目的:比较试验制剂和参比制剂体外释放的一致性。方法:采用Franz扩散池法,以0.45 μm聚醚砜膜为人工膜,7 mL脱气后的Transcutol P(二乙二醇单乙醚)-水(50∶50)为接收液,转速500 r·min-1,温度32 ℃,取样体积2 mL,于0.5、1、2、4、6 h取样,以HPLC法分别测定药物在人工膜中的释放量随时间变化的释放规律,评价试验和参比制剂体外释放的一致性。结果:试验制剂与参比制剂在接收液中的累积释放百分率分别为93.7%和89.1%,单位面积累积释放量分别为2 622.0和2 479.0 μg·cm-2,二者体外释放率比值的90%置信区间在75%~133.33%(FDA一致性规定限度)范围内。结论:试验制剂与参比制剂体外释放行为一致。
Objective: To compare the consistency in vitro release of test preparation and reference preparation. Methods: Franz diffusion cell method and 0.45 μm polyethersulfone membrane were used. 7 mL of degassed Transcutol P-water (50∶50) was used as the receiving liquid, the speed was 500 r·min-1, the temperature was 32 ℃, the sampling volume was 2 mL. Samples were taken at 0.5, 1, 2, 4 and 6 hours, and the release amount of the drug in the artificial membrane was determined with time by HPLC method. The consistency in vitro release of test preparation and reference preparation was evaluated. Results: The cumulative release percentages of test preparation and reference preparation in the receiving solution were 93.7% and 89.1%, respectively, and the cumulative release per unit area was 2 622.0 and 2 479.0 μg·cm-2, respectively. The 90% confidence interval of the ratio of the in vitro release rate of the two was within 75%-133.33% according to FDA guidelines. Conclusion: In vitro release behavior of the test preparation is consistent with that of the reference preparation.
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