论文部分内容阅读
目的:比较尼莫地平(Nim)漂浮缓释片与普通片的药物动力学、相对生物利用度及体内外相关性.方法:10例男性健康受试者自身交叉对照、单剂量po Nim漂浮缓释片或普通片各120mg,采用HPLC法测定血浆Nim浓度,单室模型拟合药物动力学参数.结果:Nim缓释片和普通片的t_(max)分别为(2.83±0.45)和(0.87±0.27)h(P<0.01),C_(max)分别为(32.82±6.36)和(48.71±8.94)ng/ml(P<0.01),AUC分别为(204.81±45.03)和(159.98±39.96)h·ng/ml(P<0.01).数据经对数转换后进行双单侧检验,两种制剂生物不等效;缓释片的相对生物利用度为(129.89±17.02)%;其体内吸收与体外释药具有显著的相关性(P<0.01).结论:Nim漂浮缓释片生物利用度优于普通片,达到剂型设计要求.
OBJECTIVE: To compare the pharmacokinetics, relative bioavailability and in vitro and in vivo correlation of Nim floating sustained-release tablets and ordinary tablets.Methods: Ten healthy male volunteers were crossed with each other, and single-dose po Nim floating The plasma concentration of Nim was determined by HPLC and the pharmacokinetic parameters were fitted by single-compartment model.Results: The t max of Nim sustained-release tablets and ordinary tablets were (2.83 ± 0.45) and (0.87 (32.82 ± 6.36) and (48.71 ± 8.94) ng / ml respectively (P <0.01), and the AUC were (204.81 ± 45.03) and (159.98 ± 39.96), respectively h · ng / ml (P <0.01) .The data were logarithmically converted to double unilateral test, and the bioavailability of the two preparations was not equal. The relative bioavailability of the sustained release tablets was (129.89 ± 17.02)%, (P <0.01) .Conclusion: The bioavailability of Nim floating sustained-release tablets is better than that of common tablets, which meets the requirements of dosage form design.