Monolithic matrix type transdermal drug delivery systems of pinacidil monohydrate: in vitro characterisation.
The monolithic matrix type transdermal drug delivery systems of pinacidil monohydrate (PM) were prepared by film casting technique on mercury substrate and characterised in vitro by drug release studies using paddle over disc assembly, skin permeation studies using Keshary and Chein diffusion cell on albino rat skin and drug-excipient interaction analysis. Four formulations were developed which differed in the ratio of matrix forming polymers, Eudragit RL-100 and PVP K-30, i.e. 8:2, 4:6, 2:8 and 6:4 and were coded as B-1, B-2, B-3 and B-4, respectively. All the four formulations carried 20% w/w of PM, 5% w/w of plasticiser, PEG-400 and 5% w/w of DMSO (based on total polymer weight) in isopropyl alcohol: dichloromethane (40:60) solvent system. Cumulative % of drug released in 48 h from the four formulations was 63.96, 55.95, 52.26 and 92.18%. The corresponding values for cumulative amount of drug permeated for the said formulations were 57.28, 50.35, 46.38 and 86.54%, respectively. On the basis of in vitro drug release and skin permeation performance, formulation B-4 was found to be better than the other three formulations and it was selected as the optimised formulation. The interaction studies carried out by comparing the results of assay, ultraviolet, infrared and TLC analyses for the pure drug, medicated and placebo formulations indicated no chemical interaction between the drug and excipients.
Department of Pharmaceutics, New Delhi, India. aqilmalik@yahoo.com
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D000180:Acrylic Resins / Q000737:chemistry; D000277:Adjuvants, Pharmaceutic / Q000737:chemistry; D000279:Administration, Cutaneous; D000818:Animals; D000959:Antihypertensive Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D002855:Chromatography, Thin Layer; D004355:Drug Stability; D005079:Excipients; D066298:In Vitro Techniques; D010539:Permeability; D020110:Pinacidil / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D011205:Povidone / Q000737:chemistry; D051381:Rats; D012869:Skin Absorption; D013055:Spectrophotometry, Infrared; D013056:Spectrophotometry, Ultraviolet; D013997:Time Factors
D000180:Acrylic Resins; D000277:Adjuvants, Pharmaceutic; D000959:Antihypertensive Agents; D005079:Excipients; C050528:Eudragit RS; D020110:Pinacidil; D011205:Povidone