Development and Evaluation of a pH-Dependent Sustained Release Tablet for Irritable Bowel Syndrome

文献类型： 外文期刊

第一作者： Zhang, Shuang-Qing

作者： Zhang, Shuang-Qing;Rahman, Ziyaur;Thumma, Sridhar;Repka, Michael A.;Zhang, Shuang-Qing;Li, San-Ming;Chen, Guo-Hua

作者机构：

关键词： tegaserod maleate;pH-dependent;sustained release;Eudragit;preformulation

期刊名称：DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY （ 影响因子：3.225； 五年影响因子：3.105 ）

ISSN： 0363-9045

年卷期： 2009 年 35 卷 1 期

页码：

收录情况： SCI

摘要： The overall objective of this study was to develop a pH-dependent sustained release tablet formulation of a model drug, tegaserod maleate (TM), which is a poorly water soluble and acid labile drug in gastric milieu. The formulation's goal was to allow the dosage form to pass through the stomach intact, start disintegrating in the upper small intestine and slowly release the active in a controlled manner. Partition coefficient, contact angle and drug-excipient compatibility were investigated as part of the preformulation studies. A pH-dependent sustained release tablet was prepared using a combination of Eudragit L100 and Eudragit S100. The effects of solubilizer, disintegrant, binder, coating polymer concentration, pore former, and plasticizer on the drug release rate were determined. The results demonstrated that approximately 90% of the drug was released in a sustained release manner in the pH 6.8 phosphate buffer within 12 h while no drug was detected when subjected to drug release studies in 0.1 mol/L hydrochloric acid for 2 h. The drug release mechanism involved stress points and/or pore formation in the coated film. The coated tablets were stable at 40C/75% RH for 3 months. These results highlighted the feasibility of this coated tablet system containing TM, which may contribute to the successful treatment of irritable bowel syndrome.

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