FORMULATION AND EVALUATION OF FLOATING TABLET OF ATENOLOL FOR THE TREATMENT OF HYPERTENSION
Main Article Content
Keywords
Direct Compression Method, Floating Tablets, HPMC, Atenolol, Dissolution, Gastro-Retentive
Abstract
The current study set out to develop a gastro-retentive atenolol floating tablet. Angina pectoris and hypertension are both treated with this beta-blocker (beta-adrenoreceptor antagonist). When used orally, it is only partially absorbed from the digestive system and only 50% of the medication is accessible; the other 25% is excreted unchanged in faeces. This problem results from insufficient absorption in the lower gastrointestinal system. To improve the oral bioavailability and therapeutic effectiveness of atenolol, the gastro-retentive floating drug delivery system (GFDDS) growth was deemed useful. The direct compression technique was used to make floating pills of atenolol (F1-F5). To reduce the floating delay, a polymer like HPMC was used together with gas-producing chemicals such citric acid and sodium bicarbonate. Evaluations were done on the blends, compressibility index, bulk density, Hausner's ratio, angle of repose and tapped density. Additionally evaluated were the tablets' hardness, diameter, weight variation, homogeneity of the drug content, friability, floating and buoyancy lag times, impact of hardness, in vitro swelling behavior, and in vitro release of drug. The USP dissolving test apparatus-II was utilised to rotate 900 cc of a hydrochloric acid buffer with a pH of 1.2 at 50 rpm while maintaining a 37.5°C temperature for the in-vitro release of drug examination
References
2. Fukuda M, Peppas NA, McGinity JW. Floating hotmelt extruded tablets for gastroretentive controlled drug release system. J Control Release. 2006;115(2):121-129.
3. Khan F, Ibn Razzak SM, Khan ZR, Azad MA, Chowdhury JA, Reza S. Theophylline loaded gastroretentive floating tablets based on hydrophilic polymers: preparation and in vitro evaluation. Pak J Pharm Sci. 2009;22(2):155-161.
4. Tamizharasi S, Rathi V, Rathi JC. Floating drug delivery system. Syst Rev Pharm. 2011;2(1):19-29.
5. Wanjari D. A review on floating drug delivery system. Int J Bioassays. 2014;3(8):10.21746.
6. Soppimath, K.S,; Kulkarni, A.R,; Rudzinski, W.E,; Aminabhavi, T.M. Microspheres as floating drug delivery system to increase the gastric residence of drugs. Drug Metab Rev., Vol. 33: 2001; pg 149-160.
7. Garg, R.; Gupta, G.D. Progress in controlled gastroretentive delivery systems. Trop. J. Pharm. Res., Vol. 7(3): 2008; pg 1055-66.
8. Anlar S, Capan Y and Hincal AA. Physico-chemical and bioadhesive properties of polyacrylic acid polymers. Pharmazie 1993; 48(4): 285-287.
9. Fox CS. Cardiovascular disease risk factors, Type 2 diabetes mellitus, and the Framingham heart study. Trends Cardiovasc Med 2010;20:90-95.
10. Lavie CJ, Milani RV, Ventura HO. Obesity and cardiovascular disease risk factor, paradox, and impact of weight loss. J Am Coll Cardiol 2009;53:1925-32.
11. Department of Health Statistics and Informatics. Causes of death 2008: data sources and methods. Geneva: World Health Organization; 2008.
12. Lim SS, Vos T, Flaxman AD, Danaei G, Shibuya K, Rohani HA, et al. A comparative risk assessment of burden of disease and injury attributable to 67 risk factors and risk factor clusters in 21 regions, 1990-2010: A systematic analysis for the global burden of disease study 2010. Lancet 2012;380:2224-60.
13. Martindale. The complete drug reference. 33 rd ed. London: Pharmaceutical Press 2002:841.
14. Lachman, L.; Lieberman, H.A.; Lachman, kaling, J.L. The theory and practice of industrial pharmacy, 3rd ed., Varghese Publishing House, Bombay, 1987; pg 67-71.
15. Lee JW, Park JH, Robinson JR. Bioadhesive- based dosage forms: the next generation. J Pharm Sci.2000; 89: 850-866.
16. M.Purushothaman, C.Saravanan. Formulation and Evaluation of Metaprolol Succinate Floating Tablets Using Peanut Husk Powder as Natural Polymer. International Journal of Chem Tech Research.2017;10(10):169-77.
17. Lachman L, Liberman HA, Kang JL. The theory and practice of industrial pharmacy. 3rd ed. Mumbai: Varghese Publishing house; 1987.p. 296-303
18. Sarfaraz Md, LingaReddy B, Doddayya H, Rajagopal UH., Design and in-Vitro Evaluation of Gastro Retentive Floating Tablets of Repaglinide. International journal of drug delivery and research, 5(3):322-332,(2013)
19. Patil H, Prashar B, Chandel A, Thakur V., Formulation and Evaluation of Floating Tablet of Pantoprazole Sodium Sequihydrate. Journal of Pharmacy Research, 5(9):4659- 4662,(2012)
20. Reddy VS, Badarinath AV, Prakash KG., Formulation and evaluation of floating tablets of ciprofloxacin hydrochloride. Asian Journal of Pharmaceutics , 12(2): 106-113,(2018)
21. Pierce MW., Transdermal delivery of sumatriptan for the treatment of acute migraine. The Journal of the American Society for Experimental Neuro Therapeutics, 7: 159- 163,(2010)
22. Srivastava, A. K.; Wadhwa, S.; Ridhurkar, D.; Mishra, B. Oral sustained delivery of atenolol from floating matrix tablets formulation and in-vitro evaluation. Drug Dev. Ind. Pharm., 2005; Vol. 31: pg 367–374.
23. Tiwari SB, Murthy TK, Pai MR, Mehta PR, Chowdary PB. Controlled release formulation of tramadol hydrochloride using hydrophilic and hydrophobic matrix system. AAPS PharmSciTech 2003;4:E31.
24. ICH guidelines for accelerated stability studies. Available from:
http//www.ikev.org/haber/stabilite/kitap/29%201.1%20Stability%20 Workshop%20ICH%20Q1AR2%20C.pdf. [Last accessed on 2011 Oct 15]