Background: Prochlorperazine maleate (PCM) is a phenothiazine antipsychotic used in the
treatment of nausea, vomiting and vertigo. It is BCS class II drug with only 12.5% bioavailability. Patents
data on PCM had shown work on conjugation and matrix formulation which suggested idea for
the present work design.
Objective: The objective of this study was to enhance solubility of drug and to optimize gastro retentive
floating capsule for controlled drug release at the targeted site for stipulated time.
Method: The solubility of drug was determined in various vehicles like oils, surfactants and cosurfactants.
Pseudo ternary phase diagrams were constructed to identify the efficient self emulsifying
region. SMEDDS were tested for micro emulsifying properties. The resultant microemulsions were
evaluated and were further selected for the floating drug delivery. Magnesium hydroxide was used as
carrier to transform SMEDDS into Solid SMEDD (S-SMEDD). Non-effervescent floating capsule
containing S-SMEDD were optimized using factorial design with independent variable HPMC K4M
and ethyl cellulose.
Results: SMEDD consists of PCM, isopropyl myristate, tween 80 and PEG 400 as a drug, oil, surfactant
and co-surfactant (1:1 ratio). Optimized formulation F5 showed 10 hrs floating time and percent
drug release 91.56±2.7% with controlled drug delivery in stomach. F5 followed Korsmeyer Peppas
release kinetics where the drug followed Fickian diffusion transport mechanism due to swelling of
polymers in controlled manner.
Conclusion: It can be concluded that SMEDD enhanced the solubility of drug and floating capsule
gave site specific drug release of PCM with the advantages of reduced dosing frequency and better