Influence of formulation variables in transdermal drug delivery system containing zolmitriptan

被引:32
作者
Subedi, Robhash Kusam [1 ]
Ryoo, Je-Phil
Moon, Cheol
Choi, Hoo-Kyun [1 ]
机构
[1] Chosun Univ, Coll Pharm, Project Team BK21, Kwangju 501759, South Korea
关键词
Zolmitriptan; Transdermal drug delivery; Percutaneous penetration; Chemical enhancers; Polymorphism; Crystallization inhibitor; CRYSTALLIZATION; PERMEATION; ADHESIVES; ENHANCERS; MATRIX; SKIN;
D O I
10.1016/j.ijpharm.2011.08.002
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The effects of different formulation variables including pressure sensitive adhesive (PSA), thickness of the matrix, solvent system, inclusion of crystallization inhibitor, loading amount of drug and enhancers on the transdermal absorption of zolmitriptan were investigated. Acrylic adhesive with hydroxyl functional group provided good adhesion force and high flux of zolmitriptan. Pseudopolymorphs of zolmitriptan were found to possess different solid-state properties that affected the permeation rate. Polyoxyethylene alkyl ethers significantly increased the permeation of zolmitriptan through hairless mouse skin. However, these enhancers induced crystallization of zolmitriptan. Kollidon (R) 30 delayed the crystallization without altering the permeation profile of zolmitriptan. Stability studies suggested that terpenes did not induce crystallization of zolmitriptan in the patch and stable formulations could be produced by using cineole and limonene, or their combination. (C) 2011 Elsevier B.V. All rights reserved.
引用
收藏
页码:209 / 214
页数:6
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