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Simultaneous optimization of percutaneous delivery and adhesion for ketoprofen poultice.

Abstract：

:Topical poultices of ketoprofen were prepared using deionized water, propylene glycol (X1), and glycerin (X2) as the vehicle in combination with hydrophilic matrix materials, including gelatin (X3) and sodium polyacrylate. A mixture design was utilized to evaluate the influence of these constituents (X1-X3) on the adhesion of the poultice and the percutaneous penetration of ketoprofen from poultices. The adhesion of the poultice was measured based on the L-Peel test method using a Tensile and Compression Testing Machine. Percutaneous delivery was conducted using nude mouse skin as the barrier. The poultice containing the highest weight fraction of gelatin demonstrated the highest value of peak stress, whereas the poultice containing 0% weight fraction of gelatin showed the smallest value among all formulations. This indicates that gelatin was the main factor determining the adhesion of the poultice. However, the interactive influence of propylene glycol with gelatin on the adhesion of the poultice cannot be ignored. On the contrary, the formulation having the maximal penetration rate was determined to be the vehicle with 0% weight fraction of gelatin and the highest percent weight fraction of glycerin. This indicates that the presence of glycerin in the poultice was able to increase the flux of ketoprofen to some extent. Quantification of individual's effect based on this mixture design resulted in a polynomial equation: Peak stress=0.033X1+0.016X2+0.12X3, flux=1.90X1+4.70X2-6.65X3. Finally, an optimized formulation with acceptable adhesion and a flux comparable to two commercial products was developed in this study.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Sheu MT,Chen LC,Ho HO

doi

10.1016/s0378-5173(01)00919-x

keywords:

subject

Has Abstract

pub_date

2002-02-21 00:00:00

pages

257-62

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S037851730100919X

journal_volume

233

pub_type

杂志文章

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