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Keywords:

  • Solubility, aqueous—salts of substituted phenanthrenemethanol antimalarial agent, effect of hydrophilic counterions;
  • Salts—substituted phenanthrenemethanol antimalarial agent, effect of hydrophilic counterions on aqueous solubility;
  • Counterions, hydrophilic—effect on aqueous solubility of substituted phenanthrenemethanol antimalarial agent;
  • Antimalarial agents—α-(2-piperidyl) -3,6- bis(trifluoromethyl) -9- phenanthrenemethanol, salts, effect of hydrophilic counterions on aqueous solubility

Abstract

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 α-(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.