Igawa T, Maitani Y, Machida Y, Nagai T
Chem Pharm Bull (Tokyo). 1989 Feb;37(2):418-21. doi: 10.1248/cpb.37.418.
The utility of the absorption promoters, sodium glycocholate (GC-Na), ethylenediamine dihydrochloride (EDTA-2Na), sodium caprylate (Cap-Na) and sodium salicylate (Sal-Na), in the intranasal administration of human fibroblast interferon-beta (HuIFN-beta) in rabbits was investigated. The optimal amount of added EDTA-2Na, Cap-Na and Sal-Na with respect to HuIFN-beta was examined for nasal absorption in the powder dosage form. Formulations of HuIFN-beta with GC-Na showed greatly enhanced intranasal HuIFN-beta absorption, as compared to the other absorption promoters. The results of a stability study on HuIFN-beta in homogenates of nasal mucosa suggested that GC-Na behaved as a hydrolysis inhibitor in the nasal mucosa and maintained the activity of HuIFN-beta.
研究了吸收促进剂甘氨胆酸钠(GC-Na)、乙二胺二盐酸盐(EDTA-2Na)、辛酸钠(Cap-Na)和水杨酸钠(Sal-Na)在兔鼻内给予人成纤维细胞β干扰素(HuIFN-β)中的作用。考察了粉末剂型中相对于HuIFN-β添加的EDTA-2Na、Cap-Na和Sal-Na的最佳量对鼻吸收的影响。与其他吸收促进剂相比,含GC-Na的HuIFN-β制剂显示鼻内HuIFN-β吸收大大增强。对鼻黏膜匀浆中HuIFN-β的稳定性研究结果表明,GC-Na在鼻黏膜中起水解抑制剂的作用,并维持HuIFN-β的活性。