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目的:制备西罗莫司固体分散体。方法:分别以聚乙烯吡咯烷酮(PVPK30)、羟丙甲纤维素(HPMC)、泊洛沙姆188(F68)和硬脂酸聚烃氧(40)酯(S40)为载体,采用溶剂-熔融法或溶剂法,制备西罗莫司固体分散体,考察其溶解度及体外溶出度,并采用DSC法和X射线衍射方法分析药物在载体中的存在状态。结果:各种固体分散体均能增加西罗莫司的溶解度,加快其体外溶出。其中泊洛沙姆188作为载体时,体外溶出度5min内达80%以上,其在水中的溶解度从0.27mg.L-1提高到27.29mg.L-1;西罗莫司在固体分散中可能以无定型态或分子状态存在。结论:固体分散体可以显著提高西罗莫司的溶解度和体外溶出度。
Objective: Preparation of sirolimus solid dispersion. Methods: Polyvinylpyrrolidone (PVPK30), hypromellose (HPMC), poloxamer 188 (F68) and polyoxyl 40 stearate (S40) Or solvent method to prepare the solid dispersion of sirolimus and investigate its solubility and in vitro dissolution rate, and analyze the existence state of the drug in the carrier by using a DSC method and an X-ray diffraction method. Results: All kinds of solid dispersions could increase the solubility of sirolimus and accelerate its dissolution in vitro. Poloxamer 188 as a carrier, in vitro dissolution within 5min reached more than 80%, its solubility in water increased from 0.27mg.L-1 to 27.29mg.L-1; sirolimus may be in the solid dispersion In amorphous or molecular state exists. Conclusion: The solid dispersion can significantly improve the solubility of sirolimus and in vitro dissolution.