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http://dx.doi.org/10.4333/KPS.2007.37.4.237

The Effect of Enhancer on the Penetration of Indapamide through Hairless Mouse Skin  

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)
Publication Information
Journal of Pharmaceutical Investigation / v.37, no.4, 2007 , pp. 237-242 More about this Journal
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.
Keywords
Indapamide; Enhancer; Transdermal drug delivery systems; Permeability;
Citations & Related Records
Times Cited By KSCI : 1  (Citation Analysis)
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