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西咪替丁、碳酸氢盐和葡萄糖对不同剂型吡喹酮生物利用度的影响。

Effect of cimetidine, bicarbonate and glucose on the bioavailability of different formulations of praziquantel.

作者信息

Metwally A, Bennett J L, Botros S, Ebeid F

机构信息

Department of Pharmacology, Theodor Bilharz Research Institute, Giza, Egypt.

出版信息

Arzneimittelforschung. 1995 Apr;45(4):516-8.

PMID:7779153
Abstract

The effects of cimetidine, bicarbonate and glucose on the bioavailability of the two brands of praziquantel (CAS 55268-74-1) available in Egypt were studied in normal healthy volunteers. Brand 1 when coadministered with cimetidine showed elevated concentration of the drug at all time intervals. The difference was statistically significant at 3, 4, 6 and 8 h following treatment. On the other hand coadministration of cimetidine with brand 2 (Distocide) showed elevated concentration of the drug 1 h post treatment. Analysis of the pharmacokinetic parameters revealed insignificant difference comparing brand 1 versus brand 1 plus cimetidine. Significant differences were observed between the elimination rate constant Ke (h-1) for brand 2 (0.017 +/- 0.004) alone versus brand 2 plus cimetidine (0.006 +/- 0.001). Coadministration of bicarbonate or glucose with either brand 2 or brand 1 tended to depress the serum concentration of praziquantel. Possible explanations of these findings are discussed.

摘要

在正常健康志愿者中研究了西咪替丁、碳酸氢盐和葡萄糖对埃及现有的两种品牌吡喹酮(CAS 55268-74-1)生物利用度的影响。品牌1与西咪替丁合用时,在所有时间间隔药物浓度均升高。治疗后3、4、6和8小时差异具有统计学意义。另一方面,西咪替丁与品牌2(Distocide)合用时,治疗后1小时药物浓度升高。药代动力学参数分析显示,品牌1与品牌1加西咪替丁相比差异不显著。单独品牌2(0.017±0.004)与品牌2加西咪替丁(0.006±0.001)的消除速率常数Ke(h-1)之间观察到显著差异。碳酸氢盐或葡萄糖与品牌2或品牌1合用时,往往会降低吡喹酮的血清浓度。讨论了这些发现的可能解释。

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