Improved Dissolution of Poorly Water Soluble TD49, a Novel Algicidal Agent, via the Preparation of Solid Dispersion

The objective of this study was to improve the extent of drug release as well as the dissolution rate of TD49, a novel algicidal agent, via the preparation of solid dispersion (SD). Among the various carriers tested, $Solutol^{(R)}$ HS15 was most effective to enhance the solubility of TD49. Subsequently, SDs of TD49 were prepared by using $Solutol^{(R)}$ HS15 and their solubility, dissolution characteristics and drug crystallinity were examined at various drug-carrier ratios. Solubili ty of TD49 was increased significantly in accordance with increasing the ratio of $Solutol^{(R)}$ HS15 in SDs. Compared to untreated powders and physical mixtures (PMs), SDs facilitated the faster and greater extent of drug release in water. Particularly, SD having the drug-carrier ratio of 1:20 exhibited approximately 90% of drug release within 1 hr. Differential scanning calorimetry (DSC) thermograms and X-ray diffraction (XRD) patterns suggested that SDs might enhance the dissolution of TD49 by changing the drug crystallinity to an amorphous form in addition to the increased solubilization of drug in the presence of $Solutol^{(R)}$ HS15. In conclusion, SD using $Solutol^{(R)}$ HS15 appeared to be effective to improve the extent of drug release and the dissolution rate of poorly water soluble TD49.