葛根素自微乳化渗透泵控释胶囊的制备

Preparation of puerarin self-microemulsifying osmotic pump controlled-release capsule

目的制备葛根素自微乳化渗透泵缓控释胶囊,通过微孔渗透泵制剂控释难溶性药物的释放,以期提高葛根素的生物利用度。方法通过构建葛根素自微乳化体系及渗透泵控释胶囊的制备,采用微乳色谱法进行定量测定。通过单因素考察确定了对药物释放影响较大的3个因素:促渗剂氯化钠的用量、包衣增重、致孔剂聚乙二醇(PEG)400用量,采用中心复合设计和效应面优化,预测了最优处方。结果葛根素自乳化渗透泵缓控释胶囊的处方为葛根素0.07 g、油酸乙酯0.25 g、聚山梨酯80 0.45 g、PEG 400 0.3 g、甘露醇1.07 g、氯化钠1.07 g;通过对制备处方和预测处方在4、8、12 h的释放度的考察,发现该缓控释胶囊符合零级释放模型。结论自微乳化渗透泵胶囊可以解决难溶性药物的控释制剂的设计要求。

Objective Through the preparation of puerarin self-microemulsifying osmotic pump controlled-release capsule and controlled-release insoluble drug to improve the bioavailability of puerarin.Methods Through the construction of selfmicroemulsifying osmotic pump controlled-release capsule of puerarin to do quantitative determination using microemulsion chromatography method.Through the single factor investigation,the three influencing factors were determined： dosage of penetration enhancer NaCl,coating weight,and porogen PEG 400.The optimal prescription was predicted by using central composite design and response surface optimization.Results The formulation for puerarin self-microemulsifying osmotic pump controlled-release capsule was puerarin 0.07 g,ethyloleate 0.25 g,Polysorbate 80 0.45 g,PEG 400 0.3 g,mannitol 1.07 g,and NaCl 1.07 g.Based on the release of preparation and prediction of prescriptions in 4,8,and 12 h,the controlled-release capsule conformed to the zero-order release model.Conclusion Self-microemulsifying osmotic pump capsule could solve the controlled-release of insoluble drugs.