FORMULATION AND EVALUATION OF FLOATING ORAL IN-SITU GEL OF METRONIDAZOLE
Objective: The objective of the present study was to formulate and evaluate a gastro-retentive in situ gelling system of metronidazole.
Methods: Sodium alginate based metronidazole floating in situ gelling systems were prepared by dissolving sodium alginate in distilled water, to which varying concentrations of viscosity enhancing polymer (methylcellulose, hydroxypropyl methylcellulose, or sodium carboxymethylcellulose), drug, and gas-forming agent (s) as calcium carbonate/and sodium bicarbonate were added and dissolved by stirring. Prepared formulae were evaluated for viscosity, floating behavior, drug content and in vitro drug release behavior.
Results: Formulation variables such as the type and concentration of viscosity enhancing polymer, the concentration of gas-forming agents affected the formulation viscosity, floating behavior and in vitro drug release.
Conclusion: The prepared in situ gelling formulations of metronidazole could float in the gastric conditions and release the drug in controlled manner. The prepared formulations appear to be promising drug delivery system for localized delivery of metronidazole for better treatment of peptic ulcer disease caused by H. pylori.
2. Pande SD, Vaidya KP, Gulhane KP. Floating drug delivery system (fdds): a new way for oral drug delivery system. Int J Pharm Clin Sci 2013;3(1):1-13.
3. Nidhi D, In Situ Gel. A novel approach of gastro retentive drug delivery. Asian J Pharm Sci Res 2013;3(3):1-14.
4. Bhalerao KK, Kamble MS, Aute PP, Dange SM, Chavan RP, Vaidya KK, et al. A short review on stomach specific floating in-situ gel. J Biomed Pharm Res 2012;1(3):1-4.
5. Vaira D, Holton J, Ricci C, Basset C, Gatta L, Perna F, et al. Review article: helicobacter pylori infection from pathogenesis to treatment-a critical reappraisal. Aliment Pharmacol Ther 2002;16(Suppl 4):105â€“13.
6. Manfredi M, Bizzarri B, Manzali E, Fugazza A, Gismondi P, et al. Which Treatment in Helicobacter pylori Infection? Clin Exp Pharmacol 2013;13(4):1-3.
7. Ayala G, Wi EH, de la Cruz-Herrera CF, Romero I. Exploring alternative treatments for helicobacter pylori infection. World J Gastroenterol 2014;20(6):1450-69.
8. Murata Y, Kofujik K, Kawashima S. Preparation of floating alginate gel beads for drug delivery to the gastric mucosa. J Biomater Sci Polymer Edn 2003;14(6):581â€“8.
9. Adebisi AO, Conway BR. Preparation and characterisation of gastroretentive alginate beads for targeting h. Pylori J Microencapsul 2014;31(1):58-67.
10. Javadzade Y, Hamedeyazda S, Adibkia K, Kiafar F, Zarrintan MH, Bazregar-Jalali M. Evaluation of drug release kinetics and physico-chemical characteristics of metronidazole floating beads based on calcium silicate and gas-forming agents. Pharm Dev Technol 2010;15(4):329-38.
11. Biswas SK, Paul S, Chowdhury A, Das J. Preparation and evaluation of gastroretentive floating pellets of metronidazole using na-alginate and hydroxyl propyl methylcellulose polymers. Pak J Biol Sci 2012;15(6):290-5.
12. GutiÃ©rrez-SÃ¡nchez PE, HernÃ¡ndez-LeÃ³n A, Villafuerte-Robles L. Effects of sodium bicarbonate on the properties of metronidazole floating matrix tablets. Drug Dev Ind Pharm 2008;34(2):171-80.
13. Bani-Jabere A, Al-Ani L, Alkhatib H, Al-Khalidi B. Prolonged Intragastric Drug Delivery Mediated by Eudragit Â® E-Carrageenan Polyelectrolyte Matrix Tablets. AAPS Pharm Sci Tech 2011;12(1):354-61.
14. Panwar P, Chourasiya D, Jain G, Sheorey RV. Formulation and evaluation of oral floatable in-situ gel of diltiazem HCL. Int J Novel Drug Deliv Tech 2012;2(1):264-70.
15. Rajalakshmi R, Diwakar Reddy N, Mothilal Naik B, Rajendra Babu V, Vijay Kumar A, Vinesha V, et al. Development and evaluation of a novel floating in-situgelling system of azithromycin dihydrate. Indo Am J Pharm Res 2013;3(4): 3821-31.
16. Patel MJ, Patel KR, Patel MR, Patel NM. Strategy for Development of pH triggered floating in-situ gel of levetiracetam. Am J Pharm Tech Res 2012;2(3): 828-41.
17. Vipul V, Basu B. Formulation and characterization of novel floating in-situ gelling system for controlled delivery of ramipril. Int J Drug Delivery 2013;5(1):43-55.
18. Rani K, Garg V, Goswami DS. Formulation and evaluation of stomach specific in situ gel of ofloxacin using natural, synthetic polymer. World J Pharm Res 2013;2(3):631-45.
19. Mahagen Y, Patidhar V, Balaram Y, Gopkumar P, Sridevi G. Formulation and evaluation of floatable in-situ gel for stomach-specific drug delivery of carbamazapine. research and reviews. J Pharm Pharm Sci 2014;3(1):37-43.
20. Al-Mamun MA, Rahman MR, Biswas S, Kundu SK, Rayhan J. Formulation and bioequivalence evaluation of extended release solid drug delivery system for metronidazole using eudragit nm30d and methocelpremium k4m as retardant material. Am J Adv Drug Delivery 2014;2(1):39-51.
21. Patel DM, Patel DK, Patel CN. Formulation and evaluation of floating oral in-situ gelling system of amoxicillin. ISRN Pharm 2011;1:1-8.
22. Choi BY, Park HJ, Hwang SJ, Park JB. Preparation of alginate beads for floating drug delivery system: effects of co2gas forming agents. Int J Pharm 2002;239:81â€“91.
23. Hasan MJ, Kamal BA. Formulation and evaluation of ranitidine hydrochloride as floating in situ gel. Int J Pharm Pharm Sci 2014;6 Suppl 2:401-5.
24. Rajinikanth PS, Mishra B. Floating in situ gelling system of acetohydroxamic acid for clearance of h. pylori. Drug Dev Ind Pharm 2008;34:577â€“87.
25. Goole J, Vanderbist F, Amighi K. Development and evaluation of new multiple-unit levodopa sustained-release floating dosage forms. Int J Pharm 2007;334:35â€“41.
26. Rajinikanth PS, Mishra B. Floating in situ gelling system for stomach site-specific delivery of clarithromycin to eradicate h. Pylori J Control Rel 2008;125:33â€“41.
27. Lemoine D, Wauters F, Bouchend S, Preat V. Preparation and characterization of alginate microspheres containing a model antigen. J Pharm Sci 1998;176:9-19.
28. Celine VL, Lai WC, Ai LC, Paul WSH. Evaluation of sodium alginate as drug release modifier in matrix tablets. Int J Pharm 2006;309:25â€“37.
29. Rohith G, Sridhar BK, Srinatha A. Floating drug delivery of a locally acting h2-antagonist: an approach using an in situ gelling liquid formulation. Acta Pharm 2009;59:345â€“54.