硝苯地平微乳凝胶的制备及其质量评价

Preparation and Quality Evaluation of Nifedipine Microemulsion Gels

关键词:  硝苯地平  微乳凝胶  制备工艺  质量评价

Key words:  nifedipine  microemulsion gels  preparation technology  quality evaluation

摘要:

目的 将硝苯地平制备成微乳凝胶，以提高其生物利用度。方法 进行凝胶基质以及透皮吸收促进剂的筛选，确定硝苯地平微乳凝胶的最佳处方，并进行初步质量评价。结果 硝苯地平微乳的处方为乳化剂OP∶无水乙醇∶油酸乙酯∶水=27∶13.5∶4.5∶55；硝苯地平微乳凝胶的处方为1.2%卡波姆940，2.5%氮酮。所制得的硝苯地平微乳平均粒径为9.963 nm，大小均匀；硝苯地平微乳凝胶24 h的累积渗透量（Q_{24 h}）达到（296.35±34.66）μg·cm^-2，稳态透皮速率为（14.20±0.23）μg·cm^-2·h^-1；经高速离心、低温、高温试验考察，硝苯地平微乳凝胶稳定性良好；经小鼠皮肤刺激性试验考察，硝苯地平微乳凝胶对皮肤刺激性和毒性较小。结论 将硝苯地平制成微乳凝胶，药物的溶解度提高，制剂质量优良。

Abstract:

OBJECTIVE To prepare nifedipine microemulsion gels to increase the bioavailability. METHODS Gelling agents and penetration enhancers were screened to determine the best prescription of nifedipine microemulsion and evaluate the quality preliminary. RESULTS The prescription of nifedipine microemulsion consisted of emulsifier OP∶anhydrous ethanol∶ethyl oleate∶water with the weight ratio of 27∶13.5∶4.5∶55. Prescription of nifedipine microemulsion gels consisted of carbomer 940(1.2%) and azone(2.5%). The average diameter of nifedipine microemulsion was 9.963 nm with uniform size. Nifedipine microemulsion gels showed highest cumulative amount(Q_24h) of (296.35±34.66)μg·cm^-2 and steady penetration rate of (14.20±0.23)μg·cm^-2·h^-1. It showed good stability after high speed centrifuging, low temperature and high temperature test. After mouse skin irritation test, nifedipine microemulsion gels had less skin irritation and toxicity.CONCLUSION Nifedipine is made in to microemulsion gel, the solubility is increased and the quality of the preparation is excellent.