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目的研究尼莫地平缓释片的药动学和相对生物利用度,评价尼莫地平缓释片2种制剂的人体生物等效性。方法18例健康男性志愿者采用自身交叉给药方案,分别单次和连续多次口服2种尼莫地平缓释片后,利用高效液相色谱法(HPLC)测定血药浓度。结果单次口服2种尼莫地平缓释片受试制剂和参比制剂的主要药动学参数为:t1/2分别为(2.70±0.48)和(2.85±0.81)h;ρmax分别为(31.00±9.13)和(32.13±10.00)μg·L-1;tmax分别为(2.97±0.88)和(2.89±0.76)h;AUC0-t分别为(177.64±42.43)和(186.41±49.37)μg·h·L-1,AUC0-∞分别为(190.20±45.22)和(204.34±54.46)μg·h·L-1,与参比制剂相比,受试制剂的相对生物利用度为(99.18±25.08)%。连续多次口服2种尼莫地平缓释片受试制剂和参比制剂达稳态后主要药动学参数为:ρssmax分别为(42.37±6.34)和(45.66±6.88)μg·L-1;ρssmin分别为(13.37±3.37)和(13.51±2.55)μg·L-1;DFss分别为(118.57±21.09)和(127.22±27.54)%,与参比制剂相比,受试制剂的相对生物利用度为(97.11±12.25)%。结论2制剂的尼莫地平缓释片具有生物等效性。
Objective To study the pharmacokinetics and relative bioavailability of nimodipine sustained-release tablets and to evaluate the bioequivalence of two preparations of nimodipine sustained-release tablets. Methods Eighteen healthy male volunteers were randomized to receive a single oral dose of nimodipine for several consecutive times, followed by continuous high-performance liquid chromatography (HPLC). Results The main pharmacokinetic parameters of the two formulations of nimodipine sustained-release tablets were (2.70 ± 0.48) and (2.85 ± 0.81) h respectively for t1 / 2 and (31.00 ± 9.13, and (32.13 ± 10.00) μg · L-1, respectively; tmax was (2.97 ± 0.88) and (2.89 ± 0.76) h respectively; AUC0-t was (177.64 ± 42.43) and (186.41 ± 49.37) μg · h · The relative bioavailability of L-1 and AUC0-∞ was (190.20 ± 45.22) and (204.34 ± 54.46) μg · h · L-1, respectively. %. The main pharmacokinetic parameters of two nimodipine sustained-release tablets and reference preparations after steady-state oral administration were ρssmax of (42.37 ± 6.34) and (45.66 ± 6.88) μg · L-1, respectively; ρssmin were (13.37 ± 3.37) and (13.51 ± 2.55) μg · L-1, respectively; DFss was (118.57 ± 21.09) and (127.22 ± 27.54)%, respectively. Compared with the reference formulation, the relative bioavailability Degree was (97.11 ± 12.25)%. Conclusion 2 preparations of nimodipine sustained-release tablets with bioequivalence.