Formulation and Evaluation of Extended Release Gastroretentive Tablets of Metroprolol Succinate
Abstract
This study aimed to produce a gastroretentive floating tablet of Metoprolol succinate and examine the effects of release retardant on in vitro drug release. Metoprolol succinate is a β1 selective antagonist used as an Anti-hypertensive, Antiarrhythmic, and Anti Angina. Metoprolol succinate has 48% oral bioavailability due to limited absorption from the lower gastrointestinal tract. The Metoprolol succinate floating tablets were designed to increase stomach retention, prolong drug release, and enhance drug bioavailability. To shorten the floating lag time, hydrophilic polymers like Hydroxypropyl methyl cellulose (HPMC K4M, K15M, and K100M), polyethylene oxide (PEO 303), and sodium bicarbonate as a gas-producing agent were incorporated into the formulation of the floating tablets. Different batches of Metoprolol succinate floating tablets were prepared by direct compression. All the formulations were evaluated for various quality control tests, such as weight variation, hardness, friability, swelling index, floating lag time, and total floating time. As a dissolution medium, 0.1 N HCl was used to conduct an in vitro release investigation on the tablets. The present study demonstrates the potential of the sustained-release floating tablets of Metoprolol succinate as an alternative to conventional formulations.
Keywords: Bioavailability, Floating tablet, antihypertensive drugs, extended release, Metoprolol succinate, Hydroxypropyl methyl cellulose.
Keywords:
Bioavailability, Floating tablet, antihypertensive drugs, extended release, Metoprolol succinate, Hydroxypropyl methyl celluloseDOI
https://doi.org/10.22270/jddt.v12i5-S.5653References
Naeem MA, Mahmood A, Khan SA, Shahiq Z, Development and evaluation of controlled release bilayer tablets containing microencapsulated tramadol and acetaminophen, Trop J Pharm Res, 2010; 9(4):347-54. https://doi.org/10.4314/tjpr.v9i4.58926
Patra CN, Kumar AB, Pandit HK, Singh SP, Devi MV, Design and evaluation of sustained release bilayer tablets of Propranolol hydrochloride, Acta Pharm, 2007; 57: 479-489. https://doi.org/10.2478/v10007-007-0038-0
Rosa M, Zia H, Rhodes T, Dosing and testing in vitro of a bioadhesive and floating drug delivery system for oral application, Int J Pharm, 1994; 105(1):65-70. https://doi.org/10.1016/0378-5173(94)90236-4
Alexander S, Juergen S, Gastroretentive drug delivery systems, Expert Opin Drug Deliv, 2006; 3:217-224. https://doi.org/10.1517/17425247.3.2.217
Deshpande RD, Gowda DV, Mahammed M, Maramwar DN, Bi-Layer Tablets-An Emerging Trend: A Review, Int J Pharm Sci Res, 2011; 2(10):2534-2544.
Sampath KP, Bowmik D, Chiranjib, Chandira M, Tripathi KK, Innovations in sustained release drug delivery system and its market opportunities, J Chem Pharm Res, 2010; 2(1):349- 360.
Parashar AK, Kakde D, Chadhar V, Devaliya R, Shrivastav V, Jain UK, A review on solid lipid nanoparticles (SLN) for controlled and targeted delivery of medicinal agents. Curr Res Pharm Sci, 2011; 1(2):37-47.
Bourne DW, Pharmacokinetics. in: Modern pharmaceutics, 4th ed. Banker GS, Rhodes CT, Eds., Marcel Dekker Inc, New York; 2002.
Rathore R, Gupta AK, Parashar AK, Formulation and Evaluation of fast dissolving films of Granisetron Hydrochloride, J Drug Delivery and Therapeutics, 2019; 9(2-A):36-38.
Kulkarni M, Vishwanathrao K, Sakarkar D, Development and validation of spectrophotometric method for determination of metoprolol succinate, International Journal of ChemTech Research, 2009; 4(4):184-189.
Chidambaram M, Krishnasamy K, Drug-Drug/Drug-Excipient Compatibility Studies on Curcumin using Non-Thermal Methods, Adv Pharm Bull, 2014; 4(3):309-12. https://doi.org/10.2174/2210303103999131211110708
Ahmed SI, Mangamoori LN, Rao YM, Formulation and characterization of matrix and triple-layer matrix tablets for oral controlled drug delivery, Int J Pharm Pharm Sci, 2010; 2(3):137-43.
Jenita JJL, Vijaya K, Suma R, Bincy R, Ayesha S, Formulation and evaluation of compression coated tablets of mezalazine for colon delivery, Int J PharmTech Res, 2010; 2 (1):535-541.
Chithaluru K, Tadikonda RR, Formulation and Evaluation of Microbially triggered compression coated tablets of Ketorolac Tromethiamine, Der Pharmacia Lettre, 2011; 3(4):29-39.
Zimmer L, Kasperek R, Poleszak E, Modern polymers in matrix tablets technology, Polim Med, 2014; 44:189-96.
Maderuelo C, Zarzuelo A, Lanao JM, Critical factors in the release of drugs from sustained release hydrophilic matrices, J Control Release, 2011; 154(1):2-19. https://doi.org/10.1016/j.jconrel.2011.04.002
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