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FORMULATE AND EVALUATE THE MUCOADHESIVE MICROSPHERE OF HMG CO-A REDUCTASE INHIBITOR FOR THE TREATMENT OF HYPERLIPIDEMIA

Journal Name:

  • The International Journal of Pharmaceutical Research and Bio-Science

Publication Year:

  • 2012

Key Words:

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Abstract (2. Language): 
The purpose of this project work was to formulate and systemically evaluate in-vitro performances of simvastatin mucoadhesive microspheres for its potential use in the treatment of hypelipidemia. Simvastatin mucoadhesive microspheres, containing carbopol-934P as mucoadhesive polymer and ethyl cellulose as carrier polymer, were prepared by w/o/w double emulsiontechnique. Results of preliminary trials indicated that the quantity of emulsifying agent, time for stirring, mucoadhesive polymers concentration, and Drug ratio affected various characteristics of microspheres. A 32 full factorial design was employed to study the effect of independent variables, mucoadhesive polymer concentration (carbopol-934P) (X1), and Surfactant concentration (Tween 80) (X2) on dependent variables, i.e. % mucoadhesion, particle size, and drug release profile. Microspheres were discrete, spherical, free showed a good percentage of drug entrapment efficiency.The morphological characteristics of the mucoadhesive microspheres were studied under a scanning electron microscope. The best batch exhibited a high drug entrapment efficiency of 76%; 95% mucoadhesion. A sustained pattern of drug release was obtained for more than 12 h. The mucoadhesive polymer-to-matrix polymer ratio had a more significant effect on the dependent variables. An in-vitro mucoadhesive test showed that simvastatin microspheres adhered more strongly to the intestinal mucous layer and could be retained in the intestinal tract for an extended period of time. In conclusion, the prolonged intestinal residence time and slow release of simvastatin resulting from the mucoadhesive microspheres could contribute to the provision of a sustained anti-hyperlipidemic effect.
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  • 5
283-308
  • English

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Available Online At www.ijprbs.com
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