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KMID : 0043320100330122003
Archives of Pharmacal Research
2010 Volume.33 No. 12 p.2003 ~ p.2009
pH-independent sustained release matrix tablet containing doxazosin mesylate: Effect of citric acid
Cha Kwang-Ho

Tran Thanh Huyen
Kim Min-Soo
Kim Jeong-Soo
Park Hee-Jun
Park Jun-sung
Cho Won-Kyung
Hwang Sung-Joo
Abstract
The aim of this study was to develop a pH-independent sustained release matrix tablets of doxazosin mesylate. The matrix tablets were prepared by direct compression technique using polyethylene oxide, sodium alginate and citric acid as a pH modifier. Formulations were evaluated for an in vitro drug release study, erosion study, and the microenvironmental pH was studied using the pH indicator methyl red. For formulations without citric acid, the extent and rate of drug release in simulated gastric fluid were much higher than those in simulated intestinal fluid. By adding the citric acid, the drug release rate in simulated intestinal fluid was increased, and microenvironmental pH values within the tablets were maintained at low pH during drug release. Furthermore, drug release from the matrix tablet containing 20% w/w citric acid was comparable to that from a commercial product, Cardura¢ç XL, and a pHindependent release could be achieved. Therefore, the incorporation of citric acid as a pH modifier to Polyethylen oxide-sodium alginate matrix tablets effectively produced pHindependent doxazocin mesylate release profiles.
KEYWORD
Citric acid, Doxazosin mesylate, pH-Independent, Polyethylen oxide
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