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.