A Comprehensive Review on the Drug: Fenofibrate
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Fenofibrate, Antihyperlipidemia, Solubility, Bioavailability, Hypercholesterolemia
Abstract
Fenofibrate is currently used as antihyperlipidemic drug, which has a direct effect on lowering cholesterol, triglycerides and LDL (Low-Density Lipids), VLDL (Very Low-Density Lipids) levels along with raising the level of HDL (High-density Lipids) in the blood. It also plays a significant role in insulin resistance metabolic disorder. This drug is mainly used for controlling diseases related to lipids like hypercholesterolemia, severe hypertriglyceridemia and dyslipidaemia. Along with statins, it significantly controls the level of hypercholesterolemia and hypertriglyceridemia. It belongs to the group of drugs called 'Fibrate'. Fenofibrate was patented in 1969. In 1974, it was synthesized as a derivative of clofibrate and launched at the French market. It was marketed in 1975. In 2017, it was available as a generic medicine. Presently this API is being marketed in around 85 countries all over the world. Fenofibrate is a BCS Class-II drug having poor water solubility. The poor aqueous solubility of this drug causes low bioavailability and limited permeability through the GIT membrane. This API degrades at higher temperatures and in a humid environment, with one of the resultant degradation products being fenofibric acid. In the present review, we have discussed the historical development, pharmacology, analytical profile with its physicochemical properties and ongoing research scenario on this API.
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References
Adkins, J. C., Faulds, D. 1997. Micronised fenofibrate: a review of its pharmacodynamic properties and clinical efficacy in the management of dyslipidemia Drugs. Journal of Europe PMC, 54(4):615– 633.
Balfour, J. A., Mctavish, D., Heel, R. C. 1990. Fenofibrate: A review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in dyslipidaemia. Drugs, 40(2):260–290.
British Pharmacopoeia 2010. The Department of Health, The Stationary Office, volume 1. London. ISBN:113228287.
Dixit, M., Rasheed, A., Daniel, S. 2015. Enhancing solubility and dissolution of Fenofibrate by spray drying technique. International Journal of Pharmaceutical Sciences, 7(1):173–177.
Elsherif, Z. A., Abas, S. S., Abdelwahab, M. H., El-Weshahy, S. 2013. Determination of Gemfibrozil and Fenofibrate in pharmaceuticals in presence of their degradation products. International Journal of Pharmacy and Pharmaceutical Sciences, 5(3):886–96.
Fazio, S. 2009. More Clinical Lessons from the FIELD Study. Cardiovascular Drugs and Therapy, 23(3):235–241. ISSN: 0920-3206, 1573-7241.
Filippatos, T. D., Elisaf, M. S. 2011. Fenofibrate plus simvastatin (fixed-dose combination) for the treatment of dyslipidaemia. Expert Opinion on Pharmacotherapy, 12(12):1945–1958. ISSN: 1465-6566, 1744-7666.
Fischer, J., Ganellin, C., Robin 2006. Analogue-based Drug Discovery. volume 474, pages 978–981. John Wiley and Sons. ISBN: 978-3-527-60749-5.
Gabhe, Y., Satish 2014. RP-HPLC Method for Identification of Reference Standards of Degradation Products of Fenofibrate. Journal of Pharmaceutical and Biomedical Science, 19:809–812.
Greally, P., Hussein, M. J., Cook, A. J., Sampson, A. P., Piper, P. J., Price, J. F. 1993. Sputum tumour necrosis factor-alpha and leukotriene concentrations in cystic fibrosis. Archives of Disease in Childhood, 68:389–392. ISSN: 0003-9888, 1468-2044.
Grundy, S. M., Cleeman, J. I., Merz, C. N., Brewer, H. B., Clark, L. T., Hunninghake, D. B., Pasternak, R. C. 2004. Implication of recent clinical trials for the National Cholesterol Education Program. Journal of American Heart Association, 110(2):227–239.
Heller, F., Harvengt, C. 1983. Effects of clofibrate, bezafibrate, fenofibrate and probucol on plasma lipolytic enzymes in normolipaemic subjects. European Journal of Clinical Pharmacology, 25(1):57–63. ISSN: 0031-6970, 1432-1041.
Hussain, M. D., Mohsin, K., Alamari, R., Ahmad, A., Raish, M., Alanzi, F. 2016. Development of self- nanoemulsifying drug delivery systems for the enhancement of solubility and oral bioavailability of fenofibrate, a poorly water-soluble drug. International Journal of Nanomedicine, (11):2829. ISSN: 1178-2013.
Jain, D., Jain, N., Raghuwanshi, R. 2008. Development and validation of RP-HPLC method for simultaneous estimation of atorvastatin calcium and fenofibrate in tablet dosage forms. Indian Journal of Pharmaceutical Sciences, 70(2):263. ISSN: 0250- 474X.
Jensen, P. Ø., Moser, C., Kharazmi, A., Presler, T., Koch, C., Høiby, N. 2006. Increased serum concentration of G-CSF in cystic fibrosis patients with chronic Pseudomonas aeruginosa pneumonia. Journal of Cystic Fibrosis, 5(3):145–151. ISSN: 1569-1993.
Kadav, A. A., Vora, D. N. 2008. Stability indicating UPLC method for simultaneous determination of atorvastatin, fenofibrate and their degradation products in tablets. Journal of Pharmaceutical and Biomedical Analysis, 48(1):120–126. ISSN: 0731-7085.
Keating, G. M., Croom, K. F. 2007. Fenofibrate: a review of its use in primary dyslipidaemia, the metabolic syndrome and type 2 diabetes mellitus. Drugs, 67(1):121–153.
Khanna, D., Fitzgerald, J. D. 2012. Systematic Non Pharmacological and Pharmacological Therapeutics Approaches to Hyperuricemia. Arthritis Care and Research, 64(10):143–146.
Klose, D., Laprais, M., Leroux, V., Siepmann, F., Deprez, B., Bordet, R., Siepmann, J. 2009. Fenofibrate-loaded PLGA microparticles: Effects on ischemic stroke. European Journal of Pharmaceutical Sciences, 37(1):43–52. ISSN: 0928-0987.
Koda-Kimble, M. A., Young, L. Y., Kradjan, W. A., Guglielmo, B. J., Alldredge, B. K., Corelli, R. L. 2005. Applied Therapeutics the Clinical Use of Drugs CD-ROM. pages 50–77, Philadelphia. Lippincott Williams and Wilkins. ISBN: 0781748453.
Koehler, D. R., Downey, G. P., Sweezey, N. B., Tanswell, A. K., Hu, J. 2004. Lung Inflammation as a Therapeutic Target in Cystic Fibrosis. American Journal of Respiratory Cell and Molecular Biology, 31(4):377–381. ISSN: 1044-1549, 1535-4989.
Lacroix, P. M., Dawson, B. A., Sears, R. W., Black, D. B., Cyr, T. D., Ethier, J.-C. 1998. Fenofibrate raw materials: HPLC methods for assay and purity and an NMR method for purity. Journal of Pharmaceutical and Biomedical Analysis, 18(3):383–402. ISSN: 0731-7085.
Lalloyer, F., Staels, B. 2010. Fibrates, Glitazones, and Peroxisome Proliferator–Activated Receptors. Arteriosclerosis, Thrombosis, and Vascular Biology, 30(5):894–899. ISSN: 1079-5642, 1524-4636.
Lassner, A., Banditt, P., Trager, U. 2001. Rapid and simple method for detection of fenofibric acid in human serum by high-performance liquid chromatography. Pharmazie Journal, 56(1):50–51.
Liu, G.-N., Shi, H.-Z., Xie, Z.-H., Shen, H.-H., Huang, H.-Q., Deng, J.-M., Liang, Q.-L., Wu, Y.-B. 2009. Epithelial neutrophil-activating peptide-78 recruits neutrophils into pleural effusion. European Respiratory Journal, 34(1):184–190. ISSN: 0903-1936, 1399-3003.
Malmendier, C. L., Lontie, J. F., Delcroix, C., Dubois, D. Y., Magot, T., De Roy, L. 1989. Apolipoproteins C-II and C-III metabolism in hypertriglyceridemic patients Effect of a drastic triglyceride reduction by combined diet restriction and fenofibrate administration. Atherosclerosis, 77(2-3):139–149. ISSN: 0021-9150.
Manninen, V., Tenkanen, L., Koskinen, P., Huttunen, J. K., Mänttäri, M., Heinonen, O. P., Frick, M. H. 1992. Joint effects of serum triglyceride and LDL cholesterol and HDL cholesterol concentrations on coronary heart disease risk in the Helsinki Heart Study. Implications for treatment. Circulation, 85:37–45. ISSN: 0009-7322, 1524-4539.
Meng, L., Zhang, W., Hang, J. 2010. Bioequivalence of micronized Fenofibrate capsule in healthy volunteers. Chinese Journal of New Drug and Clinical Remedies, 29:863–866.
Package Insert 2010. Highlights of Prescribing Information, Abbot Laboratories. Pg: 1-29.
Qiu, Y., Zhu, J., Bandi, V., Guntupalli, K. K., Jeffery, P. K. 2007. Bronchial mucosal inflammation and upregulation of CXC chemoattractants and receptors in severe exacerbations of asthma. Thorax, 62(6):475–482. ISSN: 0040-6376.
Salamaa, F. M. M., Nassar, M. W. I., El-Din, M. M. K. S., Attia, K. A. M., Kaddah, M. Y. 2011. Determination of Fenofibrate and the Degradation Product Using Simultaneous UV-Derivative Spectrometric Method and HPLC. American Journal of Analytical Chemistry, 02(03):332–343. ISSN: 2156-8251, 2156-8278.
Saurav, A., Kaushik, M., Mohiuddin, S. M. 2012. Fenofibric acid for hyperlipidemia. Expert Opinion on Pharmacotherapy, 13(5):717–722. ISSN: 1465-6566, 1744-7666.
Scott, R., O’Brien, R., Fulcher, G., Pardy, C., d’Emden, M., Tse, D., Taskinen, M. R., Ehnholm, C., Keech, A. 2009. Effects of Fenofibrate Treatment on Cardiovascular Disease Risk in 9,795 Individuals with Type 2 Diabetes and Various Components of the Metabolic Syndrome: The Fenofibrate Intervention and Event Lowering in Diabetes (FIELD) study. Diabetes Care, 32(3):493–498. ISSN: 0149-5992, 1935-5548.
Staels, B., Dallongeville, J., Auwerx, J., Schoonjans, K., Leitersdorf, E., Fruchart, J.-C. 1998. Mechanism of Action of Fibrates on Lipid and Lipoprotein Metabolism. Circulation, 98(19):2088–2093. ISSN: 0009-7322, 1524-4539.
Steiner, G. 2009. How Can We Improve the Management of Vascular Risk in Type 2 Diabetes: Insights from FIELD. Cardiovascular Drugs and Therapy, 23(5):403–408.
Tasaka, S., Mizoguchi, K., Funatsu, Y., Namkoong, H., Yamasawa, W., Ishii, M., Hasegawa, N., Betsuyaku, T. 2012. Cytokine profile of bronchoalveolar lavage fluid in patients with combined pulmonary fibrosis and emphysema. Respirology, 17(5):814–820. ISSN: 1323-7799.
Tejas, P., Patel, L. D., Adeshara, S. P., Timir, P., Sunil, M., Tushar, P. 2011. Dissolution Enhancement of Fenofibrate by Solid Dispersion Technique. Journal of Current Pharma Research, 1(2):127–134. ISSN: 2230-7834, 2230-7842.
Third Report of the National Cholesterol Education Program 2002. Expert Panel on Detection, Evaluation, and Treatment of High Blood Cholesterol in Adults (Adult Treatment Panel III) final report. 106(25):3143–3421.
Toth, P. P., Potter, D., Ming, E. E., Toth, P. P., Potter, D., Ming, E. E. 2003. Prevalence of lipid abnormalities in the United States: The National Health and Nutrition Examination Survey. Journal of Clinical lipidology, 6(4):325–330.
United States Pharmacopoeia 2009. 32 National Formulary 27, United States Pharmacopeial Convention. Pg: 2351-2354.
Vlase, L., Popa, A., Muntean, D., Leucuta, S. 2011. Pharmacokinetics and comparative bioavailability of two fenofibrate capsule formulations in healthy volunteers. Arzneimittelforschung, 60(09):560–563. ISSN: 0004-4172, 1616-7066.
Wong, T. Y., Simo, R., Mitchell, P. 2012. Fenofibrate-a potential systemic treatment for diabetic retinopathy. American Journal of Ophthalmology, 154(1):612.
Zhu, T., Ansquer, J.-C., Kelly, M. T., Sleep, D. J., Pradhan, R. S. 2010. Comparison of the Gastrointestinal Absorption and Bioavailability of Fenofibrate and Fenofibric Acid in Humans. The Journal of Clinical Pharmacology, 50(8):914–921. ISSN: 0091-2700.
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