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目的通过测定代谢产物,研究不同厂家生产的盐酸氟西汀胶囊的生物等效性。方法22名健康男性受试者采用随机交叉给药方案,分别单剂量口服40 mg盐酸氟西汀试验胶囊和参比胶囊,采用液相色谱-质谱联用法测定血浆样本中氟西汀的活性代谢产物去甲氟西汀的浓度,采用DAS软件计算药动学参数。结果口服盐酸氟西汀试验或参比胶囊后,去甲氟西汀的ρmax分别为(28.4±8.2)和(28.2±8.7)μg.L-1;tmax分别为(78.6±27.9)和(91.6±36.0)h;AUC0→t分别为(9 645.0±2 872.0)和(9 771.0±2 717.0)μg.h.L-1;AUC0→∞分别为(10 043.0±3 006.0)和(10 180.0±2 811.0)μg.h.L-1;t12分别为(164.5±43.5)和(166.8±43.2)h。试验制剂的相对生物利用度为(98.7±11.6)%。结论受试制剂与参比制剂生物等效。
Objective To study the bioequivalence of fluoxetine hydrochloride capsules produced by different manufacturers by measuring metabolites. Methods Twenty-two healthy male subjects were randomized to receive a crossover dose of 40 mg fluoxetine hydrochloride and reference capsules, respectively. The active metabolites of fluoxetine in plasma samples were determined by liquid chromatography-mass spectrometry The concentration of nafcillin product was calculated using the DAS software pharmacokinetic parameters. Results After oral administration of fluoxetine hydrochloride or reference capsules, the ρmax of nifacil was (28.4 ± 8.2) and (28.2 ± 8.7) μg.L-1, respectively; the tmax was (78.6 ± 27.9) and (91.6 ± 36.0) h; AUC0 → t were (9 645.0 ± 2 872.0) and (9 771.0 ± 2 717.0) μg.hL-1, respectively; AUC0 → ∞ were (10 043.0 ± 3 006.0) and (10 180.0 ± 2 811.0 ) μg.hL-1; t12 was (164.5 ± 43.5) and (166.8 ± 43.2) h, respectively. The relative bioavailability of the test preparation was (98.7 ± 11.6)%. Conclusions The test preparation is bioequivalent to the reference preparation.