目的 制备罗哌卡因醇质体凝胶剂并考察其体外经皮渗透性能。方法 采用乙醇注入法制备罗哌卡因醇质体,正交试验法筛选处方和制备工艺,并对其粒径、形态和包封率进行评价,以卡波姆为基质制备醇质体凝胶,用透皮扩散试验仪和小鼠腹部皮肤进行体外经皮渗透试验,考察药物累积渗透量。结果 罗哌卡因醇质体的外形为类球形,粒径为(127.6±4.8)nm,包封率为(77.58±1.07)%。罗哌卡因醇质体凝胶剂24 h的累积经皮渗透量为73.07 μg·cm-2,是普通凝胶剂的1.56倍。结论 罗哌卡因醇质体凝胶制备工艺简便,质量可控,能明显促进罗哌卡因的经皮渗透。
Abstract
OBJECTIVE To prepare ropivacaine ethosomal gel and study its transdermal permeation. METHODS The ropivacaine ethosomes were prepared by ethanol injection method. The formulation and the preparation method of ethosomes were optimized by orthogonal experiment. The particle size, morphology and encapsulation efficiency were evaluated,and the carbomer was added as the base for the preparation of the ethosomal gel. The penetration experiments of ropivacaine ethosomal gel through mouse skin were performed by Franz's cell. The cumulative penetration amount was calculated. RESULTS The obtained ethosomes were approximately spherical, the size were (127.6±4.8) nm. The entrapment efficiency of ropivacaine in ethosomes was (77.58±1.07)%. Accumulative permeation amount of ropivacaine ethosomal gel within 24 h was 73.07 μg·cm-2, which was about 1.56 times of normal gel. CONCLUSION The gel is feasible in preparation technique, controllable in quality and can significantly promote transdermal penetration of ropivacaine.
关键词
罗哌卡因 /
醇质体凝胶 /
正交设计 /
经皮吸收
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Key words
ropivacaine /
ethosomal gel /
orthogonal design /
cutaneous permeation
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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
浙江省自然科学基金资助项目(LY14E050001);台州市科技计划项目(1402ky18, 15gy58);浙江省教育厅一般科研项目(Y201432771);台州市博士后科研启动基金资助项目(2014BSH01);台州职业技术学院重点课题(2014ZD08,2015ZD09)
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