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首页> 外文期刊>Tropical Journal of Pharmaceutical Research >Preparation and In-vitro Evaluation of Gastroretentive Bupropion Hydrochloride Tablets
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Preparation and In-vitro Evaluation of Gastroretentive Bupropion Hydrochloride Tablets

机译:胃滞留安非他酮片的制备及体外评价

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Purpose: To develop a gastroretentive formulation of bupropion hydrochloride in the form of floating tablets. Methods: Floating tablets were prepared by wet granulation method using various amounts of sodium carboxymethycellulose (NaCMC), different molecular weight grade of hydroxypropyl methylcellulose (HPMC) and varying amounts of fillers (microcrystalline cellulose, lactose and tricalcium phosphate). Sodium bicarbonate was also incorporated as the gas-generating agent. The formulations were tested for their physical properties, floating lag time, duration of floating and in-vitro drug release. Results: All the tablet formulations containing either HPMC K4M or HPMC K15M as the sustainedrelease polymer together with either microcrystalline cellulose (MCC) or lactose, floated in the release medium for > 10 h. Tablets prepared with MCC released ≥ 79 % of the drug after 10 h, while those prepared with lactose released ≥ 85 % of the drug within the same period. Tablets containing NaCMC alone did not show good floating properties but when HPMC K4M was also incorporated at certain ratios, tablets with good floating behavior and suitable drug release patterns were produced. Drug release kinetic studies showed that formulations fitted best to the Higuchi model. Conclusion: The developed floating tablets of bupropion HCl exhibited prolonged drug release for ≥ 10 h, and, thus may improve bioavailability and minimize fluctuations in plasma drug concentration
机译:目的:以悬浮片剂的形式开发盐酸安非他酮的胃滞性制剂。方法:采用湿法制粒,使用各种量的羧甲基纤维素钠(NaCMC),不同分子量等级的羟丙基甲基纤维素(HPMC)和不同量的填充剂(微晶纤维素,乳糖和磷酸三钙)制备浮片。还加入碳酸氢钠作为气体发生剂。测试了制剂的物理性质,漂浮滞后时间,漂浮持续时间和体外药物释放。结果:所有包含HPMC K4M或HPMC K15M作为缓释聚合物以及微晶纤维素(MCC)或乳糖的片剂均在释放介质中漂浮> 10 h。使用MCC制备的片剂在10小时后释放了≥79%的药物,而使用乳糖制备的片剂在同一时期释放了≥85%的药物。仅含有NaCMC的片剂没有显示出良好的漂浮性,但是当还按一定比例掺入HPMC K4M时,会产生具有良好漂浮性和合适的药物释放模式的片剂。药物释放动力学研究表明,配方最适合Higuchi模型。结论:开发的盐酸安非他酮漂浮片可延长释药时间≥10小时,从而可提高生物利用度并最大程度降低血浆药物浓度的波动

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