Development of swelling/floating gastroretentive drug delivery system based on a combination of hydroxyethyl cellulose and sodium carboxymethyl cellulose for Losartan and its clinical relevance in healthy volunteers with CYP2C9 polymorphism

• Published in: European journal of pharmaceutical sciences Vol. 39; no. 1; pp. 82 - 89
• Main Authors: Chen, Ray-Neng, Ho, Hsiu-O, Yu, Chiao-Ya, Sheu, Ming-Thau
• Format: Journal Article
• Language: English
• Published: Kindlington Elsevier B.V 31.01.2010; Elsevier
• Subjects: Angiotensin II Type 1 Receptor Blockers - administration & dosage; Angiotensin II Type 1 Receptor Blockers - pharmacokinetics; Aryl Hydrocarbon Hydroxylases - genetics; Biological and medical sciences; Carboxymethylcellulose Sodium - chemistry; Cellulose - analogs & derivatives; Cellulose - chemistry; Chemistry, Pharmaceutical; Cytochrome P-450 CYP2C9; Drug Compounding - methods; Drug Delivery Systems - methods; Gastroretentive drug delivery systems; General pharmacology; Humans; Hydroxyethyl cellulose; Losartan; Losartan - administration & dosage; Losartan - pharmacokinetics; Medical sciences; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Polymorphism, Genetic; Polymorphisms; Sodium Bicarbonate - chemistry; Sodium carboxymethyl cellulose; Solubility; Tablets - administration & dosage; Tablets - chemistry; Hydroxyethyl cellulose; Gastroretentive drug delivery systems; Sodium carboxymethyl cellulose; Polymorphisms; Losartan; Imidazole derivatives; Tetrazole derivatives; Isozyme; Peptide hormone; Non peptide compound; Drug carrier; Octapeptide; Angiotensin II; Cellulose(hydroxyethyl); Human; Cellulose(carboxymethyl); Pharmaceutical technology; Swelling; Healthy subject; Enzyme; Cytochrome P450; Biphenyl derivatives; Antihypertensive agent; Sartan derivatives; Angiotensin antagonist; Floating system; Polymorphism

The aim of this study was to develop an optimal gastroretentive drug delivery system (GRDDS) for administering Losartan. Additionally, the influence of optimized GRDDS on the bioavailability of Losartan and the formation extent of active metabolite E3174 by CYP2C9 polymorphism was investigated. Swel...