Generic placeholder image

Recent Advances in Drug Delivery and Formulation

Author(s): Dipika Chavda*, Deepika Joshi, Vaishali Thakkar and Tejal Gandhi

DOI: 10.2174/2667387817666221116100127

DownloadDownload PDF Flyer Cite As
Fabrication and In Vitro Evaluation of Febuxostat Tablet for Obtaining Biphasic Drug Release Profile

Page: [317 - 327] Pages: 11

  • * (Excluding Mailing and Handling)

Abstract

Aim and Objective: The primary aim of the present investigation was to adopt the concept of quality by design (QbD) for developing Febuxostat matrix tablets containing a novel combination of polyethylene oxide (PEO), pre-gelatinized starch (PGS) and lactose for obtaining biphasic drug release.

Experimental: Febuxostat-containing matrix tablets were prepared by direct compression using 32 full factorial designs. The tablets were prepared with varying amounts of PEO WSR 301 to PGS and lactose to obtain the desired release pattern. The chosen responses were cumulative % drug released at 1, 6 and 12 hours. The evaluation of tablets was done for pre and post-compressional parameters. Compared with the marketed tablet, the optimized formulations were selected based on in vitro drug release. Dose dumping was checked in the dissolution medium containing up to 40% alcohol.

Results and Discussion: The results of the dissolution study indicated that the batch containing a 1:1 ratio of PEO WSR 301 and PGS (15 mg each) and 20 mg of Lactose showed fast initial drug release to imitate the pharmacological action followed by sustained drug release effect. The use of Lactose facilitated immediate drug release, while PEO WSR 301 and PGS exhibited the opposite effect on cumulative drug release. The results of the 32 Factorial design revealed that the concentration of Lactose is a critical parameter. Dose dumping was not observed in the alcoholic dissolution medium. Kinetic equations were fitted to the dissolution data after 1 hour of the dissolution study.

Conclusion: The type (soluble or swellable) and the concentration of excipients (low or high) dictate the tablets' drug release. The study's outcome revealed that the most critical material attribute is the amount of lactose. The novel combination of PEO, PGS and lactose can bypass existing patents and give more industrial applicability.

Graphical Abstract

[1]
Ragab G, Elshahaly M, Bardin T. Gout: An old disease in new perspective – A review. J Adv Res 2017; 8(5): 495-511.
[http://dx.doi.org/10.1016/j.jare.2017.04.008] [PMID: 28748116]
[2]
Li C, Wang J, Wang Y, et al. Recent progress in drug delivery. Acta Pharm Sin B 2019; 9(6): 1145-62.
[http://dx.doi.org/10.1016/j.apsb.2019.08.003] [PMID: 31867161]
[3]
Hu M, Tomlinson B. Febuxostat in the management of hyperuricemia and chronic gout: A review. Ther Clin Risk Manag 2008; 4(6): 1209-20.
[PMID: 19337428]
[4]
Bardin T, Richette P. The role of Febuxostat in gout. Curr Opin Rheumatol 2019; 31(2): 152-8.
[5]
Ghang B, Ahn SM, Kim J, Kim Y-G, Lee C-K, Yoo B. Discontinuing Febuxostat might cause more deaths than continuing febuxostat: The untold story from the CARES trial. Rheumatology (Oxford) 2020; 59(6): 1439-40.
[6]
Liu C, Chang W, Lee C, Shau W. Nutrition, Metabolism & Cardiovascular Diseases The net clinical bene fi ts of febuxostat versus allopurinol in patients with gout or asymptomatic hyperuricemiae. A systematic review and meta-analysis. Nutr Metab Cardiovasc Dis 2019; 29(10): 1011-22.
[http://dx.doi.org/10.1016/j.numecd.2019.06.016] [PMID: 31378626]
[7]
Kim HS, Yun YH, Shim WG, Yoon SD. Preparation and evaluation of functional allopurinol imprinted starch based biomaterials for transdermal drug delivery. Int J Biol Macromol 2021; 175: 217-28.
[http://dx.doi.org/10.1016/j.ijbiomac.2021.02.004] [PMID: 33548320]
[8]
Grangeia HB, Silva C, Simões SP, Reis MS. Quality by Design in Pharmaceutical Manufacturing: A systematic review of current status, challenges and future perspectives. Eur J Pharm Biopharm 2020; 147: 19-37.
[http://dx.doi.org/10.1016/j.ejpb.2019.12.007] [PMID: 31862299]
[9]
Kumar G, Jain V, Shende S, Jain P. Formulation and evaluation of bilayer tablets of clarithromycin and omeprazole against Helicobacter pylori infection. Pharm Innovat J 2019; 8(1): 407-12.
[10]
Vishal M, Anuj K, Pankaj P, et al. Formulation development and evaluation of Bilayer tablets of Lornoxicam. IJDDR 2012; 4(2): 173-9.http://www.ijddr.in
[11]
Maddiboyina B, Hanumanaik M, Nakkala RK, et al. Formulation and evaluation of gastro-retentive floating bilayer tablet for the treatment of hypertension. Heliyon 2020; 6(11): e05459.
[http://dx.doi.org/10.1016/j.heliyon.2020.e05459] [PMID: 33241144]
[12]
Sharma V. Formulation, optimization and evaluation of bilayer tablet of antihypertensive drug. J Drug Deliv The 2019; 9(4): 704-8.
[13]
Bermejo M, Sanchez-dengra B, Gonzalez-alvarez M. Oral controlled release dosage forms: dissolution versus diffusion. Expert Opin Drug Deliv 2020; 2020: 1750593.
[http://dx.doi.org/10.1080/17425247.2020.1750593] [PMID: 32248713]
[14]
Mishra V, Thakur S, Patil A, Shukla A. Quality by design (QbD) approaches in current pharmaceutical set-up. Expert Opin Drug Deliv 2018; 15(8): 737-58.
[http://dx.doi.org/10.1080/17425247.2018.1504768] [PMID: 30044646]
[15]
Mishra A. Preparation and evaluation of bilayer tablet for the treatment of hypertension. Nat Volatiles Essent Oils 2021; 8(5): 9098-115.
[16]
Usta DY, Demİrtaş Ö. Evaluation of in vitro dissolution characteristics of Flurbiprofen, a BCS class IIA drug. FABAD J Pharm Sci 2018; 43: 117-24.
[17]
Ubhe T, Subscription C. A brief overview on tablet and it’s types. J Adv Pharmacol 2020; 1(1): 21-31.
[18]
Samaha D, Shehayeb R, Kyriacos S. Modeling and comparison of dissolution profiles of diltiazem modified-release formulations. Dissolut Technol 2009; 16(2): 41-6.
[http://dx.doi.org/10.14227/DT160209P41]
[19]
Badawy SIF, Narang AS, Lamarche KR. Mechanistic basis for the effects of process parameters on quality attributes in high shear wet granulation. In: Handbook of Pharmaceutical Wet Granulation. Elsevier Inc. 2019; pp. 89-118.
[http://dx.doi.org/10.1016/B978-0-12-810460-6.00026-9]
[20]
Paarakh MP, Jose PANI, Setty CM, Peter GV. Release kinetics – concepts and applications. Int J Pharm Res Technol 2018; 8: 12-20.
[21]
Koradia H, Chaudhari KACSC. Formulation of unidirectional buccal tablet of Mirtazapine: An in vitro and ex vivo evaluation. J Drug Deliv Sci Technol 2018; 43: 233-42.
[http://dx.doi.org/10.1016/j.jddst.2017.10.012]
[22]
Bhagwat GB, Hands H. To evaluate accelerated stability study of a polyherbal formulation-turmocin to evaluate accelerated stability study of a polyherbal formulation-turmocin plus tablet. Int J Pharm Res Scholar 2021; 13(3): 146.
[23]
Gaikwad SS, Kshirsagar SJ. Review on Tablet in Tablet techniques. Beni Suef Univ J Basic Appl Sci 2020; 9(1): 7-14.
[24]
International Council for Harmonisation of Technical Requirements for Pharmaceuticals for Human Use. ICH Harmonised Guideline. Addendum to E11: Clinical Investigation of Medicinal Products in the Pediatric Population E11(R1) Ich. 2017; p. 18.
[25]
Kedia K, Wairkar S PT CR. Powder Technol [Internet]. 2018; 344: 665-72.
[http://dx.doi.org/10.1016/j.powtec.2018.12.068]
[26]
Lettre DP. A study over effects of process parameters on quality attributes of a table by applying QBD. Pharmacia 2010; 2(2): 208-20. Available from: http://scholarsresearchlibrary.com/ABR-vol1-iss2/ABR-2010-1-2-87-90.pdf
[27]
U.S. Food and Drug Administration (FDA). Quality by design for ANDAs: An example for immediate-release dosage forms. 2012. Available from: https://www.fda.gov/downloads/Drugs/.../UCM 304305.pdf