DESIGN AND IN VIVO EVALUATION OF CONTROLLED RELEASE GLICLAZIDE TRILAYER MATRIX TABLETS IN THE MANAGEMENT OF DIABETES MELLITUS
Abstract
The purpose of the present study was to develop and optimize multi-layered matrix tablets of Gliclazide trilayer tablets to achieve zero-order drug release for sustained plasma concentration. Gliclazide tablets were prepared by direct compression and consist of middle active layer with different grades of hydroxypropyl methylcellulose (HPMC K 4M, K 15M and K100M), Guar gum and Eudragit L 100. The tablets were also evaluated for physicochemical characteristics and release kinetics. The physicochemical characteristics of the prepared tablets were satisfactory. The developed drug delivery systems showed prolonged drug release rates over a period of 24 h. In vivo bioavailability studies were carried out on the optimized formulation (EF14), mean time to attain peak drug concentration (Tmax) was 6.00 ± 0.14 and 4.02 ± 0.12 h for the optimized and marketed product respectively, while mean maximum drug concentration (Cmax) was 124.80 ± 1.02 ng/ml and 95.12 ± 1.05 ng/ml respectively. AUC0-α and AUC0-t for optimized formulation was significantly higher (p<0.05) as compared to marketed product. A fair correlation between the dissolution profile and bioavailability for the optimized formulation was observed. The results indicate that the approach used could lead to a successful development of a controlled release formulation of the drug. The EF14 was shown significant plasma concentration with controlled release and maintained for 24 hours with patient compliance by reducing the dosage frequency, when compared with marketed product in the efficient management of Diabetes mellitus.
Keywords:
Gliclazide, Trilayer matrix tablet, HPMC, Guar gum, Pharmacokinetic studiesDOI
https://doi.org/10.25004/IJPSDR.2018.100508References
2. Efentakis M, Politis S. Comparative evaluation of various structures in polymer-controlled drug delivery systems and the effect of their morphology and characteristics on drug release. Eur. Polym. J. 2006; 42:1183–1195.
3. Conte U, Maggi L, Colombo P, La MA. Multi-layered hydrophilic matrices as constant release devices. J Control Rel. 1993; 26: 39-47.
4. Conte U, Maggi L. Modulation from Geomatrix multi-layer matrix tablets containing drugs of different solubility. Biomaterials. 1996; 17(9): 889-896.
5. Gohel MC, Parikh RK, Padshala MN, Sarvaiya KG, Jena DG. Formulation and optimization of directly compressible isoniazid is modified release matrix tablet. Indian J Pharm Sci. 2007; 69:640-5.
6. Tobyn MJ, Stani FJN, Baichwal AR, Mc Call TW. Prediction of physical properties of a novel polysaccharide-controlled release system. Int J Pharm. 1996; 128:113-22.
7. Praveen KT, Pallavi Y, Deepthi K, Narayana RP. Formulation and evaluation of Entacapone sustained release matrix tablets. The Pharma Innovation. 2014; 3(8): 80-88.
8. Lachmann L, Liebermann HA, Kanig JL. The Theory and Practice of Industrial Pharmacy, CBS publishers and distributors, New Delhi, 2007.
9. Wise DL. Handbook of Pharmaceutical Controlled Release Technology, Marcel Dekker Inc, NY, USA, 2000.
10. Abdu S, Poddar SS. A flexible technology for modified release of drugs multi layered tablets. Journal of Control Release. 2004; 97: 393-405.
11. Aboelwafa AA, Basalious EB. Optimization and In vivo pharmacokinetic study of a novel controlled release venlafaxine hydrochloride Three-Layer Tablet. AAPS Pharm Sci Tech. 2010; 11: 1026-1037.
12. Bogan RK. Treatment options for insomnia pharmacodynamics of zolpidem extended release to benefit next-day performance. Postgrad Med. 2008; 120:161-171.
13. Chidambaram N, Porter W, Flood K. Formulation and characterization of new layered diffusional matrices for zero-order sustained release. J. Control. Release. 2008; 52: 149–158;
14. Choi YW, Cui JH, Lee BJ. Formulation release characteristics and bioavailability of novel monolithic hydroxyl propyl methylcellulose matrix tablet containing acetaminophen. Journal of Control Release. 2005; 108: 351-361.
15. Dalvadi H, Patel JK. Chrnopharmaceutics pulsatile drug delivery system as current trend. Asian Journal of Pharmaceutical Sciences. 2014; 5(5): 207-30.
16. Efentakis M, Peponaki C. Formulation study and evaluation of matrix and three-layer tablet sustained drug delivery systems based on Carbopol with isosorbite mononitrate. AAPS Pharm SciTech. 2008; 9: 917-23.
17. Gautama CS, Sasha L. Fixed dose drug combinations (FDCs) rational or irrational: a view point. Br J Clin Pharmacol .2008; 65: 795-796.
18. Nada HB, Syed NA, Muhammad MHA. Validated Reversed Phase HPLC Assay for the Determination of Gliclazide in Human Plasma. Saudi Journal of Medical and Pharmaceutical Sciences. 2017; 3 (10B):1128-1132.
Published
Abstract Display: 270 
PDF Downloads: 489 How to Cite
Issue
Section
Copyright (c) 2018 B. Ram Prasad, D.V.R.N. Bhikshapathi
This work is licensed under a Creative Commons Attribution 4.0 International License.
