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KMID : 0617220030140010187
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Duksung Bulletin Phamaceutical Sciences
2003 Volume.14 No. 1 p.187 ~ p.192
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Characterization of the Physicochemical Properties of KR-31378
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Sohn Young-Taek
Park Bo-Ye
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Abstract
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KR-31378 is a new drug candidate intended for the use in the prevention of ischemia-reperfusion damage. The objective of this prefomulation study was to determine the physicochemical properties of KR-31378. The n-octanol to water partition coefficients of KR-31378 were 0.0504 at pH 3 and 0.8874 at pH 10. Accelerated stability of KR-31378 in solution and solid was estimated to be 2years and 128.6 days at 25℃, while the that in aquesou solution was 68.6 days at 25℃. The KR-31378 was also found to be unstable under the relative humidity of 76％, probably because of the hygroscopic nature of the drug. In order to study compatibility of KR-31378 with typical excipients, potential change in differential scanning calorimetry spectrum was studied in 1:1 binary mixtures of KR-31378 and Aerosil, Avicel, Eudragit, lactose, PEG, talc, CMC, PVP, starch. As a result, CMC, PVP, and starch were found to be incompatible with KR-31378, indicating the addition of these excipients may complicate the manufacturing of the formulation for the drug. Particle size distribution of KR-31378 powder was in the size range of 0.93㎛ with the mean particle size of 37.9㎛. The flowability of KR-31378 was apparently inadequate, indicating the granulation may be necessary for the processing of the drug to solid dosage forms. Crystallization of the drug with a number of organic solvents did not lead a crystalline poly morphism. In addition, dissolution of the drug from the powder was adequately rapid at 37℃ in water.
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