Formulation and in vitro evaluation of pentazocine transdermal delivery system

Biol Pharm Bull. 2008 Jul;31(7):1439-43. doi: 10.1248/bpb.31.1439.

Abstract

The aim of this study was to prepare a pentazocine (PTZ) matrix-type transdermal drug delivery system (TDDS) using acrylic pressure-sensitive adhesives. Among the five Duro-Tak adhesive polymers tested (87-9301, 87-2677, 87-201A, 87-2196, 87-2852), in vitro dissolution studies demonstrated the highest PTZ release flux from the Duro-Tak 87-9301 matrix. In addition, the effects of permeation enhancers, isopropyl myristate (IPM) and glyceryl monocaprylate (GEFA-C(8)), and drug content on PTZ skin permeation from prepared patches were evaluated using Franz diffusion cells fitted with hairless mouse skin. IPM and GEFA-C(8) were found to produce effective flux of PTZ at a patch concentration of 10% w/w and 5% w/w, respectively. The PTZ flux increased linearly as the loading dose increased up to 30%, whereas no further increase in flux was observed at loading doses of 40% and 50% due to drug crystallization in the matrix. Thus, the highest skin permeation rate (24.2 microg/cm(2)/h) was achieved when 30% of PTZ was loaded in Duro-Tak 87-9301 with 10% IPM and 5% GEFA-C(8). These results demonstrate the feasibility of a novel narcotic-antagonist analgesic matrix-type TDDS for PTZ.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acrylates / chemistry
  • Adhesives
  • Administration, Cutaneous
  • Analgesics, Opioid / administration & dosage*
  • Analgesics, Opioid / pharmacokinetics*
  • Animals
  • Chemistry, Pharmaceutical
  • Chromatography, High Pressure Liquid
  • Diffusion Chambers, Culture
  • Drug Compounding
  • Excipients
  • Mice
  • Mice, Hairless
  • Pentazocine / administration & dosage*
  • Pentazocine / pharmacokinetics*
  • Skin Absorption
  • Spectrophotometry, Ultraviolet

Substances

  • Acrylates
  • Adhesives
  • Analgesics, Opioid
  • Excipients
  • Pentazocine