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[某些活性成分和辅料对兔直肠给药乙酰水杨酸生物处置的影响]

[The effect of certain active principles and excipients on the biodisposition of rectally administered acetylsalicylic acid in the rabbit].

作者信息

Fehri B, Aiache J M, Boukef K

出版信息

J Pharm Belg. 1989 May-Jun;44(3):197-209.

PMID:2795423
Abstract

In this work, we have studied in the rabbit, bioavailability of acetylsalicylic acid contained respectively in three forms of suppositories which are made as follows: for the first by only acetylsalicyclic acid (0.1 g); for the second by the association: acetylsalicylic acid (0.1 g) and phenobarbital (0.01 g); and for the third by acetylsalicylic acid (0.01 g), ascorbic acid (0.02 g) and thiamine chloride (0.002 g). It has been shown that ascorbic acid and thiamine chloride do not change the bioavailability of acetylsalicylic acid, while phenobarbital decreases it. In this work we have also compared two pharmaceutical forms of suppositories containing acetylsalicylic acid, ascorbic acid and thiamine chloride. In one of the two forms, acetylsalicylic acid is buffered by glycocolle. The study which consisted in giving the two forms to the rabbit rectally was concerned with the effect of glycocolle on the bioavailability of acetylsalicylic acid. It was shown that making glycocolle a buffer to acetylsalicylic acid resulted in an improved absorption as well as a delayed elimination of acetylsalicyclic acid. In this study too, we have evaluated the bioavailability of acetylsalicylic acid which is released from two types of suppositories containing respectively base witepsol W31 and base cocoa butter. In order to study this bioavailability whole suppositories were administered by rectal route to the rabbits after 24 hours of fasting (balanced crossover design with 15 days of interval after each study). Statistical analysis does not reveal any significant difference between the two forms of suppositories.

摘要

在本研究中,我们在兔子身上研究了分别以三种栓剂形式存在的乙酰水杨酸的生物利用度,这三种栓剂制备如下:第一种仅含乙酰水杨酸(0.1克);第二种为乙酰水杨酸(0.1克)与苯巴比妥(0.01克)的组合;第三种为乙酰水杨酸(0.01克)、抗坏血酸(0.02克)和氯化硫胺素(0.002克)。结果表明,抗坏血酸和氯化硫胺素不会改变乙酰水杨酸的生物利用度,而苯巴比妥会降低其生物利用度。在本研究中,我们还比较了两种含有乙酰水杨酸、抗坏血酸和氯化硫胺素的栓剂剂型。在这两种剂型中的一种中,乙酰水杨酸用明胶缓冲。该研究通过给兔子直肠给药这两种剂型,关注明胶对乙酰水杨酸生物利用度的影响。结果表明,用明胶作为乙酰水杨酸的缓冲剂可提高其吸收并延迟乙酰水杨酸的消除。在本研究中,我们还评估了分别从含有维特泊W31基质和可可脂基质的两种栓剂中释放出的乙酰水杨酸的生物利用度。为了研究这种生物利用度,在禁食24小时后通过直肠途径给兔子施用整个栓剂(采用平衡交叉设计,每次研究后间隔15天)。统计分析未显示两种栓剂剂型之间有任何显著差异。

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J Pharm Belg. 1989 May-Jun;44(3):197-209.
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