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USE OF GLUTARIC ACID TO IMPROVE THE SOLUBILITY AND DISSOLUTION PROFILE OF GLIPIZIDE THROUGH PHARMACEUTICAL COCRYSTALLIZATION

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Batool F., Ahmad M., Minhas M. U., Khalid Q., Idrees H. A., Khan F. M.
Acta Poloniae Pharmaceutica - Drug Research
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2019
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vol. 76
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issue 1
103-114
EN
The purpose of current study was to improve the solubility and dissolution profile of BCS class-II drug Glipizide using glutaric acid as a coformer via various cocrystalization techniques i.e., dry grinding, liquid assisted grinding, slurry and solvent evaporation. Fourier Transform Infrared Spectroscopy (FTIR) was performed to determine the interaction between components of glipizide-glutaric acid (GPZ-GLU) cocrystals. Powder X-ray Diffraction (PXRD) studies confirmed the crystalline nature of formulated cocrystals. Scanning Electron Microscopy (SEM) revealed cylindrical to rectangular shape of cocrystals. Flow properties of GPZ-GLU cocrystals were evaluated by micromeritics analysis. Size and surface morphology was determined by zeta sizer analysis and optical microscopy. Differential scanning calorimetry (DSC) and Thermogravimetric (TGA) analysis were performed to determine the melting points as well as thermal stability of pure components and formulated GPZ-GLU cocrystals. In-vitro drug release studies were carried out using dissolution apparatus-II. GPZ-GLU cocrystals showed higher drug release at pH 6.8 as compared to pH 1.2. However, percent drug release of optimum formulations at pH 6.8 was determined as; 24%-92.2% (F3) and 12.0%-93.5% (F7). Solubility studies revealed improved solubility as compared to pure drug in water i.e., 53 folds and 54.27 folds from F3 and F7 cocrystals, respectively. Finally it was concluded that glutaric acid has improved the solubility and dissolution profile of glipizide. However, many cocrystal formers have been reported in literature that can be used to enhance the physicochemical properties as well as bioavailability of poorly soluble drugs via cocrystalization technique.
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