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KMID : 0606920100180010106
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Biomolecules & Therapeutics
2010 Volume.18 No. 1 p.106 ~ p.110
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Enhanced Bioavailability of Ambroxol by Transdermal Administration of the EVA Matrix Containing Penetration Enhancer in Rats
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Choi Jun-Shik
Shin Sang-Chul
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Abstract
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The pharmacokinetics and bioavailability of ambroxol, an expectoration improver and mucolytic agent, were studied to determine the feasibility of enhanced transdermal delivery of ambroxol from the ethylene-vinyl acetate (EVA) matrix system containing polyoxyethylene-2-oleyl ether as an enhancer in rats. The ambroxol-010 matrix system (15 mg/kg) was applied to abdominal skin of rats. Blood samples were collected via the femoral artery for 28 hrs and the plasma concentrations of ambroxol were determined by HPLC. Pharmacokinetic parameters were calculated using Lagran method computer program. The area under the curve (AUC) was significantly higher in the enhancer group (1,678 ± 1,413.3 ng/ml·hr) than that in the control group 1,112 ± 279 ng/mlㆍhr), that is treated transdermally without enhancer, showing about
151% increased bioavailability (p＜0.05). The average Cmax was increased in the enhancer group (86.0 ± 21.5 ng/ml) compared with the control group (59.0 ± 14.8 ng/ml). The absolute bioavailability was 13.9% in the transdermal control group, 21.1% in the transdermal enhancer group and 18.1% in the oral administration group compared with the IV group. The Tmax, Ka, MRT and t1/2 of ambroxol in transdermal enhancer group were increased significantly (p＜0.01) compared to those of oral administration. As the ambroxol-EVA matrix containing polyoxyethylene-2-oleyl ether and tributyl citrate was administered to rats via the transdermal routes, the relative bioavailability increased about 1.51-fold compared to the control group, showing a relatively constant, sustained blood concentration. The results of this study show that ambroxol-EVA matrix could be developed as a transdermal delivery system providing sustained plasma concentration.
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KEYWORD
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Bioavailability, Pharmacokinetics, EVA, Ambroxol, Enhancer, Transdermal administration
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