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目的:研究青霉素V钾咀嚼片在健康人体的药物动力学及生物等效性。方法:19名健康志愿者随机双交叉、单剂量口服受试制剂和参比制剂0.472g,用液相色谱-串联质谱法(LC-MS/MS)测定人血浆中青霉素V的浓度,利用DAS 2.0药物动力学软件计算有关药物动力学参数、相对生物利用度,并评价2种制剂的生物等效性。结果:受试制剂和参比制剂的t_(max)分别为(0.54±0.09)h和(0.53±0.13)h;C_(max)分别为(10.64±3.84)μg·ml~(-1)和(10.87±4.43)μg·ml~(-1);t_(1/2)分别为(0.74±0.20)h和(0.75±0.10)h。AUC_(0-6h)分别为(11.92±4.04)μg·ml~(-1)·h和(12.34±4.17)μg·ml~(-1)·h;AUC_(0-∞)分别为(12.00±4.04)和(12.43±4.17)μg·ml~(-1)·h。青霉素V钾咀嚼片的相对生物利用度为(97.9±12.8)%。结论:两种制剂具有生物等效性。
Objective: To study the pharmacokinetics and bioequivalence of penicillin V potassium chewable tablets in healthy volunteers. METHODS: Twenty-nine healthy volunteers were randomized, double crossover, single-dose oral test formulation and reference formulation of 0.472 g. The concentration of penicillin V in human plasma was determined by liquid chromatography-tandem mass spectrometry (LC-MS / MS) 2.0 Pharmacokinetics software calculates pharmacokinetic parameters, relative bioavailability, and evaluates the bioequivalence of the two formulations. Results: The t max of the test preparation and the reference preparation were (0.54 ± 0.09) h and (0.53 ± 0.13) h, respectively, and the C max were (10.64 ± 3.84) μg · ml -1 and (10.87 ± 4.43) μg · ml -1; t 1/2 was 0.74 ± 0.20 h and 0.75 ± 0.10 h respectively. AUC0-6h were (11.92 ± 4.04) μg · ml -1 · h and (12.34 ± 4.17) μg · ml -1 · h, respectively; AUC 0- ∞ were respectively ± 4.04) and (12.43 ± 4.17) μg · ml -1 · h, respectively. The relative bioavailability of penicillin V potassium chewable tablets was (97.9 ± 12.8)%. Conclusion: Both formulations are bioequivalent.