Journal of Pharmaceutical Investigation

The Korean Society of Pharmaceutical Sciences and Technology (한국약제학회)
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The Effect of Enhancer on the Penetration of Indapamide through Hairless Mouse Skin

경피흡수촉진제의 영향에 따른 인다파마이드의 피부투과

  • Seo, Hui (National Research Lab of Pharmacy, Chungnam National University) ;
  • Jeung, Sang-Young (National Research Lab of Pharmacy, Chungnam National University) ;
  • Park, Ji-Seon (National Research Lab of Pharmacy, Chungnam National University) ;
  • Shin, Byung-Cheol (Center for Drug Discovery Technologies, Korea Research Institute of Chemical Technology) ;
  • Hwang, Sung-Joo (National Research Lab of Pharmacy, Chungnam National University) ;
  • Cho, Sun-Hang (Center for Drug Discovery Technologies, Korea Research Institute of Chemical Technology)
  • 서희 (충남대학교 약학대학 제제공학실) ;
  • 정상영 (충남대학교 약학대학 제제공학실) ;
  • 박지선 (충남대학교 약학대학 제제공학실) ;
  • 신병철 (한국화학연구원 신약기반기술연구센터) ;
  • 황성주 (충남대학교 약학대학 제제공학실) ;
  • 조선행 (한국화학연구원 신약기반기술연구센터)
  • Published : 2007.08.21
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Abstract

The chemical formula of indapamide is 3-(aminosulfonyl)-4-chloro-N-(2,3-dihydro-2-methyl-1H-indol-l-yl)-benzamide, Indapamide is an oral antipertensive diuretic agent indicated for the treatment of hypertensive and edema. Indapamide inhibits carbonic anhydrase enzyme. Transdermal drug delivery systems, as compared to their corresponding classical oral or injectable dosage form counterparts, offer many advantages. The most important advantages are improved systemic bioavailability of the pharmaceutical active ingredients (PAI), because the first-pass metabolism by the liver and digestive system are avoided; and the controlled, constant drug delivery profile (that is, controlled zero-order absorption). Also of importance is the reduced dose frequency compared to the conventional oral dosage forms (that is, once-a-day, twice-a-week or once-a-week). Other benefits include longer duration of therapeutic action from a single application, and reversible action. For example, patches can be removed to reverse any adverse effects that may be caused by overdosing. In order to evaluate the effects of vehicles and penetration enhancers on skin permeation of Indapamide, the skin permeation rates of Indapamide from vehicles of different composition were determined using Franz cells fitted with excised hairless skins. Solubility of Indapamide in various solvents was investigated to select a vehicle suitable for the percutaneous absorption of Indapamide, The solvents used were Tween80, Tween20, Labrasol, Lauroglycol90 (LG90) and Peceol. Lauroglycol90 increase the permeability of indapamide approximately 3.75-fold compared with the control. Tween80, Tween20, Labrasol, Lauroglycol90 (LG90) and Peceol showed flux of $0.06ug/cm^2/hr,\;0.4ug/cm^2/hr,\;0.21ug/cm^2/hr,\;0.72ug/cm^2/hr,\;0.29ug/cm^2/hr$, respectively.

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