Coppi G, Zanotti A, Mailland F
Forschungszentrum, Poli Industria Chimica S.p.A., Rozzano, Mailand, Italien.
Arzneimittelforschung. 1992 Nov;42(11A):1397-9.
This paper reports the pharmacokinetics of three dihydroergocristine (DHEC, CAS 17479-19-5) oral formulations in six volunteers. In a randomized crossover trial the volunteers received 6 mg of the drug (1 tablet of 6 mg; 3 ml of drops containing 2 mg/ml; 1 single-dose bottle containing 6 mg); radioimmunoassay was used for the determination of the unchanged drug plasma levels. DHEC shows a plasma profile according to a 3-compartment pharmacokinetic model with a long half-life and high distribution volume. The analysis of AUC0-infinity, Cmax, tmax, and other pharmacokinetic parameters shows that the three formulations investigated are practically bioequivalent.
本文报道了三种双氢麦角汀(DHEC,化学物质登记号17479-19-5)口服制剂在6名志愿者体内的药代动力学情况。在一项随机交叉试验中,志愿者服用6毫克该药物(1片6毫克的片剂;3毫升含2毫克/毫升的滴剂;1个含6毫克的单剂量瓶);采用放射免疫分析法测定血浆中未代谢药物的水平。双氢麦角汀呈现出符合三室药代动力学模型的血浆曲线,半衰期长且分布容积大。对药时曲线下面积(AUC0-无穷大)、峰浓度(Cmax)、达峰时间(tmax)及其他药代动力学参数的分析表明,所研究的三种制剂实际具有生物等效性。