Hussain M A, Wu L S, Koval C, Hurwitz A R
Du Pont Merck Pharmaceutical Co., Experimental Station, Wilmington, Delaware 19880-0400.
Pharm Res. 1992 Jun;9(6):750-2. doi: 10.1023/a:1015895303804.
The nonopioid kappa agonist analgesic amine, DuP 747, as a hydrochloride salt exhibited an aqueous solubility of 3 mg/ml. This solubility was insufficient to provide the desired dose in a solution formulation for intramuscular administration. Aqueous solutions of the hydrochloride salt exerted surface activity behavior; however, the critical micellar concentration (CMC) was not reached at the saturation solubility. Enhanced aqueous solubility required to reach the CMC could lead to micellization of the compound and a possible i.m. solution formula. The methanesulfonate salt was more water soluble than the hydrochloride salt and yielded a micellar solution with a concentration of 60 mg/ml.
非阿片类κ激动剂镇痛药胺DuP 747的盐酸盐在水中的溶解度为3 mg/ml。这种溶解度不足以在用于肌肉注射的溶液制剂中提供所需剂量。盐酸盐的水溶液表现出表面活性行为；然而，在饱和溶解度时未达到临界胶束浓度（CMC）。达到CMC所需的增强的水溶性可能导致该化合物胶束化以及可能的肌肉注射溶液配方。甲磺酸盐比盐酸盐更易溶于水，并且产生浓度为60 mg/ml的胶束溶液。
