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次水杨酸铋制剂中水杨酸盐的吸收情况。

Salicylate absorption from a bismuth subsalicylate preparation.

作者信息

Feldman S, Chen S L, Pickering L K, Cleary T G, Ericsson C D, Hulse M

出版信息

Clin Pharmacol Ther. 1981 Jun;29(6):788-92. doi: 10.1038/clpt.1981.112.

Abstract

The active ingredient in Pepto-Bismol (PB) (Norwich-Eaton), a common antidiarrheal, is bismuth subsalicylate. The absorption of salicylate after oral PB was studied in six fasted men. Plasma concentrations of total salicylate and the urinary excretion profile of salicylate were determined as a function of time and dose. After 60 ml PB, 500.1 +/- 33.6 mg (mean +/- SD) salicylate were recovered in urine, representing 95.0 +/- 6.4% of salicylic acid equivalents in 60 ml of the formulation. Peak plasma salicylate levels were reached 0.5 to 3 hr after ingestion and averaged 40.1 +/- 17.3 micrograms/ml. Absorption of salicylate was also essentially complete after 15- and 30-ml doses of the antidiarrheal preparation, and a linear relationship between dose and recovery of salicylate in the urine was found. Salicylate kinetics was nonlinear after a multiple-dose regimen of 60 ml every 6 hr for five doses.

摘要

必奇(PB)(诺维奇伊顿公司生产)是一种常见的止泻药,其活性成分是碱式水杨酸铋。对6名空腹男性口服PB后的水杨酸盐吸收情况进行了研究。测定了总水杨酸盐的血浆浓度以及水杨酸盐的尿排泄情况随时间和剂量的变化。服用60毫升PB后,尿中回收了500.1±33.6毫克(平均值±标准差)水杨酸盐,占60毫升制剂中水杨酸当量的95.0±6.4%。摄入后0.5至3小时达到血浆水杨酸盐峰值水平,平均为40.1±17.3微克/毫升。服用15毫升和30毫升剂量的止泻制剂后,水杨酸盐的吸收也基本完成,且发现尿中水杨酸盐回收率与剂量之间呈线性关系。每6小时服用60毫升,共服用5剂的多剂量方案后,水杨酸盐动力学呈非线性。

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