Burri C, Baltz T, Giroud C, Doua F, Welker H A, Brun R
Swiss Tropical Institute, Basel.
Chemotherapy. 1993 Jul-Aug;39(4):225-34. doi: 10.1159/000239130.
With a biological assay and atomic absorption spectrometry we determined the level of melarsoprol in the serum and cerebrospinal fluid of 19 patients treated with melarsoprol in Daloa, Ivory Coast. Most serum levels were between 2 and 4 micrograms/ml 24 h after administration, and were still > or = 0.1 microgram/ml after 120 h. Levels in the cerebrospinal fluid were between 0 and 0.1 microgram/ml. Elimination was biphasic, with a pronounced beta 1 phase. Mean terminal elimination half-life of melarsoprol was about 35 h, volume of distribution was about 100 l and total clearance was about 50 ml/min. The results of these first pharmacokinetic studies on melarsoprol were used to simulate possible alternative therapy schemes which might avoid some of the problems that arise with melarsoprol use.
我们使用生物测定法和原子吸收光谱法，测定了在科特迪瓦的达洛亚接受美拉胂醇治疗的19名患者血清和脑脊液中美拉胂醇的含量。多数患者给药后24小时血清含量在2至4微克/毫升之间，120小时后仍≥0.1微克/毫升。脑脊液中的含量在0至0.1微克/毫升之间。消除呈双相性，β1期明显。美拉胂醇的平均终末消除半衰期约为35小时，分布容积约为100升，总清除率约为50毫升/分钟。这些关于美拉胂醇的首次药代动力学研究结果被用于模拟可能的替代治疗方案，这些方案或许可以避免使用美拉胂醇时出现的一些问题。
