各種分子量薬物の経鼻および経肺吸収に及ぼす吸収促進剤の影響

Abstract

Phenol red and FITC-dextrans with various molecular weight were chosen as model drugs and the absorption promoters used in this study were Na-glycocholate, Na-salicylate, ethylendiaminetetraacetic acid (EDTA) and Na-caprate, all at a concentration of 1%. Of the absorption promoters, Na-glycocholate and Na-caprate appeared to be more effective to enhance the nasal and pulmonary absorption of these drugs than Na-salicylate and EDTA : For nasal absorption, Na-glycocholate and Na-caprate showed the highest promoting effect to drug with molecular weight 4000, while the maximal effect of these promoters was observed in the pulmonary absorption of drug with molecular weight 10000. EDTA showed the greatest promoting potency to drug with molecular weight 4000 in both routes, although its promoting potency for nasal absorption was more effective than that for pulmonary absorption. In contrast, Na-salicylate did not affect the absorption of drugs with various molecular weight in both routes. In conclusion, effect of absorption promoters on nasal and pulmonary absorption of drugs was molecular weight dependent. These findings give us useful basic information to select the optimal absorption promoters for peptide and protein delivery.