Agharkar S, Lindenbaum S, Higuchi T
J Pharm Sci. 1976 May;65(5):747-9. doi: 10.1002/jps.2600650533.
Judicious choice of the salt form of a drug can greatly affect the aqueous solubility and formulation of the compound. The objective of this work was to demonstrate the effect of various counteranions on the aqueous solubility of the antimalarial agent alpha-(2-piperidyl)-3, 6-bis(trifluoromethyl)-9-phenanthrenemethanol. Several organic salts of this drug were studied. The methods of synthesis, the apparent aqueous solubilities, and in vitro dissolution tests for these salts are reported. The lactate salt was 200 times as soluble as the hydrochloride salt. This enhanced solubility suggests that parenteral administration of this drug may now be feasible.
明智地选择药物的盐形式会极大地影响化合物的水溶性和制剂。这项工作的目的是证明各种抗衡阴离子对抗疟药α-(2-哌啶基)-3,6-双(三氟甲基)-9-菲甲醇水溶性的影响。研究了该药物的几种有机盐。报告了这些盐的合成方法、表观水溶性和体外溶出试验。乳酸盐的溶解度是盐酸盐的200倍。这种溶解度的提高表明该药物的肠胃外给药现在可能是可行的。
