Preparation and Evaluation of Sustained-Release $Eudragit^{\circledR}$ Microcapsules Containing ${\beta}-Lactam$ Antibiotics

$Eudragit^{\circledR}$ 마이크로캅셀화에 의한 ${\beta}$-락탐계 항생물질의 방출제어제제 개발

  • Han, Kun (College of Pharmacy, Chungbuk National University) ;
  • Shin, Do-Su (College of Pharmacy, Chungbuk National University) ;
  • Jee, Ung-Kil (College of Pharmacy, Chungnam National University) ;
  • Chung, Youn-Bok (College of Pharmacy, Chungbuk National University)
  • Published : 1992.12.20

Abstract

Microencapsulations of amoxicillin and cephalexin, using Eudragit RS, RL, E, S and L were investigated. The microcapsules were prepared by the solvent evaporation process in liquid paraffin phase, which is based on dispersion of acetone/isopropanol containing the drug in liquid paraffin. Aluminium tristearate was used as an additive for the preparation of microcapsules. The size distribution, dissolution test and observation by SEM were examined. Good reproducibility in microcapsule preparation was observed. The microcapsules obtained were spherical and free-flowing particles. The dissolution rates of amoxicillin and cephalexin from the microcapsules were considerably decreased as compared with those from amoxicillin and cephalexin powder, respectively. As the dispersing agents (aluminium tristearate) increased, the particle size of microcapsules decreased and the dissolution rate increased. In order to control the release rate of drugs, microcapsules were prepared by mixing Eudragit RS/RL or Eudragit S/L. As Eudragit RL ratio in microcapsule of Eudragit RS/RL increased, the dissolution rate increased. As Eudragit L ratio in microcapsule of Eudragit S/L increased, the dissolution rate increased. Furthermore, the release rates of drugs from Eudragit RS/L or RS/polyelthylene glycol 1540 (PEG 1540) were examined. The dissolution rate of drugs increased with increasing of Eudragit L or PEG 1540 ratio. In conclusion, the release rates of drugs from Eudragit RS/RL or RS/PEG 1540 microcapsule could be controlled, and these microcapsules will be convenient for reducing frequency of administration.

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