Abstract
Background: Prochlorperazine maleate, a well known antiemetic is used in the treatment and prevention of nausea and vomiting. The dosage of the drug is usually 5 or 10 mg thrice or four times a day. The drug has short biological half life (6-8 hours). The bioavailability of drug is 12.5%. Due to the solubility of drug in acidic pH, the drug is absorbed rapidly from stomach.
Objective: The objective was to optimize effervescent floating matrix tablets for the drug which enhance the oral bioavailability and prevent first pass metabolism of the drug by retaining the drug in stomach.
Method: The formulations were prepared by direct compression method. 32 full factorial design was used to optimize the concentration of release retarding agents. Hydroxyethyl cellulose HHX and hydroxypropyl cellulose-H were used as release retarding agents. Sodium bicarbonate and citric acid were used as gas forming agents. The tablets were evaluated for pre-compression and post-compression parameters.
Results: From the factorial batches, formulation H7 containing 70% of hydroxyethyl cellulose HHX and 12% hydroxypropyl cellulose-H was found to be the optimized batch. Formulation H7 followed Korsmeyer Peppas release kinetics, with sustained drug release of 93.64±6.4 % and floating for 10 hours. In-vivo X-ray placebo study of optimized batch (H7) showed retention of tablet in stomach for 6±0.5 hours.
Conclusion: The study proved successful floating delivery of Prochlorperazine maleate in stomach.
Keywords: Prochlorperazine maleate, floating, hydroxyethyl cellulose, hydroxypropyl cellulose, gastric retention.
Graphical Abstract
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