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KMID : 0370220180620030179
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Yakhak Hoeji
2018 Volume.62 No. 3 p.179 ~ p.185
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Preclinical formulation strategies for discovering new drug candidates
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Kang Won-Ho
Chae Jung-Woo
Yun Hwi-Yeol
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Abstract
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To determine a rational preclinical formulation strategy for preclinical research, scientists should consider with their own work-flow and physicochemical properties acquired by each discovery stage. In general, physicochemical properties such as ionization states and kinetic solubility could be obtained in the early discovery stage. However, more detailed properties such as equilibrium solubility, pKa, pH-solubility and cLog P/D could be confirmed at the late discovery stage. For these reasons, it was hard to decide which kinds of formulation were most suitable for candidates. Therefore, the primary objective of this review was to figure out preclinical formulation strategy based on drug discovery stage, and propose case-study with real case for application. Preclinical formulation strategy of previously approved drug that has similar characteristics usually was used in early drug discovery stage. Especially if information of drug characteristics was limited, researchers were able to consider that it was alternative methods to make suspension with surfactant and cyclodextrin-drug complexation method. For late discovery stage, there are several ways to consider the characteristic of various physicochemical properties such as pH-adjustment, solubilization (using by co-solvent, surfactant) and combination of pH-adjustment and solubilization. As drug discovery work-flow are different among pharmaceutical companies, making preclinical formulation strategy from early stage of drug discovery is important for increment of success ratio of new drug development. This review could guide researchers which preclinical formulation is appropriate by suggesting rational strategy.
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KEYWORD
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Preclinical formulation strategy, physicochemical properties, solubilization, suspension
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