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目的用高效液相色谱-质谱法(LC-MS)测定受试者口服盐酸金刚乙胺制剂后的血药浓度,估算受试制剂和参比制剂的药动学参数,评价两种制剂的生物等效性和相对生物利用度。方法采用随机二交叉设计试验,20例男性健康志愿受试者,单剂量口服受试制剂盐酸金刚乙胺颗粒和参比制剂盐酸金刚乙胺片。以LC-MS测定血浆中金刚乙胺的浓度。采用BAPP3.0软件处理计算主要药动学参数。结果受试制剂和参比制剂血浆中金刚乙胺的t1/2分别为(26.46±4.48)和(27.41±4.42)h;ρmax分别为(84.5±17.7)和(93.1±17.8)μg·L-1;tmax分别为(4.08±2.86)和(4.70±3.59)h;AUC0-120h分别为(3204±691)和(3450±724)μg·h·L-1;AUC0-∞分别为(3395±767)和(3661±820)μg·h·L-1;人体相对生物利用度为(93.4±10.8)%。结论2种制剂在健康人体内具有生物等效性。
Objective To determine the plasma concentration of oral administration of rimantadine hydrochloride by LC-MS and evaluate the pharmacokinetic parameters of the test and reference preparations, and to evaluate the bioavailability of the two preparations Equivalence and relative bioavailability. Methods A randomized two-crossover design trial was conducted. Twenty healthy male volunteers were enrolled in this study. A single dose of rimantadine hydrochloride tablets and a reference preparation of rimantadine hydrochloride tablets were used. The plasma rimantadine concentration was determined by LC-MS. Using BAPP3.0 software to calculate the main pharmacokinetic parameters. Results The plasma levels of rimantadine were (26.46 ± 4.48) and (27.41 ± 4.42) h in the test and reference preparations, respectively, and the ρmax were (84.5 ± 17.7) and (93.1 ± 17.8) μg · L- 1; tmax was (4.08 ± 2.86) and (4.70 ± 3.59) h respectively; AUC0-120h was (3204 ± 691) and (3450 ± 724) μg · h · L-1; 767) and (3661 ± 820) μg · h · L-1, respectively. The relative bioavailability in human was (93.4 ± 10.8)%. Conclusion The two preparations are bioequivalent in healthy volunteers.