Journal of Pharmaceutical Investigation

The Korean Society of Pharmaceutical Sciences and Technology (한국약제학회)
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Preparation and Dissolution of Polyvinylpyrrolidone(PVP)-Based Solid Dispersion Systems Containing Solubilizers

가용화 조성물을 함유한 PVP형 고체분산체의 제조 및 특성

  • Cao, Qing-Ri (College of Pharmacy, Kangwon National University,Pharm TRI) ;
  • Kim, Tae-Wan (College of Pharmacy, Kangwon National University,Pharm TRI) ;
  • Choi, Choon-Young (College of Pharmacy, Kangwon National University,Pharm TRI) ;
  • Kwon, Kyoung-Ae (Handok Pharmaceutical Co., LTD) ;
  • Lee, Beom-Jin (College of Pharmacy, Kangwon National University,Pharm TRI)
  • 조청일 (강원대학교 약학대학,(주) 팜트리) ;
  • 김태완 (강원대학교 약학대학,(주) 팜트리) ;
  • 최춘영 (강원대학교 약학대학,(주) 팜트리) ;
  • 권경애 ((주)한독약품) ;
  • 이범진 (강원대학교 약학대학,(주) 팜트리)
  • Published : 2003.03.20
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Abstract

The PVP-based solid dispersion systems (SDs) containing lovastatin (LOS) and solubilizers (sodium lauryl sulfate, tween 80 and oleic acid) were prepared to enhance dissolution rate of practically water insoluble LOS using solvent evaporation method. Two different organic cosolvents either acetone/ethanol or acetonitrile/ethanol were used for the preparation of SDs. The LOS contents were highly decreased when acetone/ethanol cosolvents were used. The decrease of LOS contents was not caused by acetonitrile or acetone, based on HPLC data. The surface morphology as investigated by scanning electron microscope (SEM) and angle of repose as an index of flowability of SDs were highly dependent on the type and amount of solubilizers used. Based on differential scanning calorimetry (DSC) and X-ray powder diffraction data, the SDs made crystalline LOS into amorphous structure or partially eutectic mixtures. The simultaneous use of the solubilizers in SDs was also useful to increase dissolution rate of LOS in gastric or intestinal fluid. The SDs containing solubilizers reached 76% and 60% in gastric and intestinal fluid, respectively but the commercial tablet gave only less than 4%. These solubilizers in SDs could be also applicable for enhancing dissolution and bioavailability of poorly water-soluble drugs.

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References

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