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논문 기본 정보

자료유형
학술저널
저자정보
Kim Nam Ah (Dongguk University-Seoul) Oh Hee Kyung (Dongguk University-Seoul) 이재철 (동국대학교) 최영희 (동국대학교) 정성훈 (동국대학교)
저널정보
한국약제학회 Journal of Pharmaceutical Investigation Journal of Pharmaceutical Investigation 제51권 제1호
발행연도
2021.1
수록면
53 - 60 (8page)

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Purpose Even though butein can be a promising candidate for anti-inflammatory and anti-diabetic activities, it is poorly soluble limiting its availability for product development. Size reduction and solid dispersion (SD) were adopted independently to evaluate their feasibility for enhancement in solubility as well as bioavailability. Methods To reduce the particle size, milling method was carried out under dry and wet conditions. For solid dispersion preparation, simple solvent evaporation method was used with hydrophilic excipients including PVP K-30 and Poloxamer 407. Physicochemical properties such as crystallinity, size, and kinetic solubility of prepared formulations were assessed using dynamic light scattering, X-ray powder diffraction, differential scanning calorimetry, and solubility. In vivo pharmacokinetic study was also conducted with selected samples. Results Butein is weakly basic with its pKa 6.76 and log P 3.81 based on the Henderson-Hasselbalch equation. High temperature and basic pH were degradative stresses as significant color change in solution. Milling decreased the size distribution down to 4.2 μm without dramatic change in the solubility. However, the solubility of solid dispersion increased from 3.15 up to 114.57 μg/mL, suggesting amorphous state increased solubility significantly. Its amorphous state was confirmed by DSC and PXRD. In addition, oral absorption of SD in vivo confirmed its enhanced pharmacokinetic parameters; faster Tmax, higher Cmax and AUC. Conclusions Solid dispersion exhibited enhancement in pharmacokinetic parameters compared to size reduction, suggesting its feasibility for solid dispersion formulation.

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