Baldwin P A, Klingbeil C K, Grimm C J, Longenecker J P
California Biotechnology Inc., Mountain View 94043.
Pharm Res. 1990 May;7(5):547-52. doi: 10.1023/a:1015885204249.
The ability of a novel permeation enhancer, sodium tauro-24,25-dihydrofusidate (STDHF), to increase the systemic delivery of human growth hormone (hGH) after intranasal administration was investigated in rat, rabbit, and sheep. Formulations of hGH with STDHF exhibited greatly enhanced nasal absorption at concentrations of STDHF above its critical micelle concentration. The increase in bioavailability was 11-fold in rats and in rabbits and 21-fold in sheep for formulations containing 0.5% STDHF as compared to those without STDHF. Glycocholate or taurocholate at 0.5% was three to five times less effective than STDHF at enhancing hGH absorption in rats. Additionally, the pulsatile absorption kinetics observed after intranasal delivery more closely resemble the endogenous secretory pattern of hGH than those obtained following subcutaneous administration.
在大鼠、兔子和绵羊中研究了一种新型渗透促进剂牛磺-24,25-二氢fusidate钠（STDHF）在鼻内给药后增加人生长激素（hGH）全身递送的能力。hGH与STDHF的制剂在高于其临界胶束浓度的STDHF浓度下表现出大大增强的鼻腔吸收。与不含STDHF的制剂相比，含0.5% STDHF的制剂在大鼠和兔子中的生物利用度提高了11倍，在绵羊中提高了21倍。0.5%的甘氨胆酸盐或牛磺胆酸盐在增强大鼠hGH吸收方面的效果比STDHF低三到五倍。此外，鼻内给药后观察到的脉冲吸收动力学比皮下给药后获得的更接近hGH的内源性分泌模式。
