目的: 建立环孢素眼用乳剂体外释放方法。方法: 采用Franz扩散池,聚偏氟乙烯膜滤膜,以缓冲盐-无水乙醇(40∶60)为接收液,时间点为60、125、190、255、320、385 min。结果: 方法学验证表明,体外释放方法的滤膜惰性、专属性、灵敏度、选择性均符合规定。测定方法的定量限为0.07 μg·mL-1,在0.07~44.62 μg·mL-1范围呈现良好的线性关系,回收率为98.9%。依据FDA的判定原则,自研制剂与参比制剂体外释放行为一致。结论: 本法适合环孢素眼用乳剂的体外释放度评价。
Objective: To develop a method for characterizing in vitro release of cyclosporine ophthalmic emulsion. Methods: The Franz diffusion cell and the polyvinylidene fluoride membrane were adopted with buffer-ethanol (40∶60) as receiving media. The sampling time was set at 60,125,190,255,320,385 min, respectively. Results: The in vitro release method showed that the inertia of membrane, specificity, sensitivity and selectivity met the requirements. The validation of HPLC showed that the quantitative limit of the method was 0.07 μg·mL-1 and a good linear relationship between the concentration range of 0.07-44.62 μg·mL-1. The average recovery was 98.9%. Compared with the original preparation by FDA guideline, the in vitro release of the self-developed preparation was the same as the reference preparation. Conclusions: This method is suitable for the in vitro release evaluation of cyclosporine eye drops.
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