Pontiroli A E, Perfetti M G, Fattor B, Pozza G
Istituto Scientifico San Raffaele, Cattedra di Clinica Medica, Universita degli Studi di Milano, Italy.
J Clin Endocrinol Metab. 1989 Apr;68(4):821-4. doi: 10.1210/jcem-68-4-821.
Several peptide hormones are effective when administered intranasally (in); these include oxytocin, vasopressin, insulin, glucagon, and calcitonin. With regard to GHRH and CRH, previous studies demonstrated that their bioavailability following in administration was very low. In this study we evaluated the serum GH response to 50 micrograms GHRH iv and to 700 micrograms GHRH in, the latter given alone and with 5 and 15 mg sodium-glycocholate (SGC), a surfactant, in six normal men. The bioavailability of in GHRH, calculated as net GH secretory area, was very low, and increased to 7% that of iv GHRH when SGC was used. In the same men, 50 micrograms CRH was administered both iv and in, alone and with 5 and 15 mg SGC. The bioavailability of in CRH, calculated as net cortisol secretory area, was very low and increased to 100% that of iv CRH when 15 mg SGC was used. These data indicate that the efficacy of GHRH and CRH administered in is significantly augmented by SGC.
几种肽类激素经鼻内给药时有效;这些激素包括催产素、血管加压素、胰岛素、胰高血糖素和降钙素。关于生长激素释放激素(GHRH)和促肾上腺皮质激素释放激素(CRH),先前的研究表明,经鼻内给药后它们的生物利用度非常低。在本研究中,我们评估了6名正常男性静脉注射50微克GHRH以及鼻内给予700微克GHRH后的血清生长激素反应,后者单独给药以及与5毫克和15毫克的表面活性剂甘氨胆酸钠(SGC)一起给药。经鼻内给予的GHRH的生物利用度(以生长激素净分泌面积计算)非常低,当使用SGC时,其生物利用度增加到静脉注射GHRH的7%。在同一批男性中,静脉注射和鼻内给予50微克CRH,单独给药以及与5毫克和15毫克SGC一起给药。经鼻内给予的CRH的生物利用度(以皮质醇净分泌面积计算)非常低,当使用15毫克SGC时,其生物利用度增加到静脉注射CRH的100%。这些数据表明,SGC可显著提高经鼻内给予的GHRH和CRH的疗效。