Formulation and characterization of orodispersible tablet of glimepiride

Abstract

The present study is regarding, Glimepiride is one derivatives of sulfonyl urea used in the treatment of Type II DM which classified as class-II (BCS) of high permeability and low degree of solubility. The endeavor is to improve its solubility by solvent vaporization method to enhance the rate of dissolution of glimepiride. Soluplus (Polyvinyl caprolactampolyvinyl acetate-polyethylene glycol graft co-polymer) , PVP k40 (Polyvinylpyrrolidone) and PEG k5 are blended with the drug in various proportions (1:1,1:3) and prepared Soluplus1, Soluplus2, PEG1, PEG2, PVP1 and PVP2 as solid dispersion. The optimized formula of solid dispersion PVP1 is added to sodium starch glycolate and cross-carmellose. The disintegration profile will appear diminished in the drug release from the dosage form at a determined period of time. Differential scanning calorimetry appeared to a reduction in its crystallinity in solid dispersions. Scanning electron microscope and particle size analysis show a reduction in the drug particle size as solid dispersions. Fourier transform infrared spectroscopy does not show an interaction between them. Hence, that PVP1 batch will be considered from nine oral dissolving tablets dosage form. Finally, orally disintegrating tablets are estimated for various parameters; for instance, disintegration time, the content of the drug, wetting time, and in vitro release profile show a conventional result. The selected formula F6 shows a good result in disintegration time during 13-second and in-vitro drug release profile achieves 96% at the end of 40 minutes.

Introduction

Orodispersible tablets (ODTs) are important in the pharmaceutical formulation for both over-the-counter drugs and prescription; they improve patient acceptability, low cost and simple methods. The disintegration of such dosage form is determined by the size and hardness of tablets.^[1] Thus the goal of current study is to compress the component into tablet that characterized by fast dissolving through rapid disintegration and high drug release from the formula during a short period of time.^[2] It is also considered as a single dose solid dispersion that used orally inside the mouth cavity, which dissolves in saliva with rapid onset of action. ODTs are produced by adding cross-povidone, sodium cross-carmellose, and sodium starch-glycolate.^[3] There are different techniques used in the production of ODTs like lyophilization, mass extrusion, spray drying, molding, sublimation, and direct compression.^[4]

The preparation of solid dispersion relies on the disintegration rate which can be enhanced by improve surface area to avoid the precipitation within the carrier, solid including in the solution and improve the wetting properties due to direct interaction with hydrophilic polymer carrier, to take a shape of a metastable crystalline structure.^[5] Therefore adjusting the drug/polymer ratio and selecting the suitable method have direct effect on the type of solid dispersion and drug release behavior ^[6]

The polyethylene glycol (PEG) 5k, Soluplus, and polyvinylpyrrolidone (PVP) 40k are the foremost utilized polymer to carry solid dispersion and their capability to form atomic adduct compounds.^[7] The presence of hydroxyl and carbonyl group tends to enhance water solubility, bioavailability, and stability.^[8] Hence, the use of such polymers has a crucial role in improving the dissolution rate profile for the drug and consequently the absorption.^[9] Glimepiride has low water solubility (<0.004 mg/ml) and dissolution properties may cause poor bioavailability.^[10] Additionally, Glimepiride is a weak acid (pKa 6.2), and has low solubility in acidic media, so it is a challenge to overcome this issue by formulating Glimepiride as ODTs to obtain rapid release of the drug in the oral cavity with a few second to achieve a high percent of drug release from the formula.^[11] Subsequently, to improve the therapeutic efficacy by enhancement of solubility and dissolution rate of Glimepiride.

Materials

Glimepiride was a gift from Al Warqaa Medical Store for Chemicals Baghdad and Soluplus, PVP 40k, and PEG 5k were purchased from Al-Noor Medical Store for Chemicals. Sodium starch glycolate and sodium croscarmellose are purchased from Al-Noor Medical store.

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Formulation and characterization of orodispersible tablet of glimepiride, Kinani Ahmad AB Yosef, Taghi Hassanien Sagban, Year : 2022 | Volume:  13 | Issue Number:  4 | Page: 252-260