Siegers C P, Iven H, Strubelt O
Arzneimittelforschung. 1977;27(6a):1271-4.
Plasma concentrations and renal excretion of 14,15-dihydro-14beta-hydroxy-(3alpha,16alpha)-eburnamenine-14-carbonic acid methylester (vincamine, Vincapront) were studied in 5 healthy volunteers following the oral intake of 30 or 60 mg vincamine, respectively. After the higher dose (60 mg vincamine), the treatment was continued by the daily intake of 3 X 20 mg vincamine for 5 days. Plasma vincamine levels were determined in the morning prior to the ingestion of the first 20-mg dose and in the evening 2 h after the intake of the third 20-mg dose. Our results prove that vincamine is rapidly liberated and absorbed from the tablet formulation used, the maximum plasma levels being reached 90 min after ingestion and amounting to a mean value of 139 ng/ml after 30 mg and to a mean of 252 ng/ml after 60 mg of vincamine. There was a biphasic elimination of vincamine after both doses indicating a process of distribution influencing also the elimination phase. In the 24-h urine, unchanged vincamine amounted to 5.8% of the applied dose after 30 mg and to 7.3% after 60 mg vincamine. Vincamine did not accumulate during the daily intake of 60 mg for 6 days. Side-effects were not observed in any volunteer during the period of observation.
分别对5名健康志愿者口服30毫克或60毫克长春胺(长春西汀,Vincapront)后,研究了14,15 - 二氢 - 14β - 羟基 -(3α,16α)- 长春胺 - 14 - 碳酸甲酯的血浆浓度和肾脏排泄情况。在服用较高剂量(60毫克长春胺)后,继续每日服用3×20毫克长春胺,持续5天。在摄入首剂20毫克之前的早晨以及摄入第三剂20毫克后2小时的晚上测定血浆长春胺水平。我们的结果证明,长春胺从所用片剂制剂中迅速释放并吸收,摄入后90分钟达到最大血浆水平,30毫克长春胺后平均值为139纳克/毫升,60毫克长春胺后平均值为252纳克/毫升。两种剂量后长春胺均呈现双相消除,表明分布过程也影响消除阶段。在24小时尿液中,30毫克长春胺后未变化的长春胺占给药剂量的5.8%,60毫克长春胺后为7.3%。在每日摄入60毫克长春胺,持续6天的过程中,长春胺未蓄积。在观察期间,未在任何志愿者中观察到副作用。