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Transdermal delivery of naloxone: effect of water, propylene glycol, ethanol and their binary combinations on permeation through rat skin.

Abstract：

:The effect of the solvent systems water, ethanol (EtOH), propylene glycol (PG) and their binary combinations was studied on the ex vivo permeation profile of the opioid receptor antagonist, naloxone, through rat skin. Fourier transform-infrared (FT-IR) spectroscopic studies were done to investigate the effect of enhancers on the biophysical properties of the stratum corneum (SC), in order to understand the mechanism of permeation enhancement of naloxone by the solvent systems used. The flux of naloxone was found to increase with increasing concentrations of EtOH, upto 66% in water, and PG upto 50% in water. The maximum flux of 32.85 microg cm(-2) h(-1) was found with 33% PG in EtOH. The FT-IR spectra of SC treated with EtOH showed peak broadening at 2920 cm(-1) at all concentrations of EtOH studied indicating that EtOH increases the translational freedom (mobility) of lipid acyl chains. Theoretical blood levels well above the therapeutic concentration of naloxone can be achieved with the solvent system comprising 33% PG in EtOH and hence, provides flexibility in choice of patch size depending on the addiction status of the patient to be treated.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Panchagnula R,Salve PS,Thomas NS,Jain AK,Ramarao P

doi

10.1016/s0378-5173(01)00634-2

keywords:

subject

Has Abstract

pub_date

2001-05-21 00:00:00

pages

95-105

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(01)00634-2

journal_volume

219

pub_type

杂志文章

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