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目的 :提高难溶性药物环孢素 (CsA)的溶出速率。方法 :选择聚乙二醇 (PEG4 0 0 0 )和聚乙烯吡咯烷酮 (PVPK3 0 )两种载体 ,分别以溶剂熔融法和溶剂法制备CsA固体分散体 ;建立HPLC法检测固体分散体的体外溶出度 ,并考察不同载体、不同比例及溶出介质、桨法转速对CsA溶出速率的影响。对溶出度结果用Weibull分布模型进行拟合 ,计算体外溶出参数T50 和Td,并进行方差分析。结果 :使用HPLC法测定CsA的体外溶出量准确、稳定、可靠、载体无干扰。制备成的固体分散体能显著提高CsA的体外溶出速率 ,PVPK3 0 载体的固体分散体的溶出速率明显快于PEG4 0 0 0载体的固体分散体。溶出介质对药物溶出没有明显影响。结论 :CsA∶PVPK3 0 为 1∶6的固体分散体具有良好的体外速释作用。
Objective: To improve the dissolution rate of sparingly soluble CsA. Methods: Two kinds of carriers, polyethylene glycol (PEG4000) and polyvinylpyrrolidone (PVPK3O), were selected to prepare solid dispersions of CsA by solvent melting method and solvent method respectively. The dissolution of solid dispersions in vitro was established by HPLC , And investigate the influence of different carrier, different ratio and dissolution medium, paddle speed on CsA dissolution rate. Weibull distribution model was used to fit the dissolution results. The in vitro dissolution parameters T50 and Td were calculated and analyzed by ANOVA. Results: The HPLC method was used to determine the in vitro dissolution rate of CsA accurately, stably and reliably without interference of carrier. The prepared solid dispersion can significantly improve the dissolution rate of CsA in vitro. The dissolution rate of solid dispersion of PVPK30 carrier is obviously faster than the solid dispersion of PEG40000. Dissolution medium had no significant effect on drug dissolution. Conclusion: The solid dispersions with CsA: PVPK3o of 1: 6 have good in vitro immediate release.