Abstract

A moderate drug permeating rate (flux) is desirable for long-acting transdermal patches. In this work, a novel simple method of controlling bisoprolol (BSP) flux by ion-pair strategy was initiated. Different ion-pair complexes including bisoprolol maleate (BSP-M), bisoprolol tartarate, bisoprolol besilate, and bisoprolol fumarate were prepared and their fluxes through rabbit abdominal skin were determined separately in vitro. Furthermore, permeation behavior from isopropyl myristate, solubility index in pressure-sensitive adhesives, determined by DSC, and n-octanol/water partition coefficient (log P) were investigated to illustrate the mechanism of drug permeation rate controlling. The results showed that compared to free BSP (J = 25.98 ± 2.34 μg/cm(2)/h), all BSP ion-pair complexes displayed lower and controllable flux in the range of 0.11 to 4.19 μg/cm(2)/h. After forming ion-pair complexes, the capability of BSP to penetrate through skin was weakened due to the lowered log P and increased molecule weight. Accordingly, this study has demonstrated that the flux of BSP could be controlled by ion-pair strategy, and among all complexes investigated, BSP-M was the most promising candidate for long-acting transdermal patches.

Links

Publisher Full Text

Authors

Song W, Cun D, Xi H, Fang L

Institution

Department of Pharmaceutical Sciences, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, Liaoning, 110016, China.

Source

AAPS PharmSciTech 13:3 2012 Sep pg 811-5

MeSH

Administration, Cutaneous
Animals
Bisoprolol
Delayed-Action Preparations
Organ Culture Techniques
Rabbits
Skin
Skin Absorption
Transdermal Patch

Pub Type(s)

Journal Article

Language

eng

PubMed ID

22639239