沙格列汀二甲双胍缓释片的体外评价

In vitro evaluation of saxagliptin and metformin hydrochloride sustainedrelease tablets

为评价自研的沙格列汀二甲双胍缓释片与参比制剂体外释放行为的一致性,分别在pH 1.0盐酸溶液、pH 4.5醋酸盐缓冲液、pH 6.8磷酸盐缓冲液与纯化水4种溶出介质中比较自研制剂和参比制剂间溶出曲线的相似性,并对自研制剂和参比制剂在pH 1.0盐酸溶出介质中的凝胶形态和凝胶强度进行比较。结果显示,在4种溶出介质中自研制剂和参比制剂中沙格列汀的15 min溶出度均大于85%,盐酸二甲双胍的ƒ2相似因子分别为89、83、80、86,均大于50,自研制剂两种药物的溶出行为均与参比制剂一致。自研制剂亲水凝胶骨架的体积膨胀率、吸水增重率、溶蚀率与参比制剂一致;自研制剂的凝胶强度与参比制剂一致。结果表明,自研制剂和参比制剂体外释放行为一致,为体内生物等效性试验提供了良好的保障。

In order to evaluate the consistency of the release behavior between the self-made saxagliptin and metformin hydrochloride sustained-release tablets and the reference preparations in vitro,the similarity of the dissolution curves between the self-made preparations and the reference preparations in four dissolution mediums:HCl(pH 1.0),acetate buffer saline(pH 4.5),phosphate buffer saline(pH 6.8)and pure water,and the gel morphology and strength of the self-made preparations and the reference preparations in the HCl(pH 1.0)solution medium were compared.Results showed that in four dissolution mediums,the dissolution rates of saxagliptin in the self-made preparations and the reference preparations at 15 min were greater than 85%,and theƒ2 similarity factors of metformin hydrochloride were 89,83,80,86,all greater than 50,so the dissolution of the self-made preparations was consistent with those of the reference preparations.The volume expansion rate,water absorption rate and erosion rate were consistent with those of the reference preparations,and the gel strength of the self-made preparations was the same as that of the reference preparations.The in vitro release behaviors of the self-made preparations and the reference preparations are consistent,which provide a good guarantee for bioequivalence.