FORMULATION AND EVALUATION OF GASTRO RETENTIVE FLOATING TABLET OF AMLODIPINE BESYLATE USING NATURAL ORGANIC POLYMERS
DOI:
https://doi.org/10.22159/ijap.2022v14i4.44600Keywords:
Amlodipine besylate, Acacia gum, Xanthan gum, Floating tablets, Gastro-retentive tabletsAbstract
Objective: This study was designed to formulate and evaluate the gastro retentive floating tablets of Amlodipine besylate by using different proportions of four polymers, namely xanthan gum, gum acacia, carbopol 940, and HPMC K 100 M.
Methods: Nine different batches of the floating tablets were formulated by direct compression technique. The constant amount of gas generating agents, namely, sodium bicarbonate and citric acid, were used for the floating character. The powder blend was subjected to pre-compression parameters analysis and the prepared tablets were evaluated for post-compression parameters such as hardness, friability, drug content, weight variation, floating lag time, total floating time, and swelling index. In vitro dissolution study was carried out for 12 h as per the specification of Indian Pharmacopeia 2018.
Results: For the optimized batch (4th batch), all the physicochemical parameters like angle of repose (33.47), Carr’s index (17.46%), Hausner’s ratio (1.21), weight variation (221 mg), hardness (5.2 Kg/cm2), friability (0.1%), thickness (3.92 mm), dissolution (94.65% at 12 h), and drug content (92.5%) were within the acceptable limit. Furthermore, swelling index, floating lag time, and total floating time was reported to be 203.0%, 7.5 seconds,>12 h, respectively. Fourier Transform Infrared Spectroscopy analysis suggested that there is no drug excipients interaction.
Conclusion: Hence, this study suggested that gastro retentive floating tablets of Amlodipine besylate can be formulated to enhance gastric residence time and thereby improve its drug release characteristics.
Downloads
References
Shinkar DM, Aher PS, Kothawade PD, Maru AD. Formulation and in vitro evaluation of fast dissolving tablet of verapamil hydrochloride. Int J Pharm Pharm Sci. 2018;10(10):93-9. doi: 10.22159/ijpps.2018v10i10.28714.
Reddy PS, Bose PSC, Saritha D, Sruthi V. Formulation and evaluation of colon targeted matrix tablet using natural tree gums. Int J Pharm Pharm Sci. 2018;10(9):92-7. doi: 10.22159/ijpps.2018v10i9.27255.
Roy A, Arees R, Blr M. Formulation development of oral fast-dissolving films of Rupatadine fumarate. Asian J Pharm Clin Res. 2020;13(11):67-72.
Deshpande AA, Shah NH, Rhodes CT, Malick W. Development of a novel controlled-release system for gastric retention. Pharm Res. 1997;14(6):815-9. doi: 10.1023/a:1012171010492, PMID 9210203.
Klausner EA, Lavy E, Friedman M, Hoffman A. Expandable gastroretentive dosage forms. J Control Release. 2003;90(2):143-62. doi: 10.1016/s0168-3659(03)00203-7, PMID 12810298.
Dash S, Murthy PN, Nath L, Chowdhury P. Kinetic modeling on drug release from controlled drug delivery systems. Acta Pol Pharm. 2010;67(3):217-23. PMID 20524422.
Mehta M, Neeta, Pandey P, Mahajan S, Satija S. Gastro retentive drug delivery systems: an overview. Res J Pharm Technol. 2018;11(5):2157-60. doi: 10.5958/0974-360X.2018.00398.0.
Makwana A, Sameja K, Parekh H, Pandya Y. Advancements in controlled release gastroretentive drug delivery system: a review. J Drug Delivery Ther. 2012;2(3):12-21. doi: 10.22270/jddt.v2i3.164.
Singh BN, Kim KH. Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention. J Control Release. 2000;63(3):235-59. doi: 10.1016/s0168-3659(99) 00204-7, PMID 10601721.
Patel VF, Patel NM, Yeole PG. Studies on formulation and evaluation of ranitidine floating tablets. Indian J Pharm Sci. 2005;67(6):703-9.
Streubel A, Siepmann J, Bodmeier R. Gastroretentive drug delivery systems. Expert Opin Drug Deliv. 2006;3(2):217-33. doi: 10.1517/17425247.3.2.217, PMID 16506949.
Ma H, Azharuddin M, As R, Vu R, Sirisha Y. Surface response methodology for development and optimization of naproxen sustained release tablets. Asian J Pharm Clin Res. 2014;7(1):125-33.
Murdoch D, Heel RC, Amlodipine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in cardiovascular disease. Drugs. 1991;41(3):478-505. doi: 10.2165/00003495-199141030-00009, PMID 1711448.
Taylor AA, Shoheiber O. Adherence to antihypertensive therapy with fixed‐dose amlodipine besylate/benazepril HCl versus comparable component‐based therapy. Congest Heart Fail. 2003;9(6):324-32. doi: 10.1111/j.1527-5299.2003.03269.x, PMID 14688505.
Government of India. Indian Pharmacopoeia, controller of publications, Delhi; 2018. p. 11143-4.
C Shaikh, Sanap D, Bhusari DV, Jain S, Kochar PP, Sanchati VN. Formulation and evaluation of ibuprofen gastro-retentive floating tablets. Univ J Pharm Res. 2018;3(4):19-23. doi: 10.22270/ujpr.v3i4.178.
Hu L, Li L, Yang X, Liu W, Yang J, Jia Y. Floating matrix dosage form for dextromethorphan hydrobromide based on gas forming technique: in vitro and in vivo evaluation in healthy volunteers. Eur J Pharm Sci. 2011;42(1-2):99-105. doi: 10.1016/j.ejps.2010.10.010, PMID 21050887.
Kumar RS, Annu K, Latha BK, Mallika T. Design, optimization and evaluation of ibuprofen fast dissolving tablets employing starch phthalate-a novel superdisintegrant. Int J Curr Pharm Sci. 2019;11(5):47-53. doi: 10.22159/ijcpr.2019v11i5.35702.
Ichikawa M, Kato T, Kawahara M, Watanabe S, Kayano M. A new multiple-unit oral floating dosage system. II: In vivo evaluation of floating and sustained-release characteristics with p-aminobenzoic acid and isosorbide dinitrate as model drugs. J Pharm Sci. 1991;80(12):1153-6. doi: 10.1002/jps.2600801212, PMID 1815074.
Sharma S, Seth N, Gill NS. Formulation and evaluation of fast dissolving tablets of buspirone using coprocessed superdisintegrants. Int J Curr Pharm Sci. 2019;11(5):31-7. doi: 10.22159/ijcpr.2019v11i5.35698.
Pandey J, Khanal B, Bhandari J, Bashyal R, Pandey A, Mikrani AA. Physicochemical evaluation of diploknema butyracea seed extract and formulation of ketoconazole ointment by using the fat as a base. J Food Qual. 2021;2021:1-11. doi: 10.1155/2021/6612135.
Poudel A, Pandey J, Lee HK. Geographical discrimination in curcuminoids content of turmeric assessed by rapid UPLC-DAD validated analytical method. Molecules. 2019;24(9):1805. doi: 10.3390/molecules24091805, PMID 31083285.
Koirala S, Nepal P, Ghimire G, Basnet R, Rawat I, Dahal A. Formulation and evaluation of mucoadhesive buccal tablets of aceclofenac. Heliyon. 2021;7(3):e06439. doi: 10.1016/j.heliyon.2021.e06439, PMID 33786387.
Ramasamy T, Kandhasami UDS, Ruttala H, Shanmugam S. Formulation and evaluation of xanthan gum based aceclofenac tablets for colon targeted drug delivery. Braz J Pharm Sci. 2011;47(2):299-311. doi: 10.1590/S1984-82502011000200011.
Ichikawa M, Watanabe S, Miyake Y. A new multiple-unit oral floating dosage system. I: Preparation and in vitro evaluation of floating and sustained-release characteristics. J Pharm Sci. 1991;80(11):1062-6. doi: 10.1002/jps.2600801113, PMID 1815057.
Wen H, Park K, editors. Oral controlled release formulation design and drug delivery: theory to practice. John Wiley & Sons; 2011.
Pare A, Yadav SK, Patil UK. Formulation and evaluation of effervescent floating tablet of amlodipine besylate. Res J Pharm Technol. 2008;1(4):526-30.
Samiyathuneesa P, CP SN, Siva P. Formulation and evaluation of atorvastatin floating tablet. Int J Novel Trends Pharm Sci. 2017;7(5):130-8.
Strubing S, Metz H, Mader K. Characterization of poly (vinyl acetate) based floating matrix tablets. J Control Release. 2008;126(2):149-55. doi: 10.1016/j.jconrel.2007.11.013, PMID 18180069.
Singh S, Prajapati K, Pathak AK, Mishra A. Formulation and evaluation of floating tablet of captopril. Int J PharmTech Res. 2011;3(1):333-41.
Nanjwade BK, Veerendra K, Nanjwade SAA. Development and evaluation of gastroretentive floating tablets of glipizide based on effervescent technology. J Drug Metab Toxicol. 2012;3(3):1-5. doi: 10.4172/2157-7609.1000121.
Kumar BP, Kavitha P, Devi KJ. Formulation design and evaluation of mucoadhesive buccal tablets of nitroglycerin. Int J Pharm Pharm Sci. 2014;6(7):251-9.
Balamurugan M, Saravanan VS, Ganesh P, Senthil SP, Hemalatha PV, Pandya S. Development and in vitro evaluation of mucoadhesive buccal tablets of domperidone. Res J Pharm Technol. 2008;1(4):377-80.
Perioli L, Ambrogi V, Rubini D, Giovagnoli S, Ricci M, Blasi P. Novel mucoadhesive buccal formulation containing metronidazole for the treatment of periodontal disease. J Control Release. 2004;95(3):521-33. doi: 10.1016/ j.jconrel.2003.12.018, PMID 15023463.
Shakya R, Thapa P, Saha RN. In vitro and in vivo evaluation of gastroretentive floating drug delivery system of ofloxacin. Asian J Pharm Sci. 2013;8(3):191-8. doi: 10.1016/j.ajps.2013.07.025.
Qazi F, Shoaib MH, Yousuf RI, Qazi TM, Mehmood ZA, Hasan SM. Formulation development and evaluation of diltiazem HCl sustained release matrix tablets using HPMC K4M and K100M. Pak J Pharm Sci. 2013;26(4):653-63. PMID 23811439.
Padmavathy J, Saravanan D, Rajesh D. Formulation and evaluation of ofloxacin floating tablets using HPMC. Int J Pharm Pharml Sci. 2011;3(1):170-3.
Hussain MN, Al Masum MA, Akhter S, Sharmin F, Reza MS. Formulation and evaluation of gastro retentive floating tablets of simvastatin using hydrophilic rate retardant. Bangla Pharma J 2012;15(2):119-26. doi: 10.3329/bpj.v15i2.12575.
Shaha SH, Patel JK, Pundarikakshudu K, Patel NV. An overview of a gastro-retentive floating drug delivery system. Asian J Pharm Sci. 2009;4(1):65-80.
Streubel A, Siepmann J, Bodmeier R. Floating matrix tablets based on low density foam powder: effects of formulation and processing parameters on drug release. Eur J Pharm Sci. 2003;18(1):37-45. doi: 10.1016/s0928-0987(02)00223-3, PMID 12554071.
Published
How to Cite
Issue
Section
Copyright (c) 2022 SUSMA ACHARYA, JITENDRA PANDEY, HARI PRASAD JOSHI, GYANU PARAJULI, NARAYANI POUDEL, SRIJANA POUDEL, SHILA GURUNG
This work is licensed under a Creative Commons Attribution 4.0 International License.
