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目的研究一种可促进普罗布考口服淋巴吸收的胶束给药系统。方法使用甲氧基聚乙二醇磷脂酰乙醇胺(mPEG-DSPE)作为载体材料,制备载普罗布考胶束给药系统并进行优化,并通过清醒大鼠淋巴插管模型评价其提高药物口服淋巴转运的作用。结果经处方优化以后,以mPF~DSPE作为载体材料制备的载普罗布考胶束的包封率>90%。清醒大鼠淋巴插管模型考察结果表明,载药胶束8 h内的淋巴转运药物累积量约为混悬组的3倍。结论 mPEC-DSPE胶束给药系统可显著提高普罗布考的淋巴转运量。
Objective To study a micellar drug delivery system that can promote oral absorption of probucol. Methods Methoxypolyethylene glycol phosphatidylethanolamine (mPEG-DSPE) was used as a carrier material to prepare and optimize the probucol loading micellar delivery system and to evaluate its efficacy by increasing lymphatic intubation in conscious rats The role of transit. Results After prescription optimization, the entrapment efficiency of loaded probucol micelles with mPF ~ DSPE as carrier material was> 90%. The awake rat model of lymphatic intubation results showed that within 8 h drug-loaded micelles lymphatic transit drug accumulation about 3 times the suspension group. Conclusion The mPEC-DSPE micellar delivery system can significantly increase the lymphocyte transport of probucol.