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Preparation of Lovastatin Matrix Sustained-Release Pellets by Extrusion-Spheronization Combined with Microcrystal Dispersion Technique
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  • Preparation of Lovastatin Matrix Sustained-Release Pellets by Extrusion-Spheronization Combined with Microcrystal Dispersion Technique
  • Preparation of Lovastatin Matrix Sustained-Release Pellets by Extrusion-Spheronization Combined with Microcrystal Dispersion Technique
저자명
He. Haibing,Shi. Bo,Cai. Cuifang,Tang. Xing
간행물명
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
권/호정보
2011년|34권 11호|pp.1931-1938 (8 pages)
발행정보
대한약학회
파일정보
정기간행물|ENG|
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기타
이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
서지반출

기타언어초록

The poorly water-soluble drug lovastatin (LVA) is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A reductase and has a slow dissolution rate. In this study, a microcrystal dispersion (MCD) technique was used in the preparation of LVA to increase its dissolution rate and then combining with an extrusion-spheronization method, microcrystalline cellulose (MCC) matrix sustained-release pellets containing LVA-MCD were developed and characterized in vitro. Photomicrographs indicated that LVA-MCD existed as fine crystals, of which the mean particle size was reduced from $65.75{mu}m$ to $3.97{mu}m$ and the dried LVA-MCD powders released completely within 2 hours. SEM results during the release process showed that pellets possessed a matrix structure and after the dissolution test, this matrix structure became loose and porous. The release of LVA was fast and complete, and accumulated release by the optimal formulation was: 0.5 h ($20.23{pm}3.40%$), 2 h ($56.87{pm}2.85%$), 4 h ($78.71{pm}$3.42%), and 8 h ($96.81{pm}3.30%$). The 3 months accelerating test at $40^{circ}C$ and 75% RH demonstrated that drug release of pellets was not changed and drug degradation was less than 1%. Thus, a novel MCD process with MCC matrix was feasible and effective to get complete release without a lag time for the poorly water soluble drug, LVA, with high stability.