FORMULATION AND EVALUATION OF PROCHLORPERAZINE MALEATE SUSTAINED RELEASE FLOATING TABLET

Ahmed Abdulameer Albadry,Fouad A. Al-saady,Wedad K. Ali

doi:10.22159/ijpps.2017v9i2.15665

Abstract

Objective: The objective of this study was to formulate once daily sustained oral release floating tablet of prochlorperazine maleate, this floating tablet has many advantages like reduction in dosing frequency, increase bioavailability, enhance patient compliance, and improve drug solubility.Methods: The prochlorperazine maleate floating tablets were formulated by using hydrophilic swellable polymer and gas generating agent. In this study, 15 formulas were prepared with many variables in order to achieve an optimum dissolution and floating behaviour for the floating tablet. The all prepared formulas were tested for bulk density, tap density, angle of repose, Carr's Index, thickness, weight variation, hardness, friability, drug content, in vitro dissolution test, in vitro buoyancy, and swelling index.Results: Formula (F2) that contain 55% (w/w) <a href="https://www.google.iq/url?sa=t&amp;rct=j&amp;q=&amp;esrc=s&amp;source=web&amp;cd=3&amp;ved=0ahUKEwjh383ow9LPAhWF6RQKHRChCVgQFggpMAI&amp;url=https%3A%2F%2Fwww.ulprospector.com%2Fen%2Fna%2FFood%2FDetail%2F895%2F563462%2FBenecel-Hydroxypropylmethylcellulose-HPMC-K4M&amp;usg=AFQjCNGgfyJECkumK5cpU_6luVwwJ2fKxA&amp;bvm=bv.135258522,d.d24">hydroxypropyl methylcellulose</a> k4M (HPMCK4M), 5 % (w/w) sodium bicarbonate (NaHCO3) have acceptable flow properties and compressibility index and good physical properties with floating lag time (16±0.57) seconds and total floating time (32±0.29) h with 100% release of prochlorperazine maleate at the end of 24 h. Fourier transform infrared spectroscopy (FTIR) study of optimum formula (F2) showed no chemical interaction between the drug and the excipients that used in the formula.Conclusion: It can be concluded that that the selected formula (F2) can be a promising formula for the preparation of gastro retentive floating drug delivery systems of prochlorperazine maleate.

Highlights

Oral route of drug administration for the majority of therapeutic applications remains the most favored preference with obvious benefits including ease of administration, flexibility in formulation and patient compliance [1].Effective oral drug delivery may depend upon the factors such as gastric emptying process, drug release from the dosage form, gastrointestinal transit time and site of drugs absorption [2]
Prochlorperazine maleate was obtained from Furat pharmaceutical industries (Iraq), hydroxypropyl methyl cellulose (HPMC) hydroxypropyl methylcellulose k4M (HPMCK4M), HPMCK15M, HPMCK100M, carbopol 934, carbopol 940, avicel PH 101 (MCC) were obtained from Jiangsu yew pharmaceutical co. limited, sodium bicarbonate (NaHCO3) was obtained from Samara drug industry (Iraq), spray dried lactose, talc, magnesium stearate was obtained from Middle east laboratories co limited (Iraq); mannitol was obtained from Provizerpharma (India)
The angle of repose of all formulations was between 28.22 ° to 43.26 °, while the result of the Carr's index and Hausner ratio was between 10.26% to 21.34%, and 1.11 to 1.27 respectively

Summary

Introduction

Effective oral drug delivery may depend upon the factors such as gastric emptying process, drug release from the dosage form, gastrointestinal transit time and site of drugs absorption [2]. An important factor for a complete drug absorption in the gastrointestinal tract (GIT) is the transition time of the dosage form [3]. The absorbed drugs from the gastrointestinal tract (GIT) and drugs show short half-life are eliminated rapidly from the systemic circulation [5] To overcome this physiological problem, many types of research and patent literature illustrated attempts of creating new dosage forms that are able to prolong the time that required for the dosage form to leave the stomach [6]

Methods

Results

Conclusion