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一粒1000毫克的对乙酰氨基酚栓剂与两粒500毫克的栓剂生物等效吗?

Is one paracetamol suppository of 1000 mg bioequivalent with two suppositories of 500 mg.

作者信息

Närvänen T, Halsas M, Smal J, Marvola M

机构信息

Department of Pharmacy, University of Helsinki, Finland.

出版信息

Eur J Drug Metab Pharmacokinet. 1998 Apr-Jun;23(2):203-6. doi: 10.1007/BF03189340.

Abstract

A common belief is that one tablet or suppository containing, e.g. 100 mg of a drug can be substituted, without any changes in the therapeutic effect, with two units of the same brand containing 50 mg of the drug. In the present study a single dose of paracetamol was administered to healthy volunteers as (a) two tablets of 500 mg, (b) two suppositories of 500 mg, and (c) one suppository of 1000 mg. There were statistically significant differences in all bioavailability parameters (t(max), C(max) and AUC) between the three treatments. The relative bioavailability of the 500 mg suppositories was 77% and that of the 1000 mg suppositories 66%. The absorption rate from suppositories was markedly lower than from the tablets. Especially low absorption rate was obtained with the suppository of 1000 mg. The two strengths, although having the same trade name, were not therefore bioequivalent.

摘要

一种普遍的看法是,例如一片或一粒含有100毫克药物的片剂或栓剂,可以用两片同一品牌的含有50毫克药物的制剂替代,而治疗效果不会有任何变化。在本研究中,对健康志愿者单次给予对乙酰氨基酚,给药方式为:(a)两片500毫克的片剂,(b)两粒500毫克的栓剂,以及(c)一粒1000毫克的栓剂。三种治疗方法在所有生物利用度参数(t(max)、C(max)和AUC)上均存在统计学上的显著差异。500毫克栓剂的相对生物利用度为77%,1000毫克栓剂的相对生物利用度为66%。栓剂的吸收速率明显低于片剂。1000毫克的栓剂吸收速率尤其低。因此,这两种规格虽然商品名相同,但生物不等效。

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