牛磺-24,25-二氢fusidate钠对清醒大鼠头孢西丁和去甘氨酰胺精氨酸加压素直肠吸收的增强作用

Rectal absorption enhancement of cefoxitin and desglycinamide arginine vasopressin by sodium tauro-24,25-dihydrofusidate in conscious rats.

作者信息

van Hoogdalem E J, Heijligers-Feijen C D, Mathôt R A, Wackwitz A T, van Bree J B, Verhoef J C, de Boer A G, Breimer D D

机构信息

Division of Pharmacology, State University of Leiden, Sylvius Laboratories, The Netherlands.

出版信息

J Pharmacol Exp Ther. 1989 Nov;251(2):741-4.

PMID:2810123

Abstract

The effects of sodium tauro-24,25-dihydrofusidate (STDHF), an enhancer of nasal insulin absorption, on the rectal absorption of cefoxitin and desglycinamide arginine vasopressin (DGAVP) were evaluated in the rat. Cefoxitin and DGAVP proved to be poorly absorbed rectally without STDHF, but their bioavailability was considerably increased by STDHF in concentrations of 0.15 to 8% w/v. Both rectal infusion and rectal bolus delivery resulted in complete cefoxitin absorption at 4% w/v of STDHF. Delivery rate appeared to be an important factor in the effect of 4% w/v of STDHF on DGAVP bioavailability; on infusion a mean DGAVP bioavailability (+/- S.D.) of 47 +/- 12% was obtained, whereas after bolus delivery it amounted to 27 +/- 6%. For both compounds the effect of STDHF was significant at 0.5% w/v. It is concluded that STDHF is capable of actively enhancing the rectal absorption of poorly absorbed drugs, including small peptides.

摘要

牛磺-24,25-二氢fusidate钠（STDHF）是一种鼻腔胰岛素吸收增强剂，本研究在大鼠中评估了其对头孢西丁和去甘氨酰胺精氨酸加压素（DGAVP）直肠吸收的影响。结果表明，在没有STDHF的情况下，头孢西丁和DGAVP经直肠吸收较差，但当STDHF浓度为0.15%至8%（w/v）时，它们的生物利用度显著提高。在4%（w/v）的STDHF作用下，直肠输注和直肠推注给药均能使头孢西丁完全吸收。给药速率似乎是4%（w/v）的STDHF对DGAVP生物利用度产生影响的一个重要因素；输注时，DGAVP的平均生物利用度（±标准差）为47±12%，而推注给药后为27±6%。对于这两种化合物，0.5%（w/v）的STDHF即可产生显著效果。研究得出结论，STDHF能够有效增强包括小肽在内的难吸收药物的直肠吸收。