title: Effect of permeation enhancers on the in vitro percutaneous absorption of pentazocine.
abstract: The effect of permeation enhancers on the percutaneous absorption of pentazocine (PTZ) was investigated in excised hairless mice using Franz diffusion cells in vitro. The enhancing effect on the percutaneous absorption of PTZ from the isopropyl myristate (IPM) solution system was improved with glyceryl monocaprylate (GEFA-C(8)), which is a kind of glycerol ester of fatty acid (GEFA). The flux of PTZ through the skin was ca. 4 times higher compared with IPM alone, while a less enhancing effect of glyceryl dicaprylate (GEFA-DiC(8)) and glyceryl tricaprylate (GEFA-TriC(8)) on the skin permeation of PTZ was found. Moreover, maximum enhancement of PTZ flux was observed with glyceryl monocaproate (GEFA-C(6)) among various alkyl chains (C(2)-C(18)) of monoglycerides. These results indicated that the IPM solution system combination with GEFA may be used to develop a transdermal formulation with improved skin permeation of PTZ.
authors.affiliation: Research Unit of Pharmaceutics, College of Pharmacy, Nihon University; Funabashi, Chiba, Tokyo.
authors.forename: Takayuki
authors.initials: T
authors.lastname: Furuishi
authors.forename: Sachiko
authors.initials: S
authors.lastname: Oda
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Saito
authors.forename: Toshiro
authors.initials: T
authors.lastname: Fukami
authors.forename: Toyofumi
authors.initials: T
authors.lastname: Suzuki
authors.forename: Kazuo
authors.initials: K
authors.lastname: Tomono
mesh_terms: D000818:Animals; D004952:Esters / Q000494:pharmacology; D005990:Glycerol / Q000494:pharmacology; D008297:Male; D051379:Mice; D008812:Mice, Hairless; D009226:Myristates / Q000494:pharmacology; D010423:Pentazocine / Q000493:pharmacokinetics*; D010539:Permeability; D012869:Skin Absorption; D012995:Solubility; D013329:Structure-Activity Relationship
chemical_list: D004952:Esters; D009226:Myristates; C008205:isopropyl myristate; D005990:Glycerol; D010423:Pentazocine