Leflunomide is a Non-steroidal Anti-Inflammatory drug, which is poorly water soluble. In present study attempt has been made to prepare and characterize inclusion complexes of drug with Beta Cyclodextrin (?-CD). The phase solubility analysis indicated the formation of a 1:1 molar inclusion complex of drug with ?-CD. Apparent stability constant (KC) was 674 K-1 for ?-CD complex. The inclusion complexes were prepared by three different methods viz. coprecipitation, kneading and microwave irradiation method. The prepared complexes were characterized using dissolution study, FTIR and X-ray diffractometry. The inclusion complex prepared with ?-CD by kneading method exhibited greatest enhancement in solubility (18 mg/100ml) and fastest dissolution (T90 = 29 min.) of Leflunomide.
Cite this article:
P. R. Mahaparale, V. P. Thorat. Enhancement of Solubility of Leflunomide with -cyclodextrin inclusion complexation. Research J. Pharm. and Tech. 2021; 14(2):809-812. doi: 10.5958/0974-360X.2021.00142.6
P. R. Mahaparale, V. P. Thorat. Enhancement of Solubility of Leflunomide with -cyclodextrin inclusion complexation. Research J. Pharm. and Tech. 2021; 14(2):809-812. doi: 10.5958/0974-360X.2021.00142.6 Available on: https://www.rjptonline.org/AbstractView.aspx?PID=2021-14-2-38
1. Reynolds, J. E. F., Eds., In; Martindale The Extra Pharmacopeia, 31st Edn., Pharmaceutical Press, London, 2002, 711-712, 53-55.
2. Budawari, S., The Merck Index, 13th Edn., Merck and Co., Inc., Whitehouse, NJ, 2003, 971.
3. Loftsson T., Brewster M. E. and Masson M., Role of cyclodextrins in improving oral drug delivery, Am. J. Drug Deliv. 2004; 2: 1-15.
4. Deshmukh S. S., Potnis V. V., Shelar D. B. and Mahaparale P. R., Studies on inclusion complexes of ziprasidone hydrochloride. With β –cyclodextrin and hydroxypropyl β –cyclodextrin, Indian Drugs, 2007; 677-682.
5. Mahaparale P. R., Malpure P. S., Sanap D. A., Kachare V. T. and Kasture P. V., Development of dissolution medium of leflunomide, The Indian Pharmacist, April 2007; 69- 70.
6. Reddy M. N., Chowdary K. P. R. and Diwan P. V., β -cyclodextrin complexes of celecoxib: molecular modeling, characterization and dissolution studies, AAPS Pharm. Sci., 2004; 6 (1); article 7.
7. Higuchi T., Connors K. A., Phase solubility techniques, Adv. Anal. Chem. Instr., 1965; 4: 117- 212.
8. Martin E. M., Cyclodextrin and their uses: A Review, Process Biochemistry, 2003; 30:5-7
9. Aulton M. E, The science of dosage form design, II edition, Churchill Livingstone, 2002; 16: 23, 234.
10. Preeti V. Bankar, Improved Dissolution Rate of Leflunomide using Hydroxypropyl-β-Cyclodextrin Inclusion Complexation by Freeze-Drying Method, International Journal of Drug Delivery, 2012; 4:498-506.
11. Kane R. N., Kuchekar B. S., Preparation, physicochemical characterization, dissolution and formulation studies of Telmisartan Cyclodextrin inclusion complexes, Asian J. Pharm., 2010; 4:2-9.
12. Pandya P., Pandey N., Singh S. K., Kumar M. Formulation and characterization of ternary complex of poorly soluble duloxetine hydrochloride. Journal of Applied Pharmaceutical Science, 2015; 5 (06) : 088-096.
13. Pradeep R. Vavia, Inclusion Complexation of Nimesulide with beta-Cyclodextrins, Drug Development and Industrial Pharmacy, 1999; 25(4):543–545.