS and AG were 5:5, 6:4, 7:3, 8:2, and 9:1. The prepared Co-PCS-AG excipients were characterized in terms of morphology,particle size distribution, moisture content, pH, flow-ability properties, and swelling index. Based on the results, three types of Co-PCS-AG excipients,which were 7:3, 8:2, and 9:1, were selected for use in FDT formulation of ginger extract. The FDTs were then examined for tablet hardness, tabletfriability, wetting time, and disintegration time.Results: The results indicated that Co-PCS-AG 9:1 was ideal excipient to be used in FDT formulation, as it revealed good flow properties and swellingindex compare to the other ratios. The Co-PCS-AG excipients were formulated into tablets and evaluated. Analysis of the ginger extract FDTs revealedthat the FDT prepared using Co-PCS-AG 9:1 excipient had the best performance with tablet hardness, friability, wetting time, and disintegration timeof 0.7 kp, 2.12%, 93 seconds, and 134 seconds, respectively.Conclusions: Co-PCS-AG 9:1 excipient is a potential excipient with ideal binder, disintegrant, and filler properties for use in FDT formulation.

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Shanware, Sidhhi, Kamlesh Wadher, Jayashree Taksande, and Milind Umekar. "Lepidium sativum Linn: Applications and Pharmaceutical Excipient Properties." International Journal of ChemTech Research 13, no. 4 (2020): 374–82. http://dx.doi.org/10.20902/ijctr.2019.130406.

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Natural gums and mucilages are familiar for their medicinal and pharmaceutical excipient properties. Mucilages from plant sources are found to be very potential, interesting and valuable in development of desired pharmaceutical dosage forms. Lepidium sativum Linn (Family Cruciferae)is oe of the mucilage containing edible annual herb used to treat various human ailments.The plant possesses flavonoids, coumarins, sulphur glycosides, triterpenes, sterols and various imidazole alkaloids. Parts of plats such as leaves, fruits and seeds along with various extracts of them have different pharmaceutical activities. Lepidium sativum seeds contains large amounts of mucilaginous constituents when soaked in water and a transparent gel forms around the whole seed. It mainly consists of polysaccharides, especially cellulose and uronic acid. Recently mucilarge obtained from its seeds been explored for its excipient property in the development and design of various pharmaceutical dosage forms. This review mainly focuses on application and pharmaceutical excipients properties of mulicage of Lepidium sativum Linn.

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Iyan Sopyan, Ni Made Widya Sukma Santi, Alif Virisy Berlian, Noer Erin Meilina, Qisti Fauza, and Restu Amelia Apriyandi. "A review: Pharmaceutical excipients of solid dosage forms and characterizations." International Journal of Research in Pharmaceutical Sciences 11, no. 2 (April 3, 2020): 1472–80. http://dx.doi.org/10.26452/ijrps.v11i2.2020.

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Excipients play an important role in formulating dosage forms. Exertion is empowered to help manufacture, provide, or collect dosage forms. Although considered pharmacological, excipients may consider a drug, due to chemical or physical interactions with the composition of the drug. Excipients have many functions in pharmaceutical dosage forms, including enhancing active ingredients in dosage forms, assisting active ingredients, disintegration, lubricants, binders, and suppliers. Each excipient has different characteristics. In this review, a library of studios is provided relating to the function, function, and content of solid excipients in a solid sedan. Various choices can be used on different compositions; resulting, this difference is also different. In this example, describe the types of excipients that can be used for various components in solid preparations that can be used in the formulation of solid preparations and select the right type of excipient according to the character of the desired solid preparation. In this review also presented a method, combining in and characterizing solid excipients to see the quality. The most commonly used methods for analysis of solid excipients are flow properties, compressibility index, Hausner index ratios, and angle of repose, while the instrumentation commonly used is Fourier transform infrared spectroscopy (FTIR), H and C-Nucleo magnetic resonance (H-CNMR), Scanning electron microscopy (SEM), Particle size analysis (PSA), X-ray diffraction (XRDP) and Differential scanning calorimeter (DSC).

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Mishra, Ashwani, and A. K. Pathak. "Plasticizers: A Vital Excipient in Novel Pharmaceutical Formulations." Current Research in Pharmaceutical Sciences 7, no. 1 (May 8, 2017): 01–10. http://dx.doi.org/10.24092/crps.2017.070101.

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Amaral Silva, Daniela, Raimar Löbenberg, and Neal Davies. "Are Excipients Inert? Phenytoin Pharmaceutical Investigations with New Incompatibility Insights." Journal of Pharmacy & Pharmaceutical Sciences 21, no. 1s (April 20, 2018): 19s—31s. http://dx.doi.org/10.18433/jpps29745.

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PURPOSE: The U.S. Pharmacopeia defines excipients as substances other than the active pharmaceutic ingredient (API) that are added in a drug delivery system in order to aid in the manufacturing process and enhance stability, bioavailability, safety, effectiveness and delivery of the drug. The 1968 phenytoin intoxication outbreak in Brisbane, Australia, is a classic example of an API–excipient interaction. When administered with CaSO4 the absorption of phenytoin was reduced due to an interaction between the API and the excipient. When CaSO4 was replaced by lactose, the amount of drug absorbed was much higher, resulting in the observed intoxication. It was hypothesized that phenytoin was converted to a calcium salt prior to ingestion. The purpose of this study was to mechanistically investigate the interactions between excipients and phenytoin to confirm the hypothesis of the previous reports. METHODS: Titration experiments with phenytoin and calcium salt were performed. Isothermal micro calorimetry was used to determine incompatibilities between excipients, phenytoin and milk. NMR was used to characterize the compounds. Dissolution tests containing CaSO4, lactose or sorbitol as excipients were also performed. Both Canadian and United States of America commercially available capsules were tested with milk and water. RESULTS: The calorimeter results indicate that phenytoin sodium interacts with CaSO4 in aqueous media and the dissolution profile of CaSO4 containing capsules showed a reduced dissolution rate. In addition, phenytoin sodium also interacts with lactose through a Maillard reaction that can occur at body temperature. Likewise, commercial Phenytoin sodium products interacted with milk and the products containing lactose showed browning in water. CONCLUSION: In Canada and the USA, the reference product contains lactose as an excipient in the formulation, whereas the Canadian generic formulations do not contain lactose. Any clinical relevance of these difference has not been determined. A new incompatibility between phenytoin and lactose has been discovered and an incompatibility with calcium was confirmed, which may have implications in regard to excipients and food effects. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

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AbouDaya, Mohammed, Stephen Tomlin, and Asia N. Rashed. "P47 Extent of paediatric exposure to pharmaceutical excipients: an exploratory study." Archives of Disease in Childhood 105, no. 9 (August 19, 2020): e31.1-e31. http://dx.doi.org/10.1136/archdischild-2020-nppg.56.

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AimThe assumption that excipients are inactive therefore non-harmful to patients is a declining opinion due to raised safety concerns of excipient activity, particularly in children.1 There is limited data on the safety of excipients in children and a lack of standardisation of the risk-benefit use of excipients in the different paediatric populations.2 This study aimed to investigate the extent of excipient exposure in children taking long-term oral liquids, admitted to Hospital, and to identify whether patients could be switched to a solid alternative due to the harm posed from liquid formulations.MethodA prospective observational study conducted in a UK paediatric hospital. The electronic medication chart for hospitalised children aged 0–18 years on long-term (for ≥6 weeks) oral liquid medicines, were reviewed over a four-week period. A priority list of eight excipients (called harmful excipients) with known reported hazards was developed based on literature: propylene glycol, ethanol, parabens, benzyl alcohol, aspartame, sorbitol, polysorbate 80 and benzoic acid. The list was used to determine the extent of children exposure to the harmful excipients. Considering patient factors (age, swallowing ability, treated condition), prescribed dose and availability of solid dosage forms, the included long-term liquid medicines were assessed for a potential solid form alternative by a specialist paediatric clinical pharmacist.ResultsA total of 302 oral liquid medicine formulations prescribed for 60 patients (age range 10 days – 17 years) were included in the study, of which 68.9% (208/302) were long-term oral liquid formulations. The 208 oral liquid formulation contained a total of 1044 excipients resulted in 17.4 (± 9) excipients per patients. Majority of patients (98.3%, 59/60) were exposed to at least one harmful excipient in their medicines. Children aged 2–11 years and 6–11 years were exposed the most to harmful excipients (mean 8.2 ± 4.9 exposure per patient). Parabens (81.7%, 49/60) was the most common harmful excipient patients were exposed to, followed by sorbitol (76.7%, 46/60), ethanol (75.0%, 45/60) and propylene glycol (70.0%, 42/60). Considering patient factors, prescribed dose and availability of solid formulations, it was found that almost third of the prescribed long-term oral liquid medicines (33.0%, 68/208) could be switched to tablet or capsule forms by pharmacist without any change to the prescribed dose. While for another 3.4% (7/208) long-term liquid medicines could be switched to solid dosage forms with prescriber approval, as prescribed doses would need to be adjusted slightly.ConclusionThe study highlights the extent of excipients exposure in children on long-term oral liquid medicines, many of which could potentially be harmful. Healthcare professionals should aim to reduce the long-term risks of excipients by providing an oral solid substitute to replace oral liquid formulation, where possible, and ensuring excipients are within safe, acceptable limits.ReferencesFabiano V, Mameli C, Zuccotti GV. Paediatric pharmacology: remember the excipients. Pharmacol Res 2011;63:362–365.Buckley L, Salunke S, Thompson K, et al. Challenges and strategies to facilitate formulation development of pediatric drug products: Safety qualification of excipients. Int J Pharm 2018; 536:563–569.

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Domínguez-Robles, Stewart, Rendl, González, Donnelly, and Larrañeta. "Lignin and Cellulose Blends as Pharmaceutical Excipient for Tablet Manufacturing via Direct Compression." Biomolecules 9, no. 9 (August 28, 2019): 423. http://dx.doi.org/10.3390/biom9090423.

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Extensive efforts are being made to find alternative uses for lignin (LIG). In the present work the use of this biopolymer as excipient to prepare tablets was studied. For this purpose, LIG was combined with microcrystalline cellulose (MCC) and used as excipients to prepare directly compressed tablets containing a model drug, tetracycline (TC). The excipients contained different concentrations of LIG: 100%, 75%, 50%, 25% and 0% (w/w). Two different compression forces were used (two and five tonnes). When formulations were prepared using LIG as the only excipient, tablets were formed, but they showed lower densities and crushing strength than the ones obtained with only MCC or LIG/MCC blends. Moreover, tablets prepared using five tonnes of compression force showed TC releases ranging from 40% to 70% of the drug loading. On the other hand, the tablets prepared using two tonnes of compression force showed a faster and more efficient TC release, between 60% and 90%. The presence of LIG in the tablets modified significantly the release profile and the maximum amount of TC released. Finally, a DPPH (2,2-diphenyl-1-picrylhydrozyl) assay was performed to confirm that the presence of LIG provided antioxidant properties to the formulations. Accordingly, LIG has potential as a pharmaceutical excipient.

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Kriegel, Christina, Matthias Festag, Ravuri S. K. Kishore, Dieter Roethlisberger, and Georg Schmitt. "Pediatric Safety of Polysorbates in Drug Formulations." Children 7, no. 1 (December 20, 2019): 1. http://dx.doi.org/10.3390/children7010001.

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Polysorbates 20 and 80 are the most frequently used excipients in biotherapeutics, the safety data for which have been well documented in adults. The polysorbate content in therapeutic formulations that are administered to children, however, has been less clearly regulated or defined with regard to safety. In pediatric patients, excessive amounts of polysorbate in biotherapeutics have been linked to hypersensitivity and other toxicity-related effects. To determine safe levels of polysorbates for young patients, we have developed the progressive pediatric safety factor (PPSF), an age- and weight-based tool that estimates the amount of parenterally administered polysorbates 20 and 80 in formulations that will avoid excipient-related adverse events. Compared with existing modalities for calculating maximum acceptable doses of excipients for initial clinical trials in pediatrics, the PPSF is far more conservative, thus constituting an added margin of safety for excipient exposure in the most sensitive subpopulations—i.e., neonates and infants. Further, the PPSF may be applied to any relevant excipient, aiding pharmaceutical developers and regulatory authorities in conservatively estimating the safety assessment of a biotherapeutic’s formulation, based on excipient levels.

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Surini, Silvia, Lusiana Ariani, Kurnia Ss Putri, Hayun Hayun, and Effionora Anwar. "COPROCESSED EXCIPIENTS OF CROSSLINKED AMYLOSE AND XANTHAN GUM FOR USE IN CONTROLLED RELEASE DOSAGE FORMS." International Journal of Applied Pharmaceutics 10, no. 1 (December 20, 2018): 59. http://dx.doi.org/10.22159/ijap.2018.v10s1.13.

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Objective: This study was aimed to obtain a new excipient that can be used as a polymer matrix for the formulation of controlled release dosage forms.Methods: This study used coprocessing and crosslinking methods on amylose and xanthan gum (XG) to obtain a new excipient that can be usedfor controlled release matrix of pharmaceutical dosage forms. The coprocessing step was conducted by drum drying, and the crosslinking step wasprepared using 6 and 12% sodium trimetaphosphate (STMP). The produced novel excipients were characterized in terms of infrared (IR) spectrum,substitution degree, moisture content, swelling index, and gel strength.Results: Our results showed that amylose–XG excipients crosslinked using 6% STMP have greater gel strength and better swelling indexes thanexcipients crosslinked using 12% STMP. All coprocessed excipients exhibited no differences in their IR spectra, whereas the crosslinked excipientsdid, indicating a structural change due to the addition of phosphate groups. Crosslinking amylose–xanthan-coprocessed excipients using 6% STMPproduced degrees of substitution (DSs) of 7–8 phosphates per 100 monomeric subunits. The excipients had a moisture content of 8.21–12.85%, andthe pH of a 1% solution of excipients was 6.21–6.43. In addition, the swelling index and gel strength of the excipient where both amylose and XG werecrosslinked together Were more than 1 where only amylose was crosslinked.Conclusion: The crosslinking amylose–xanthan-coprocessed excipient using 6% STMP is more suitable for use in controlled release dosage forms,particularly when the polymer ratio is 1:1.

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Tian, Beiqian, Zhiyong Ding, Shuyi Zong, Jinyue Yang, Na Wang, Ting Wang, Xin Huang, and Hongxun Hao. "Manipulation of Pharmaceutical Polymorphic Transformation Process Using Excipients." Current Pharmaceutical Design 26, no. 21 (June 24, 2020): 2553–63. http://dx.doi.org/10.2174/1381612826666200213122302.

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Background: In the pharmaceutical field, it is vital to ensure a consistent product containing a single solid-state form of the active pharmaceutical ingredient (API) in the drug product. However, some APIs are suffering from the risk of transformation of their target forms during processing, formulation and storage. Methods: The purpose of this review is to summarize the relevant category of excipients and demonstrate the availability and importance of using excipients as a key strategy to manipulate pharmaceutical polymorphic transformation. Results: The excipient effects on solvent-mediated phase transformations, solid-state transitions and amorphous crystallization are significant. Common pharmaceutical excipients including amino acids and derivatives, surfactants, and various polymers and their different manipulation effects were summarized and discussed. Conclusion: Appropriate use of excipients plays a role in manipulating polymorphic transformation process of corresponding APIs, with a promising application of guaranteeing the stability and effectiveness of drug dosage forms.

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Barros, Ilka de Carvalho, Lécia Maria da Silva Freire, José Lamartine Soares Sobrinho, Edson Cavalcanti Silva Filho, and Lívio César Cunha Nunes. "Evaluation of the Potential of Mesocarp Babassu Powder as a Technological Excipient to Pharmaceutical Industry - Part I." Materials Science Forum 869 (August 2016): 874–79. http://dx.doi.org/10.4028/www.scientific.net/msf.869.874.

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The excipients were considered mere substances capable of facilitating and protecting the drug administration. Currently, are essential constituents, which guarantee the performance of the product and optimize the therapeutic effect. In search of a new material, the present work, wthrough a rheological study, thermal (TG / DTG) and X-ray diffraction (DRX) studies, evaluated the use of babassu mesocarp powder (MB) as technological excipient. The results of the rheological characteristics of MB as well as their granules against the microcrystalline cellulose and starch were satisfactory for use as an excipient. The thermal characteristics revealed similarity between MB, starch and cellulose, however, the greatest similarity was with the starch. The DRX data revealed that the MB has an amorphous structure similar to the structure of starch, corroborated the data obtained by TG / DTA. Therefore we conclude that the MB has favourable properties for use as an excipient in the pharmaceutical industry.

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Dzitko, Jakub, Przemyslaw Zalewski, Daria Szymanowska, Piotr Garbacki, Magdalena Paczkowska, and Judyta Cielecka Piontek. "The Influence of Excipients on the Physicochemical and Biological Properties of a Bactericidal, Labile Ester Prodrug in a Salt Form – A Case Study of Cefetamet Pivoxil Hydrochloride." JOURNAL OF ADVANCES IN CHEMISTRY 15, no. 2 (August 23, 2018): 6218–34. http://dx.doi.org/10.24297/jac.v15i2.7560.

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The article presents an innovative approach to a bactericidal drug design based on a cephem prodrug analogue – cefetamet pivoxil hydrochloride. The emergence of cefetamet pivoxil hydrochloride excipient systems (mannitol, hydroxypropyl methyl cellulose, pregelatinised starch, lactose monohydrate, magnesium stearate, polyvinylpyrrolidone) caused changes in the physicochemical properties of cefetamet pivoxil hydrochloride. They are significant for planning the development of an innovative pharmaceutical formulation. The biological activity profile of the prodrug was also modified. FTIR spectra were used to study interactions between cefetamet pivoxil hydrochloride and the excipients. The theoretical approach to the analysis of experimental spectra enabled precise indication of cefetamet pivoxil hydrochloride domains responsible for interaction with the excipients. The interactions between cefetamet pivoxil hydrochloride and the excipients resulted in some important physicochemical modifications: acceptor fluid-dependent changes in solubility and the dissolving rate as well as a decrease in the chemical stability of cefetamet pivoxil hydrochloride in the solid state, especially during thermolysis. The interactions between cefetamet pivoxil hydrochloride and the excipients also had biologically essential effects. There were changes in its permeability through artificial biological membranes simulating the gastrointestinal tract, which depended on the pH value of the acceptor solution. Cefetamet pivoxil hydrochloride combined with the excipient systems exhibited greater bactericidal potential against Staphylococcus aureus. Its bactericidal potential against Enterococcus faecalis, Pseudomonas aeruginosa and Proteus mirabilis doubled. The new approach provides an opportunity to develop treatment of resistant bacterial infections. It will enable synergy between the excipient and the pharmacological potential of an active pharmaceutical substance with modified physicochemical properties induced by the drug carrier.

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Mai, Yang, Liu Dou, Christine M. Madla, Sudaxshina Murdan, and Abdul W. Basit. "Sex-Dependence in the Effect of Pharmaceutical Excipients: Polyoxyethylated Solubilising Excipients Increase Oral Drug Bioavailability in Male but Not Female Rats." Pharmaceutics 11, no. 5 (May 10, 2019): 228. http://dx.doi.org/10.3390/pharmaceutics11050228.

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It is known that males and females respond differently to medicines and that differences in drug behaviour are due to inter-individual variability and sex specificity. In this work, we have examined the influence of pharmaceutical excipients on drug bioavailability in males and females. Using a rat model, we report that a portfolio of polyoxyethylated solubilising excipients (polyethylene glycol 2000, Cremophor RH 40, Poloxamer 188 and Tween 80) increase ranitidine bioavailability in males but not in females. The in vivo sex and excipient effects were reflected in vitro in intestinal permeability experiments using an Ussing chamber system. The mechanism of such an effect on drug bioavailability is suggested to be due to the interaction between the excipients and the efflux membrane transporter P-glycoprotein (P-gp), whose expression in terms of gene and protein levels were inhibited by the solubilising agents in male but not in female rats. In contrast, the non-polyoxyethylated excipient, Span 20, significantly increased ranitidine bioavailability in both males and females in a non-sex-dependent manner. These findings have significant implications for the use of polyoxyethylated solubilising excipients in drug formulation in light of their sex-specific modulation on the bioavailability of drugs that are P-gp substrates. As such, pharmaceutical research is required to retract from a ‘one size fits all’ approach and to, instead, evaluate the potential impact of the interplay between excipients and sex on drug effect to ensure effective pharmacotherapy.

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Gao, Rui, Yi Jin, Qing-Yi Yang, Bai-Wang Sun, and Jun Lin. "Study of stability and drug-excipient compatibility of estradiol and pharmaceutical excipients." Journal of Thermal Analysis and Calorimetry 120, no. 1 (November 1, 2014): 839–45. http://dx.doi.org/10.1007/s10973-014-4234-0.

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Caballero, ML, and S. Quirce. "Delayed Hypersensitivity Reactions Caused by Drug Excipients: A Literature Review." Journal of Investigational Allergology and Clinical Immunology 30, no. 6 (December 10, 2020): 400–408. http://dx.doi.org/10.18176/jiaci.0562.

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The European Medicines Agency (EMA) defines excipients as the constituents of a pharmaceutical form apart from the active substance. Delayed hypersensitivity reactions (DHRs) caused by excipients contained in the formulation of medications have been described. However, there are no data on the prevalence of DHRs due to drug excipients. Clinical manifestations of allergy to excipients can range from skin disorders to life-threatening systemic reactions. The aim of this study was to perform a literature review on allergy to pharmaceutical excipients and to record the DHRs described with various types of medications, specifically due to the excipients contained in their formulations. The cases reported were sorted alphabetically by type of medication and excipient, in order to obtain a list of the excipients most frequently involved for each type of medication.

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Steinberg, Marshall, and Irwin Silverstein. "The Use of Unallowed Excipients." International Journal of Toxicology 22, no. 5 (September 2003): 373–75. http://dx.doi.org/10.1177/109158180302200506.

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The laws governing the U.S. Food and Drug Administration (FDA) do not provide for the approval of stand-alone excipients. Current regulations do not permit the use of excipients, but allow their use. The acceptance process for excipients is slow and only recently did the FDA propose draft guidance for nonclinical studies for pharmaceutical excipients. The FDA has made four suggestions to the U.S. Pharmacopoeia concerning including excipient monographs in the National Formulary for excipients not yet allowed. This article reviews these four proposals to identify the proposal that is most appropriate.

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B., Uphadek, Shinkar D. M., Patil P. B., and Saudagar R. B. "MORINGA OLEIFERA AS A PHARMACEUTICAL EXCIPIENT." International Journal of Current Pharmaceutical Research 10, no. 2 (March 15, 2018): 13. http://dx.doi.org/10.22159/ijcpr.2018v10i2.25883.

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Plant gums and mucilages are being used due to their abundance in nature, safety and economy. Additives play an important role in pharmaceutical preparations like tablet, lotions, suspensions, syrups and ointments. Recent trends towards the use of the natural and nontoxic products which demand the replacement of synthetic excipients with natural ones. Moringaoleifera gum has good mucoadhesive polymer, disintegrating agent and binder. Moringa Oleiferagum show that it has high potential for industrial application especially in the food, textile and pharmaceutical industries.

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Rasheed, Shebina P., M. Shivashankar, Sanal Dev, and A. K. Azeem. "Treatment of biowaste to pharmaceutical excipient." Materials Today: Proceedings 15 (2019): 316–22. http://dx.doi.org/10.1016/j.matpr.2019.05.011.

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Chaiya, Pornsit, and Thawatchai Phaechamud. "Differential Scanning Calorimetric Analysis for Incompatibility: Sodium Stearate/Magnesium Stearate and Acidic Compounds." Key Engineering Materials 859 (August 2020): 307–12. http://dx.doi.org/10.4028/www.scientific.net/kem.859.307.

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Compatibility investigation was performed between stearate lubricants (sodium stearate and magnesium stearate) and acidic pharmaceutical compounds (ibuprofen, indomethacin and valproic acid) and citric acid as acidic pharmaceutical excipient using differential scanning calorimetry (DSC). Alteration in DSC thermogram was found in all mixtures. There was a presence of melting endothermic peak of stearic acid in all mixtures (except that of stearate lubricants and indomethacin) indicating breakage of salt form of stearate lubricants depended on the physicochemical properties of drug compounds and pharmaceutical excipient. Therefore, the avoidance for using stearate lubricants with acidic pharmaceutical compounds and excipient should be concerned in development of pharmaceutical formulations.

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Barros, Ilka de Carvalho, Lécia Maria da Silva Freire, José Lamartine Soares Sobrinho, Edson Cavalcanti Silva Filho, and Lívio César Cunha Nunes. "Development and Evaluation of Capsule of Sodium Diclofenac and Paracetamol Using Mesocarp Babassu Powder as Excipient - Part II." Materials Science Forum 869 (August 2016): 849–53. http://dx.doi.org/10.4028/www.scientific.net/msf.869.849.

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The capsules are pharmaceutical forms extremely versatile used to administer drugs orally, thus demonstrating the relevance of search for new excipients. Therefore, it was aimed to demonstrate the technological feasibility of babassu mesocarp powder (MB) as an excipient in development of diclofenac capsules 50mg and paracetamol 500 mg. Two lots of capsule were produced for each active ingredient separately using MB and microcrystalline cellulose (MC) as an excipient. The analytical results of quality control of all lots remained within the limits accepted by the Brazilian Pharmacopoeia. Although the values of dissolution time coming from lots of CM and MB, the statistical analysis revealed that lots manufactured with MB showed a profile of release superior to CM, demonstrating the potential of MB as an excipient once the lots produced with MB showed a disintegration and dissolution equivalent to those obtained with CM lots.

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Ramesh, Kanteti V. R. N. S., Hemant Yadav, and Omar Sarheed. "Safety of Pharmaceutical Excipients and Regulatory Issues." Applied Clinical Research, Clinical Trials and Regulatory Affairs 6, no. 2 (July 3, 2019): 86–98. http://dx.doi.org/10.2174/2213476x05666181105123750.

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Background:Pharmaceutical excipients are critical in the formulation of any dosage form. Not many additives employed in the drug product manufacture have properties, which meet the desired qualities that the finished product must have. Therefore, it is mandatory to mix the drug substance with other substances to overcome the deficiencies. As a result, almost all pharmaceutical products are mixtures of active pharmaceutical ingredient and additives. So, there is a compelling need of these substances and normally they occupy the major part of any drug product. Excipients are of different chemical categories that have varying physicochemical properties like solubility, miscibility and the nature and source of these materials vary. With growing number of pharmaceutical excipients and polymers, the question of evaluating their toxicity is becoming a complex issue. Many polymers and novel excipients are now available in the market and with their diverse chemical nature and different sources and presence of impurities and their adverse effects will further complicate the safety profiling of these excipients.Conclusion:This review article will discuss the unwanted biological activities of some commonly used excipients and issues of the supply of the pharmaceutical excipients that need to be highly regulated and monitored to ensure availability of quality and pure excipient compounds.

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Kirteebala Pawar, Dhawal Rajendra Shinde, Dipak Dhondu Shivgan, Sagar Namdev Sherker, Shivam Devdendra Sharma, Rishikesh Ramasare Sharma, and Smita Takarkhede. "Natural polymers in pharmaceutical drug delivery: A review." World Journal of Biology Pharmacy and Health Sciences 4, no. 3 (December 30, 2020): 082–90. http://dx.doi.org/10.30574/wjbphs.2020.4.3.0101.

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In pharmaceutical formulation two main ingredients are required which is API and excipient. And excipient contains many components which plays vital role in manufacturing of dosage form as well as improve pharmaceutical parameters of the dosage form. Polymers used in any dosage form as excipient. Polymers have influencing capacity towards drug release and should be compatible, stable, non-toxic and economic etc. Generally, polymers are classified into three categories i.e natural, semi-synthetic and synthetic polymers. Nowadays, many pharmaceutical companies inclined towards using natural polymers due to many problems created with drug release and side effects. Polymers plays various application in formulation as excipient like to provide uniform drug delivery, rate controlling agent, taste masking agent, protective and stabilizing agents, etc. So that this review discuss about various natural polymers, there advantages over synthetic polymers and role of polymers in designing drug delivery system.

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Putri, Margaretha Efa, Anis Yohana Chaerunisaa, and Marline Abdassah. "Cellulose Nanocrystals Preparation as Pharmaceuticals Excipient : a Review." Indonesian Journal of Pharmaceutics 2, no. 2 (March 4, 2020): 42. http://dx.doi.org/10.24198/idjp.v2i2.26422.

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Cellulose nanocrystals is a cellulose derivates which has been widely researched and observed as an chemical agent. Different with cellulose that has been widely used as pharmaceutical excipient especially in solid dosage form, cellulose in nanocrystals form is not available in pharmaceutical grade. Cellulose nanocrystals have different characteristics and quality which is depend on its preparation including sourcing, isolation procedure, and hydrolysis reaction involved. This difference is very important to deeply observed its impact in pharmaceutical dosage form with different active ingredients. In addition, cellulose nanocrystals should meet FDA requirement as pharmaceutical excipient. This review describe cellulose nanocrystals preparation and its characteristics, its application to active pharmaceutical ingredients, and its properties in order to meet FDA requirement.Keywords: Cellulose, nanocrystals, pharmaceutical excipient

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Gurav, Sachin B., and Neela M. Bhatia. "Assessment of Structural Compatibility of Saxagliptin in Physical Mixtures with some excipient by Using HPLC." Current Pharmaceutical Analysis 16, no. 8 (September 28, 2020): 1074–82. http://dx.doi.org/10.2174/1573412915666190617153004.

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Introduction: Saxagliptin hydrochloride is an oral hypoglycemic agent used for the treatment of type 2 diabetes mellitus. Saxagliptin is unstable because it undergoes an intra-molecular cyclisation reaction to form a cyclicamidine in both solution and solid states. In pharmaceutical development of saxagliptin it is important to select the excipients which are compatible and help to minimize the formation of cyclicamidine. In excipient compatibility study for saxagliptin it is essential to identify the formation of cyclicamidine and other related substances. Materials and Methods: In the current work, the method for quantification of saxagliptin, cyclicamidine and its related substances by high performance liquid chromatographic was developed and validated. This method was used as screening technique for assessing the compatibility of saxagliptin with some pharmaceutical excipients. These were evaluated by analyzing the pure saxagliptin and saxagliptin- excipient in physical mixture, which were stored under different conditions at 40°C/75% Relative Humidity (RH) for one month. The method was successfully validated as per ICH guidelines. Results and Conclusion: The results of compatibility study demonstrate the suitability of saxagliptin with Methocel, Polyethylene Glycol (PEG), Opadry Red, Opadry pink, Opadry white, and Opadry Pink.

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Saju, Fels, and Chinju M. Sivaraman. "Scope of herbal mucilage in pharmaceutical formulations. A review." Herba Polonica 67, no. 1 (March 1, 2021): 46–57. http://dx.doi.org/10.2478/hepo-2021-0001.

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Summary The aim of the article was to obtain maximum information about plant mucilage, its sources and applications in the pharmaceutical industry. This study focuses on the scientific articles and books available in Internet resources and college library that deal with the sources, applications, extraction and isolation of plant mucilage. Mucilage is obtained mainly from plant sources and can be isolated easily. Due to the low cost, easy availability, non-toxicity, non-irritancy, and biocompatibility, mucilage is of great demand in the field of pharmaceuticals. Hibiscus rosa-sinensis L., Trigonella foenum-graecum L., Abelmoschus esculentus L, Plantago ovata Forssk. and Aloe barbadensis L. are some common sources of mucilage. The isolation methods vary depending on the part of the plant where mucilage is present. It is commonly used as gelling agent, suspending agent, binder, and disintegrant. Since it is hydrophilic in nature, chances of deterioration are higher. In this review, different mucilage sources and their isolation methods are discussed in detail. Mucilage is used as excipient in many formulations of tablets, suspensions, gels, etc. The study explores the potential of plant mucilage as an excipient in pharmaceutical formulations. The biodegradable and biocompatible properties of this inexpensive excipient make it more favourable for the newer formulation development.

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Shur, Jagdeep, Robert Price, David Lewis, Paul M. Young, Grahame Woollam, Dilraj Singh, and Stephen Edge. "From single excipients to dual excipient platforms in dry powder inhaler products." International Journal of Pharmaceutics 514, no. 2 (December 2016): 374–83. http://dx.doi.org/10.1016/j.ijpharm.2016.05.057.

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Zupanets, Kateryna O., Sergii K. Shebeko, Kseniia L. Ratushna, and Oleksandr V. Katilov. "Cumulative Risks of Excipients in Pediatric Phytomucolytic Syrups: The Implications for Pharmacy Practice." Scientia Pharmaceutica 89, no. 3 (July 5, 2021): 32. http://dx.doi.org/10.3390/scipharm89030032.

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Expectorant phytomucolytic syrups are widely used pediatric OTC-medicines. Physicians, pediatricians, and pharmacists are traditionally concerned with the efficacy of the active ingredients in cough syrups, and rarely consider the safety aspects of excipients that however are not absolutely “inactive” and are proved to initiate some negative reactions and interactions with other drugs. This paper presents a review, categorization, and comparative analysis of the safety profile of excipients contained in the 22 best-selling OTC pediatric phytomucolytic syrups available in pharmaceutical markets in Ukraine and Germany and proposes an approach to the consideration of the excipients’ safety risks for a pharmacist in the process of pharmaceutical care. The study has revealed that only one of the twenty-two analyzed syrups does not contain any potentially harmful excipients. The results of this analysis were used for developing a specific decision tool for pharmacists that can be used for minimizing excipient-initiated reactions when delivering OTC phytomucolytic syrups for children.

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Preuss, James F., Catherine E. Goddard, Russell C. Clarke, Peter R. Platt, and Paul HM Sadleir. "Anaphylaxis to intravenous paracetamol containing povidone. A case report and narrative review of excipient allergy related to anaesthesia." Anaesthesia and Intensive Care 48, no. 5 (September 2020): 404–8. http://dx.doi.org/10.1177/0310057x20940318.

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Investigation of intraoperative anaphylaxis includes the exclusion of potential trigger agents the individual was exposed to within a plausible interval preceding the reaction. Occasionally, none of these agents will test positive. In this situation it is important to consider that excipients may be responsible for anaphylaxis, that the dilutions prepared to test the medication may not contain an appropriate concentration of the excipient to induce a positive skin reaction, or if an alternative formulation of the medication is tested, it may not contain the culprit excipient. This case describes a patient, who previously experienced an anaphylactic reaction to Betadine® (Sanofi-Aventis Australia Pty Ltd, North Ryde BC, NSW) experiencing anaphylaxis in the recovery period after general anaesthesia where Betadine was avoided. The recently administered therapeutics were excluded by skin testing, however further investigation determined that a povidone-containing formulation of paracetamol had been administered. Skin testing with povidone-containing paracetamol resulted in a positive reaction in the patient, but not in a volunteer control. Pharmaceutical excipients are added to medications to increase absorption, shelf-life and efficacy. Different brands of the same drug may contain different excipients. When testing for anaphylaxis with such compounds one must be sure the dilution is appropriate for both the parent compound and the excipient to ensure the accuracy of skin-prick and intradermal testing. This case demonstrates the potential for excipients to cause severe allergy and the importance of detailed history pertaining to previous allergic episodes as even the most unlikely of medications can potentially result in anaphylaxis due to excipients.

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Hall, C. M. "Probable adverse reaction to a pharmaceutical excipient." Archives of Disease in Childhood - Fetal and Neonatal Edition 89, no. 2 (March 1, 2004): 184F—184. http://dx.doi.org/10.1136/adc.2002.024927.

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Mullarney, Matthew P., and Bruno C. Hancock. "Mechanical property anisotropy of pharmaceutical excipient compacts." International Journal of Pharmaceutics 314, no. 1 (May 2006): 9–14. http://dx.doi.org/10.1016/j.ijpharm.2005.12.052.

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Júlio, Tamíris Amanda, Igor Fernando Zâmara, Jerusa Simone Garcia, and Marcello Garcia Trevisan. "Compatibility and stability of valsartan in a solid pharmaceutical formulation." Brazilian Journal of Pharmaceutical Sciences 49, no. 4 (December 2013): 645–51. http://dx.doi.org/10.1590/s1984-82502013000400003.

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Valsartan (VAL) is a highly selective blocker of the angiotensin II receptor that has been widely used in the treatment of hypertension. Active pharmaceutical ingredient compatibility with excipients (crospovidone, hypromellose, magnesium stearate, microcrystalline cellulose and titanium dioxide) is usually evaluated in solid pharmaceutical development. Compatibility and stability can be evaluated by liquid chromatography. Studies were performed using binary mixtures of 1:1 (w/w) VAL/excipient; samples were stored under accelerated stability test conditions (40 ºC at 75% relative humidity). The results indicate that VAL is incompatible with crospovidone and hypromellose, which reduced the VAL content and gave rise to new peaks in the chromatogram due to degradation products.

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Paul, McCague, Brennan Hilary, and Wallace Scott. "P13 Medication use and excipient exposure in paediatrics in a secondary care setting." Archives of Disease in Childhood 103, no. 2 (January 19, 2018): e1.17-e1. http://dx.doi.org/10.1136/archdischild-2017-314584.24.

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Background and aimPaediatric patients are widely exposed to a range of excipients which may cause harm to this vulnerable patient group. Legal requirement to disclose quantitative information on excipients changed in 2010,2 however, since most formulations were licensed prior to this date, there is a lack of potentially critical information available to currently practising pharmacists and clinicians. The aim of this study was to quantify excipient exposure to children in a secondary care setting.MethodA cohort study was conducted within Altnagelvin Area Hospital Paediatric Ward (Northern Ireland, Western Health and Social Care Trust) in January 2017. Medicines prescribed to patients throughout the study were recorded and exposure to ethanol, sodium benzoate and propylparaben was quantified.Exposure was then compared to proposed safe limits. Off-label and unlicensed use of medicines was assessed as a secondary aim. This study was classified as a service evaluation and ethical approval was not required.ResultsA total of 91 patients were enrolled in the study. Patient age ranged from 5 days to 15 years. The mean number of items prescribed per patient was 3.0. Analysis revealed that 75.8% of patients were exposed to ≥1 excipient of interest including ethanol, sodium benzoate and propylparabens. Excipient safety levels as proposed by the European Medicines Agency or World Health Organisation (where available) were not exceeded.Quantitative excipient information were not available for two products. There was both off-label and unlicensed use ofmedicines, with off-label prescribing (9.6%) being more common than the use of unlicensed medicines (0.4%).ConclusionThe paediatric population is exposed to potentially harmful excipients contained in commonly prescribed medicines. Although exposure within this study falls within existing safety limits, further research into paediatric specific safe exposure limits are required. It is notable that despite contacting themanufacturer, quantitative excipient information were not available for two products. Safety limits when considered together with quantitative excipient information will allow clinicians to complete an informed risk-benefit analysis for paediatric patients.ReferencesTulec C. Paediatric formulations in practice. In Costello I, Long PF, Wong IK, Tulec C, Yeung V (Ed.), Paediatric drug handling 2007:pp. 43–74. London: Pharmaceutical Press.European Commission. A guideline on summary of product characteristics [Online]2009;2:1–29. http://ec.europa.eu/health//sites/health/files/files/eudralex/vol-2/c/smpc_guideline_rev2_en.pdf [Accessed: 14th April 2017].

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Macuja, John Carlo O., Laurence N. Ruedas, and Rebecca C. Nueva España. "Utilization of Cellulose from Luffa cylindrica Fiber as Binder in Acetaminophen Tablets." Advances in Environmental Chemistry 2015 (March 31, 2015): 1–8. http://dx.doi.org/10.1155/2015/243785.

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Cellulose is an important pharmaceutical excipient. This study aimed to produce cellulose from the fiber of Luffa cylindrica as an effective binder in the formulation of acetaminophen tablets. This study was divided into three phases, namely, (I) preparation of cellulose from Luffa cylindrica, (II) determination of the powder properties of the LC-cellulose, and (III) production and evaluation of acetaminophen of the tablets produced using LC-cellulose as binder. The percentage yield of LC-cellulose was 61%. The values of the powder properties of LC-cellulose produced show fair and passable flow properties and are within the specifications of a powdered pharmaceutical excipient. The mean tablet hardness and disintegration time of the LC-cellulose tablets have a significant difference in the mean tablet hardness and disintegration time of the tablets without binder; thus the cellulose produced improved the suitability of acetaminophen in the dry compression process. However, the tablet properties of the tablets produced using LC-cellulose as binder do not conform to the specifications of the US pharmacopeia; thus the study of additional methods and excipients is recommended.

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Rouaz, Khadija, Blanca Chiclana-Rodríguez, Anna Nardi-Ricart, Marc Suñé-Pou, Dèbora Mercadé-Frutos, Josep María Suñé-Negre, Pilar Pérez-Lozano, and Encarna García-Montoya. "Excipients in the Paediatric Population: A Review." Pharmaceutics 13, no. 3 (March 13, 2021): 387. http://dx.doi.org/10.3390/pharmaceutics13030387.

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This theoretical study seeks to critically review the use of excipients in the paediatric population. This study is based on the rules and recommendations of European and American drug regulatory agencies. On the one hand, this review describes the most frequent excipients used in paediatric medicine formulations, identifying the compounds that scientific literature has marked as potentially harmful regarding the side effects generated after exposure. On the other hand, this review also highlights the importance of carrying out safety -checks on the excipients, which, in most cases, are linked to toxicity studies. An excipient in the compilation of paediatric population databases is expected to target safety and toxicity, as in the STEP database. Finally, a promising pharmaceutical form for child population, ODT (Orally Disintegrating Tablets), will be studied.

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Fawcett, T. G., S. Gates-Rector, A. M. Gindhart, M. Rost, S. N. Kabekkodu, J. R. Blanton, and T. N. Blanton. "Formulation analyses of high-volume prescription drugs." Powder Diffraction 34, no. 2 (April 23, 2019): 130–42. http://dx.doi.org/10.1017/s0885715619000253.

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A collection of 65 formulated tablets and capsules were analyzed for phase composition by full pattern matching powder diffraction methods. The collection contained 32 of the top 200 prescription drugs sold in 2016 as well as many high-volume prescriptions and over the counter drugs from prior years. The study was used to evaluate new methods of analysis as well as the efficacy of programs designed to collect references on high volume excipients and pharmaceuticals for inclusion in the Powder Diffraction File™. The use of full pattern matching methods as well as reference pattern additions of many common excipients enabled major phase excipient identification in all formulations. This included identification of crystalline, nanocrystalline, and amorphous ingredients because full pattern matching involved the use of characteristic coherent and incoherent scatter. Oftentimes identification of the major excipients significantly aided the clean identification of the active pharmaceutical ingredients (APIs) and their polymorphic form, even at low concentrations (1–10 wt. %). Overall 93% of the APIs were identified, most through a PDF®material reference, but also through patent cross-referencing and similarity analysis comparisons.

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Patel, Hetal, and Mukesh Gohel. "A Review on Enteric Coated Pellets Composed of Core Pellets Prepared by Extrusion-Spheronization." Recent Patents on Drug Delivery & Formulation 13, no. 2 (August 29, 2019): 83–90. http://dx.doi.org/10.2174/1872211313666190212115139.

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Enteric coated dosage form bypasses the stomach and releases the drug into the small intestine. Advantages of enteric coated pellets in comparison with enteric coated tablets are a) Pellets provide rapid onset of action and faster drug release due to the smaller size than tablets and b) Pellets exhibit less residence time of acid-labile drugs in the stomach compared to tablets. Dosage form coat can be damaged by longer resistance time in the stomach. The present review summarizes the current state of enteric coated pellets where core pellets are prepared by extrusion-spheronization technique and the enteric coating is applied in a fluidized bed processor. Two approaches are involved in the preparation of core pellets. In the first approach, a mixture of drug and excipient(s)/co-processed excipient is passed through extruders to prepare core pellets. In the second approach, excipient core pellets are prepared by extrusion technique and the drug is layered onto it before the enteric coating. The excipients present in the core pellets decide immediate or extended release of drug in the intestine. The coprocessed excipient pellets provide less batch variability and provide a platform for layering of many drugs before enteric coating. Some patents included enteric coating pellets [CN105456223 (A), CN105596310 (A), CN105616371 (A), CN105663095 (A), CN101611766B, CN106511862 (A), CN106668018 (A), CN106727381 (A), CN106924222 (A), TW200624127 (A), US 2017/0165248A1, US 2017/0224720A1] are discussed.

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Bazeed, Alaa Yosf, Ahmed Nouh, Ebtessam Ahmed Essa, and Gamal El Maghraby. "Hydrophilic Sugars for Enhancing Dissolution Rate of Cilostazol: Effect of Wet Co-Processing." Pharmaceutical Sciences 27, no. 1 (October 2, 2020): 111–20. http://dx.doi.org/10.34172/ps.2020.64.

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Background: Cilostazol is an anti-platelets drug with considerable antithrombotic effects in vivo. Therefore, it is widely used by elderly patients. However, it suffers from poor bioavailability due to its low aqueous solubility. The objective of this work was to enhance the dissolution of cilostazol with the aim of formulating fast dissolving tablets for geriatrics and those of swallowing difficulties. Methods: Ethanol-assisted co-grinding of cilostazol with sugar-based excipients was adopted. Sucralose and mannitol were used for this purpose as hydrophilic excipient as well as taste improving agents. The obtained products were investigated regarding differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), X-ray diffraction, scanning electron microscope (SEM) and in vitro drug dissolution. Fast disintegrating tablets were prepared and evaluated. Results: Thermal behavior of the developed products reflected reduced crystallinity, it also suggested possible existence of new crystalline species with sucralose. Eutexia was also suggested for mannitol mixtures, that was supported by X-ray diffraction data. SEM indicated size reduction with the deposition of the drug as submicron particles over the excipient surface. Co-processing markedly improved cilostazol dissolution compared to unprocessed drug. The optimized formulations were successively formulated into fast disintegrating tablets. Conclusion: This investigation introduced the wet grinding strategy with sugar excipients as a platform for the formulation of easy to use tablets with optimum drug release.

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Gebert, Mark S., and David R. Friend. "Purified Guar Galactomannan as an Improved Pharmaceutical Excipient." Pharmaceutical Development and Technology 3, no. 3 (January 1998): 315–23. http://dx.doi.org/10.3109/10837459809009859.

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Baldrick, Paul. "The safety of chitosan as a pharmaceutical excipient." Regulatory Toxicology and Pharmacology 56, no. 3 (April 2010): 290–99. http://dx.doi.org/10.1016/j.yrtph.2009.09.015.

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Martini, A., C. Torricelli, L. Muggetti, and R. De Ponti. "Use of Dehydrated Beta-Cyclodextrin as Pharmaceutical Excipient." Drug Development and Industrial Pharmacy 20, no. 15 (January 1994): 2381–93. http://dx.doi.org/10.3109/03639049409042644.

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Baldrick, Paul. "Pharmaceutical Excipient Development: The Need for Preclinical Guidance." Regulatory Toxicology and Pharmacology 32, no. 2 (October 2000): 210–18. http://dx.doi.org/10.1006/rtph.2000.1421.

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Farquharson, Amelia, Zachery Gladding, Gary Ritchie, Chetan Shende, Joseph Cosgrove, Wayne Smith, Carl Brouillette, and Stuart Farquharson. "Drug Content Uniformity: Quantifying Loratadine in Tablets Using a Created Raman Excipient Spectrum." Pharmaceutics 13, no. 3 (February 27, 2021): 309. http://dx.doi.org/10.3390/pharmaceutics13030309.

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Raman spectroscopy has proven valuable for determining the composition of manufactured drug products, as well as identifying counterfeit drugs. Here we present a simple method to determine the active pharmaceutical ingredient (API) mass percent in a sample that does not require knowledge of the identities or relative mass percents of the inactive pharmaceutical ingredients (excipients). And further, we demonstrated the ability of the method to pass or fail a manufactured drug product batch based on a calculated acceptance value in accordance with the US Pharmacopeia method for content uniformity. The method was developed by fitting the Raman spectra of 30 Claritin® tablets with weighted percentages of the Raman spectrum of its API, loratadine, and a composite spectrum of the known excipients. The mean loratadine mass of 9.79 ± 40 mg per 100 mg tablet compared favorably to the 10.21 ± 0.63 mg per 100 mg tablet determined using high-performance liquid chromatography, both of which met the acceptance value to pass the 10 mg API product as labelled. The method was then applied to a generic version of the Claritin product that employed different excipients of unknown mass percents. A Raman spectrum representative of all excipients was created by subtracting the API Raman spectrum from the product spectrum. The Raman spectra of the 30 generic tablets were then fit with weighted percents of the pure loratadine spectrum and the created excipient spectrum, and used to determine a mean API mass for the tablets of 10.12 ± 40 mg, again meeting the acceptance value for the 10 mg API product. The data suggest that this simple method could be used to pass or fail manufactured drug product batches in accordance with the US Pharmacopeia method for content uniformity, without knowledge of the excipients.

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M, Achor, and Zaharadeen U. A. "Binding Properties of Ethyl Starch obtained from Ipomoea batatas as a Pharmaceutical Excipient." International Journal of Pharma Research and Health Sciences 7, no. 3 (June 2019): 2962–67. http://dx.doi.org/10.21276/ijprhs.2019.03.02.

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Journal articles on the topic 'Pharmaceutical excipient'

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