STUDIES ON SOLID DISPERSIONS OF LEFLUNOMIDE

  • MAHAPARALE PR Department of Pharmaceutics, Government College of Pharmacy, Aurangabad, Maharashtra, India.
  • THORAT VP Department of Pharmaceutics, Siddhi College of Pharmacy, Chikhali, Pune, Maharashtra, India.

Abstract

Objective: Leflunomide is Non steroidal Anti-Inflammatory drug, which is poorly water soluble. In present study attempt has been made to prepare and characterize solid dispersions of leflunomide to increase solubility of drug.

Method:  In Preparation of solid dispersion of leflunomide different polymer like PEG 4000, PEG 6000, Poloxamer 188 and Poloxamer 407 were used.  Effects of several variables such as type of carrier used, drug: carrier ratios, method of preparation were studied. The evaluation of solid dispersions was done by solubility study, dissolution study and X-ray diffractometry.

 Result: Improvement in dissolution of drug was observed in all solid dispersions as compared to pure drug alone. Solid dispersions prepared using Poloxamer 188 showed fastest in vitro drug release. Solid dispersions prepared using solvent evaporation method showed relatively faster drug release than melt evaporation method. XRD patterns indicated reduced crystallinity of drug particles, which suggests mechanism of enhanced solubility and dissolution of drug in solid dispersion systems.

Conclusion:

 A significant result obtained with the study indicated that solid dispersion by solvent evaporation can successfully be further explored and employed to improve solubility and dissolution characteristics of poorly soluble drugs.

Keywords: Leflunomide, Solid dispersion, Carrier

Keywords: Leflunomide, Solid dispersion, Carrier

Author Biography

MAHAPARALE PR, Department of Pharmaceutics, Government College of Pharmacy, Aurangabad, Maharashtra, India.

pharmaceutics

References

1. Shah H. Dissolution improvement of nebivolol hydrochloride using solid dispersion adsorbate technique. Asian J Pharm 2015;9:49-55.
2. Serajuddin AT. Solid dispersion of poorly water soluble drugs: Early promises, subsequent problems and recent breakthroughs. J Pharm Sci 1999;88:1058-66.
3. Higuchi T, Connors KA. Phase solubility techniques. Adv Anal Chem Instrum 1965;4:117-212.
4. Mahaparale PR, Malpure PS, Sanap D, Kachare VT, Kasture PV. Development of dissolution medium of leflunomide. Indian Pharm 2007;6:69-70.
5. Batra V, Shirolkar SV, Mahaparale PR, Kasture PV. Solubility and dissolution enhancement of glipizide by solid dispersion technique. Indian J Pharm Educ Res 2008;42:373-8.
6. Deshpande KB, Ganesh NS. Orodispersible tablets-an overview of formulation and technology. Int J Pharm Bio Sci 2011;2:531-9.
7. Ratnakar R, Goswami L. Formulation and evaluation of fast dissolving tablet of telmisartan. Int J Pharm Chem Sci 2013;2:2078-85.
8. Mehta A, Tyagi R, Shukla A. Formulation and evaluation of solid dispersion of an antidiabetic drug. Curr Trends Biotech Pharm 2009;3:76-84.
9. Amidon GL, Lennernas H, Shah VP, Crisen JR. A theoretical basis for a biopharmaceutics drug classification: The correlation of in vitro drug products dissolution and in vivo bioavailability. Pharm Res 1995;12:413-24.
10. Somasundaram J, Mekonnen T. Formulation and evaluation of diltiazem hydrochloride oral dispersible tablets. Int J Pharm Health Care Res 2013;1:184-90.
11. Arora SC, Sharma PK, Irchhaiya R, Khatkar A, Singh N, Gagoria J. Development, characterization and solubility study of solid dispersions of azithromycin dihydrate by solvent evaporation method. J Adv Pharm Technol Res 2010;1:221-8.
12. Pekamwar SS. Formulation and evaluation of solid dispersion of lopinavir by using different techniques. Int Res J Pharm 2015;6:663-9.
13. Deshkar SS, Sonkamble K, Mahore J. Formulation and optimization of nanosuspension for improving solubility and dissolution of gemfibrozil. Asian J Pharm Clin Res 2019;12:157-63.
14. Yadav S, Veena M, Sriniva 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.
15. Shah I, Bhatt S, Yadav A. Enhancement of solubility and dissolution of nebivolol by solid dispersion technique. Int J Pharm Pharm Sci 2014;6:566-71.
16. Mohan A, Sangeetha G. In vitro-in vivo evaluation of fast dissolving tablets containing solid dispersion of oxcarbazepine. Int J Pharm Pharm Sci 2016;8:124-31.
17. Mannem V, Suryadevara V. Formulation and evaluation of telmisartan solid dispersion using Entada scandens seed starch and poloxamer 188 as superdisintegrantss. Asian J Pharm Clin Res 2018;11:474-81.
18. Manimaran V, Dhamodharan N. Devlopment of fast dissolving tablets of amlodipine besylate by solid dispersion technology using poloxamer 407 and poloxamer 188. Asian J Pharm Clin Res 2017;10:135-41.
19. Singh G, Singh N. Development and characterization of nevirapine loaded amorphous solid dispersions for solubility enhancement. Asian J Pharm Clin Res 2019;12:176-82.
20. Swain RP, Subudhi BB. Amorphous solid dispersions of pioglitazone hydrochloride using cremophor RH 40 and poloxamer 188: In vitro and in vivo evaluation. Indian Drug 2019;56:45-55.
21. Jadhav P, Yadav A. Formulation, optimization, and in vitro evaluation of polymeric nanosuspension of flurbiprofen. Asian J Pharm Clin Res 2019;12:183-91.
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How to Cite
PR, M., and T. VP. “STUDIES ON SOLID DISPERSIONS OF LEFLUNOMIDE”. Asian Journal of Pharmaceutical and Clinical Research, Vol. 13, no. 6, Apr. 2020, pp. 187-90, doi:10.22159/ajpcr.2020.v13i6.31283.
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