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KMID : 0370220190630060384
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Yakhak Hoeji
2019 Volume.63 No. 6 p.384 ~ p.389
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Solubility Enhancement of Poorly Water-Soluble Drugs by Hot-Melt Extrusion Technology and Effects of Surfactant on Dissolution Test
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Choi Sung-Min
Jeon Yong-Koo
Lee Ju-Hyun
Kang Chin-Yang
Park Jun-Bom
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Abstract
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Solid dispersions (SDs) were manufactured by hot-melt extrusion (HME) technology to enhance the solubilityof the poorly soluble drugs (fenofibrate, celecoxib and cilostazol). Soluplus and Kollidon VA64 were selected as polymersdue 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 andsolubility of poorly water-soluble drugs, a dissolution test was performed using the paddle method per the USPharmacopeia Apparatus II. Distilled water with 0.5% sodium lauryl sulfate (SLS) was used as dissolution media. Theextrudates 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, thedissolution test was continuously performed by changing the amount of SLS. As a result, the drug release from theextrudate with cilostazol was higher than cilostazol alone in the dissolution media containing 0.1% SLS. Based on thisresult, 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.
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KEYWORD
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Cilostazol, Fenofibrate, Celecoxib, Hot-Melt Extrusion, Solid Dispersion, Sodium Lauryl Sulfate (SLS)
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