Fabrication and evaluation of captopril modified-release oral formulation

Pharm Dev Technol. 2009;14(6):679-86. doi: 10.3109/10837450902922744.

Abstract

The present research was directed towards fabrication of modified-release captopril oral formulation. A 3(2) full factorial design was employed for optimization using captopril to Compritol ATO 888 ratio (X1) and extragranular fraction of ethyl cellulose (X2) as independent variables. The percentage drug released in 1 h (Y1) and the time required to release 80% of the drug (Y2) were selected as dependent variables. Eutectic blend of camphor and menthol was used as a solvent to facilitate the drug distribution in matrix. The optimized batch containing 50 mg captopril, 160 mg Compritol ATO 888 and 220 mg ethyl cellulose was formulated by overlapping the contour plots of Y1 and Y2. The responses Y1 and Y2 of optimized batch were 25% and 520 min, respectively. The kinetics of drug release was best explained by Korsmeyer-Peppas model. The results of artificial neural network were superior in prediction power than the factorial design for both the responses (Y1 and Y2).

Publication types

  • Evaluation Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Algorithms
  • Analysis of Variance
  • Biological Availability
  • Camphor / chemistry
  • Captopril / administration & dosage*
  • Captopril / chemistry
  • Captopril / pharmacokinetics
  • Cellulose / analogs & derivatives
  • Cellulose / chemistry
  • Chemistry, Pharmaceutical
  • Delayed-Action Preparations / administration & dosage
  • Delayed-Action Preparations / chemistry*
  • Delayed-Action Preparations / pharmacokinetics
  • Drug Stability
  • Excipients / chemistry
  • Fatty Acids / chemistry
  • Humans
  • Kinetics
  • Menthol / chemistry
  • Models, Biological*
  • Models, Statistical
  • Neural Networks, Computer
  • Regression Analysis
  • Spectroscopy, Fourier Transform Infrared

Substances

  • Delayed-Action Preparations
  • Excipients
  • Fatty Acids
  • Menthol
  • glyceryl behenate
  • Camphor
  • ethyl cellulose
  • Cellulose
  • Captopril