Search results for "Excipient"

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…

Partially Quarternized Amino Functional Poly(methacrylate) Terpolymers: Versatile Drug Permeability Modifiers

2011

Partially quarternized poly(methacrylate) terpolymers (Q-BBMCs) have been synthesized, based on the basic butylated methacrylate copolymer (BBMC/EUDRAGIT E), an excipient approved by the Food and Drug Administration (FDA) and to date mainly applied for tablet coatings. Via straightforward polymer modification reactions, a series of Q-BBMCs with quarternization degrees of 22%, 42%, and 65% has been prepared. Apical to basolateral transport across Caco-2 cell monolayers was investigated, employing the paracellular transported compounds trospium and mannitol. At pH 6.5 quarternization resulted in increased permeation enhancement up to 2.8-fold compared to BBMC, that is, up to 7.3-fold compared…

The New Life Of Exhausted Bentonite From The Grape Processing Industry: From Waste To Precious Resource To Produce Novel Raw Materials Enriched In Po…

Introduction: 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 point1. The exhausted bentonite, from the grape processing industries, could become a precious matrix to produce new pharmaceutical/cosmetic excipients enriched in functional polyphenols2. Materials & Methods: The exhausted bentonite recovered after the fining process (supplied by Bono&Ditta s.p.a., Campobello di Mazara TP, Italy) was stored at -20°C. Solid-liquid extractions on both freeze-dried and as-collected (wet) bentonite were carried out by using PEG200 or propylene glycol as solvents. The l…

Comparative enhancer effects of Span20 with Tween20 and Azone on the in vitro percutaneous penetration of compounds with different lipophilicities.

2000

Sorbitan monolaurate (Span20) was used in this study to analyze the influence of the polar functional group on the effects that non-ionic surfactants have on skin permeability. Its ethoxylate derivative polysorbate 20 (Tween20) and Azone, both with the same C12 alkyl chain as Span20, were used for comparative purposes. We evaluated the relative potency of the three molecules as enhancers in the permeability of a series of compounds with lipophilicities ranging from log Poct=-0.95 to log Poct=2.33. The influence of the enhancer concentration was also studied. For this purpose the epidermis of Wistar rat was pretreated with ethanolic solutions (1 and 5%, w/v) of each enhancer. Our results ind…

Physicochemical compatibility of mixtures of dornase alfa and tobramycin containing nebulizer solutions

2008

Patients suffering from cystic fibrosis (CF) often need to inhale multiple doses of different nebulizable drugs per day. Patients attempt to shorten the time consuming administration procedure by mixing drug solutions/suspensions for simultaneous inhalation. The objective of this experimental study was to determine whether mixtures of the nebulizer solution dornase alfa (Pulmozyme) with tobramycin nebulizer solutions (TOBI and GERNEBCIN 80 mg) are physico-chemically compatible. Drug combinations were prepared by mixing the content of one respule Pulmozyme with either one respule TOBI or one ampoule GERNEBCIN 80 mg. Test solutions were stored at room temperature and exposed to light. Dornase…

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…

The influence of Span®20 on stratum corneum lipids in Langmuir monolayers: comparison with Azone®

2000

Recently we have proved that Span 20 has the same enhancer effect as Azone on in vitro percutaneous penetration of lipophilic compounds (logP(oct) from 1.34 to 2.33). The purpose of this work is to study the interactions of Span 20 with stratum corneum lipids monolayers and to compare them with Azone. The surface pressure-area characteristics of Span 20 in mixed monolayers with different model lipids (ceramides, cholesterol, free fatty acids and two mixtures of ceramides+cholesterol, and ceramides+cholesterol+free fatty acids) in similar proportions to that which exists in human stratum corneum lipids were recorded as compression isotherms at 25 degrees C. Azone was also investigated on mon…

Blood pressure reduction in hypertensive patients after withdrawal of effervescent medication

2009

Background Raised blood pressure associated with the sodium excipient content of soluble or effervescent analgesic has been previously reported. However, the influence of other anions associated with sodium on blood pressure is still controversial. Methods Observational study of elderly hypertensive patients with uncontrolled blood pressure treated with effervescent paracetamol (3 g/day) for osteoarthritis. Blood pressure was measured before and after (4 weeks or more) switching paracetamol from an effervescent format to a tablet form in 34 patients. Blood pressure was recorded by community pharmacists during a pharmacotherapeutic follow-up service. Results Sodium intake in an effervescent …