2010 · 10 citations · 11 references
PharmacyPharmaceuticsPharmacologyBioavailabilityDrug DeliveryPharmaceutical FormulationBioavailability EnhancementDrug SolubilityFormulation Effects On BioavailabilityOral Bioavailability EnhancementSolubility EnhancementSolubility OptimizationAqueous Solubility ImprovementAqueous Solubility OptimizationDissolution Of Solid DispersionsLow SolubilitySolid Dispersion FormulationSolubilitySolubility - Dissolution RelationshipSolubility Determination
Meloxicam, a non‐steroidal anti‐inflammatory drug is widely use d in the treatment of rheumatoid arthritis, ankylosing spondulytis and osteoarthritis. One of the major problems with this drug is its low solubility in biological fluids, which results into poor bioavailability after oral administration. Therefore solid dispersions of meloxicam were prepared using hydrophilic carriers polyvinyl pyrrolidone (PVP) and poly ethylene glycol (PEG6000) to increase its aqueous solubility, solid dispersions of meloxicam were prepared using 32 factorial design with PVP and PEG6000 as independent variables while maintaining the amount of meloxi cam (150mg) and the ratio of lactose and micro crystalline cellulose (4:1) constant. The methods used for the preparation of these dispersions were physical mixing, co‐grinding and solvent evaporation technique. The prepared dispersions were evaluated in terms of drug content, wettability, In‐vitro drug release study and screened dispersions were evaluated for In‐vivo anti‐inflammatory activity. The drug content of the prepared dispersions was found to be in the range of 98% ‐ 100% indicating the application of the present methods for the preparation of solid d ispersions with high content uniformity. Absence of significant drug‐carrier interaction was confirmed by IR data. In‐vitro release profiles of all dispersions were comparatively evaluated and also studied against pure meloxicam. Faster dissolution was exhibited by Formulation containing meloxicam (150 mg), PVP (250mg), PEG6000 (125mg) and lactose: MCC 3gm (4:1) prepared by solvent evaporation method. The efficacy was evaluated by anti‐inflammatory activity on albino rats using carrageenan induced rat paw edema model. Solid dispersions of meloxicam showed increase in anti‐inflammatory activity as compared to pure meloxicam. Dispersions studied remained stable during stability studies. The increase in dissolution rate and anti‐inflammatory effect of meloxicam by solid dispersion technique may be due to increase wettability and hydrophilic nature of carriers.
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