DEVELOPMENT AND EVALUATION OF MUCOADHESIVE TABLETS OF CLOTRIMAZOLE AND ITS β- CYCLODEXTRIN COMPLEX FOR THE TREATMENT OF CANDIDIASIS

摘要

Clotrimazole.is.an.antifungal.agent.widely.used.as.a.first.line.treatment.for.oral.candidiasis..Clotrimazole.is.a.poorly.water.soluble.drug,.so.solubility.is. main. constraints.for.its. oral. bioavailability..An. attempt.has.been.made.to. increase. its.solubility.by.complexation.with. β‐cyclodextrin.and.then.formulating.mucoadhesive.tablets.of.best.formulation.with.β‐cyclodextrin..Mucoadhesive.tablet.formulations.were.prepared.by.direct.compression.technique.using.various.concentrations.of.HPMC.K4M,.Carbopol‐934p.on.a.10.station.pilot.press.using.13.mm.flat.faced.punches.(PPID,.Chamunda,.India)..All.the. formulations. were. evaluated.for. weight. variation,.hardness,.thickness,.%. swelling.index,.mucoadhesive. strength.and.in.vitro.drug.release. of. the. drug. in. simulated. saliva. solution. pH. 6.8.. In. vitro. drug. release. of. clotrimazole. was. best. explained. by. zero. order. equation. and.formulations.F1.to. F5. were.found. to. be. following. anomalous. diffusion.and.F6.was.found.to.be.following.fickian.diffusion..The.formulations. F5.showed.maximum.drug.release.for.12.h.study,.therefore.this.formulation.was.optimized. by. complexing.the. clotrimazole. with.β‐cyclodextrin.(1:1.molar.ratio).which.resulted.in.increase.the.dissolution.rate.of.the.formulation.F.6..The.stability.studies.showed.that.there.is.no.decrease.in.the.drug.content.of.all.formulations.for.the.period.of.3.months