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Study On Flurbiprofen Gels

Posted on:2009-12-21Degree:MasterType:Thesis
Country:ChinaCandidate:J HuangFull Text:PDF
GTID:2134360245950553Subject:Pharmacy
Abstract/Summary:PDF Full Text Request
Flurbiprofen,as a non-selectivity inhibitor of Cycloxygenase,is a non-steroidal anti-inflammatory agent which has anti-inflammatory,analgesic and anti-pyretic properties and was used in treatment of osteoarthritis,rheumatoid arthritis.However,it has a short half-life and severely gastrointestinal discomfort after oral administration.The percutaneous administration of flurbiprofen is a way to minimize these gastrointestinal adverse effects and frequent administration.For this reason,we are to develop a flurbiprofen hydrogel because of its easy preparation and steady quality.At first,the apparent partition coefficients(APC)of Flu,as well as the solubilities in various solvents at 32℃were determined.The result showed that Flu has a good stability in PBS,its solubility increased along with the increase of pH value in PBS,and the APC of Flu is 68.2.We researched the effect of four different matrixes on the drug amount in rat skin,release profiles and permeation profiles of Flu gel in vitro.The result indicated that the speed of drug release and permeation through rat skin raise with the decrease of the matrix concentration. And the release profiles of Flu from all matrixes were in line with Higuchi equation. Propylene glycol alginate,CMC-Na,and 1%carbomer gels have relative fast release.The flux and accumulation permeation amount of 4%CMC-Na and 1%carbomer gels were the most powerful.HPMC was inferior in the four matrixes on the release profiles and permeation profiles.All kinds of matrixes have no significant difference on the drug amount in rat skin.We also studied the effect of seven penetration enhancers and their mixtures on the permeation profiles of flurbiprofen gels through rat skin in vitro.After this,we prepared the inclusion compound of FIu-HP-β-CD,the monoethanolamine salt and Sodium salt of Flu,separately.At last,we researched the permeation profiles of the monoethanolamine salt,Sodium salt and the inclusion compound.Consequently,PG,Menthol,oleic acid,pyrolidone and high concentration DMSO had promotion on permeation profiles of Flu. But urea and azone had significant inhibitory action.In this study,The mixture of 25%ethanol,5%menthol and 15%glycerin was found to be the most powerful enhancer mixture.The best concentration of Flu was 2%,and the flux of Flu gel was 309.4±15.6ug.cm-2·h-1and the accumulation permeation amount in 12h was 3789.1±326.2 ug·cm-2.The flux and accumulation permeation amount of Flu was slightly less than monoethanolamine salt and remarkably more than Sodium salt.And HP-β-CD had significant inhibitory action on the permeation profile of Flu.Finally,we prepared three batches sample of Flu gels,and the stability test showed that they were stable.
Keywords/Search Tags:flurbiprofen, matrix, transdermal penetration, the drug amount in rat skin, penetration enhancer
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