Lee W A, Ennis R D, Longenecker J P, Bengtsson P
Gilead Sciences, Inc., Foster City, California 94404.
Pharm Res. 1994 May;11(5):747-50. doi: 10.1023/a:1018992716621.
Serum levels of radioimmunoactive salmon calcitonin (sCT) were determined in 10 healthy volunteers after intranasal administration (IN) of 100-, 205-, and 450-IU of sCT with 0.5% sodium tauro-24,25-dihydrofusidate (STDHF), a 200-IU commercial IN formulation, and a 100-IU intramuscular (IM) formulation. Relative to the IM dose, the bioavailabilities of the IN formulations containing 0.5% STDHF were 3.9, 7.9, and 7.4%, respectively. The 200-IU commercial formulation resulted in serum levels above the limit of detection in only 5 of 10 patients, with an average bioavailability of 1.6%.
在10名健康志愿者经鼻内给予100国际单位、205国际单位和450国际单位的鲑鱼降钙素(sCT)(分别添加0.5%的牛磺-24,25-二氢fusidate(STDHF))、一种200国际单位的商用鼻内制剂以及一种100国际单位的肌肉注射(IM)制剂后,测定了血清中放射免疫活性鲑鱼降钙素(sCT)的水平。相对于肌肉注射剂量,含0.5% STDHF的鼻内制剂的生物利用度分别为3.9%、7.9%和7.4%。200国际单位的商用制剂仅在10名患者中的5名患者体内导致血清水平高于检测限,平均生物利用度为1.6%。