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조영호(Young Ho Cho),이종화(Jong Hwa Lee),김학형(Hak Hyung Kim),이계원(Gye Won Lee) 한국생물공학회 2011 KSBB Journal Vol.26 No.3
Itraconazole is a triazole antifungal agent to inhibit most fungal pathogens. To improve the oral absorption and dissolution of poorly water-soluble itraconazole, microsponge system composed of Eudragit<SUP>®</SUP> E100 and polyvinyl alcohol (PVA) formulated by quasi-emulsion solvent diffusion method, and its physicochemical properties and pharmacokinetic parameters of itraconazole were studied. The microsponge of itraconazole were discrete free flowing microsized particles with perforated orange peel like morphology as visualized by scanning electron microscope (SEM). Results showed that the drug loading efficiency, production yield, and particle size of itraconazole microsponge were affected by drug to polymer ratio, the volume of internal phase containing methylene chloride, stirring rate and the concentration of PVA used. Also, the results showed that the dissolution rate of itraconazole from the microsponges was affected by drug to polymer ratio. In other words, the release rate of itraconazole from micropsonges was increased from at least 27.43% to 64.72% after 2 h. The kinetics of dissolution mechanism showed that the dissolution data followed Korsmeyer-Peppas model. Therefore, these results suggest that microsponge system can be useful for the oral delivery of itraconazole by manipulating the release profile.
유드라짓 및 폴리에틸렌글리콜 고체 매트릭스로 제조한 히드로코르티손 좌제의 서방성 평가
한건,김학형 한국약제학회 1990 Journal of Pharmaceutical Investigation Vol.20 No.1
Hydrocortisone (HC) sustained-release suppositories were prepared by using a solid matrix of methacrylic acid-methacrylic acid methyl ester copolymer (Eudragit L_(100)^R: EL) as a poorly water soluble carrier and polyethylene glycole 1540 (PEG) as an water soluble carrier. HC release rate was controlled by complexation with β-cyclodextrin (β-CyD) which was confirmed by X-ray diffractometry, IR-spectroscopy and differential scanning calorimetry. Release rate of HC from the EL-PEG matrix suppositories decreased with increase of EL contents. The release rate from HC-β-CyD complex decreased in the following order: HC-β-CyD/PEG > HC/PEG > HC-β-CyD/EL_(10%)-PEG > HC/EL_(10%)-PEG > HC-β-CyD/EL_(15%)-PEG > HC/EL_(15%)-PEG > HC-β-CyD/EL_(20%)-PEG > HC/EL_(20%)-PEG. The crystallinity of HC in polymer matrix was identified using X-ray diffractometer and the surface of matrix suppositories after release test was examined by scanning electron microscopy. The sustained release of HC from these matrix suppositories was attributed to the network structure of EL.