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使用一种新的立体选择性高效液相色谱法对醋丁洛尔及其代谢物双醋洛尔在人体中的处置进行的初步研究。

Preliminary study of the disposition in man of acebutolol and its metabolite, diacetolol, using a new stereoselective hplc method.

作者信息

Sankey M G, Gulaid A, Kaye C M

出版信息

J Pharm Pharmacol. 1984 Apr;36(4):276-7. doi: 10.1111/j.2042-7158.1984.tb04370.x.

DOI:10.1111/j.2042-7158.1984.tb04370.x
PMID:6144783
Abstract

A new stereospecific hplc method that is capable of simultaneously quantitating the S-(-)- and R-(+)-enantiomers of acebutolol and its major metabolite, diacetolol, in plasma and urine, is described. When applied to the assay of biological fluids collected during single and chronic oral dosing with acebutolol (Sectral), this procedure failed to reveal any important stereoselectivity in the disposition of either acebutolol or diacetolol in man. This may occur because acebutolol is metabolized by hydrolysis and N-acetylation, whereas the other beta-blockers which exhibit some degree of stereoselective disposition (e.g. metoprolol and propranolol) are primarily metabolized by oxidation.

摘要

本文描述了一种新的立体专一性高效液相色谱法,该方法能够同时定量测定血浆和尿液中醋丁洛尔及其主要代谢物双醋洛尔的S-(-)-和R-(+)-对映体。当应用于单次和长期口服醋丁洛尔(心得静)期间收集的生物体液的测定时,该程序未能揭示人体中醋丁洛尔或双醋洛尔处置过程中的任何重要立体选择性。这可能是因为醋丁洛尔通过水解和N-乙酰化代谢,而其他表现出一定程度立体选择性处置的β受体阻滞剂(如美托洛尔和普萘洛尔)主要通过氧化代谢。

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Preliminary study of the disposition in man of acebutolol and its metabolite, diacetolol, using a new stereoselective hplc method.使用一种新的立体选择性高效液相色谱法对醋丁洛尔及其代谢物双醋洛尔在人体中的处置进行的初步研究。
J Pharm Pharmacol. 1984 Apr;36(4):276-7. doi: 10.1111/j.2042-7158.1984.tb04370.x.
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The pharmacokinetics of acebutolol in man, following the oral administration of acebutolol HCl as a single dose (400 mg), and during and after repeated oral dosing (400 mg, b.d.).盐酸醋丁洛尔单次口服给药(400毫克)后,以及多次口服给药期间和之后(400毫克,每日两次)在人体中的药代动力学。
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Comparison of beta-adrenoceptor selectivity of acebutolol and its metabolite diacetolol with metoprolol and propranolol in normal man.醋丁洛尔及其代谢产物双醋洛尔与美托洛尔和普萘洛尔在正常人体内的β-肾上腺素受体选择性比较。
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Using supported liquid extraction together with cellobiohydrolase chiral stationary phases-based liquid chromatography with tandem mass spectrometry for enantioselective determination of acebutolol and its active metabolite diacetolol in spiked human plasma.采用支撑液液萃取结合基于纤维二糖水解酶手性固定相的液相色谱-串联质谱法对加标人血浆中的醋丁洛尔及其活性代谢物双醋洛尔进行对映体选择性测定。
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[Acebutolol and diacetolol: their binding to plasma proteins and erythrocytes and secretion with the saliva].醋丁洛尔和双醋洛尔:它们与血浆蛋白及红细胞的结合以及随唾液的分泌
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