Fabrication and Optimization of Novel Glipizide Sustained Release Matrices for Solubility and Dissolution Enhancement by Solid Dispersion Through Hydrophillic Carriers

Abstract

The present research work was to improve the dissolution rate of glipizide which belongs to BCS II drug by enhancing its aqueous solubility using different hydrophilic carriers like PEG 6000 and hydroxylpropyl methylcellulose E15 (HPMC E15). The solid dispersion was embedded into the matrix of polymers to sustain the release pattern of drug. The various solid dispersion formulations were prepared by employing fusion method using different carriers. Further solid dispersion formulations were subjected to different in-vitro evaluation tests for solubility, drug content uniformity, drug-polymer interaction, DSC study and invitro drug release study. Tablets were prepared by direct compression method and evaluated for various physical parameters. A direct compression method using response surface methodology, followed by optimization of the evaluated parameters was employed to get the final optimized formulation. The results of drug content uniformity showed the uniform dispersion of glipizide in solid dispersion formulations. The DSC endothermic peak at 216.08°C due to glipizide was partially and completely disappeared in solid dispersion formulation indicating that drug was completely dispersed in formulations. In-vitro drug release showed 80.35% in 60 minutes for the best solid dispersion formulation S3 (ratio 1:3). Among all the formulations, F4 shows 92.87% better sustained release at the end of 12 hrs. The release co-efficient values 'n' (˂0.5) indicated that the drug release followed fickian diffusion mechanism based on formulation factors. The stability studies were carried out according to ICH guideline and result found of selected formulation was stable. Keywords: Glipizide, Solid dispersion, Xanthan gum, MatricesArticle Info: Received 18 Sep, 2017; Review Completed 29 Oct, 2017; Accepted 29 Oct, 2017; Available online 15 Nov, 2017 Cite this article as:Shende MA, Fiske PV, Fabrication and optimization of novel glipizide sustained release matrices for solubility and dissolution enhancement by solid dispersion through hydrophillic carriers, Journal of Drug Delivery and Therapeutics. 2017; 7(6):38-48

Solubility Measurement and Various Solubility Parameters of Glipizide in Different Neat Solvents

“…after solubility experiments/equilibrium. The T fus value of GLZ was determined as 484.60 K by Dash et al 3 Choudhary et al determined the T fus value of GLZ as 478.20 K. 18 Shende and Fiske found the T fus value of GLZ as 489.28 K. 19 The determined T fus value of GLZ at 484.21 K in the proposed study was very close to that reported by Dash et al 3 1. The solubility of GLZ in water has been reported by many researchers.…”

“…The solubility, dissolution, and eventually the bioavailability of GLZ can be improved by different techniques such as development of liquisolid tablets by using poly­(ethylene glycol)-400 (PEG-400) as a liquid vehicle, polymeric microparticles, , polymeric nanoparticles, co-solvent solubilization approach, complexation of GLZ with α and β-cyclodextrins, − solid self-nanoemulsification, microemulsion technology, , preparation of osmotically controlled oral drug-delivery system, solid dispersion, − nanosuspension, microwave-generated bionanocomposites, transdermal drug-delivery system, floating bioadhesive drug-delivery system, and microcrystallization . The solubility data of GLZ in various neat solvents (NS) are scarce in research database.…”

Solid Dispersions of Anthelmintics and Plant Protection Preparations

“…It is known that SD is the dispersion of one or more active ingredients in a carrier or matrix in a solid state. There are various methods for obtaining SD, which can be divided into the following [5]: Usually, SD are widely used in medicine [6][7][8][9][10], because these systems can provide many additional advantages:…”

Solid Dispersions of Biologically Active Substances

“…Usually SD are widely used in medicine [6][7][8][9][10], because these systems can provide many additional advantages: 1. to increase the solubility of poorly soluble drugs, thereby increasing the rate of dissolution, absorption and bioavailability. 2. to improve the drug output of ointments creams and gels.…”