Formulation development and evaluation of taste-masked Moxifloxacin dispersible tablets for the treatment of pediatric tuberculosis
Abstract
Moxifloxacin (MOX) is a fluoroquinolone antibiotic, a second-line anti-TB drug widely used in the treatment of multidrug-resistant tuberculosis (MDR TB) and drug-susceptible TB. MOX have taste and smell issues with low patient compliance, especially in the pediatric population. MOX taste-masked dispersible tablets were developed by direct compression method using mannitol, aspartame as a sweetening agent and lemon flavor as a flavoring agent. The prepared granules were evaluated for flow properties and compressed tablets for hardness, friability, content uniformity, weight variation, DT and in-vitro drug release. Instrumental analysis like FTIR, DSC and XRD was also performed. The flow properties of the granules of batch F6 were found to be excellent based on the results obtained. The weight variation and content uniformity of the tablets was found to be excellent F6 due to the excellent flow properties of the granules. All of the tablets in the study disintegrated between 22 (F6) to 135 seconds (F1), meeting the official requirement (3 minute) for dispersible tablets. The optimized batch showed complete drug release within 10 minutes time period. The FTIR and DSC study found no incompatibility between the drug excipients. The MOX in the final formulation was present in crystalline form, as shown by XRD. The dispersible MOX tablets could be a better option for treating pediatric TB.
Keywords:
tuberculosis, moxifloxacin, dispersible tablets, taste mask, disintegrationDOI
https://doi.org/10.25004/IJPSDR.2023.150208References
Batista LA, Silva KJ, e Silva LM, de Moura YF, Zucchi FC. Tuberculosis: A granulomatous disease mediated by epigenetic factors. Tuberculosis. 2020; 123:101943.
Abel L, El-Baghdadi J, Bousfiha AA, Casanova JL, Schurr E. Human genetics of tuberculosis: a long and winding road. Philosophical Transactions of the Royal Society B: Biological Science. 2014;369(1645):20130428.
D’Attilio L, Santucci N, Bongiovanni B, Bay ML, Bottasso O. Tuberculosis, the disrupted immune-endocrine response and the potential thymic repercussion as a contributing factor to disease physiopathology. Frontiers in Endocrinology. 2018; 9:214.
Schaaf HS, Moll AP, Dheda K. Multidrug-and extensively drug resistant tuberculosis in Africa and South America: epidemiology, diagnosis and management in adults and children. Clinics in Chest Medicine. 2009;30(4):667-683.
Ernest TB, Elder DP, Martini LG, Roberts M, Ford JL. Developing paediatric medicines: identifying the needs and recognizing the challenges. Journal of Pharmacy and Pharmacology. 2007;59(8):1043-1055.
Nahirya-Ntege P, Cook A, Vhembo T, Opilo W, Namuddu R, Katuramu R, Tezikyabbiri J, Naidoo-James B, Gibb D, ARROW Trial Team. Young HIV-infected children and their adult caregivers prefer tablets to syrup antiretroviral medications in Africa. PLoS One. 2012;7(5):e36186.
Hannan PA, Khan JA, Khan A, Safiullah S. Oral dispersible system: A new approach in drug delivery system. Indian Journal of Pharmaceutical Sciences. 2016;78(1):2-7.
Kumar N, Pahuja S. Dispersible Tablets: An Overview. Journal of Medical Pharmaceutical and allied Sciences. 2019;8(3):2175-2191.
Baguley D, Lim E, Bevan A, Pallet A, Faust SN. Prescribing for children–taste and palatability affect adherence to antibiotics: a review. Archives of Disease in Childhood. 2012;97(3):293-297.
Zheng H, He W, Jiao W, Xia H, Sun L, Wang S, Xiao J, Ou X, Zhao Y, Shen A. Molecular characterization of multidrug-resistant tuberculosis against levofloxacin, moxifloxacin, bedaquiline, linezolid, clofazimine, and delamanid in southwest of China. BMC Infectious Diseases. 2021;21(1):1-6.
Nanjwade V K, Manv i F V, Nanjwade BK . Formulation and evaluation of dispersible tablets of lomefloxacin HCL. International Journal of Drug Development and Research. 2013;5(1):103-113
Gohel MC, Bansal G, Bhatt N. Formulation and evaluation of orodispersible taste masked tablets of famotidine. Pharma Bio World. 2005;3(5):75-80.
Khairnar G, Mokale V, Naik J. Formulation and development of nateglinide loaded sustained release ethyl cellulose microspheres by O/W solvent emulsification technique. Journal of Pharmaceutical Investigation. 2014;44(6):411-422.
Masaeli R, Kashi TS, Dinarvand R, Tahriri M, Rakhshan V, Esfandyari-Manesh M. Preparation, characterization and evaluation of drug release properties of simvastatin-loaded PLGA microspheres. Iranian Journal of Pharmaceutical Research. 2016;15(Suppl):205-211.
Chaudhari SP, Dave RH. To prepare and characterize microcrystalline cellulose granules using water and isopropyl alcohol as granulating agents and determine its end-point by thermal and rheological tools. Drug Development and Industrial Pharmacy. 2015;41(5):744-752.
Irigoiti Y, Yamul DK, Navarro AS. Co-crystallized sucrose with propolis extract as a food ingredient: Powder characterization and antioxidant stability. Food Science and Technology. 2021; 143:111164.
Ahmed S, Islam S, Ullah B, Biswas SK, Azad AS, Hossain S. A review article on pharmaceutical analysis of pharmaceutical industry according to pharmacopoeias. Oriental Journal of Chemistry. 2020;36(1):1-10.
Shah RB, Tawakkul MA, Khan MA. Comparative evaluation of flow for pharmaceutical powders and granules. Aaps Pharmscitech.2008;9(1):250-258.
Stirnimann T, Di Maiuta N, Gerard DE, Alles R, Huwyler J, Puchkov M. Functionalized calcium carbonate as a novel pharmaceutical excipient for the preparation of orally dispersible tablets. Pharmaceutical Research. 2013;30(7):1915-1925.
Rowe RC, Sheskey PJ, Weeler PJ, editors. Handbook of pharmaceutical excipients. 4th ed. London and Washington DC: The Pharmaceutical Press; 2003.
Setty CM, Prasad DV, Gupta VR, Sa B. Development of fast dispersible aceclofenac tablets: effect of functionality of superdisintegrants. Indian Journal of Pharmaceutical Sciences. 2008;70(2):180-185.
Chaulang GM, Patil KS, Ghodke DS, Yeole PG, Bhosale AV, Hardikar SR. Effect of some physical parameters and crospovidone on directly compressed frusemide tablets. Asian Journal of Pharmaceutics. 2008;2(4):235-240.
Published

