Journal article

Oxazolidines: prodrugs for the delivery of β-aminoalcohols through human skin from aqueous solution

JA Young-Harvey, ID Rae, IH Pitman

International Journal of Pharmaceutics | Published : 1986

Abstract

Ephedrine (I) is delivered through human skin, in vitro, significantly faster from aqueous solutions of 3,4-dimethyl-5-phenyl-oxazolidine (II) with pH values between 7.0 and 10.88 than from corresponding solutions of I. The difference in penetration rates was most marked at pH 7.0 where 917 μg and < 10 μg of I was delivered through 1.3 cm2 of skin in 24 h from 1% w/v solutions of II and I, respectively. No detectable amounts of I were delivered through 1.3 cm2 of skin in 24 h from 1% w/v solutions of I or II in propylene glycol and delivery of I was faster from 1% w/v solutions of I in liquid paraffin than from corresponding solutions of II. Compound II has a lower pKa value than compound I ..

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