Journal of Pharmaceutical Investigation

The Korean Society of Pharmaceutical Sciences and Technology (한국약제학회)
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Improved Dissolution and Characterization of Solid Dispersed Atorvastatin Calcium

아토르바스타틴 칼슘 고체분산체의 특성화 및 용출율 개선

  • Lee, Jun-Hee (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University) ;
  • Ku, Jeong (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University) ;
  • Park, Jung-Soo (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University) ;
  • Park, Jong-Hak (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University) ;
  • Ahn, Sik-Il (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University) ;
  • Mo, Jong-Hyun (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University) ;
  • Kim, Yun-Tae (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University) ;
  • Rhee, John-M. (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University) ;
  • Lee, Hai-Bang (Nanobiomaterials Laboratory, Korea Research Institute of Chemical Technology) ;
  • Khang, Gil-Son (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University)
  • 이준희 (전북대학교 BK-21 고분자 BIN융합연구팀) ;
  • 구정 (전북대학교 BK-21 고분자 BIN융합연구팀) ;
  • 박정수 (전북대학교 BK-21 고분자 BIN융합연구팀) ;
  • 박종학 (전북대학교 BK-21 고분자 BIN융합연구팀) ;
  • 안식일 (전북대학교 BK-21 고분자 BIN융합연구팀) ;
  • 모종현 (전북대학교 BK-21 고분자 BIN융합연구팀) ;
  • 김윤태 (전북대학교 BK-21 고분자 BIN융합연구팀) ;
  • 이종문 (전북대학교 BK-21 고분자 BIN융합연구팀) ;
  • 이해방 (한국화학연구원 나노생체재료연구팀) ;
  • 강길선 (전북대학교 BK-21 고분자 BIN융합연구팀)
  • Published : 2008.04.21
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Abstract

To overcome the solubility of poorly water-soluble drug, the formation of solid dispersion using a spray-dryer with polymeric material, that can potentially enhance the dissolution rate extend of drug absorption was considered in this study. $Eudragit^{(R)}$ E100 as carrier for solid dispersion is acrylate copolymer that soluble in acidic buffer solutions (below pH 5.0). It was used to increase dissolution of atorvastatin calcium as a water-insoluble drug in acidic environments. In this study, a spray-dryer was used to prepare solid dispersion of atorvastatin calcium and $Eudragit^{(R)}$ E100 for purpose of improving the solubility of drug. Atorvastatin calcium and $Eudragit^{(R)}$ E100 were dissolved in ethanol and spray-dryed. DSC and XRD were used to analyze the crystallinity of the sample. It was found that atorvastatin calcium is amorphous in the $Eudragit^{(R)}$ E100 solid dispersion. FT-IR was used to analyze the salt formation by interaction between atorvastatin calcium and $Eudragit^{(R)}$ E100. Comparative dissolution study exhibited better dissolution characteristics than the commercial drug ($Lipitor^{(R)}$) as control. The dissolution rate of atorvastatin calcium was markedly increased in solid dispersion system in simulated gastric juice (pH 1.2). This study proposed that this solid dispersion system improved the bioavailability of poorly water-soluble atorvastatin calcium.

Keywords

References

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