目的 采用高压均质结合冷冻干燥法制备辅酶Q10-γ-环糊精纳晶混悬物,对制备工艺进行优化,并对产品质量进行评价。方法 以纳晶混悬物包载率和平均粒径作为评价指标,采用响应面设计法筛选处方及制备工艺,并对产品的稳定性及体外透皮性能进行考察。结果 最佳制备条件:γ-环糊精与药物质量比7.76∶1,超声温度40 ℃,超声时间28.33 min,均质压力40 MPa。此条件下得到纳晶混悬物产品的平均包载率为48.39%,平均粒径324 nm。体外透皮吸收试验测得该纳晶混悬物的稳态渗透速率常数为5.68 μg·cm-2·h-1。 结论 该制备方法简便可行,产品质量稳定,适于工业生产。
Abstract
OBJECTIVE To prepare coenzyme Q10-γ-cyclodextrin nano-crystal suspension using high pressure homogeneous combining freeze-drying method, optimize the preparation technology, and evaluate the quality of the product. METHODS Encapsulation efficiency and mean particle size of inclusion complex were used as indicators, and response surface method was performed for optimizing preparation process and formulations. The stability and transdermal performance in vitro of the inclusion complexes were investigated. RESULTS The optimal technical parameters were as follows: the mass ratio of γ-cyclodextrin and drug, 7.76∶1; ultrasonic temperature, 40 ℃; ultrasonic time, 28.33 min; homogeneous pressure, 40MPa. Under such conditons, an average encapsulation efficiency of 48.39% and average particle size of 324nm were obtained for the nano-crystal suspension. The transdermal experiment in vitro showed that the infiltration rate of inclusion was 5.68 μg·cm-2·h-1. CONCLUSION The preparation method is simple and feasible. The product quality is stable. Moreover, it is easy to manufacture.
关键词
辅酶Q10 /
纳晶混悬物 /
响应面法 /
体外透皮
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Key words
coenzyme Q10 /
nano-crystal suspension /
response surface method /
transdermal in vitro
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中图分类号：
R944
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参考文献
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脚注
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基金
齐齐哈尔市科学技术计划项目(SFGG-201340)
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