고온용융압출 기술을 적용한 난용성 약물의 가용화 및 용출시험에서의 계면활성제의 농도의 영향

• 영문명: Solubility Enhancement of Poorly Water-Soluble Drugs by Hot-Melt Extrusion Technology and Effects of Surfactant on Dissolution Test
• 발행기관: 대한약학회
• 저자명: 최성민(Sung-min Choi) 전용구(Yong-Koo Jeon) 이주현(Ju-Hyun Lee) 강진양(Chin-Yang Kang) 박준범(Jun-Bom Park)
• 간행물 정보: 『약학회지』제63권 제6호(2019년), 384~389쪽, 전체 6쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 2019.12.30

영문 초록

Solid dispersions (SDs) were manufactured by hot-melt extrusion (HME) technology to enhance the solubility of the poorly soluble drugs (fenofibrate, celecoxib and cilostazol). Soluplus and Kollidon VA64 were selected as polymers due to their thermoplastic and hydrophilic behaviors. The SDs with three types of active pharmaceutical ingredients (APIs) were prepared using a twin-screw HME system, at three processing temperatures. To check drug release behaviors and solubility of poorly water-soluble drugs, a dissolution test was performed using the paddle method per the US Pharmacopeia Apparatus II. Distilled water with 0.5% sodium lauryl sulfate (SLS) was used as dissolution media. The extrudates containing fenofibrate and celecoxib showed enhanced drug release profiles compared to the APIs alone. However, in case of cilostazol, the extrudate had a lower dissolution rate than the API. To solve this phenomenon, the dissolution test was continuously performed by changing the amount of SLS. As a result, the drug release from the extrudate with cilostazol was higher than cilostazol alone in the dissolution media containing 0.1% SLS. Based on this result, the dissolution medium containing 0.1% SLS or less was considered as more suitable media than containing 0.5% SLS solution, which is mentioned in the cilostazol US Pharmacopeia (USP) monograph.

목차

서 론(Introduction)

실험방법(Experimental Methods)

결과 및 고찰(Results and Discussion)

결 론(Conclusion)

감사의 말씀(Acknowledgement)

Conflict of Interest

References

키워드

Cilostazol Fenofibrate Celecoxib Hot-Melt Extrusion Solid Dispersion Sodium Lauryl Sulfate (SLS)