DEVELOPMENT, FORMULATION AND EVALUATION OF A BILAYER GASTRIC RETENTIVE FLOATING TABLETS OF RANITIDINE HCL AND CLARITHROMYCIN USING NATURAL POLYMERS
DOI:
https://doi.org/10.22159/ijpps.2017v9i9.20290Keywords:
Ranitidine HCl, Clarithromycin, Super disintegrants, Neem gum, Damar gum, copal gum, Gastric retention, Immediate release, Controlled release, Bilayer floating tabletAbstract
Objective: Bilayer gastric retentive floating tablets (BGRFT) with ranitidine HCl and clarithromycin using natural gums have been developed to prolong the gastric residence time and increase drug bioavailability. Literature review revealed no published studies on the present study.
Methods: Immediate release (IR) layer prepared by using different diluents and super disintegrants like sodium starch glycolate, crosscarmellose sodium and crospovidone. Controlled released (CR) layer prepared by using neem gum, damar gum and copal gum. Prepared tablets were evaluated for in vivo and in vitro buoyancy, in vitro dissolution studies and fourier transformation-infrared spectroscopy (FTIR). Drug release was evaluated with zero and first order for release kinetics, Higuchi, Hixson-Crowell erosion models for release mechanism.
Results: Prepared IR layer followed first order rate kinetics and CR layer followed zero order rate kinetics with non-Fickian diffusion mechanism. BGRFT also showed similar results as that of the individual layer. Optimized formulations were characterized by FTIR studies and found no interactions between drug and polymer.
Conclusion: The results demonstrate the feasibility of the model in the development of BGRFT. BGRFT enhanced the drug release and finally the bioavailability of clarithromycin when compared with commercial tablet (Biomycin 250). The present study could establish the suitability of neem gum as CR polymer in the design of BGRFT.
Downloads
References
Amit Kumar Nayak, Ruma Maji, Das B. Gastroretentive drug delivery systems: a review. Asian J Pharm Clin Res 2010;3:1-10.
Marshall BJ, Warren JR. Unidentified curved bacilli in the stomach of patients with gastritis and peptic ulceration. Lancet 1984;323:1311-5.
PS Rajinikanth, B Mishra. Floating in situ gelling system for stomach site-specific delivery of clarithromycin to eradicate H. pylori. J Crit Rev 2008;125:33-41.
Chawla G, Gupta P, Koradia V, Bansal AK. Gastroretention a means to address regional variability in intestinal drug absorption; 2003. p. 50-68.
Streubel A, Siepmann J, Bodmeier R. Gastroretentive drug delivery systems. Expert Opin. Drug Delivery 2006;3:217-33.
Dhiman S, Singh TG, Rehni AK, Sood S, Arora S. Gastroretentive: a controlled release drug delivery system. Asian J Pharm Clin Res 2011;4:5-13.
Uddin M, Rathi PB, Siddiqui AR, Sonawane AR, Gadade DD. Recent development in floating delivery systems for gastric retention of drugs an overview. Asian J Pharm Biomed Sci 2011;1:26-42.
Zaware SR, Gaikwad PD, Bankar VH, Pawar SP. A review on floating drug delivery system. Indian J Pharm Sci 2010;2:834-47.
Debjit B, Chiranjib B, Margret C, Jayakar B, Samapath Kumar KP. Floating drug delivery system-a review. Pharm Lett 2009;1:199-218.
Mayavanshi AV, Gajjar SS. Floating drug delivery systems to increase gastric retention of drugs: a review. Res J Pharm Technol 2008;1:345-8.
Garg R, Gupta GD. Progress in controlled gastroretentive delivery systems. Trop J Pharm Res 2008;7:1055-66.
US Pharmacopoeia and National Formulary. USP 24 NF 19, United state pharmacopoeial convention, Inc. 12601 Twinbrook parkway, Rockville, USA; 2000. p. 1462-3.
Indian Pharmacopoeia, Ghaziabad, published by the Indian Pharmacopoeia Commission; 2010. p. 2043-4.
Narendra C, Srinath MS, Babu G. Optimization of bilayer floating tablet containing metoprolol tartrate as a model drug for gastric retention. AAPS PharmSciTech 2006;7:34E1-E7.
Dheeraj L Patingrao, Pramod Kadu. Formulation and evaluation of clarithromycin gastroretentive dosage form. J Curr Pharma Res 2014;6:82-9.
Clarithromycin. USP 24 NF 19. The official compendia of standards. The United States Pharmacopoeia Convention. Clarithromycin tablets; 2000. p. 425-26.
Varelas CG, Dixon DG, Steiner C. Zero order from biphasic polymer hydrogels. J Crit Rev 1995;34:185-92.
Gibaldi M, Feldman S. Establishment of sink conditions in dissolution rate determinations–theoretical considerations and applications to non disintegrating dosage forms. J Plant Sci 1967;56:1238-42.
Gibaldi M, Perrier D. Pharmacokinetics, drugs and the pharmaceutical sciences. 2nd Edition. Marcel Dekker, Inc, New York and Basel; 1982. p. 15.
Higuchi T. Mechanism of sustained-action medication. Theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J Plant Sci 1963;52:1145-9.
Hixson AW, Crowell JH. Dependence of reaction velocity upon surface and agitation (I) theoretical consideration. ‎Ind Eng Chem Res 1931;23:923-31.
Korsmeyer R, Gurny R, Peppas N. Mechanisms of solute release from porous hydrophilic polymers. Int J Pediatr 1983;15:25-35.
Peppas NA. Analysis of Fickian and non-Fickian drug release from polymers. Pharm Acta Helv 1985;60:110-1.
Singh I, Kumar P. Preformulation studies for direct compression suitability of cefuroxime axetil and paracetamol: a graphical representation using sedem diagram. Acta Pol Pharm 2012;69:87-93.
Singh BN, Kim KH. Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention. J Crit Rev 2000;63:235–59.
Arora S, Ali J, Ahuja A, Khar RK, Baboota S. Floating drug delivery systems: a review. AAPS PharmSciTech 2005;6:372–90.
Baumgartner S. Optimisation of floating matrix tablets and evaluation of their gastric residence time. Int J Pharm 2000;195:125–35.
Srikanth MV, Janaki Ram B, Sunil SA, Sreenivasa Rao N, KV Ramana murthy. Gastroretentive drug delivery systems: novel approaches and its evaluation–a review. Int J Pharm Sci Rev Res 2011;10:203–16.
Padmaja B, Ramakrishna R, Goutham G. Formulation and evaluation of fast dissolving tablets of ranitidine hydrochloride. Am J Physiol 2015;9:165-9.
Rajeswari S, Sravya K, Ramana Murthy KV. Optimisation of hydrodynamically balanced tablets of clarithromycin: an approach to prolong and increase the local action by gastric retention. IJNDDS 2014;6:173-82.
Uhumwangho MU, Latha K, Sunil SA, Srikanth MV, Ramana Murthy KV. Formulation of gastro-retentive floating tablets of diltiazem hydrochloride with carnauba wax by melt granulation technique. J Pharm Allied Sci 2010;7:979–86.
Fulbandhe VM, Jobanputra CR, Wadher KJ, Umekar MJ, Bhoyar GS. Evaluation of release retarding property of gum damar and gum copal in combination with hydroxypropyl methylcellulose. Indian J Pharm Sci 2012;74:189-94.
Gangurde AB, Malode SS, Bhambar RS. Preliminary evaluation of neem gum as tablet binder. Indian J Pharm Educ Res 2008;42:344-7.
Goswami DS, Sharma M. Development of new mucoadhesive polymer from natural source. Asian J Pharm Clin Res 2012;5:247-50.
Morkhade DM, Fulzele SV, Satturwar PM, Joshi SB. Gum copal and gum damar: novel matrix forming materials for sustained drug delivery. Indian J Pharm Sci 2006;68:53-8.
VM Fulbandhe, CR Jobanputra, GS Bhoyar. Evaluation of release retarding property of gum damar and gum copal in combination with hydroxypropyl methylcellulose. Indian J Pharm Sci 2012;74:189-94.
Shikha J, Vikas J, Mahajan SC. Design and characterization of gastroretentive bilayer tablet of amoxicillin trihydrate and ranitidine hydrochloride for H. Pylori Infection. Indian J Pharm Educ Res 2014;48 Suppl 1:118-31.
Rajesh Kumar P, Hiremath D, Rajendra Reddy S. Design and evaluation studies on novel floating tablets for peptic ulcer treatment. J Adv Pharm Educ Res 2011;2:159-76.
Gnanaprakash K. Formulation and evaluation of floating drug delivery system of anti ulcer drugs. [Unpublished dissertation]. Jawaharlal Nehru technological University, Anantapuram, Chapter 6; 2013. p. 105.
Ramadevi B, Srinath N, Nagavani S, Ramadevi S, Lakshmi Durga P. Design, development and in vitro evaluation of gastro retentive alginate floating beads for ranitidine hydrochloride. J Curr Pharma Res 2013;5:377-81.
Patel R, Singh RS, Panchal RS, Stuti G, Lalit K. Formulation and optimization of floating matrix tablet of ranitidine hydrochloride. Int J Chem Pharm 2011;2:1-5.
Murthy NV, Kumar RS, Perumal P. Controlled release mucoadhesive microspheres of clarithromycin for the treatment of Helicobacter Pylori infection. Pharm Lett 2012;4:993-1004.
Shahbaziniaz M, Foroutan SM, Bolourchian N. Dissolution rate enhancement of clarithromycin using ternary ground mixtures: nanocrystal formation. Iran J Pharm Res 2013;12:587-98.
Gastroretentive delivery system of clarithromycin and proton pump inhibitor using different polymers for Helicobactor Pylori Infection. [Unpublished dissertation]. Delhi Institute of Pharmaceutical Sciences and Research (DIPSAR), University of Delhi, Pushp Vihar, Sector-3, New Delhi-110017, India; 2011. p. 109-10.
Aphale S, Shinde S, Dhat S, Bagul U, Saluja J. Development and evaluation of hollow microspheres of clarithromycin as a gastroretentive drug delivery system using Eudragit polymers. Int J Pharma Bio Sci 2011;2:344-58.