Formulation and Evaluation of Gliclazide Solid Dispersions Incorporated Tablets for Controlled Drug Release
Abstract
The current study deals with formulation and evaluation of gliclazide solid dispersion with HP β Cyclodextrin to enhance solubility and incorporate into tablet formulation for controlled release of gliclazide. Gliclazide solid dispersion (SD) prepared using varying ratios of HP β Cyclodextrin and evaluated. The optimized SD formulation incorporated into tablet by using hydroxypropyl cellulose, HPMC K 100M. The drug dissolution from tablet formulation analyzed and characterize. The formulation SD3 comprising of drug and polymer in 1:3 ratio displayed 43-fold increase in solubility when compared to pure drug. The formulation SD13 displayed maximum yield of 98.96% and maximum drug content of 99% chosen optimal for tablet formulation. FTIR studies revealed that there is no incompatibility between drug and polymers found. XRD studies revealed that the optimized solid dispersion formulation was found to be in amorphous state. Around 15 formulations of controlled release tablet blends evaluated for micrometric properties show that all the formulations posses’ good flow properties. Formulation F15 with maximum drug content of 99.99% and drug release of 99.96 % over 16h was chosen optimal and characterized. The release kinetics suggest that drug release followed zero order and release from tablets was anomalous non- fickian diffusion super case II transport. The results show that combination of solid dispersion and application of hydrophilic and hydrophobic polymers in matrix formation can facilitate better dissolution and absorption profile with greater patient compliance.
Keywords:
Gliclazide, antihyperglycemic agent, solid dispersion, controlled release tablet, Hydroxypropyl cellulose, HPMC K 100 MDOI
https://doi.org/10.25004/IJPSDR.2020.120606References
Colombo P, Bettini R, Santi P. Swellable matrices for controlled drug delivery: gel-layer behaviour, mechanisms and optimal performance. Pharm Sci Technol Today. 2000;3:198–204.
Kim S, Gupta B, Moon C. Employing an optimized spray-drying process to produce ezetimibe tablets with an improved dissolution profile. J Pharm Invest. 2016; 46:583–592.
Son GH, Lee BJ, Cho CW. Mechanisms of drug release from advanced drug formulations such as polymeric-based drug-delivery systems and lipid nanoparticles. J Pharm Invest. 2017; 47:287–296.
Palmer KJ, Brogden R,Gliclazide N. An update of its pharmacological properties and therapeutic efficacy in NIDDM. Drugs. 1993;46: 92–125.
Lobenberg R, Amidon GL. Modern bioavailability, bioequivalence and biopharmaceutics classification system: new scientific approaches to international regulatory standards. Eur J Pharm Biopharm. 2000;50:3–12.
Desai KGH, Kulkarni AR, Aminabhavi TM. Solubility of rofecoxib in presence of methanol, ethanol and sodium lauryl sulfate at (298.15, 303.15 and 308.15).KJChemEng Data. 2003;48:942–945.
Kovacic B, Vrecer F, Planinsek O. Design of a drug delivery system with bimodal pH dependent release of a poorly soluble drug. Pharmazie. 2011;66(6):465–466.
Tran HTT, Park JB, Hong KH, Choi HG, Han HK, Lee J. Preparation and characterization of pH-independent sustained release tablet containing solid dispersion granules of a poorly water soluble drug. Int J Pharm. 2011;415(1–2):83–88.
Kanaujia P, Lau G, Ng WK, WidjajaE, Hanefeld A, Fischbach M. Nanoparticle formation and growth during in vitro dissolution of ketoconazole solid dispersion. J Pharm Sci. 2011;100(7): 2876–2885.
Patel MR, San Martin-Gonalez MF. Characterization of ergocalciferol loaded solid lipid nanoparticles. J Food Sci. 2012;77(1): N8–N13.
Perge L, Robitzer M, Guillemot C, Devoisselle JM, Quignard F, Legrand P. New solid lipid microparticles for controlled ibuprofen release: formulation and characterization study. Int J Pharm. 2012;422(1–2):59–67.
Kim HJ, Lee SH, Lim EA, Kim JS.Formulation optimization of solid dispersion of mosapride hydrochloride. Arch Pharm Res. 2011;34(9):1467–1475.
Patil MP, Gaikwad NJ. Preparation and characterization of gliclazide-polyethylene glycol 4000 solid dispersions.Acta Pharm. 2009;59:57-65.
Jalali MB, Maleki N, Garjani A, Khandar AA. Enhancement of dissolution rate and anti-inflammatory effects of piroxicam using solvent deposition technique.Drug DevInd Pharm. 2002; 28:681-86.
Yadav PS, Kumar V, Singh UP, Bhat HR, Mazumder B. Physicochemical characterization and in vitro dissolution studies of solid dispersions of ketoprofen with PVP K30 and d-mannitol. Saudi Pharmaceutical Journal. 2013; 21(1):77–84.
Djuris J, Nikolakakis I, Ibric S,Djuric Z, Kachrimanis K. Preparation of carbamazepine-Soluplus solid dispersions by hot-melt extrusion, and prediction of drug-polymer miscibility by thermodynamic model fitting. Eur J Pharm Biopharm. 2013;84(1):228-237.
Dong Z, Chatterji A, Sandhu H, Choi DS, Chokshi H, Shah N. Evaluation of solid state properties of solid dispersions prepared by hot-melt extrusion and solvent co-precipitation. Int J Pharm. 2008;355(1- 2):141–149.
Sunitha R, Venugopal K, Satyanarayana S. Formulation and Development Studies on Enhancement of Dissolution Rate of BCS Class II Antidiabetic Drug. Int J Drug Dev Res. 2018; 10:1–6.
Adibkia K, Barzegar-Jalali M, Maheri-Esfanjani H.Physicochemical characterization of naproxen solid dispersions prepared via spray drying technology. Powder Technology.2013; 246:448–455.
Mehta A, Vasanti S, Tyagi R, Shukla A. Formulation and evaluation of solid dispersion of an antidiabetic drug. Curr Trends Biotech Pharm. 2009; 3:76-84.
Makiko F, Hideko O, Yu suke S, Honami T, Masuo K, Yoshiteru W. Preparation, characterization, and tableting of a solid dispersion of indomethacin with crospovidone. Int J Pharm. 2005; 293:145–53.
Dhruv Prakash, Manoj Kumar. Formulation and Evaluation of Film Coated Tablet of Rosuvastatin. AJPTI.2015; 3(16):1-9.
Ahammad Tanbir, Hasan Moynul, Islam Md, Islam Muhammad, Rahman Habibur. Effect of Granulation Technique and Drug-Polymer Ratio on Release Kinetics of Gliclazide from Methocel K4M Matrix Tablet. IJPSR. 2010;2(4):1063-1068.
Yoshihisa Matsuda, Yuhko Minamida, Shin Ichi Hayashi. Comparative evaluation of tablet lubricants: Effect of application method on tablet hardness andejectability after compression. J Pharm Sci. 2006; 65(8):1155-1160.
Senthilnathan B, Rupenagunta A. Formulation development and evaluation of venlafaxine hydrochloride orodispersible tablets. Int J Pharmtech Res.2011;2(4):913–921.
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