难溶性药物固体分散体的配方及评价

Komal Chandrakant Jadhav, Sourabh Sukumar Hegaje, Sadhana Uttam Jadhav, Rupesh Sopanrao Vaidhya, Mayuresh Ramesh Redkar
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引用次数: 0

摘要

固体分散是目前应用最广泛、最成功的方法之一,可提高难溶性药物的溶解度、溶出率和生物利用度。固体分散是基于药物以固体状态分散在惰性水溶性载体中的概念。几种水溶性载体如甲基纤维素、尿素、乳糖、柠檬酸、聚乙烯醇吡咯烷酮和HPMC、环糊精、聚乙二醇4000和6000作为固体分散载体。在目前的研究工作中,固体分散技术可以成功地用于改善胡椒碱和磺胺甲恶唑的溶出度。为此,以HPMC e100和2-羟丙基-环糊精为载体,采用溶剂蒸发法以1:1的比例制备了这些药物的固体分散体。制备的固体分散体对纯胡椒碱和磺胺甲恶唑的饱和溶解度和体外溶出度进行了研究。胡椒-2羟丙基-环糊精固体分散体以1:1的比例溶解速度较快。
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Formulation and Evaluation of Solid Dispersion of Poorly Soluble Drugs
Solid dispersion is one of the method, which was most widely and successfully applied to improve the solubility, dissolution rates and consequently the bioavailability of poorly soluble drugs. The solid dispersion based on the concept that the drug is dispersed in an inert water- soluble carrier at solid state. Several water-soluble carriers such as methyl cellulose, urea, lactose, citric acid, polyvinyl pyrrolidone and HPMC, cyclodextrin, polyethylene glycols 4000 and 6000 are used as carriers for solid dispersion. In the current research work, the solid dispersion technique can be successfully used for the improvement of dissolution of piperine and sulfamethaoxazole. In this regards, solid dispersions of these drugs were prepared by using HPMC E 100 and 2-Hydroxyproplyl beta cyclodextrin as a carrier in 1:1 ratio by solvent evaporation method. The saturation solubility and in-vitro dissolution studies of prepared solid dispersions were examined against pure piperine and sulfamethaoxazole. Faster dissolution was exhibited by piperine-2 hydroxypropyl beta cyclodextrin solid dispersion containing 1:1 ratio.
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