尼莫地平片剂生物利用度和健康人药代动力学研究

STUDIES ON THE BIOAVAILABILITY AND PHARMACOKINETICS OF NIMODIPINE TABLET IN HUMAN BODY

用高效液相色谱法测定了6名健康志愿者口服二种尼莫地平片剂的相对生物利用度和药代动力学参数。结果表明:尼莫地平在人体内的浓度—时间数据可用一室开放模型拟合,主要动力学参数与国外文献报道一致。新片剂和普通片的人体相对生物利用度分别为82.39%和16.01%。

The article determined the bioavailability and pharmacokinetic parameters of two kinds of nimodipine tablets produced by Tianjin Center Pharmaceutical Factory in 6 healthy volunteers using HPLC method. The commercially available conventional tablet A and the tablet formulation B were compared with the reference solution C in vivo. The pharmacokinetic parameters of nimodipine in vivo were estimated by using PKBP--N1 program on the basis of one compartment open model. After administration of 120 mg dose of B, the pharmacokinetic parameters were as follows: Tp=0.977 h, C_(max)=44.28ng/ml, ka=2.02 h^(-1), t 1/2=1.63 h, Vd=26. 25 L/ kg, AUC=130.56 ng·h^(-1)·ml^(-1). The result imply that nimodipine is absorbed rapidly, distributed widely in the body, and also eliminated at a fairly rapid rate. The bioavailability of A and B relative to C was 16.01% and 82. 39% respectively. The new tablet formulation B is superior to tablet A.