Physical characterizations and sustained release profiling of gastroretentive drug delivery systems with improved floating and swelling capabilities

• Published in: International journal of pharmaceutics 2013-01, Vol.441 (1-2), p.162-169
• Main Authors: Chen, Ying-Chen, Ho, Hsiu-O, Lee, Tzu-Yu, Sheu, Ming-Thau
• Format: Article
• Language: English
• Subjects: Angiotensin II Type 1 Receptor Blockers - administration & dosage; Angiotensin II Type 1 Receptor Blockers - pharmacokinetics; Cellulose - analogs & derivatives; Cellulose - chemistry; Chitosan; Chitosan - chemistry; Delayed-Action Preparations; Drug Compounding - methods; Drug Delivery Systems; Excipients - chemistry; Floating; Gastroretentive drug delivery system; Hydroxyethylcellulose; Losartan; Losartan - administration & dosage; Losartan - pharmacokinetics; sodium bicarbonate; Sodium Bicarbonate - chemistry; Swelling; Tablets; Time Factors; Viscosity
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2012.12.002

Gastroretentive drug delivery systems with more than 16h with a swelling ratio over 2 and an adjustable sustained release profile The aim was to develop gastroretentive drug delivery systems (GRDDSs) by combining floating and swelling. GRDDS tablets formulated with hydroxyethylcellulose (HEC), chitosan (CS) and sodium bicarbonate (SB) for evaluating floating capacity (floating lag time and duration) and swelling characteristics. CS was used because it was swellable in acidic media and biocompatible. Losartan was incorporated into the optimized formulations for sustained release profiling. Results demonstrated that for those formulations at HEC:CS ratio of 5:5 containing CS, both the floating lag time and floating duration were optimal and reached the preferred swelling effect and sustain for 24h. Adding SB improved the floating capabilities for all ratios of HEC:CS, but reduced the swelling ability for those formulations containing a higher portion of low viscosity grade CS. Sustained release profiles for losartan in those formulations were achievable, using all viscosity grades of CS at all examined HEC:CS ratios; however, it is more adjustable at different HEC:CS ratios when using a lower viscosity grade of CS. Optimized GRDDS formulations for losartan composed of an equivalent ratio of HEC to CS with 20mg SB resulted in the tablets floating for more than 16h and an adjustable sustained release profile.