Matrix type transdermal drug delivery systems of metoprolol tartrate: in vitro characterization.
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.
Aqil
Mohamed
M
Department of Pharmaceutics, Faculty of Pharmacy, New Delhi--110062, India. aquilmalik@yahoo.com
Sultana
Yasmin
Y
Ali
Asgar
A
D000279:Administration, Cutaneous; D000319:Adrenergic beta-Antagonists / Q000008:administration & dosage* / Q000493:pharmacokinetics; D000818:Animals; D002855:Chromatography, Thin Layer; D005079:Excipients; D006207:Half-Life; D066298:In Vitro Techniques; D008790:Metoprolol / Q000008:administration & dosage* / Q000493:pharmacokinetics; D051381:Rats; D012869:Skin Absorption; D013055:Spectrophotometry, Infrared; D013056:Spectrophotometry, Ultraviolet
D000319:Adrenergic beta-Antagonists; D005079:Excipients; D008790:Metoprolol