FORMULATION AND EVALUATION OF FEBUXOSTAT FAST DISSOLVING TABLETS USING ENTADA SCANDENS SEED STARCH AND POLOXAMER-188 AS SUPERDISINTEGRANTS

  • SANDEEP DOPPALAPUDI Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chandramoulipuram, Chowdavaram, Guntur, Andhra Pradesh, India 522019
  • VIDYADHARA SURYADEVARA Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chandramoulipuram, Chowdavaram, Guntur, Andhra Pradesh, India 522019,
  • CHIRUDEEP JUJALA Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chandramoulipuram, Chowdavaram, Guntur, Andhra Pradesh, India 522019,

Abstract

Objective: The present study focused on solubility enhancement of the Biopharmaceutical Classification System (BCS) Class-II drug, Febuxostat using various super disintegrants.


Methods: Starches were extracted from Entada scandens seed powder by alkali method i.e., sodium hydroxide at 0.1%, 0.25% and 0.5% concentrations and water. Starches were evaluated for various phytochemical and physicochemical tests. Solid dispersions of Febuxostat were prepared by fusion method using poloxamer-188 alone and by mixing poloxamer-188 with Entada scandens seed starch. Various physical parameters were evaluated for these solid dispersions. Tablets were prepared using Febuxostat solid dispersions and varying concentrations of Entada scandens seed starch by direct compression technique. Pre and post-compression parameters were evaluated along with in vitro drug release studies, characterization studies like Fourier Transform Infra-Red spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy (SEM), X-Ray Diffraction (XRD) and stability studies.


Results: Phytochemical tests revealed the presence of starch in all extracts. Starch prepared from 0.5% sodium hydroxide (ESS4) showed best physicochemical properties. In vitro dissolution studies revealed that solid dispersion F4 containing Febuxostat and poloxamer-188 in 1:3 ratios showed better drug release. Formulation FE5 containing F4 solid dispersion with 12.5% w/w of ESS4 showed enhanced drug release. FT2 tablets having 12.5% w/w of ESS4 showed better drug release when compared to others. FTIR and DSC studies revealed no major interactions between drug and excipients. XRD studies revealed the nature of formulations. Accelerated stability studies showed that all tablets were stable.


Conclusion: The super disintegrant property of Entada scandens seed starch was evaluated.

Keywords: Febuxostat, Entada scandens,, Solid dispersions, Fast dissolving, Fast dissolving tablets, Poloxamer-188

Author Biographies

SANDEEP DOPPALAPUDI, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chandramoulipuram, Chowdavaram, Guntur, Andhra Pradesh, India 522019

Department of Pharmacology, Assistant Professor and Ph.D. Scholar

VIDYADHARA SURYADEVARA, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chandramoulipuram, Chowdavaram, Guntur, Andhra Pradesh, India 522019,

Department of Pharmaceutics,

Professor and Principal

CHIRUDEEP JUJALA, Chebrolu Hanumaiah Institute of Pharmaceutical Sciences, Chandramoulipuram, Chowdavaram, Guntur, Andhra Pradesh, India 522019,

DEPARTMENT OF PHARMACEUTICS,

M.PHARMACY STUDENT

References

1. Sanjaymitra PVSS, Ganesh GNK. Dissolution and solubility enhancement strategies: current and novel prospective. J Crit Rev 2018;5:1-10.
2. Saharan VA, Kukkar V, Kataria M, Gera M, Chowdhury PK. Dissolution enhancement of drugs, part i: technologies and effect of carriers. Int J Health Res 2009;2:107-24.
3. Dhirendra K, Lewis S, Udupa N, Atin K. Solid dispersion: a review. Pak J Pharm Sci 2009;22:234-46.
4. Sreenivas SA, Gadad AP, Patil MB. Formulation and evaluation of Ondansetron hydrochloride directly compressed mouth dissolving tablets. Indian Drugs 2006;43:35-7.
5. Thomus R. Fast dissolving tablets: an overview. Eur J Pharm Sci 2007;32:58-68.
6. Bhowmik D, Chiranjib B, Yadav J, Chandira RM, Sampath KP. Emerging trends of disintegrants used in the formulation of solid dosage form. Schol Res Lib 2010;2:495-504.
7. Krishna MC, Sirish V. Formulation, development and evaluation of fast disintegrating tablets of cinitapride hydrogen tartrate by using direct compression technique. Int J Curr Pharm Res 2017;9:98-103.
8. Santosh KR, Ankita G. Design, optimization and evaluation of Piroxicam fast dissolving tablets employing starch tartrate-a new super disintegrant. Int J Appl Pharm 2019;11:89-97.
9. Sunada H, Bi Y. Preparation, evaluation and optimization of rapidly disintegrating tablets. Powder Technol 2002;122:188-98.
10. Dey SK, Rahman M, Ahmed A, Khatun A, Siraj A. Phytochemical screening and pharmacological activities of entada scandens seeds. Int J Appl Res Nat Prod 2013;6:34-9.
11. Love BL, Barrons R, Veverka A, Snider KM. Urate-lowering therapy for gout: focus on febuxostat. Pharmacotherapy 2010;30:594–608.
12. Fateatun N, Jiaur RM, Sultan MM, Sorifa A, Aminul IT, Ahmed M. Physicochemical properties of flour and extraction of starch from jack fruit seed. Int J Nutr Food Sci 2014;3:347-54.
13. Menaka T, Nagaraja G, Yogesh DB, Sunil Kumar US, Prakash L. Physicochemical properties of flour and isolated starch from jackfruit seeds (Artocarpus Heterophyllus). Res J Pharm Sci 2011;1:14-8.
14. Sharda S, Bishambar S, Kirtika M, Monalisha N, Neha K, Shalini M. Solid dispersions: A tool for improving the solubility and dissolution of metronidazole. Int J Drug Delivery 2013;5:94-8.
15. Appa RB, Shivalingam M, Kishore RYV, Somesekhara R, Rajesh K, Sunitha N. Formulation and evaluation of aceclofenac solid dispersions for dissolution rate enhancement. Int J Pharm Sci Drug Res 2010;2:146-50.
16. Okunlola A, Odeku OA. Comparative evaluation of starches obtained from Dioscorea species as intragranular tablet disintegrants. J Drug Delivery Sci Technol 2008;18:445-7.
17. Shukla D, Subhashis C, Sanjay S, Brahmeshwar M. Mouth dissolving tablets II: an overview of evaluation techniques. Pharm Sci 2009;77:327–41.
18. Dharna A, Neelam S, Sukhbir S, Sandeep A. Solid dispersions: a review on drug delivery system and solubility enhancement. Int J Pharm Sci Res 2013;4:2094-105.
19. Sangeeta M, Abhisek P. Dissolution enhancement of seroquel by solid dispersion techniques. Asian J Pharm Clin Res 2016;9:284-7.
20. Shashikumar Y, Veena M, Srinivas M. Solid dispersion technique to enhance the solubility and dissolution rate of aripiprazole by fusion method. Int J Pharm Pharm Sci 2016;8:187-92.
21. Biraju P, Dhaval P, Ramesh P, Chirag P, Tejas S, Sanja SD. Development and in vitro evaluation of fast dissolving tablets of glipizide. Int J Pharm Pharm Sci 2009;1:15-8.
22. Prasanna LA, Anand KM, Vamsi KM, Annie VK, Ashwini G. Formulation and development of irbesartan (Poorly Water Soluble Drug) immediate-release tablets. Int Res J Pharm 2012;3:34-7.
23. Roy CPA, Bhattacharyya AK, Chattopadhyay P. Study on functional properties of raw and blended Jackfruit seed flour (a non-conventional source) for food application. Indian J Nat Prod Resour 2012;3:56-9.
24. Vidyadhara S, Sasidhar RL, Lakshmi HD, Vijetha P, Vijetha K. Studies on jack fruit seed starch as a novel natural super disintegrant for the design and evaluation of Irbesartan fast-dissolving tablets. Integr Med Res 2017;6:280-91.
Statistics
110 Views | 47 Downloads
Citatons
How to Cite
DOPPALAPUDI, S., SURYADEVARA, V., & JUJALA, C. (2019). FORMULATION AND EVALUATION OF FEBUXOSTAT FAST DISSOLVING TABLETS USING ENTADA SCANDENS SEED STARCH AND POLOXAMER-188 AS SUPERDISINTEGRANTS. International Journal of Applied Pharmaceutics, 11(5), 241-250. https://doi.org/10.22159/ijap.2019v11i5.34779
Section
Original Article(s)