Volume : 11, Issue : 01, January – 2024
Title:
DEVELOPMENT AND EVALUATION OF FAST DISSOLVING TABLETS OF EFAVIRENZ BY SOLUBILITY ENHANCEMENT TECHNIQUE
Authors :
N.Kartheek, Pasam Jyothirmayi, Abbineni Anusha,Dr. N.srinivasa Rao
Abstract :
Efavirenz (EFV) is an anti-retroviral agent with low aqueous solubility. To enhance the solubility of EFV by using the concept of mixed hydrotropy. Initially, solubility of EFV was determined individually in sodium acetate, sodium citrate, urea and sodium benzoate at concentration of 10% w/v solutions. Highest solubility was obtained in 10% sodium benzoate solution. Highest solubility was obtained in 1:6:1 ratio of Urea + Sodium benzoate + Sodium acetate. This optimized combination was utilized in the preparation of solid dispersions by using distilled water as a solvent. Fourier-transform infrared to show no drug-hydrotropes interaction has occurred. Formulation of FAST dissolving tablets of Efavirenz using mixed hydrotrophy technique with different concentrations of super disintegrants such as Crosspovidone and Sodium Starch Glycolate were prepared by using direct compression method. Dissolution studies of prepared tablets were done using USP Type II apparatus. The batch CF3 tablets show 98.3% cumulative drug release within 40 min. The miraculous enhancement in solubility and bioavailability of Efavirenz was clear indication of the potent mixed hydrotropy to be used in future for other poorly water-soluble drugs in which low bioavailability is a major concern.
KEYWORDS: Efavirenz, Mixed hydrotropy, Solid dispersions, fast dissolving tablets.
Cite This Article:
Please cite this article in press N.Kartheek et al., Development And Evaluation Of Fast Dissolving Tablets Of Efavirenz By Solubility Enhancement Technique, Indo Am. J. P. Sci, 2024; 11 (01).
Number of Downloads : 10
References:
1. Sikarra D, Shukla V, Kharia AA, Chatterjee DP. Research article techniques for solubility enhancement of poorly soluble drugs: An overview. J Med Pharm Allied Sci. 2012; 1: 1–22.
2. Behera AL, Sahoo SK, Patil SV. Enhancement of solubility: A pharmaceutical overview. Pharm Lett, 2010; 2: 310–8.
3. Limbachiya MI, Agarwal M, Sapariya A, Soni S. Solubility enhancement techniques for poorly soluble drugs: Review. Int J Pharm Sci Rev Res, 2011; 4: 71–86.
4. Saleh AM, El-Khordagui LK. Hydrotropic agents: A new definition. Int J Pharm. 1985; 24: 231–8.
5. Kapadiya N, Singhvi I, Mehta K, Karwani G, Dhrubo JS. Hydrotropy: A promising tool for solubility enhancement: A review. Int J Drug Dev Res, 2011; 3: 26–33.
6. Kim JY, Kim S, Papp M, Park K, Pinal R. Hydrotropic solubilization of poorly water-soluble drugs. J Pharm Sci. 2010; 99: 3953–65.Lee J, Lee SC, Acharya G, Chang CJ, Park K. Hydrotropic solubilization of paclitaxel: Analysis of chemical structures for hydrotropic property. Pharm Res, 2003; 20: 1022–30
7. Kwan K C, Oral bioavailability and first-pass effects, Drug Metabolism and Disposition,Vol. 25, 12.
8. Petri N, Bergman E, Forsell P,Hedeland M, Bondesson U, Knutson L and Hans Lennernäs H, First-pass effects of verapamil on the intestinal absorption and liver disposition of fexofenadine in the porcine model, September 2010, 38(9)
9. Dresser G K, Kim R B, and Bailey DG, Effect of grapefruit juice volume on the reduction of Fexofenadine bioavailability: possible role of organic anion transporting polypeptides. ClinPharmacol Ther 2005, 77: 170–177
10. Fromm M F, Busse D, Kroemer H K, and Eichelbaum M (1996) Differential induction of prehepatic and hepatic metabolism of verapamil by rifampin.Hepatology 24: 796–801
11. The Biopharmaceutics classification system (BCS) guidance, Center for Drug Evaluation and Research, US Food and Drug Administration, 2001, http://www.fda.gov/cder.
12. Wu C.Y., Benet L.S., Predicting drug disposition via application of BCS: Transport /Absorption elimination interplay & development of a biopharmaceutical drug disposition classification system. Pharmaceutical research, 22(1): 23-27, (2005
13. Shinde AJ. et al, “Solubilization of poorly soluble drugs: A Review”, Pharmainfo.net 2007; 5: 6.
14. Shiv M. Solubility Enhancement: Need.pharmainfo.net.2009.
15. .P. B. Myrdal and S. H. Yalkowsky,“Solubilization of drugs in aqueousmedia,” in Encyclopedia of Pharmaceutical Technology,
16. AMartin,Solubility and Distribution Phenomena, Physical Pharmacy andPharmaceutical Sciences, Lippincott Williams andWilkins, 6th edition, 2011.
17. Varun Raj Vemula*1, Venkateshwarlu Lagishetty1, Srikanth Lingala 2Volume 5, Issue 1, November – December 2010; Article-007Solubility is the phenomenon of dissolution of solid in liquid phase to give a homogenous system
18. Patil S.K., Wagh K.S., Parik V.B., Akarte A.M., Baviskar D.T., Strategies for solubility enhancement of poorly soluble drug. International journal of pharmaceutical science review and research, 8(2): 74-80, (2011)
19. Chaudhari A., Nagachi U., Gulati N., Sharma V.K., Khosa R.K., Enhancement of solubilisation and bioavailability of poorly soluble drugs by physical and chemical modification; A recent review. Journal of advance pharmacy education and research, 2(1): 32-67, (2012)
20. Blagden N., de Matas M., Gavan P.T., York P., Crystal engineering of active pharmaceutical ingredients to improve solubility and dissolution rates. Advanced Drug Delivery Reviews, 59(7): 617–630, (2007)