Journal of Pharmaceutical Investigation

  • 제37권6호
  • /
  • Pages.339-347
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  • 2007
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  • 2093-5552(pISSN)
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  • 2093-6214(eISSN)
한국약제학회 (The Korean Society of Pharmaceutical Sciences and Technology)
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자가미세유화를 통한 아토르바스타틴 칼슘의 난용성 개선

Improvement of Solubility of Atorvastatin Calcium Using Self-Microemulsion Drug Delivery System(SMEDDS)

  • 이준희 (전북대학교 BK-21 고분자 BIN융합연구팀) ;
  • 최명규 (전북대학교 BK-21 고분자 BIN융합연구팀) ;
  • 김윤태 (전북대학교 BK-21 고분자 BIN융합연구팀) ;
  • 김명진 (전북대학교 BK-21 고분자 BIN융합연구팀) ;
  • 오재민 (전북대학교 BK-21 고분자 BIN융합연구팀) ;
  • 박정수 (전북대학교 BK-21 고분자 BIN융합연구팀) ;
  • 모종현 (전북대학교 BK-21 고분자 BIN융합연구팀) ;
  • 김문석 (한국화학연구원 나노생체재료연구팀) ;
  • 강길선 (전북대학교 BK-21 고분자 BIN융합연구팀) ;
  • 이해방 (한국화학연구원 나노생체재료연구팀)
  • Lee, Jun-Hee (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University) ;
  • Choi, Myoung-Kyu (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University) ;
  • Kim, Yun-Tae (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University) ;
  • Kim, Myoung-Jin (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University) ;
  • Oh, Jae-Min (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University) ;
  • Park, Jung-Soo (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University) ;
  • Mo, Jong-Hyun (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University) ;
  • Kim, Moon-Suk (Nanobiomaterials Laboratory, Korea Research Institute of Chemical Technology) ;
  • Khang, Gil-Son (BK-21 Polymer BIN Fusion Research Team, Chonbuk National University) ;
  • Lee, Hai-Bang (Nanobiomaterials Laboratory, Korea Research Institute of Chemical Technology)
  • 발행 : 2007.12.21
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초록

SMEDDS is mixture of oils, surfactants, and cosurfactants, which are emulsified in aqueous media under conditions of gentle agitation and digestive motility that would be encountered in the gastro-intestinal(GI) tract. The main purpose of this work is to prepare self-microemulsifying drug delivery system(SMEDDS) for oral bioavailability enhancement of a poorly water soluble drug, atorvastatin calcium. Solubility of atorvastatin calcium was determined in various vehicles. Pseudo-ternary phase diagrams were constructed to identity the efficient self-emulsification region and particle size distributions of the resultant micro emulsions were determined using a laser diffraction sizer. Optimized formulations for in vitro dissolution and bioavailability assessment were $Capryol^{(R)}$ 90(50%), Tetraglycol(16%), and $Cremophor^{(R)}$ EL(32%). The release rate of atorvastatin from SMEDDS was significantly higher than the conventional tablet ($Lipitor^{(R)}$), 2-fold. Our studies illustrated the potential use of SMEDDS for the delivery of hydrophobic compounds, such as atorvastatin calcium by the oral route.

키워드

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