Journal of Pharmaceutical Investigation

The Korean Society of Pharmaceutical Sciences and Technology (한국약제학회)
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Effects of Vehicles and Penetration Enhancers on the Percutaneous Absorption of Apomorphine

기제와 피부투과촉진제가 아포모르핀의 피부투과에 미치는 영향

  • 최영근 (성균관대학교 약학대학) ;
  • 최옥 (성균관대학교 약학대학) ;
  • 김건남 (성균관대학교 약학대학) ;
  • 박은석 (성균관대학교 약학대학) ;
  • 지상철 (성균관대학교 약학대학)
  • Published : 2003.06.20
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Abstract

In order to evaluate the effects of vehicles and penetration enhancers on skin permeation of apomorphine, the skin permeation rates of apomorphine from vehicles of different composition were determined using Franz diffusion cells fitted with excised rat skins. Solubility of apomorphine in various solvents was investigated to select a vehicle suitable for the percutaneous absorption of apomorphine. The solvents used were propylene glycol (PG), $Transcutol^{\circledR},\;Labrasol^{\circledR},\;Labrafac hydro WL^{\circledR},\;Labrafil WL 2609 BS^{\circledR}$ and isopropyl alcohol. Even though permeation rates of apomorphine from each vehicle were low $(0.008-0.36\;{\mu}g/cm^2/hr)$, the combination of PG and $Labrafac^{\circledR}$ increased it significantly. The permeation rates of apomorphine from $PG/Labrafac^{\circledR}$ mixtures increased as the volume fraction of PG in the mixture increased. The maximum permeation rate of $18\;{\mu}g/cm^2/hr$ was achieved at 30% of PG, which decreased with further increase of PG fraction. A series of fatty acids, alcohols and monoterpenes were employed as penetration enhancers. Incorporation of each enhancer in the $PG/Labrafac^{\circledR}$ (30:70) mixture at the level of 10% improved the skin permeation significantly. The highest permeation rate, $117\;{\mu}g/cm^2/hr$, was attained with myristic acid.

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