尼莫地平口腔崩解片的药动学及相对生物利用度研究

Study on pharmacokinetics and relative bioavailability of nimodipine orally disintegrating tablet

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-t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 pharmacokineties 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 disintegeating 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 T max; （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 disintegeating tablet was capable of releasing rapidly, and had an enhanced bioavailability as compared with market tablet.