Department of Pharmaceutics, MAEER’s Maharashtra Institute of Pharmacy, MIT Campus, S. No. 124, Kothrud, Pune 411038, Savitribai Phule Pune University, India
Prochlorperazine maleate is a phenothiazine antipsychotic used principally in the treatment of nausea, vomiting and vertigo. Biological half- life of the drug is about 6 to 8 hrs and oral dose is 5 or 10 mg thrice or four times a day. The mean absolute bioavailability for drug is 12.5%. Due to the solubility of drug in acidic pH, it is mainly absorbed from stomach.
Site specific oral floating delivery of prochlorperazine maleate will prolong the gastric retention time, increases the drug bioavailability, reduces frequency of administration and can result in better patient compliance.
The tablets were prepared by direct compression technique. Floating drug delivery was developed using gas forming agent and release retarding agent i.e. hydroxyethyl cellulose HHX (Natrosol HHX) and polymethyl methacrylate (PMMA). 32 full factorial design was used for optimization. Prepared tablets were evaluated for pre and post compression parameters.
From the factorial batches it was observed that formulation containing 68.5% of hydroxyethyl cellulose HHX and 15% of polymethyl methacrylate had shown a drug release of 91.56 ± 2.7% with floating upto 10 hrs following Korsmeyer Peppas release kinetics.
In- vivo placebo X-ray study for optimized batch F6 had shown good gastroretention ability for 6 ± 0.5 hrs. In- vitro and in- vivo study confirmed the site specific floating delivery for drug.
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