非那雄胺血浆浓度测定及其生物等效性研究

Determination of Finasteride in Human Plasma and Study on Its Bioequivalence

目的建立非那雄胺血药浓度的液相色谱-质谱联用(LC-MS)测定法,用于人体生物等效性研究。方法采用随机双交叉试验设计,20名健康受试者口服受试制剂和参比制剂2mg,用LC-MS法测定人血浆中的非那雄胺浓度。结果受试制剂和参比制剂的0～24h药时曲线下面积(AUC0-24)分别为(123.95±25.47)μg.h/L和(126.35±28.16)μg.h/L,AUC0-∞分别为(126.12±27.48)μg.h/L和(129.85±29.12)μg.h/L,峰浓度(Cmax)分别为(22.17±3.83)μg/L和(22.48±4.69)μg/L,达峰时间(tmax)分别为(3.1±0.6)h和(2.9±0.8)h,半衰期(t1/2)分别为(4.2±0.3)h和(4.3±0.5)h。受试制剂的相对生物利用度为(99.4±9.2)%。结论两种非那雄胺片剂具有生物等效性。

Objective To study the pharmacokinetics and relative bioavailability of finasteride tablets in Chinese healthy volunteers. Methods Twenty male healthy volunteers received 2 mg finasteride tablet orally in a random crossover design. Drug concentrations in plasma were determined by LC- MS, Results The main pharmacokinetic parameters of tested and reference tablets were as follows： AUC（0-24）： （123.95 ± 25.47）μg ·h/L, （126.35±28, 16）μg ·h/L, AUC（0-∞）： （126. 12 ±27.48）μg ·h/L, （129.85 ±29. 12）μg ·h/L, Cmax： （22. 17 ±3.83）μg/L, （22. 48 ± 4. 69）μg/L, tmax：（3. 1 ± 0.6）h, （2. 9 ± 0. 8）h, t1/2： （4. 2 ± 0. 3）h, （4. 3 ± 0. 5）h, respectively. The relative bioavailability of the test tablet was （99. 4 ± 9.2）%. Conclusion The two kinds of tablets are bioequivalent.