Naringin a potent antioxidant used as bioavailibility enhancer for terbinafine hydrochloride
Keywords:
Bioavailability, flavone, naringin, cytochromeAbstract
The poor bioavailability of drugs has been identified as the single most important challenge in oral drug delivery. Prominent among the factors responsible for this are the oxidative metabolic activity of the intestinal and hepatic cytochrome P450 enzyme family. Naringin and naringenin which are the major phytochemical component of grapefruit juice, a well-known cytochrome P450 3A4 inhibitor and flavone glycoside, is antioxidant in nature and occurs naturally in the pericarp of citrus fruit, and particularly of grapefruit (Citrus paradisii) where it is the predominant flavonoid found and is responsible for the bitter taste associated with the fruit. CYP3A4 which is a class of CYP – 450 (microsomal enzyme) is responsible for the oxidative metabolic reaction of various substrates which decreases the bioavailability of drug.
Downloads
References
Yadav, A.V. and Prakashan, N. Routes of administration of drugs In: Pharmacology and Toxicology.19th Ed. 2008; p4-12.
Greenblatt DJ. Update on drug interactions with grapefruit juice: an evidence-based review. Pharmacy Times. 2010; 95–104.
Paine MF, Widmer WW, Hart HL, et al. A furanocoumarin-free grapefruit juice establishes furanocoumarins as the mediators of the grapefruit juice-felodipine interaction. Am J Clin Nutr. 2006; 83(5):1097–105.
Paine MF, Khalighi M, Fisher JM, Shen DD, Kunze KL, Marsh CL, Perkins JD, Thummel KE. Characterization of interintestinal and intraintestinal variations in human CYP3A-dependent metabolism. J Pharmacol Exp Ther. 1997; 283:1552-62.
Murray M. Mechanisms and significance of inhibitory drug interactions involving cytochrome P450 enzymes (Review). Int J Mol Med 1999; 3:227-38.
Texas grapefruit history (http://www.texasweet.com/About-Texas-Citrus/Texas-Grapefruit-History), TexaSweet. Retrieved 2 July 2008.
Veronese ML, Gillen LP, Burke JP, Dorval EP, Hauck WW, Pequignot E, Waldman SA, Greenberg HE. Exposure-dependent inhibition of intestinal and hepatic CYP3A4 in vivo by grapefruit juice. Journal of Clinical Pharmacology. 2003; 43 (8):831–9.
Bailey DG, Malcolm J, Arnold O, Spence JD. “Grapefruit juice– drug interactions". Br J Clin Pharmacol . 1998; 46 (2): 101–10.
Ho PC, Saville DJ, Coville PF, Wanwimolruk S. Content of CYP3A4 inhibitors, naringin, naringenin and bergapten in grapefruit and grapefruit juice products. Pharm Acta Helv, 2000; 74(4):379–85.
Ho PC, Saville DJ, Coville PF, Wanwimolruk S. Content of CYP3A4 inhibitors, naringin, naringenin and bergapten in grapefruit and grapefruit juice products. Pharm Acta Helv. 2000; 74(4):379–85.
Schmiedlin-Ren P, Edwards DJ, Fitzsimmons ME, et al. Mechanisms of enhanced oral availability of CYP3A4 substrates by grapefruit constituents. Decreased enterocyte CYP3A4 concentration and mechanism-based inactivation by furanocoumarins. Drug Metab Dispos. 1997; 25(11):1228–33.
Guo LQ, Fukuda K, Ohta T, Yamazoe Y. Role of furanocoumarin derivatives on grapefruit juice-mediated inhibition of human CYP3A activity. Drug Metab Dispos. 2000; 28(7):766–71.
Bailey DG, Arnold JM, Strong HA, et al. Effect of grapefruit juice and naringin on nisoldipine pharmacokinetics. Clin Pharmacol Ther, 1993; 54(6):589–94.
D. M. Brahmankar& Sunil B. Jaiswal, Biopharmaceutics & Pharmacokinetics A Treatise, IstEdn, VallabhPrakashan. 2006; 296- 297.
Davis, W. B. Determination of flavanones in citrus fruits. Anal. Chem.1947; 19: 476-478.
Hendrickson, R., and J. W. Kesterson. Chemical analysis of citrus bioflavanoids. Proc. Fla. State Hort.Soc.1957; 70: 196-203.
Kesterson, J. W., and R. Hendrickson. Naringin, a bitter principle of grapefruit. Fla. Agr. Exp. Sta.Bui.1953; 51 1.
Ting, S. V. Enzymic hydrolysis of naringin in grapefruit. J. Agr. Food Chem.1958; 6: 546.
Published
How to Cite
Issue
Section
Copyright (c) 2020 Akanksha Singh, Divya Juyal, Vikram Singh, Geeta Rawat
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.
