The Flux of Select NSAIDs through Silicone Membranes from Mineral Oil

Pharmaceutics

Paul S. Mertz¹ 

[1] Department of Medicinal Chemistry, University of Florida, P.O. Box 100485, Gainesville, FL 32610, USA; E-Mail

关键词: solubility in mineral oil;    solubility in water;    silicone membrane surrogate;    human skin in vitro;    Roberts–Sloan equation;   

DOI  :  10.3390/pharmaceutics6030354

来源: mdpi

【 摘 要 】

Here we report the experimental log maximum fluxes of n = 9 non-steroidal anti-inflammatory drugs (NSAID) through silicone membranes from the lipid mineral oil (experimental (Exp.) log J_MPMO) and correlate those Exp. log J_MPMO values with their experimental log maximum fluxes through human skin in vivo from mineral oil (Exp. log J_MHMO). The correlation was only fair (r² = 0.647) for n = 9 but improved dramatically if Nabumetone was removed from the correlation (n = 8, r² = 0.858). Non-linear regression of the n = 8 Exp. log J_MPMO values as the dependent variable against their log solubilities in mineral oil (log S_MO) and in pH 7.4 or 1.0 buffers (log S_7.4 or S_1.0, respectively), and their molecular weights as independent variables in the Roberts–Sloan (RS) equation gave a new set of coefficients for the independent variables in RS. Those coefficients have been used to calculate log J_MPMO values which have been correlated with the Exp. log J_MPMO values to give r² = 0.911 if log S_7.4 and r² = 0.896 if log S_1.0 were used as aqueous phases. Thus, silicone membranes appear to be good surrogates for predicting flux through human skin if the vehicle is a lipid such as mineral oil.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.