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不同溶媒及其体积对大鼠氨苯蝶啶口服吸收的影响

Effect of various vehicles and vehicle volumes on oral absorption of triamterene in rats.

作者信息

Patton T F, Gilford P

出版信息

J Pharm Sci. 1981 Oct;70(10):1131-4. doi: 10.1002/jps.2600701010.

Abstract

The oral bioavailability of triamterene in rats was investigated after its administration as a suspension in lipid and aqueous vehicles in addition to lactic acid solution. Triamterene is poorly soluble in both aqueous and lipid vehicles. A 1-ml oral dose volume showed that lipid vehicles may provide some enhancement of oral availability compared with aqueous suspensions. However, when the vehicle volume was reduced to a realistic dosage form volume for the rat, peanut oil and aqueous suspensions were indistinguishable from each other with respect to peak height, peak time, and overall bioavailability. For a given vehicle small vehicle volumes resulted in a better relative oral availability than did large vehicle volumes.

摘要

除乳酸溶液外,将氨苯蝶啶以悬浮液形式分别溶于脂质和水性载体中,研究其在大鼠体内的口服生物利用度。氨苯蝶啶在水性和脂质载体中的溶解度都很低。1毫升的口服剂量表明,与水性悬浮液相比,脂质载体可能会提高口服生物利用度。然而,当载体体积减小到大鼠实际剂型的体积时,花生油和水性悬浮液在峰高、峰时间和总体生物利用度方面没有差异。对于给定的载体,较小的载体体积比较大的载体体积能产生更好的相对口服生物利用度。

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