渗透促进剂对喷他佐辛体外经皮吸收的影响。

Effect of permeation enhancers on the in vitro percutaneous absorption of pentazocine.

作者信息

Furuishi Takayuki, Oda Sachiko, Saito Hiroaki, Fukami Toshiro, Suzuki Toyofumi, Tomono Kazuo

机构信息

Research Unit of Pharmaceutics, College of Pharmacy, Nihon University; Funabashi, Chiba, Tokyo.

出版信息

Biol Pharm Bull. 2007 Jul;30(7):1350-3. doi: 10.1248/bpb.30.1350.

DOI:10.1248/bpb.30.1350

PMID:17603180

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.

摘要

在体外使用Franz扩散池，在切除毛发的小鼠身上研究了渗透促进剂对喷他佐辛（PTZ）经皮吸收的影响。单辛酸甘油酯（GEFA-C(8)）是一种脂肪酸甘油酯（GEFA），它对PTZ从肉豆蔻酸异丙酯（IPM）溶液体系中的经皮吸收具有增强作用。与单独使用IPM相比，PTZ透过皮肤的通量约高4倍，而二辛酸甘油酯（GEFA-DiC(8)）和三辛酸甘油酯（GEFA-TriC(8)）对PTZ皮肤渗透的增强作用较小。此外，在单甘油酯的各种烷基链（C(2)-C(18)）中，单己酸甘油酯（GEFA-C(6)）对PTZ通量的增强作用最大。这些结果表明，IPM溶液体系与GEFA联合使用可用于开发一种提高PTZ皮肤渗透性的透皮制剂。