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Release Capsules (release + capsule)
Selected AbstractsInvestigation on different levels of in vitro,in vivo correlation: gemfibrozil immediate release capsuleBIOPHARMACEUTICS AND DRUG DISPOSITION, Issue 6 2008Mohammad-Reza Rouini Abstract Gemfibrozil is a practically water-insoluble, high-dose drug. It represents a typical drug with dissolution rate controlled bioavailability. The aim of this study was to select a dissolution condition for gemfibrozil immediate release capsules, resulting in the best in vitro/in vivo correlation (IVIVC). Five 300,mg gemfibrozil products, including the innovator and four generic products were selected. In vitro dissolution test methods with a standard paddle, round-bottomed vessel of 1,l capacity, and potassium phosphate buffer as the dissolution medium (referred to as conditions I, II and III, respectively) were developed. The products were administered to 12 healthy volunteers and thereby different pharmacokinetic parameters were calculated. Correlations between the in vitro and in vivo calculated parameters were investigated. Of the single point parameters investigated, the best results were seen in the relation between the percent dissolved in 10, 20 and 45,min and the time to 90% dissolution from the in vitro side and the AUCs and Cmax from the in vivo side. The correlation between MRT and MDT was also investigated, and no significant correlation was found in the three above-mentioned conditions. The Wagner-Nelson method was used to calculate the percent remaining to be absorbed. Superimposition of the percent in vivo absorption and the in vitro dissolution curves was used to investigate a multiple point correlation. A remarkable superimposition between in vivo and in vitro curves in conditions I and II was observed. Copyright © 2008 John Wiley & Sons, Ltd. [source] Polymer film formulations for the preparation of enteric pharmaceutical capsulesJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 2 2010Alan M. Smith Abstract Objectives Standard pharmaceutical capsules are designed to dissolve in the acidic environment of the stomach releasing the encapsulated contents for absorption. When release is required further along the gastrointestinal tract capsules can be coated with acid insoluble polymers to enable passage through the stomach and dissolution in the intestine. This paper describes formulations that have the potential to be used to produce two-piece hard capsules for post-gastric delivery without the requirement of an exterior coat. Methods The formulation uses three polysaccharides: sodium alginate, hypromellose and gellan gum to provide acid insolubility and the ability to form capsules using standard industrial equipment. Key findings The rheological profile, on cooling, of the base material, water content and thickness of the films were shown to be comparable with those of commercial capsules. The capsules remained intact for 2 h in 100 mm HCl at pH 1.2, and within 5 min of being removed from the acid and submerged in phosphate-buffered saline at pH 6.8 were ruptured. Conclusions Selected formulations from this study have potential for use as delayed release capsules. [source] Maintenance of Crohn's disease over 12 months: fixed versus flexible dosing regimen using budesonide controlled ileal release capsulesALIMENTARY PHARMACOLOGY & THERAPEUTICS, Issue 9 2001J. R. B. Green Background: It may be possible to achieve more effective management of Crohn's Disease by introducing a flexible dosage regimen sensitive to patients' needs. Aim: Comparison of the efficacy and tolerability of a fixed vs. flexible budesonide controlled ileal release treatment regimen for the prevention and management of relapse in Crohn's disease patients. Budesonide controlled ileal release is an oral formulation which delivers drug directly to disease sites in the ileum and ascending colon, by preventing more proximal release and absorption. Methods: A randomized, double-blind comparison of a fixed dose of budesonide controlled ileal release (6 mg o.m.) and a flexible dose of budesonide controlled ileal release (3, 6 or 9 mg o.m.) for 12 months, in 143 patients in remission from ileal or ileo,caecal Crohn's Disease. Results: Very low rates of clinical relapse in Crohn's disease were achieved with budesonide controlled ileal release 6 mg o.m. There was no significant difference between the treatment groups with respect to the survival estimate of percentage of treatment failures (flexible group 15%, fixed group 19%; P=0.61). The average consumed dose of budesonide was comparable in both groups (5.8 mg flexible, 6.0 mg fixed). Similar proportions of patients reported adverse events (flexible 100%, fixed 97%). There were 33 serious adverse events (flexible 19, fixed 14) and 13 withdrawals due to significant adverse events (flexible 9, fixed 4). Conclusion: Maintenance treatment with budesonide controlled ileal release 6 mg o.m. is well-tolerated and is associated with low rates of clinical relapse in stable Crohn's disease over 12 months. Flexible dosing remains an option for individual patients, but this study has shown no advantage over a standard fixed dosing regimen. [source] The assessment of human regional drug absorption of free acid and sodium salt forms of Acipimox, in healthy volunteers, to direct modified release formulation strategyBIOPHARMACEUTICS AND DRUG DISPOSITION, Issue 9 2009Rajeev Menon Abstract Acipimox is an analog of nicotinic acid and is indicated for the treatment of dyslipidemia. It is also believed to improve glucose control by enhancing insulin sensitivity. The purpose of this study was to direct modified release (MR) formulation strategy by comparing the bioavailability of two forms of acipimox (free acid and sodium salt) from the distal small bowel (DSB) and colon with an immediate release formulation. Two parallel groups of healthy volunteers completed an open label, non-randomized, three-way crossover study. The rate and extent of acipimox absorption was highest following administration of the immediate release capsules, and was not influenced by the form of the drug administered. Following administration to the DSB, the relative bioavailability was approximately 52% and 30% for the salt form and free acid form, respectively. Following administration to the colon, the extent of absorption was further reduced. The data indicate that bioavailability from the DSB was limited by the solubility of the drug coupled with an absorption window, whilst absorption from the colon was limited by permeability. The study provided detailed information to support and guide the formulation strategy for a MR form of acipimox, which may improve the treatment of adult patients with type II diabetes and dyslipidemia. Copyright © 2009 John Wiley & Sons, Ltd. [source] Investigation on different levels of in vitro,in vivo correlation: gemfibrozil immediate release capsuleBIOPHARMACEUTICS AND DRUG DISPOSITION, Issue 6 2008Mohammad-Reza Rouini Abstract Gemfibrozil is a practically water-insoluble, high-dose drug. It represents a typical drug with dissolution rate controlled bioavailability. The aim of this study was to select a dissolution condition for gemfibrozil immediate release capsules, resulting in the best in vitro/in vivo correlation (IVIVC). Five 300,mg gemfibrozil products, including the innovator and four generic products were selected. In vitro dissolution test methods with a standard paddle, round-bottomed vessel of 1,l capacity, and potassium phosphate buffer as the dissolution medium (referred to as conditions I, II and III, respectively) were developed. The products were administered to 12 healthy volunteers and thereby different pharmacokinetic parameters were calculated. Correlations between the in vitro and in vivo calculated parameters were investigated. Of the single point parameters investigated, the best results were seen in the relation between the percent dissolved in 10, 20 and 45,min and the time to 90% dissolution from the in vitro side and the AUCs and Cmax from the in vivo side. The correlation between MRT and MDT was also investigated, and no significant correlation was found in the three above-mentioned conditions. The Wagner-Nelson method was used to calculate the percent remaining to be absorbed. Superimposition of the percent in vivo absorption and the in vitro dissolution curves was used to investigate a multiple point correlation. A remarkable superimposition between in vivo and in vitro curves in conditions I and II was observed. Copyright © 2008 John Wiley & Sons, Ltd. [source] | ||||||||||