Human pharmacokinetics of chloroquine and proguanil delivered in a single capsule for malaria chemoprophylaxis.

J E Touze, A Keundjian, T Fusai, J C Doury
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Abstract

Two antimalarial prophylactic regimens were compared in 17 healthy volunteers. Regimen A consisted of daily ingestion of a single capsule containing 100 mg base chloroquine (CQ) and 200 mg proguanil (PG). Regimen B consisted of daily ingestion of separate tablets of CQ (100 mg base) and PG (two 100 mg tablets). Both treatments lasted for 12 days. Effective chloroquine levels were reached after 72 hours with both regimens (49.9 ng/ml for treatment A and 36.7 ng/ml for treatment B). Proguanil and cycloguanil plasma levels were significantly lower on sampling obtained at H3 (three hours later) and H6 (six hours later) on day 1 in the regimen A (p < 0.002). Thereafter there were no significant difference between the two regimens. Both regimens were well tolerated, but regimen A using the capsule appeared better accepted and facilitates compliance.

用于疟疾化学预防的氯喹和proguanil单胶囊的人体药代动力学。
在17名健康志愿者中比较了两种抗疟疾预防方案。方案A包括每日服用含有100 mg碱氯喹(CQ)和200 mg proguanil (PG)的单粒胶囊。方案B包括每日单独服用CQ片(100 mg基片)和PG片(2片100 mg基片)。两组治疗均持续12天。两种方案在72小时后均达到有效的氯喹水平(治疗A为49.9 ng/ml,治疗B为36.7 ng/ml)。在方案A第1天H3(3小时后)和H6(6小时后)取样时,Proguanil和cycloguanil血浆水平显著降低(p < 0.002)。此后,两种方案之间没有显著差异。两种方案均耐受良好,但使用胶囊的方案A似乎更容易接受并促进依从性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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