van Hoogdalem E J, Heijligers-Feijen C D, Verhoef J C, de Boer A G, Breimer D D
Division of Pharmacology, Sylvius Laboratories, State University of Leiden, The Netherlands.
Pharm Res. 1990 Feb;7(2):180-3. doi: 10.1023/a:1015837004307.
The bile salt derivative sodium tauro-24,25-dihydrofusidate (STDHF) has been reported to promote nasal absorption of insulin. In the present study the effect of STDHF on rectal insulin absorption was investigated in rats. At concentrations of 1 and 4% (w/v) it enhanced insulin bioavailability from 0.2 +/- 0.2 (control) to 4.2 +/- 3.2 and 6.7 +/- 2.1%, respectively, as assessed by radioimmunoassay. Insulin preparations with STDHF reduced blood glucose concentrations considerably in a concentration-dependent way. Coadministration of STDHF with Na2EDTA (0.25%, w/v) tended to increase further insulin bioavailability and hypoglycemic response. Varying the site of rectal administration did not influence these parameters.
据报道，胆汁盐衍生物牛磺-24,25-二氢fusidate钠（STDHF）可促进胰岛素的鼻腔吸收。在本研究中，研究了STDHF对大鼠直肠胰岛素吸收的影响。通过放射免疫测定评估，在1%和4%（w/v）的浓度下，它分别将胰岛素的生物利用度从0.2±0.2（对照）提高到4.2±3.2%和6.7±2.1%。含有STDHF的胰岛素制剂以浓度依赖的方式显著降低了血糖浓度。将STDHF与Na2EDTA（0.25%，w/v）共同给药倾向于进一步提高胰岛素的生物利用度和降糖反应。改变直肠给药部位不影响这些参数。
