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KMID : 0369819990290010037
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Jorunal of Korean Pharmaceutical Sciences
1999 Volume.29 No. 1 p.37 ~ p.45
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Improvement of Dissolution Rate of Poorly Water Soluble Drug Using Self - microemulsifying Drug Delivery System
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김계현/Kim KH
이윤석/배준호/지상철/박은석/Rhee YS/Bae JH/Chi SC/Park ES
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Abstract
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A self-microemulsifying drug delivery system (SMEDDS) was developed to enhance the solubility and dissolution rate of poorly water soluble drug, biphenyl dimethyl dicarboxylate, DDB. The system was optimized by evaluating the solubility of DDB and the microemulsion existence range after the preparation of microemulsions with varying compositions of triacetin and surfactant-cosurfactant mixtures (Labrasol as surfactant (S) and the combination of Transcutol, Cremophor RH 40 and Plurol oleique as cosurfactant (CoS)). SMEDDS in this study markedly improved the solubility of DDB in water up to 10 ㎎/㎖ and the size of the o/w microemulsion droplets measured by dynamic light scattering showed a narrow monodisperse size distribution with an average diameter less than 50 nm. The microemulsion existing range is increased proportional to the ratio of S/CoS, however, it decreased remarkably as the oil content was more than 20%. In vitro dissolution study of SMEDDS showed a significantly increased dissolution rate of DDB in water (>12 fold over DDB powder), and SMEDDS also had significantly greater permeability of DDB in Caco-2 cell compared to powders.
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