Formulation and in vitro Evaluation of Fast Dissolving Tablets of Febuxostat Using Co-Processed Excipients

Author(s): Manpreet Kaur, Amit Mittal, Monica Gulati, Deepika Sharma, Rajesh Kumar*

Journal Name: Recent Patents on Drug Delivery & Formulation
Continued as Recent Advances in Drug Delivery and Formulation

Volume 14 , Issue 1 , 2020

Graphical Abstract:


Abstract:

Background: Febuxostat is a novel, orally-administered, powerful, non-purine, xanthine oxidase inhibitor used for treating gout and ceaseless tophaceous gout. The drug exhibits low bioavailability (about 49%) which is ascribed to its dissolution rate-limited absorption.

Objective: The current work is aimed to provide a novel strategy to improve the dissolution profile and thus, the bioavailability of Febuxostat.

Methods: Formulation of Fast Dissolving Tablets (FDT) is anticipated to provide immediate release of the drug, which in turn, will improve its dissolution profile to provide the initial surge in plasma concentration required in an acute gout attack. Incorporation of co-processed excipients in a tablet is known to improve the compressibility and disintegration characteristics of the tablets, which, in turn, result in enhanced in vitro drug release and improved bioavailability. A combination of crospovidone (it rapidly wicks saliva into the tablet to create the volume development and hydrostatic weight important to give quick disintegration) and microcrystalline cellulose (a highly compressible ingredient with good wicking and absorbing capacity) was, therefore, used as co-processed excipients.

Results: The tablets were prepared by direct compression technique with the application of a 32 randomized full factorial design. The prepared tablets were able to release more than 80% of the drug within 10 minutes of the start of dissolution testing and were able to show a better drug release profile in comparison to available marketed formulation.

Conclusion: So, it can be concluded that the developed fast release formulation was found to exhibit convincing in vitro results and may prove a boon in the treatment of acute gout attack after establishing in vivo potential.

Keywords: Bioavailability, co-processed excipients, crospovidone, fast dissolving tablets, febuxostat, gout, microcrystalline cellulose.

[1]
Kumari MS, Prasanthi CH, Bhargavi CHS, Kumari MP, Ushasri S. Reassessment of novel co-processed multifunctional excipient. Int Res J Pharm App Sci 2013; 3: 122-8.
[2]
Shangraw RF. Emerging trends in the use of pharmaceutical excipients. Pharm Technol 1997; 21: 36-42.
[3]
The IPEC excipient information package (EIP) template and user guide . 2009.www.ipec-europe.org/UPLOADS/Excipients_Insight_nov09_final(1).
[4]
Bardin T, Richette P. Definition of hyperuricemia and gouty conditions. Curr Opin Rheumatol 2014; 26(2): 186-91.
[http://dx.doi.org/10.1097/BOR.0000000000000028] [PMID: 24419750]
[5]
Wahab Al-Allaf A. Gout: evidence-based update with new therapeutic strategies. Sudan Med J 2012; 48: 165-75.
[6]
Choi HK, Mount DB, Reginato AM. Pathogenesis of gout. Ann Intern Med 2005; 143(7): 499-516.
[http://dx.doi.org/10.7326/0003-4819-143-7-200510040-00009] [PMID: 16204163]
[7]
Yin YF, Guo Y, Song WD, et al. Improving solubility and oral bioavailability of febuxostat by polymer-coated nanomatrix. AAPS PharmSciTech 2018; 19(2): 934-40.
[http://dx.doi.org/10.1208/s12249-017-0905-z] [PMID: 29079988]
[8]
Yamanaka H, Tamaki S, Ide Y, et al. Stepwise dose increase of febuxostat is comparable with colchicine prophylaxis for the prevention of gout flares during the initial phase of urate-lowering therapy: results from FORTUNE-1, a prospective, multicentre randomised study. Ann Rheum Dis 2018; 77(2): 270-6.
[http://dx.doi.org/10.1136/annrheumdis-2017-211574] [PMID: 29102957]
[9]
Tang J, Bao J, Shi X, Sheng X, Su W. Preparation, optimisation, and in vitro-in vivo evaluation of febuxostat ternary solid dispersion. J Microencapsul 2018; 35(5): 454-66.
[http://dx.doi.org/10.1080/02652048.2018.1526339] [PMID: 30229692]
[10]
Lide DR. CRC Handbook of Chemistry and Physics. 85th ed CRC Press: Internet Version. 2005.
[11]
Sowjanya G, Devi T, Sri VV, Pratyusha V, Venkata LN, Seshagiri RJ. Development and validation of UV spectroscopic methods for simultaneous estimation of ciprofloxacin and tinidazole in tablet formulation. Int Curr Pharm J 2012; 1: 317-21.
[http://dx.doi.org/10.3329/icpj.v1i10.11849]
[12]
Eraga SO, Arhewoh MI, Uhumwangho MU, Iwuagwu MA. Characterisation of a novel, multifunctional, co-processed excipient and its effect on release profile of paracetamol from tablets prepared by direct compression. Asian Pac J Trop Biomed 2015; 5: 768-72.
[http://dx.doi.org/10.1016/j.apjtb.2015.07.008]
[13]
Patel S, Patel M. Development of directly compressible co-processed excipient for dispersible tablets using 32 full factorial design. Int J Pharm Pharm Sci 2009; 1: 125-48.
[14]
Madan JR, Dagade RH, Awasthi R, Dua K. Formulation and solid state characterization of carboxylic acid-based co-crystals of tinidazole: An approach to enhance solubility. Polim Med 2018; 48(2): 99-104.
[http://dx.doi.org/10.17219/pim/105609] [PMID: 31033260]
[15]
Elkhodairy KA, Hassan MA, Afifi SA. Formulation and optimization of orodispersible tablets of flutamide. Saudi Pharm J 2014; 22(1): 53-61.
[http://dx.doi.org/10.1016/j.jsps.2013.01.009] [PMID: 24493974]
[16]
Rane DR, Gulve HN, Patil VV, Thakare VM, Patil VR. Formulation and evaluation of fast dissolving tablet of albendazole. Int Curr Pharm J 2012; 1: 311-6.
[http://dx.doi.org/10.3329/icpj.v1i10.11848]
[17]
Banker GS, Anderson NR. In The Theory and Practice of Industrial Pharmacy. Lachman L, Lieberman HA, Kanig JL. (Eds).Varghese publishing house, Mumbai. 1990; pp. 296-302..
[18]
The Unit States Pharmacopoeial Convention. United States of Pharmacopeia-National Formulary. USP 30- NF 25 2007. Rockville, MD, USA, 2007..
[19]
Banker GS, Anderson NR. In: The Theory and Practice of Industrial Pharmacy. Lachman L, Lieberman HA, Kanig JL. (Eds). Varghese publishing house, Mumbai. 1987; 293-9.
[20]
Thahera PD, Latha AK, Shailaja T, Nyamathulla S, Uhumwangho MU. Formulation and evaluation of Norfloxacin gastro retentive drug delivery systems using natural polymers. Int Curr Pharm J 2012; 1: 155-64.
[http://dx.doi.org/10.3329/icpj.v1i7.10809]
[21]
Khan KA. The concept of dissolution efficiency. J Pharm Pharmacol 1975; 27(1): 48-9.
[http://dx.doi.org/10.1111/j.2042-7158.1975.tb09378.x] [PMID: 235616]
[22]
Chaudhari PD, Chaudhari S, Kolhe SR, Dave KV, More DM. Formulation and evaluation of fast dissolving tablets of famotidine. Indian Drugs 2005; 42: 641-9.
[23]
Perge L, Robitzer M, Guillemot C, Devoisselle JM, Quignard F, Legrand P. New solid lipid microparticles for controlled ibuprofen release: formulation and characterization study. Int J Pharm 2012; 422(1-2): 59-67.
[http://dx.doi.org/10.1016/j.ijpharm.2011.10.027] [PMID: 22027394]
[24]
Pawar PG, Darekar AB, Saudagar RB. Formulation development and evaluation of febuxostat loaded microsponges. Int J Res Advent Technol 2019; 7: 523-33.
[http://dx.doi.org/10.32622/ijrat.752019326]
[25]
Rangaraj N, Shah S, Maruthi AJ, et al. Quality by design approach for the development of self-emulsifying systems for oral delivery of febuxostat: Pharmacokinetic and pharmacodynamic evaluation. AAPS PharmSciTech 2019; 20(7): 267.
[http://dx.doi.org/10.1208/s12249-019-1476-y] [PMID: 31346822]
[26]
Kini A, Patel SB. Phase behavior, intermolecular interaction, and solid state characterization of amorphous solid dispersion of Febuxostat. Pharm Dev Technol 2017; 22(1): 45-57.
[http://dx.doi.org/10.3109/10837450.2016.1138130] [PMID: 26853838]
[27]
Lokesh P, Kunchu K, Tamizh T. Fast disintegrating tablets: an overview of formulation, technology and evaluation. Res J Pharm Biol Chem Sci 2011; 2: 598-601.
[28]
Gouda R, Baishya H, Qing Z. Application of mathematical models in drug release kinetics of carbidopa and levodopa ER tablets. J Dev Drugs 2017; 6: 1-8.


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Article Details

VOLUME: 14
ISSUE: 1
Year: 2020
Published on: 13 October, 2020
Page: [48 - 62]
Pages: 15
DOI: 10.2174/1872211314666191224121044

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