A water soluble Beta-cyclodextrin-epichlorohydrin complex (β-CDEPI) was synthesized by one-step condensation polymerization. Drug-β-CDEPI inclusion complexes were prepared and characterized. Inclusion complexes prepared using lyophilization technique was used to formulate orodispersible tablets. Compatibility studies showed no interaction and characterization proved substantial inclusion complex formation. Drug content was found between 97-99%. In-vitro disintegration time was found to be less than 3 minutes and all the formulations showed complete drug release of 100% within 15 minutes. The formulations were found to be stable for a period of 6 months. β-CDEPI polymer enhances the solubility and thus effectively can be utilized to improve the aqueous solubility of poorly water soluble drugs.
Objective: The present work was aimed at preparation of mesalazine microspheres by a non-aqueous solvent evaporation method using eudragit S 100 and eudragit L 100 as pH dependent polymers for colon targeting.
Methods:The ratio of drug to polymer was varied and the effect of formulation variables revolutions per minute (RPM) (1000, 1500, 2000 and 2500) and concentration of span 80 (1%, 1.5%, 2% and 2.5%) were studied. Prepared microspheres were evaluated for particle size, percent drug entrapment, granular analysis, in vitro drug release studies, Fourier transformed infrared spectroscopy (FT-IR) Differential Scanning Calorimetry (DSC), X-ray diffraction (XRD) and scanning electron microscopy (SEM) studies.Results: Particle size has decreased and percent drug entrapment had increased with increase in RPM in all formulations. When the span 80 concentration increased, the particle size of the microsphere formulations increased and percent drug entrapment decreased in eudragit S 100 microspheres; whereas in eudragit L 100 microspheres, as the concentration of span 80 increased, the particle size of the microsphere formulations decreased. The prepared microspheres sustained the drug release over a period of 12 h.
Conclusion:Thus eudragit S 100 and eudragit L 100 microspheres could constitute a promising approach for colon-specific and sustained delivery of mesalazine for the treatment of inflammatory bowel disease.
Introduction:Liquisolid technique is used in delivery of lipophilic and poorly water soluble drugs through oral route. It involves dissolving water insoluble drugs in nonvolatile solvents and converting into acceptably flowing and compressible powders. The objective of the present work was to enhance the dissolution rate of ketoprofen using microcrystalline cellulose as carrier, aerosil 200 as coating material, and polyethylene glycol as nonvolatile water miscible liquid vehicle.Materials and Methods:The drug concentration was kept constant in all formulations at 40% w/w. Optimization was carried out using Box–Behnken design by selecting liquid load factor, amount of coating material, and amount of magnesium oxide as independent variables; cumulative percentage drug release and angle of repose were considered as dependent variables.Results:The Fourier transform infrared (FTIR) and differential scanning calorimetry (DSC) studies revealed that there was no possible interaction between drug and tablet excipients. Prepared ketoprofen liquisolid tablets were evaluated for hardness, weight variation, friability, in-vitro disintegration time, drug content uniformity, and in-vitro dissolution studies. The optimized formulation yielded the response values, which were very close to the predicted values. The accelerated stability studies conducted showed that liquisolid tablets were not affected by ageing and there were no appreciable changes in the drug content.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.