Search results for "EXCIPIENTS"
showing 10 items of 56 documents
Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Ondansetron.
2019
Literature data pertaining to the physicochemical, pharmaceutical, and pharmacokinetic properties of ondansetron hydrochloride dihydrate are reviewed to arrive at a decision on whether a marketing authorization of an immediate release (IR) solid oral dosage form can be approved based on a Biopharmaceutics Classification System (BCS)-based biowaiver. Ondansetron, a 5HT3 receptor antagonist, is used at doses ranging from 4 mg to 24 mg in the management of nausea and vomiting associated with chemotherapy, radiotherapy, and postoperative treatment. It is a weak base and thus exhibits pH-dependent solubility. However, it is able to meet the criteria of "high solubility" as well as "high permeabi…
On the difficulty of assessing the specific surface area of magnesium stearate
2001
Abstract The water content of as-received commercial magnesium stearate batches from animal and vegetable sources have been modified by ageing in humid air at room temperature or by vacuum treatment. The complete adsorption–desorption isotherms of nitrogen and krypton vapours by samples of these as received and modified materials have been measured at liquid nitrogen temperature after standardised vacuum degassing. They are greatly affected by the initial water content of the material. In particular: (a) the BET surface area values computed from the adsorption branch vary widely and is increasing with increasing water content; (b) anomalous hysteresis of varying amplitude is observed in all…
Designing robust immediate release tablet formulations avoiding food effects for BCS class 3 drugs
2019
Abstract Food induced viscosity in the gastrointestinal tract is reported to reduce the bioavailability of tablets containing BCS class 3 drugs, mainly by retarding their disintegration and dissolution of the active pharmaceutical ingredient. The role of formulation factors in minimizing this negative food effect is largely unknown. Combinations of disintegrants were studied together with soluble and insoluble fillers and trospium chloride as model drug substance. Different batches of tablets were compressed at 10 kN and 30 kN, by incorporating different combinations of croscarmellose sodium (CSS), cross-linked (CPD) and sodium starch glycolate (SSG) at low level i.e, 2% + 2% and high level…
Green Extraction of Polyphenols from Waste Bentonite to Produce Functional Antioxidant Excipients for Cosmetic and Pharmaceutical Purposes: A Waste-t…
2022
In an ever-growing perspective of circular economy, the development of conscious, sustainable and environmental-friendly strategies to recycle the waste products is the key point. The scope of this work was to validate the waste bentonite from the grape processing industries as a precious matrix to extract polyphenols by applying a waste-to-market approach aimed at producing novel functional excipients. The waste bentonite was recovered after the fining process and opportunely pre-treated. Subsequently, both the freeze dried and the so-called “wet” bentonites were subjected to maceration. PEG200 and Propylene Glycol were selected as solvents due to their ability to dissolve poly…
Biowaiver Monographs for Immediate-Release Solid Oral Dosage Forms: Folic Acid.
2018
This work presents a review of literature and experimental data relevant to the possibility of waiving pharmacokinetic bioequivalence studies in human volunteers for approval of immediate-release solid oral pharmaceutical forms containing folic acid as the single active pharmaceutical ingredient. For dosage forms containing 5 mg folic acid, the highest dose strength on the World Health Organization Essential Medicines List, the dose/solubility ratio calculated from solubility studies was higher than 250 mL, corresponding to a classification as "not highly soluble." Small, physiological doses of folic acid (≤320 μg) seem to be absorbed completely via active transport, but permeability data f…
Influence of poloxamers on the dissolution performance and stability of controlled-release formulations containing Precirol® ATO 5
2005
Abstract Lipid excipients are usually used for the development of sustained-release formulations. When used in relatively high quantities, Precirol ® ATO 5 imparts sustained-release properties to solid oral dosage forms, by forming a lipid matrix. To control or adjust the drug release kinetics from such lipid matrix however, one must often resort to complementary ingredients or techniques. This study investigates the influence of poloxamers (Lutrol ® ) included in lipid matrices composed of glyceryl palmitostearate (Precirol ® ATO 5) on their dissolution performance and their stability. The addition of these hydrophilic polymers in the lipid matrix increased the amount of theophylline relea…
Investigation of various shellac grades: additional analysis for identity.
2009
Background: A number of different grades of shellac are commercially available and most of them are known only as generic shellac and are not further differentiated. The investigated grades of shellac in this study are based on different insect strains, host trees, refining methods, and products from different suppliers. Method: The Gardner/Iodine color values of alcoholic and aqueous solutions of the various shellac grades were measured. Glass transition temperatures and pKa-values were determined. To assess chemical differences in the tested shellac grades, MALDI-TOF analysis was performed. Results: Differences were found in color, TG, and pKa-values and in the mass spectra by MALDI-TOF a…
In vivo methods for drug absorption - comparative physiologies, model selection, correlations with in vitro methods (IVIVC), and applications for for…
2013
This review summarizes the current knowledge on anatomy and physiology of the human gastrointestinal tract in comparison with that of common laboratory animals (dog, pig, rat and mouse) with emphasis on in vivo methods for testing and prediction of oral dosage form performance. A wide range of factors and methods are considered in addition, such as imaging methods, perfusion models, models for predicting segmental/regional absorption, in vitro in vivo correlations as well as models to investigate the effects of excipients and the role of food on drug absorption. One goal of the authors was to clearly identify the gaps in today's knowledge in order to stimulate further work on refining the e…
Biowaiver monographs for immediate release solid oral dosage forms: quinidine sulfate.
2009
Literature data are reviewed relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of new multisource and reformulated immediate release (IR) solid oral dosage forms containing quinidine sulfate. Quinidine sulfate's solubility and permeability, its therapeutic use and index, pharmacokinetics, excipient interactions and reported BE/bioavailability (BA) problems were taken into consideration. The available data are not fully conclusive, but do suggest that quinidine sulfate is highly soluble and moderately to highly permeable and would likely be assigned to BCS Class I (or at worst BCS III). In view of the inconclusiveness of the data and, more imp…
Application of fractal geometry to dissolution kinetic study of a sweetener excipient
2001
Abstract In the context of relationship study between dissolution kinetic and particle morphology using the fractal geometry tool, we use a commercially available quality of saccharin powder. The characterization of molecular feature and image analysis study allows us to conclude to the statistic self-similarity of particles of four sieved particles size fractions, permitting the fractal approach. Calculation of reactive fractal dimension is performed using two forms of mass transfer equation: −d Q /d t = kQ D R /3 Δ C and −d Q /d t = k′R D R −3 Δ C , with Δ C ={ C f /[ln C s /( C s − C f )]}. Based on comparison of the surface fractal dimension D S on the two values of reactive fractal di…