中心组合设计在阿司匹林软膏处方优化中的应用

Application of Central Composite Design in Optimization of the Formulation of Aspirin Ointment

目的确定阿司匹林软膏剂的最佳处方。方法以6 h累积渗透量和皮肤刺激性为考察指标,选择阿司匹林软膏处方中对指标影响较显著的3个因素:十二烷基硫酸钠、枸橼酸三钠、三乙醇胺为考察对象,采用中心组合设计法对阿司匹林软膏处方进行优化。结果阿司匹林软膏的最佳处方是:十二烷基硫酸钠1.41%,枸橼酸三钠3.50%,三乙醇胺3.00%。按照优化处方制备了3批阿司匹林软膏样品,其6 h平均累积渗透量为990.18μg·cm-2,产品无明显刺激性。结论中心组合设计法应用简便、预测性好,制备的阿司匹林软膏符合设计要求。

OBJECTIVE To optimize the formulation of aspirin ointment. METHODS With cumulative permeation quantity within 6 h and shin irritation as indexes, the method of central composite design was used to optimize the formulation of aspirin oint- ment, taking the most important three ingredients including sodium lauryl sulfate（ X1 ）, sodium citrate （X2 ）and triethanolamine（ X3 ） as the study subjects. RESULTS The optimized formulation of aspirin ointment was composed of 1.41% sodium lauryl sulfate, 3.5% sodium citrate and 3.0% triethanolamine. Three batches of aspirin ointment were prepared using the optimized formulation, for which the average cumulative permeation quantity within 6 h was 990. 18 μg.cm -2, and no obvious shin irritation was observed. CONCLUSION Central composite design is successfully used to optimize the formulation of aspirin ointment.