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KMID : 0370019940080000093
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Chung-Ang Journal of Pharmacal Sciences
1994 Volume.8 No. 0 p.93 ~ p.100
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Transdermal Penetrations of Pivaloyloxymethyl Indomethacin from Various Ointment Bases
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Abstract
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Transdermal penetrations of pivaloyloxymethyl indomethacin(IND-PV), a potential derivative of indomethacin(IND), were characterized by diffusion study in various ointment bases, which are oleaginous, w/o and o/w type emulsions, water soluble and hydrogel bases. And the consstencies of all ointment bases were adjusted within the range of 99±5 dyne/㎠. The degree of penetration of either IND-PV or IND through hairless nouse skin was different in various ointment bases, showing the results as decreasing order as follows : macrogol＞w/o type＞o/w type＞gel type＞vaseline ointment. IND-PV was hydrolyzed by the enzyme during penetration through the hairless mouse skin, and detected as IND in the receptor compartment. However, it has been revealed that IND-PV didn´t penetrate through the dialysis membrance, which were in contrast to the penetrations of IND, due to the limited solubility of IND-PV in diffusion medium and the absence of hydrolytic enzyme in the dialysis membrance. Therefore it might be possible to conclude that IND-PV penetrates the hairless mouse skin depending on the enzymatic hydrolysis mainly in addition to the lipophilicity of the drug. In this trasdermal penetraton, the absorption of IND-PV was not rate-limited by a simple passive diffusion, but and enzymatic hydrolytic process.
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