Tan-ariya P, Na-Bangchang K, Ubalee R, Thanavibul A, Thipawangkosol P, Karbwang J
Department of Microbiology, Faculty of Science, Mahidol University, Bangkok, Thailand.
Southeast Asian J Trop Med Public Health. 1998 Mar;29(1):18-23.
The pharmacokinetics of a single oral dose of artemether (300 mg) and pyrimethamine (100 mg) given as each individual drug alone or as a drug combination (artemether 300 mg plus pyrimethamine 100 mg), were investigated in 8 healthy male Thai volunteers. Both artemether and pyrimethamine were rapidly absorbed after oral administration. Elimination of pyrimethamine was however, a relatively slow process compared with artemether, and thus resulted in a long terminal phase elimination half-life (50-106 hours). Pharmacokinetics of artemether and dihydroartemisinin following a single oral dose of artemether alone or in combination with pyrimethamine were similar. In contrast, coadministration of artemether resulted in significantly increased Cmax (medians of 818 vs 1,180 ng/ml) and contracted the apparent volume of distribution (medians of 3 vs 2.56 l/kg) of pyrimethamine.
在8名健康的泰国男性志愿者中，研究了单剂量口服蒿甲醚（300毫克）和乙胺嘧啶（100毫克）单独给药或联合给药（蒿甲醚300毫克加乙胺嘧啶100毫克）后的药代动力学。口服给药后，蒿甲醚和乙胺嘧啶均迅速吸收。然而，与蒿甲醚相比，乙胺嘧啶的消除是一个相对缓慢的过程，因此导致较长的终末相消除半衰期（50 - 106小时）。单剂量口服蒿甲醚单独给药或与乙胺嘧啶联合给药后，蒿甲醚和双氢青蒿素的药代动力学相似。相比之下，蒿甲醚的共同给药导致乙胺嘧啶的Cmax显著增加（中位数分别为818 vs 1180纳克/毫升），并使乙胺嘧啶的表观分布容积缩小（中位数分别为3 vs 2.56升/千克）。
