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

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

International journal of pharmaceutics (2012-12-15)
Ying-Chen Chen, Hsiu-O Ho, Tzu-Yu Lee, Ming-Thau Sheu
ABSTRACT

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 16 h and an adjustable sustained release profile.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Hydroxyethyl-cellulose, viscosity 90-160 cP, 5 % in H2O(25 °C)
Sigma-Aldrich
Hydroxyethyl-cellulose
Sigma-Aldrich
2-Hydroxyethyl cellulose, average Mv ~90,000
Sigma-Aldrich
2-Hydroxyethyl cellulose, average Mv ~1,300,000
Sigma-Aldrich
2-Hydroxyethyl cellulose, average Mw ~380,000
Sigma-Aldrich
2-Hydroxyethyl cellulose, average Mv ~720,000