栀子苷乳剂的制备工艺及质量评价

Preparation and quality evaluation of gardenoside emulsion

目的制备油包水型栀子苷乳剂,对处方工艺进行优化并进行质量评价。方法通过单因素考察和混料设计,以乳化时间、析油时间和静置分层时间为指标,研究处方对乳剂性质的影响,并筛选出最佳的制备工艺,得到最优的栀子苷乳剂。并对乳剂的性质、稳定性、含量和体外释放进一步考察。结果栀子苷乳剂的平均粒径为(5.48±0.02)μm,PDI值为0.125±0.096;离心加速实验4 000 r/min离心15 min未见分层;栀子苷乳剂的平均质量分数为92.14%,RSD为1.86%(n=3);6 h内栀子苷乳剂在pH 4.5、6.8、7.4的环境下体外释放分别最高达105.32%、98.41%、98.70%,而在pH 1.2的环境下体外释放最高为63.45%;最后通过拟合方程来解释释药规律。结论高速剪切机械法可用于栀子苷乳剂的制备,优化后处方的质量评价符合要求。

Objective To prepare water-in-oil gardenoside emulsion,optimize its formulation process,and evaluate the quality.Methods The formulation was optimized based on emulsification time,oil floating time and phase separation time,and investigated the optimal gardenoside emulsion by the single factor investigation and mixture design.The properties,stability,content,and in vitro release of the emulsion were also studied.Results The mean particle size of gardenoside emulsion was(5.48 ± 0.02) μm and the value of PDI was 0.125 ± 0.096;Centrifugation accelerated test was performed at 4 000 r/min for 15 min without delamination;The average mass fraction of gardenoside emulsion was 92.14% and RSD was 1.86%(n = 3);The in vitro release of gardenoside emulsions at pH 4.5,6.8,and 7.4 was up to 105.32%,98.41%,and 98.70%,respectively,while the in vitro release at pH 1.2 was up to 63.45%;Finally,the law of drug release was explained by fitting equation.Conclusion The high speed shear mechanical method can be used to prepare gardenoside emulsion,and the quality evaluation of the optimized prescription meets the requirements.