Abstract
Objective: Promethazine theoclate is a BCS Class II drug having anti-histaminic property and mainly used for the treatment of motion sickness and postoperative emesis. The main objective of the research work was to formulate and optimize immediate release pellets of promethazine theoclate by using the extrusion-spheronization technique to offer immediate release dosage form suitable for treatment of nausea and vomiting associated with motion sickness and post-operative conditions.Methods: Immediate release pellets of promethazine theoclate were prepared by using microcrystalline cellulose (MCC) and corn starch as filler and disintegrant respectively along with other excipients. Pellet formulation was further optimized for bulk density, disintegration time and percent drug release after 10 min. using 32 factorial design. Formulations were also characterized for drug-polymer interactions using Differential Scanning Calorimetry (DSC), surface morphology by Scanning Electron Microscopy (SEM) and other physicochemical properties.Results: Optimised pellet formulation contains 2.5:4.5:1 ratio of MCC: Corn Starch: Drug and spheronization time of 60 seconds showing highest percent yield of 78% and immediate drug release of 100.52±0.65% after 10 min.Conclusion: Promethazine theoclate pellets formulated in this study can serve as an alternative to tablet dosage form which can give immediate drug release for treatment of motion sickness and postoperative emesis.
Highlights
Promethazine theoclate is BCS Class II, H1 antihistaminic drug mainly used in the treatment of motion sickness and postoperative emesis [1, 2]
Drug-excipient compatibility studies for promethazine theoclate along with the excipients used in the formulation was checked using Differential Scanning Calorimetry (DSC) technique
Percent friability of prepared pellets was found to be within 0.32±0.35 to 0.80±0.19 which was acceptable as the standard limit for percent friability which is
Summary
Promethazine theoclate is BCS Class II, H1 antihistaminic drug mainly used in the treatment of motion sickness and postoperative emesis [1, 2]. It has 25% bioavailability due to its poor aqueous solubility which is the major limiting factor for its absorption and delayed onset of action [3]. Promethazine theoclate tablets are available in the market as immediate release single-unit dosage form for oral administration. Among the various types of multiple-unit dosage forms, pellets have attracted more attention due to their unique clinical and technical advantages. Pellet drug delivery system offers various therapeutic advantages such as dose tailoring as well as it helps in reducing inter and intrapatient variability by reducing fluctuations in peak plasma concentrations with no significant reduction in bioavailability [7, 8]
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