Formulation and in vitro evaluation of pentazocine transdermal delivery system.
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.
Furuishi
Takayuki
T
Research Unit of Pharmaceutics, College of Pharmacy, Nihon University, Chiba, Japan.
Io
Takeshi
T
Fukami
Toshiro
T
Suzuki
Toyofumi
T
Tomono
Kazuo
K
D000179:Acrylates / Q000737:chemistry; D000269:Adhesives; D000279:Administration, Cutaneous; D000701:Analgesics, Opioid / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D000818:Animals; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D015194:Diffusion Chambers, Culture; D004339:Drug Compounding; D005079:Excipients; D051379:Mice; D008812:Mice, Hairless; D010423:Pentazocine / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D012869:Skin Absorption; D013056:Spectrophotometry, Ultraviolet
D000179:Acrylates; D000269:Adhesives; D000701:Analgesics, Opioid; D005079:Excipients; D010423:Pentazocine