World Journal of
Pharmaceutical and Life Sciences

FORMULATION DEVELOPMENT AND CHARACTERIZATION OF MICROSPHERES OF QUETIAPINE FUMERATE

Saba Rukhsar* and Rahul Dubey

 

ABSTRACT

The aim of present work is to formulate the microspheres of anti-psychotic drug Quetiapine fumerate using the chitosan to enhance its bioavailability and sustain its action and evaluate by various parameters. Quetiapine is a dibenzothiazapine derivative belongs to the atypical antipsychotic category. It is used in the treatment of schizophrenia as well as for the treatment of acute manic episodes associated with bipolar I disorder. Reported side effects of QF are Somnolence, dizziness, dry mouth, abdominal pain, anorexia, constipation, and dyspepsia after oral therapy. Since this drug is usually taken for long period so patient compliances are also very important. The plasma half-life of the drug is 6 hours and oral bioavailability is only 9% which makes frequent dosing necessary to maintain the therapeutic blood level of the drug for long term treatment. Therefore, controlled release microspheres of QF were prepared to give its sustaining release action. The micro particles drug delivery system is a physical approach to alter and improve the pharmacokinetic and pharmacodynamics properties of various types of drug molecules. They have been used in vivo to protect the drug entity in the systemic circulation, restrict access of the drug to the chosen sites and to deliver the drug at a controlled and sustained rate to the site of action with enhanced therapeutic benefit, while minimizing side effects. The drug polymer ratio and the ratio of emulsifier influenced the % yield, drug loading, particle size, entrapment efficiency and drug release behavior of drug. Quetiapine fumerate microspheres were prepared successfully by using the ionic- gelation emulsification method. Prepared microspheres showed good % yield and drug loading. Encapsulation efficiency of microspheres was good for all formulations. Quetiapine fumerate is an antipsychotic drug of atypical neuroleptics. It is used in the treatment of schizophrenia and bipolar disorders. Polymers chitosan and Eudragit were selected on the basis of their coating property and non-toxicity. The result of the finding showed excellent controlled release. Result from present study concluded that quetiapine fumerate microspheres in combination with chitosan and eudragit produced smooth, flexible micospheres. Further, result of the drug content within the formulation was in the range of 33.08±0.03 to 88.30±0.02. The cumulative percent drug releases in 24 hours were found to be 88.30% in in-vitro drug release. An increase in drug polymer ratio was found to helpful in entrapment increase and to control the release of drug and the Eudragit S – 100 coating retard the release of drug to the enteric pH and make formulation targeted delivery system.

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