FORMULATION AND EVALUATION OF FLOATING MATRIX TABLETS OF LEVOFLOXACIN HEMIHYDRATE USING HYDROXYPROPYL METHYLCELLULOSE K4M TO TREAT HELICOBACTER PYLORI INFECTION
DOI:
https://doi.org/10.22159/ajpcr.2018.v11i6.20296Keywords:
Levofloxacin hemihydrate, Buoyancy, Gastric retentive drug delivery system and floating matrix tabletAbstract
Objective: The aim of the study was to develop a floating drug delivery system of levofloxacin (LVF) hemihydrate for sustained drug delivery to improve the extended retention in the stomach, oral bioavailability, and local site-specific action in the stomach.
Methods: Preparation of LVF tablets using melt granulation method using hydroxypropyl methylcellulose (HPMC) K4M with sodium bicarbonate as gas generating agent. From LFTA1 to LFTA5, formulations were developed and evaluated for floating properties for swelling characteristics and in vitro drug release studies. In vitro dissolution was carried out using USP II paddle method using 0.1N HCI pH buffer at 50 rpm and samples were measured at 294 nm using ultraviolet-visible spectroscopy.
Results: Obtained Fourier-transform infrared charts indicated that there is no positive evidence for the interaction between LVF and ingredients of the optimized formula. In vitro drug release was performed and drug release kinetics were evaluated using the linear regression method and were found to be followed the zero-order release by diffusion controlled release. Optimized formula was found to be LFTA4 with 20% of a polymer with 99.03% of drug release with 12 h of floating time and 32 s floating lag time.
Conclusion: Matrix tablets (LFTA4) formulated employing 20% HPMC K4M are best suited to be used for gastroretentive dosage form of LVF.
Downloads
References
Hirtz J. The GIT absorption of drug in man: A review of current concepts and methods of investigation. Br J Clin Pharmacol 1985;19:77-83.
Baumgartner S, Kristl J, Vrecer F. Optimization of floating matrix tablets and evaluation of their gastric residence time. Int J Pharm 2000;195:125-35.
Fell JT,White HL, Collet JH. Prolonged gastric retention using floating dosage forms. Pharm Technol 2000;24:82-90.
Mathura RS, Sanghvi NM. Novel drug delivery systems for captopril. Drug Dev Ind Pharm 1992;18:1567-74.
Klausner EA, Lavy E, Friedman M, Hoffman A. Expandable gastro retentive dosage forms. J Control Release 2003;90:143-62.
Shaha SH, Patel JK, Pundarikakshudu K. An overview of a gastroretentive floating drug delivery system. Asian J Pharm Sci 2009;4:65-80.
Rouge N, Allémann E, Gex-Fabry M, Balant L, Cole ET, Buri P, et al. Comparative pharmacokinetic study of a floating multiple-unit capsule, a high-density multiple-unit capsule and an immediate release tablet containing 25mg atenolol. Pharm Acta Helv 1998;73:81-7.
Singh BN, Kim KH. Floating drug delivery systems: An approach to oral controlled drug delivery via gastric retention. J Control Release 2000;63:235-59.
Khalifa MM, Sharaf RR, Aziz RK. Helicobacter pylori: A poor man’s gut pathogen? Gut Pathog 2010;2:2.
Hessey SJ, Spencer J, Wyatt JI, Sobala G, Rathbone BJ, Axon AT, et al. Bacterial adhesion and disease activity in Helicobacter associated chronic gastritis. Gut 1990;31:134-8.
Kassab NM, Amaral MS, Singh AK, Santoro MI. Development and validation of UV spectrophotometric method for determination of levofloxacin in pharmaceutical dosage forms. Quim Nova 2010;33:968- 71.
Antos D, Schneider-Brachert W, Bästlein E, Hänel C, Haferland C, Buchner M, et al 7-day triple therapy of Helicobacter pylori infection with levofloxacin, amoxicillin, and high-dose esomeprazole in patients with known antimicrobial sensitivity. Helicobacter 2006;11:39-45.
Gisbert, JP, Pajares, JM. Treatment of Helicobacter pylori infection: The past and the future. Eur J Intern Med 2010;21:357-9.
Shakya R, Thapa P, Saha RN. In vitro and in vivo evaluation of gastro retentive floating drug delivery system of ofloxacin. Asian J Pharm Sci 2013;8:191-8.
Diren S, Zeynep FK. Bioavailability File: Levofloxacin. J Pharm Sci 2007;32:197-208.
Chowdary KP, Prakasarao KS. Formulation development of etoricoxib tablets employing HP β cyclodextrin- Poloxamer 407- PVP K30: A factorial study. Asian J Pharm Clin Res 2012;5:161-4.
Chowdary KP, Prakasarao KS, Madhuri D. Formulation and evaluation of etoricoxib tablets employing cyclodextrin- Poloxamer 407- PVP K30 inclusion complexes. Int J Appl Bio Pharm Tech 2011;2:43-8.
Shanmugam S. Granulation techniques and technologies: Recent progresses. Bioimpacts 2015;5:55-63.
Chowdary KP, Sundari PT, Prakasarao KS. Formulation and evaluation of piroxicam and aceclofenac tablets employing Prosolve by direct compression method. Asian J Chem 2009;21:5847-50.
Patel SR, Patel PR, Vora CN, Patel ND, Patel JK. Formulation, process parameters optimization and evaluation of delayed release tablets of rabeprazole sodium. Int J Pharm Pharm Sci 2010;2:144-56.
Dey S, Dutta S, Mazumder B. Formulation and evaluation of floating matrix tablet of atenolol for gastro retentive drug delivery.Int J Pharm Pharm Sci 2012;4:433-7.
El-Zahaby SA, Kassem AA, El-Kamel AH. Design and evaluation of gastroretentive levofloxacin floating mini-tablets-in-capsule system for eradication of Helicobacter pylori. Saudi Pharm J 2014;22:570-9.
Jagdale SC, Agavekar AJ, Pandya SV, Kuchekar BS, Chabukswar AR. Formulation and evaluation of gastroretentive drug delivery system of propranolol hydrochloride. AAPS Pharm Sci Tech 2009;10:1071-9.
Mouzam MI, Dehghan M, Asif S, Sahuji T, Chudiwal P. Preparation of a novel floating ring capsule-type dosage form for stomach specific delivery. Saudi Pharm J 2011;19:85-93.
Dash S, Murthy PN, Nath L, Chowdhury P. Kinetic modeling on drug release from controlled drug delivery systems. Acta Pol Pharm 2010;67:217-23.
Ramu B, Pandiyan PS. Formulation and evaluation of gastroretentive floating bioadhesive tablets of hydrochlorothiazide. Asian J Pharm Clin Res 2017;10:150-5.
Published
How to Cite
Issue
Section
The publication is licensed under CC By and is open access. Copyright is with author and allowed to retain publishing rights without restrictions.