원문정보
The Microsponge Delivery System of Itraconazole: Preparation, Characterization and Release Studies
초록
영어
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® 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.
목차
1. 서론
2. 재료 및 방법
2.1. 기기 및 시약
2.2. Quasi-emulsion solvent diffusion method에 의한 이트코나졸 마이크로스폰지의 제조
2.3. 수득율, 약물 함량 및 봉입효율
2.4. 마이크로스폰지의 표면특성
2.5. 이트라코나졸 마이크로스폰지의 용출실험 및 용출메카니즘
3. 결과 및 고찰
3.1. 마이크로스폰지의 제조
3.2. 마이크로스폰지의 제조에 미치는 인자: 폴리머 대 약물의 비율
3.3. 내상, 외상 및 유화제의 양
3.4. 교반속도
3.5. 이트라코나졸 마이크로스폰지의 용출평가 및 용출메카니즘
4. 결론
References