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원보 ; 고체분산체 및 포접화합물을 이용한 난용성 약물인 이부프로펜의 용출 속도의 증가
Original Articles ; Enhancement of Dissolution Rate of Poorly Water - soluble Ibuprofen using Solid Dispersions and Inclusion Complex .
이범진 , 이태섭 ( Beom Jin Lee , Tae Sub Lee )
약제학회지 25권 1호 31-36(6pages)
UCI I410-ECN-0102-2008-510-000815313

Solid dispersions and inclusion complex were prepared for the enhancement of solubility and dissolution rate of poorly water-soluble ibuprofen(IPF) as a model drug. Polyethylene glycol 4000(PEG4000) and polyvinylpyrrolidone(PVP) were used for the preparation of solid dispersion. 2-Hydroxypropyl-β-cyclodextrin(2-HPβCD) was also used for the preparation of inclusion complex. The solubility of IPF increased as the concentration of PEG4000, PVP and 2-HPβCD increased. Solubilization capacity of 2- HPβCD was increased about 10 times when compared to PEG 4000 and PVP. The dissolution rate of drug from solid dispersions and inclusion complex in the simulated gastric fluid was enhanced when compared to pure IPF and commercial BR4ⓡ tablet as a result of improvement of solubility. In case of solid dispersions, dissolution rate of drug was proportional to polymer concentration in the formulation. The marked enhancement of dissolution rate of drug by inclusion complexation with 2-HPβCD was noted. However, dissolution rate of drug from solid dispersions and inclusion complex in the simulated intestinal fluid was not significant because IPF was readily soluble in that condition. From these findings, water-soluble polymers and cyclodextrin were useful to improve solubility and dissolution rate of poorly water-soluble drugs. However, easiness and reliability of preparation method, scale-up and cost of raw materials must be considered for the practical application of solid dispersion and inclusion complex in pharmaceutical industry.

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