尼莫地平口腔崩解片的药动学及相对生物利用度研究

摘要

目的 研究尼莫地平口腔崩解片在人体内的药动学,比较其与市售尼莫地平片人体内药物动力学及相对生物利用度.方法 将6名健康志愿者随机分成两组,交叉单剂量口服尼莫地平口腔崩解片A和市售片B各60 mg,采用HPLC 法测定血浆中尼莫地平的浓度.结果 口服尼莫地平口腔崩解片A和市售片B后,主要药代动力学参数分别为Cmax(256.23±54.64) g/ml、( 102.415±36.96) g/ml;Tmax分别为(0.7049±0 035)h、(1.3317±0.123) h;T1/2分别为(0.2734±0.031)h、(1.1958±0.141) h;AUC0-1分别为(622.77±98.03) g/(ml·h)、(354.63±96.24)g/(ml·h).尼莫地平口腔崩解片A相对于市售片B的人体生物利用度为177.27％.结论 自制尼莫地平口崩片速释效果明显,并能提高生物利用度.%Objective To research the pharmacokinetics and relative bioavailability of Nimodipine rapid disintegeating tablet in human body, which was compared with Nimodipine market tablets. Methods 6 cases of health volunteer were divide into two groups randomly , alternately taking rapid disintegrating tablet A and market tablet B of Nimodipine 60mg single dosage orally, HPLC was used to determine the concentration of Nimodipine in blood. Results The main Pharmacokinetics parameters after single oral administration Nimodipine rapid disintegeating tablet A and Nimodipine market tablet B were (256.23 ±54.64) g/ml, (102.415 ±36. 96) g/ml in Cmax (0. 7049 ±0. 035) h, (1. 3317 ±0. 123) h in Tmax; (0.2734 ±0.031) h, (1.1958±0. 141) h in T1/2; (622.77 ±98.03) g/(ml · h), (354.63 ±96.24) g/(ml · h) in AUC0-t, respectively. The bioavailability of rapid disintegeating tablet was 177.27% relative to market tablet. Conclusion Nimodipine rapid disintegealing tablet was capable of releasing rapidly, and had an enhanced bioavailahility as compared with market tablet.