Matrix type transdermal drug delivery systems of metoprolol tartrate: in vitro characterization

Acta Pharm. 2003 Jun;53(2):119-25.

Abstract

The monolithic matrix type transdermal drug delivery system of metoprolol tartrate were prepared by the film casting on a mercury substrate and characterised in vitro by drug release studies, skin permeation studies and drug-excipients interaction analysis. Four formulations were developed, which differed in the ratio of matrix-forming polymers. Formulations MT-1, MT-2, MT-3 and MT-4 were composed of Eudragit RL-100 and polyvinyl pyrrolidone K-30 with the following ratios: 2:8, 4:6, 6:4 and 8:2, respectively. All the four formulations carried 10% (m/m) of metoprolol tartrate, 5% (m/m) of PEG-400 and 5% (m/m) of dimethyl sulfoxide in isopropyl alcohol: dichloromethane (40:60). Cumulative amounts of the drug released in 48 hours from the four formulations were 61.5, 75.4, 84.3 and 94.5%, respectively. The corresponding values for cumulative amounts of the permeated drug for the said formulations were 53.5, 62.5, 69.8 and 78.2%. On the basis of in vitro drug release and skin permeation performance, formulation MT-4 was found to be better than the other three formulations and it was selected as the optimized formulation.

MeSH terms

  • Administration, Cutaneous
  • Adrenergic beta-Antagonists / administration & dosage*
  • Adrenergic beta-Antagonists / pharmacokinetics
  • Animals
  • Chromatography, Thin Layer
  • Excipients
  • Half-Life
  • In Vitro Techniques
  • Metoprolol / administration & dosage*
  • Metoprolol / pharmacokinetics
  • Rats
  • Skin Absorption
  • Spectrophotometry, Infrared
  • Spectrophotometry, Ultraviolet

Substances

  • Adrenergic beta-Antagonists
  • Excipients
  • Metoprolol