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  • 1. Presented By:Raviraj V. JakapureM.Pharm Sem IIDept Of Pharmaceutics.A seminar onRESEARCH ARTICLEFormulation and evaluation ofmefenamic acid emulgel for topicaldeliveryUnder guidance ofMr. S.P. AnantwarAssistant Professor,Dept. Of PharmaceuticsN. D. M. V. P. S’S COLLEGE OF PHARMACY, NASHIK.4/20/20131
  • 2.  Published in Saudi Pharmaceutical Journal( IMPACT FACTOR : 0.66 ) Production and hosting by ELSEVIER AUTHOR NAME: Rachit Khullar*, Deepinder Kumar, NimrataSeth, Seeme SainiDept of Pharmaceutics, Rayat Instt ofpharmacy, Punjab, IndiaReceived on 27 june 2011; Accepted 11 aug20114/20/20132
  • 3. CONTENTS Purpose Introduction to emulgel Advantges , Disadvantages Important constituents of emulgel Monograph of mefenamic acid Method of preparation Evaluation Results and discussion Conclusion References4/20/20133
  • 4. PURPOSE The objective of the study was to prepare emulgelof mefenamic acid, a NSAID, usingCarbapol 940 as a gelling agent. Mentha oil andclove oil were used as penetration enhancers.Theemulsion was prepared and it was incorporatedin gel base The formulations were evaluated for rheologicalstudies, spreading coefficientstudies, bioadhesion strength, skin irritationstudies, in vitro release, ex vivo releasestudies, anti-inflammatory activity and analgesicactivity4/20/20134
  • 6. ADVANTAGES Hydrophobic drugs can be easily incorporated Better stability Better loading capacity Production feasibility and low preparation cost No intensive sonication Controlled release Patient compliance4/20/20136
  • 7. DISADVANTAGES Drug of Large particle size NOT easy to absorbthrough skin Poor permeability Skin irritation Occurrence of bubble4/20/20137
  • 8. Important constituents Aqueous material: Water, Alcohol Oils: IPM (7-7.5%), Light liguid paraffin (7-5%) Emulsifiers Gelling agents HPMC (2-5%), Sod. CMC(1%), Carbopol 940(1%) Permeation enhancers Oleic acid(1%), Lecithine (1%) Menthol (4-6%)4/20/20138
  • 9. Material and methods Mefenamic acid was obtained as a gift samplefrom Lexicon Biotech Pvt. Ltd. Baddi (HimachalPradesh), Carbopol 940 was obtained from Loba chemicalsMumbai. Dialysis membrane was procured from Himedia, Mumbai All other chemicals used were of analytical gradeand were used without any further chemical 4/20/20139
  • 10. Method of preparation4/20/201310
  • 11. MEFENAMIC ACIDClass: Nonsteroidal Anti-inflammatoryAgentsChemical Name: N-(2,3-xylyl)anthranilicacidMolecular Formula: C15H15NO2.Mechanism of actionMefenamic acid is a competitiveinhibitor of COX-1 and COX-2, whichare responsible for the first committedstep in prostaglandin biosynthesis.- Decreasing the activity of theseenzymes thus reduces the productionof prostaglandins, which are implicatedin inflammation and pain processes. 4/20/201311
  • 12. Preparation of mefenamic acid emulgel Carbopol 940 Purified water GEL Span 20 Liquid paraffin OILPHASE Tween 20 Purified water AQUEOUSPHASE 1. Mefenamic acid ETHANOL 2. Methyl & Propyl paraben PROPYLENEGLYCOL Oil phase Aq phase stirring coolEMULSION GEL4/20/201312
  • 13. Evaluation parameters Physical Examination:Appearance, colour, consitency Rheological study diagram: Skin irritation test: Undesirable skin changes inrats. 4/20/201313
  • 14.  Invitro release studies Exvivo release studies: Using wistar male rat skin4/20/201314
  • 15.  Stability studiesThe prepared emulgels were packed inaluminum collapsibletubes (5 g) and subjected to stabilitystudies at 5 C, 25 C/60% RH, 30 C/65% RH, and 40 C/75% RHfor a periodof 3 months. Samples were withdrawn at15-day time intervalsand evaluated for physicalappearance, pH, rheological propertiesand drug content4/20/201315
  • 16. Results and discussion Physicalappearance Emulgel formulationswere yellowish whiteviscous creamypreparation with a smoothhomogeneous texture andglossy appearance. Rheologicalstudies The tests were performed at100 rpm for 10 min.Figure . Viscosity of the formulations F1–F4 (mean± SD). 4/20/201316
  • 17.  Skin irritation test No allergic symptoms likeinflammation, redness, irritation appeared on rats upto 24 h. Invitro release studies The study showed the release of the drugs fromits emulsified gel formulation can be ranked in thedescending order:F4 > F1 > F2 >F3 where the amounts of the drugrelease of the drug released after 240 min were56.01%, 53.48%, 52.23%, 51.21%, respectively4/20/201317
  • 18. Figure . In vitro cumulative % drug releaseof formulation F1–F44/20/201318
  • 19.  Stability studies All the prepared emulgel formulations were found to be stableupon storage for 3 months, no change was observed in theirphysical appearance, pH, rheological properties and drugcontent.4/20/201319
  • 20. Conclusion In the coming years, topical drug delivery will be usedextensively to impart better patient compliance. Sinceemulgel is helpful in enhancingspreadability, adhesion, viscosity and extrusion, thisnovel drug delivery become popular. Moreover, theywill become a solution for loading hydrophobic drugsin water soluble gel bases for the long term stability. Topical emulgels of mefenamic acid were formulatedand subjected to physicochemical studies & can beused as an antiinflammatory analgesic agent fortopical drug delivery.4/20/201320
  • 21. References Ansel, H.C., Allen Jr, L.V., Popovich, N.G., 1999.Pharmaceutical Dosage Forms and Drug DeliverySystems, 7th ed. Lippincott Williams and Wilkins, New York. Bonacucina, G., Cespi, M., Palmieri, G.F., 2009.Characterization and stability of emulsion gels based onacrylamide/sodium acryloyldimethyl taurate copolymer. AAPSPharmSciTech. 2, 10. Choi, H.G., Yong, C.S., Sah, H., Jahng, Y., Chang, H.W., Son,J.K., Lee, S.H., Jeong, T.C., Rhee, J.D., Baek, S.H., etal., 2003. Physiochemical characterization of diclofenacsodium loaded poloxamer gels as a rectal delivery systemwith fast absorption.Drug Dev. Ind. Pharm. 29, 545–553. Crunkhorn, P., Mencock, S.C., 1971. Mediators ofinflammation induced in rat paw carregeenan. Br. J.Pharmacol. 42, 371–402. 4/20/201321
  • 22. CRITICISM Positive points: Hydrophobic drugs can be incorporated intoemulgels for their long term stability. Negative points: 1. Cracking, Creaming & Phase inversion ofemulsion was not focused. 2. The release of drug from prepared formulationwas not compared with marketed product.4/20/201322
  • 23. •THANK YOU4/20/201323