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乙醇摄入对犬体内丙氧芬吸收及生物转化的影响。

The effect of ethanol intake on propoxyphene absorption and biotransformation in dogs.

作者信息

Olsen H, Aune H, Lilleaasen P, Gulliksen M, Bodd E, Mørland J

出版信息

Alcohol Clin Exp Res. 1986 Aug;10(4):393-6. doi: 10.1111/j.1530-0277.1986.tb05111.x.

DOI:10.1111/j.1530-0277.1986.tb05111.x
PMID:3530016
Abstract

The effect of ethanol (0.5 and 1.0 g/kg) on gastrointestinal absorption and presystemic biotransformation of propoxyphene (4 mg/kg) was studied in dogs in a crossover design. Low ethanol doses (0.5 g/kg) had no effect on the bioavailability of propoxyphene. High ethanol doses (1.0 g/kg) enhanced the bioavailability of orally administered propoxyphene significantly (p less than 0.05). With this dose of ethanol, the area under the blood concentration versus time curve (AUC)0-5 h of propoxyphene was approximately 200% of the control value. The level of norpropoxyphene, a major metabolite of propoxyphene, was significantly decreased (p less than 0.05) after administration of high ethanol doses. In all blood samples, after propoxyphene administration, an unidentified metabolite of propoxyphene was found, which formation was dose dependently inhibited by ethanol.

摘要

采用交叉设计研究了乙醇(0.5和1.0 g/kg)对犬体内丙氧芬(4 mg/kg)胃肠道吸收及首过生物转化的影响。低剂量乙醇(0.5 g/kg)对丙氧芬的生物利用度无影响。高剂量乙醇(1.0 g/kg)显著提高了口服丙氧芬的生物利用度(p<0.05)。给予该剂量乙醇后,丙氧芬血药浓度-时间曲线下面积(AUC)0-5 h约为对照值的200%。高剂量乙醇给药后,丙氧芬的主要代谢产物去甲丙氧芬水平显著降低(p<0.05)。丙氧芬给药后,在所有血样中均发现一种未鉴定的丙氧芬代谢产物,其生成受到乙醇的剂量依赖性抑制。

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Alcohol Clin Exp Res. 1986 Aug;10(4):393-6. doi: 10.1111/j.1530-0277.1986.tb05111.x.
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