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In order to formulate biphenyl dimethyl dicarboxylate(DDB) aqueous solutions, the effects of various solubilizing agents such as cosolvents(PG, PEG 400, glycerin, ethanol), surfactants(poloxamer 407, Cremophor(R) RH40, Solutol(R), Tween 80, sodium lauryl sulfate), complexation agent(CELDEX(R) CH-20) and others(urea, niacinamide, propylene carbonate, HPMC) on the solubility of DDB in water were evaluated. The solubility of DDB in water was about 0.21mcg/ml at 20oC, while its solubility in PEG 400 was 5,000 times higher than that in water. 60% PEG 400 aqueous solution was selected as an optimum solvent system, and surfactants or other solubilizing agents were added to prevent DDB from recrystalization. The addition of surfactants in water increased the solubility of DDB from 15- to 34-fold, however, CELDEX(R) CH-20 and other agents studied showed negligible effects on the solubility of DDB in water. The 60% PEG 400 aqueous solution containing 5% Cremophor(R) RH40 was appeared as the formula of choice. It showed acceptable physical stability after stored for 7 days at 4oC.
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