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Formulation and evaluation of different floating tablets containing metronidazole to target stomach.
Curr Drug Deliv. 2015; 12(4):425-43.CD

Abstract

The purpose of this study is to formulate and develop tablets dosage form containing Metronidazole which has swelling and floating properties as a gastroretentive controlled-release drug delivery system to improve drug bioavailability. Fifteen different formulations of effervescence-forming floating systems were designed using HPMC K15M, xanthan gum, co-povidone, Eudragit® RL PO, pluronic® F-127 and/or polypropylene foam powder as swelling agents and sodium bicarbonate with/ without citric acid as gas-forming agents at different compositions. Six out of these 15 formulations which have satisfactory tablet floating behaviour were further studied with the incorporation of Metronidazole. The tablets were evaluated based on tablet physicochemical properties, floating behaviour, swelling ability and drug dissolution studies which were carried out using 0.1M HCl at 37°C for 8 hours. Furthermore, evaluation of the powder mixtures using Fourier transform infrared (FT-IR) spectroscopy, differential scanning calorimetry (DSC) and scanning electron microscope (SEM) were investigated. Most of the tablets show good physicochemical properties except for F11 which contains pluronic® F-127 as its release-retarding matrix-forming polymer. Other formulations show high swelling capacity, ability to float for at least 8 hours in vitro and have sustained drug release characteristics. Data obtained indicated that F3 which contains HPMC (12.5%w/w), xanthan gum (25%w/w), co-povidone (12.5%w/w) and sodium bicarbonate (31.7%w/w) is a suitable formulation with short floating lag time, good floating behaviour and sustained drug release for at least 8 hours in vitro with a zero order kinetic. Combinations of HPMC K15M and xanthan gum as swelling agents show synergistic effect in retarding drug release and are suitable in providing the most sustained drug release system.

Authors+Show Affiliations

Loh ZC
No affiliation info available
Elkordy AA
Faculty of Applied Sciences, School of Pharmacy, Health and Well-being, University of Sunderland, Sunderland, SR1 3SD, UK. amal.elkordy@sunderland.ac.uk.

MeSH

Administration, OralAnti-Infective AgentsCalorimetry, Differential ScanningChemistry, PharmaceuticalDelayed-Action PreparationsDrug CarriersExcipientsGastric AbsorptionGastric MucosaHumansKineticsMetronidazoleMicroscopy, Electron, ScanningPowdersRheologySolubilitySpectroscopy, Fourier Transform InfraredTabletsTechnology, Pharmaceutical

Pub Type(s)

Evaluation Study
Journal Article

Language

eng

PubMed ID

25924732

Citation

Loh, Zhiao C., and Amal A. Elkordy. "Formulation and Evaluation of Different Floating Tablets Containing Metronidazole to Target Stomach." Current Drug Delivery, vol. 12, no. 4, 2015, pp. 425-43.
Loh ZC, Elkordy AA. Formulation and evaluation of different floating tablets containing metronidazole to target stomach. Curr Drug Deliv. 2015;12(4):425-43.
Loh, Z. C., & Elkordy, A. A. (2015). Formulation and evaluation of different floating tablets containing metronidazole to target stomach. Current Drug Delivery, 12(4), 425-43.
Loh ZC, Elkordy AA. Formulation and Evaluation of Different Floating Tablets Containing Metronidazole to Target Stomach. Curr Drug Deliv. 2015;12(4):425-43. PubMed PMID: 25924732.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Formulation and evaluation of different floating tablets containing metronidazole to target stomach. AU - Loh,Zhiao C, AU - Elkordy,Amal A, PY - 2015/01/12/received PY - 2015/03/28/revised PY - 2015/04/20/accepted PY - 2015/5/1/entrez PY - 2015/5/1/pubmed PY - 2016/5/4/medline SP - 425 EP - 43 JF - Current drug delivery JO - Curr Drug Deliv VL - 12 IS - 4 N2 - The purpose of this study is to formulate and develop tablets dosage form containing Metronidazole which has swelling and floating properties as a gastroretentive controlled-release drug delivery system to improve drug bioavailability. Fifteen different formulations of effervescence-forming floating systems were designed using HPMC K15M, xanthan gum, co-povidone, Eudragit® RL PO, pluronic® F-127 and/or polypropylene foam powder as swelling agents and sodium bicarbonate with/ without citric acid as gas-forming agents at different compositions. Six out of these 15 formulations which have satisfactory tablet floating behaviour were further studied with the incorporation of Metronidazole. The tablets were evaluated based on tablet physicochemical properties, floating behaviour, swelling ability and drug dissolution studies which were carried out using 0.1M HCl at 37°C for 8 hours. Furthermore, evaluation of the powder mixtures using Fourier transform infrared (FT-IR) spectroscopy, differential scanning calorimetry (DSC) and scanning electron microscope (SEM) were investigated. Most of the tablets show good physicochemical properties except for F11 which contains pluronic® F-127 as its release-retarding matrix-forming polymer. Other formulations show high swelling capacity, ability to float for at least 8 hours in vitro and have sustained drug release characteristics. Data obtained indicated that F3 which contains HPMC (12.5%w/w), xanthan gum (25%w/w), co-povidone (12.5%w/w) and sodium bicarbonate (31.7%w/w) is a suitable formulation with short floating lag time, good floating behaviour and sustained drug release for at least 8 hours in vitro with a zero order kinetic. Combinations of HPMC K15M and xanthan gum as swelling agents show synergistic effect in retarding drug release and are suitable in providing the most sustained drug release system. SN - 1875-5704 UR - https://www.unboundmedicine.com/medline/citation/25924732/Formulation_and_evaluation_of_different_floating_tablets_containing_metronidazole_to_target_stomach_ DB - PRIME DP - Unbound Medicine ER -