Molecular interaction between glimepiride and Soluplus®-PEG 4000 hybrid based solid dispersions: Characterisation and anti-diabetic studies.

作者: Joy Nneji Reginald-Opara , Anthony Attama , Kenneth Ofokansi , Chukwuebuka Umeyor , Frankline Kenechukwu

DOI: 10.1016/J.IJPHARM.2015.11.007

关键词:

摘要: The objective of this study was to evaluate a novel blend polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol 6000 grafted copolymer (Soluplus®) and polyethylene (PEG) 4000 for solubility enhancement, physicochemical stability anti-diabetic efficacy the produced solid dispersions containing glimepiride, biopharmaceutics classification system (BCS) class II sulphonylurea. Different batches glimepiride (SD) were prepared by solvent evaporation method using individual polymers blends at different ratios. Soluplus®-PEG (sol-PEG) hybrid polymer based characterized differential scanning calorimetry (DSC), fourier transform infrared (FTIR) spectroscopy, micromeritics dissolution studies. In vivo activity determined measuring changes in blood glucose concentrations albino rats. showed good flow properties excellent practical yield. Drug content release from formulations increased when Soluplus® used as main matrix polymer. kinetics drug all followed first order. Solid state characterization confirmed formation amorphous Sol-PEG no strong drug-polymer interaction observed. reduction rats Sol-PEG-Glim SDs significantly (p<0.05) higher more sustained compared with plain sample commercially available product. Optimized SD (SP1 SP3) level 100% 9.81% 8.97%, respectively, Tmax 3h. found be stable over period 6 months (at 40°C, 70% RH) significant content. Thus, polymeric hybrids represent promising tool enhanced delivery glimepiride.

参考文章(40)
C. Pérez-Alonso, C.I. Beristain, C. Lobato-Calleros, M.E. Rodríguez-Huezo, E.J. Vernon-Carter, Thermodynamic analysis of the sorption isotherms of pure and blended carbohydrate polymers Journal of Food Engineering. ,vol. 77, pp. 753- 760 ,(2006) , 10.1016/J.JFOODENG.2005.08.002
Peter P. Fu, Qingsu Xia, Huey-Min Hwang, Paresh C. Ray, Hongtao Yu, Mechanisms of nanotoxicity: generation of reactive oxygen species. Journal of Food and Drug Analysis. ,vol. 22, pp. 64- 75 ,(2014) , 10.1016/J.JFDA.2014.01.005
Massimiliano di Cagno, Thorbjørn Terndrup Nielsen, Kim Lambertsen Larsen, Judith Kuntsche, Annette Bauer-Brandl, β-Cyclodextrin-dextran polymers for the solubilization of poorly soluble drugs International Journal of Pharmaceutics. ,vol. 468, pp. 258- 263 ,(2014) , 10.1016/J.IJPHARM.2014.04.029
Nirika Bhasin, CURRENT TRENDS IN SOLID DISPERSION: A REVIEW Journal of Drug Delivery and Therapeutics. ,vol. 4, pp. 80- 86 ,(2014) , 10.22270/JDDT.V4I3.869
Y. S. Tanwar, Bindu Yadav, Applications of solid dispersions ,(2015)
K. ArunPrasad, N. Narayanan, G. Rajalakshmi, PREPARATION AND EVALUATION OF SOLID DISPERSION OF TERBINAFINE HYDROCHLORIDE ,(2010)