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서지반출
Solid Dispersion Formulations of Megestrol Acetate with Copovidone for Enhanced Dissolution and Oral Bioavailability
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  • Solid Dispersion Formulations of Megestrol Acetate with Copovidone for Enhanced Dissolution and Oral Bioavailability
  • Solid Dispersion Formulations of Megestrol Acetate with Copovidone for Enhanced Dissolution and Oral Bioavailability
저자명
Hong. Soon-Wook,Lee. Bong-Sang,Park. Su-Jun,Jeon. Hong-Ryeol,Moon. Ki-Young,Kang. Mean-Hyung,Park. Sang-Han,Choi. Sung-Up,Song.
간행물명
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
권/호정보
2011년|34권 1호|pp.127-135 (9 pages)
발행정보
대한약학회
파일정보
정기간행물|ENG|
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기타
이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
서지반출

기타언어초록

In order to enhance the dissolution profile and oral bioavailability of megestrol acetate (MA), solid dispersions of MA (MASDs) were formulated with copovidone and crystal sugar as a hydrophilic polymeric carrier and an inert core bead, respectively. Solvent evaporation method and fluidized bed coating technique were employed. MASDs were categorized as crystalline solid dispersion by the characterization of differential scanning calorimetry and X-ray diffraction. The mass-median diameters of MASDs were in a range of 1.4 to $2.6{mu}m$. Based on drug to polymer ratio, MASD (1:1) and (1:2) were considered as optimized formulations, resulting in a smooth-surfaced homogeneously coated layer with enhanced dissolution rate. Dissolution of MASD was gradually increased up to 15 min, after which it reached a plateau. For the initial period, dissolution rates were in the decreasing order of MASD (1:2) ${geq}$ MASD (1:1) > MASD (1:3) > MASD (1:5) > MASD (1:0.5) > MA powder. In the comparative pharmacokinetic study with Megace OS, a reference drug product, MASD (1:1) showed improved bioavailability of over 220% with 2-fold higher $C_{max}$ and 30% faster $T_{max}$. We conclude that MASD (1:1) is a good candidate for the development of oral solid dosage forms.