抗酸剂对拉替拉韦药代动力学无临床相关影响。
Lack of a clinically relevant effect of an antacid on the pharmacokinetics of lersivirine.
机构信息
Pfizer Global Research and Development, New London, CT 06320, USA.
出版信息
Antimicrob Agents Chemother. 2010 May;54(5):2209-11. doi: 10.1128/AAC.01110-09. Epub 2010 Feb 16.
Abstract
Lersivirine (UK-453,061) is a next-generation nonnucleoside reverse transcriptase inhibitor that displays potent antiviral activity. Lersivirine solubility is pH dependent; therefore, the effect of coadministration of antacid on the pharmacokinetics of lersivirine in healthy subjects was investigated. The ratio of adjusted geometric means (750 mg lersivirine plus 20 ml Maalox Max/750 mg lersivirine alone) for the area under the curve from time zero extrapolated to infinite time (AUC(inf)) was 101.86%, showing that coadministration of an antacid had no effect on lersivirine exposure. Coadministration appeared to be safe and relatively well tolerated.
摘要
利匹韦林（UK-453,061）是一种新一代非核苷类逆转录酶抑制剂，具有很强的抗病毒活性。利匹韦林的溶解度取决于 pH 值；因此，研究了抗酸剂与利匹韦林同时给药对健康受试者中利匹韦林药代动力学的影响。调整后的几何均值比（750mg 利匹韦林加 20ml Maalox Max/750mg 利匹韦林单独给药）的 AUC（inf）比值为 101.86%，表明抗酸剂的同时给药对利匹韦林的暴露没有影响。联合用药似乎是安全的，且具有较好的耐受性。
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