Development of matrix controlled transdermal delivery systems of pentazocine: In vitro/in vivo performance.
The present study aimed to develop hydroxypropyl methylcellulose based transdermal delivery of pentazocine. In formulations containing lower proportions of polymer, the drug released followed the Higuchi kinetics while, with an increase in polymer content, it followed the zero-order release kinetics. Release exponent (n) values imply that the release of pentazocine from matrices was non-Fickian. FT-IR, DSC and XRD studies indicated no interaction between drug and polymer.The in vitro dissolution rate constant, dissolution half-life and pharmacokinetic parameters (C(max), t(max), AUC(s), t(1/2), Kel, and MRT) were evaluated statistically by two-way ANOVA. A significant difference was observed between but not within the tested products. Statistically, a good correlation was found between per cent of drug absorbed from patches vs. C(max) and AUC(s). A good correlation was also observed when per cent drug released was correlated with the blood drug concentration obtained at the same time point. The results of this study indicate that the polymeric matrix films of pentazocine hold potential for transdermal drug delivery.
Prasad Verma
Priya Ranjan
PR
Department of Pharmaceutical Sciences, Birla Institute of Technology, Mesra, Ranchi-835215, India. prpverma275730@yahoo.com
Chandak
Ashok R
AR
D000279:Administration, Cutaneous; D000701:Analgesics, Opioid / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D018360:Crystallography, X-Ray; D003692:Delayed-Action Preparations; D004304:Dosage Forms; D004337:Drug Carriers; D004339:Drug Compounding; D005260:Female; D006207:Half-Life; D065347:Hypromellose Derivatives; D008297:Male; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D008954:Models, Biological; D010423:Pentazocine / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D033362:Powder Diffraction; D011817:Rabbits; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013678:Technology, Pharmaceutical / Q000379:methods
D000701:Analgesics, Opioid; D003692:Delayed-Action Preparations; D004304:Dosage Forms; D004337:Drug Carriers; D065347:Hypromellose Derivatives; D008747:Methylcellulose; D010423:Pentazocine