185 Original article Pharmacokinetic profile of rutin after intramuscular administration in rats favours its in vivo anti-inflammatory activity in carrageenan- induced rodent model of inflammation Falguni D. Modi , Shailesh K. Bhavsar*, Jatin H. Patel, Rasesh D. Varia, Lalit C. Modi**, Megha Modi and Nitin Kale Department of Veterinary Pharmacology and Toxicology, College of Veterinary Science and A.H., Navsari Agricultural University, Navsari-396450, Gujarat, India *Department of Veterinary Pharmacology and Toxicology, College of Veterinary Science and A.H., Anand Agricultural University, Anand-388110, Gujarat, India **Department of Veterinary Gynecology, College of Veterinary Science and A.H., Navsari Agricultural University, Navsari-396450, Gujarat, India Received February 10, 2019: Revised March 27, 2019: Accepted March 29, 2019: Published online June 30, 2019 Abstract The study was planned to evaluate pharmacokinetic profile and in vivo anti-inflammatory property of rutin following intramuscular administration (100 mg/kg, intramuscular) in rats. Carrageenan-induced paw edema assay was carried out separately to study in vivo anti-inflammatory property of rutin. The plasma rutin concentration was assayed using High Performance Liquid Chromatography (HPLC) . The pharmacokinetic parameters like the maximum plasma drug concentration ( C max ), time for maximal concentration ( T max ), elimination half-life (t ½ ), apparent volume of distribution (Vd (area) ), total body clearance (Cl (B) ) and mean residence time (MRT) were 21.11 0.46 g/ml, 1.83 ± 0.17 h, 9.11 1.50 h, 16.34 2.32 l/kg, 1.27 0.04 l/h/kg and 4.79 0.55 h, respectively. The drug concentration of 0.21 0.02 g/ml in plasma was detected at 24 h. In carrageenan-induced paw edema assay, rutin (100 mg/kg) significantly decreased edema volume from 1 to 6 h in comparison to carrageenan group and vehicle group. Per cent inhibition of inflammation after 6 h of rutin administration was 29.94 ± 1.49. Intramuscular administration of rutin produced satisfactory pharmacokinetic profile with promising in vivo anti-inflammatory activity in rats. Keywords: Pharmacokinetic profile, anti-inflammatory activity, rutin, intramuscular, rat 1. Introduction Inflammation is the complex biological response of vascular tissues to harmful stimuli such as pathogens, damaged cells or irritants. Inflammation is a protective attempt by the organism to remove the injurious stimuli as well as to initiate the healing process for the tissue (Jayakumari et al., 2012). Currently available analgesic and anti-inflammatory agents include corticosteroids and nonsteroidal anti-inflammatory drugs (Khan et al., 2015). Long term use of these drugs may cause side effects pertaining to liver and kidney (Bhadarka et al ., 2018). Thus, the discovery of new anti- inflammatory compounds is still on great demand by scientists in academia and industry. Drugs of herbal origin provide a rational means for the treatment of several ailments in human and animals (Nayanabhirama, 2016). It is important to mention that traditional medicinal systems are at a transitional stage in the development of Author for correspondence: Dr. Falguni D. Modi Assistant Professor, Department of Veterinary Pharmacology and Toxicology, College Veterinary Science and A.H., Navsari Agricultural University, Navsari-396450, Gujarat, India E-mail: fdmodi@nau.in Tel.: +91-7600049181 Copyright © 2019 Ukaaz Publications. All rights reserved. Email: ukaaz@yahoo.com; Website: www.ukaazpublications.com modern medicines in developing countries (Thakur et al., 2018). Active principles from many herbs have shown promising anti- inflammatory activity. Amongst them, flavonoids have been reported to show promising anti-inflammatory properties, either in vitro or in vivo (Vasudevan et al., 2007). Rutin (3, 3', 4', 5, 7-pentahydroxyflavone-3-rhamnoglucoside) is a flavonol, abundantly found in plants, such as passion flower, buckwheat, tea, and apple, and also called as quercetin-3-rutinoside and sophorin (Kreft et al.,1997). Rutin has been described as cell- protecting agents because of their antioxidant and antinociceptive and it was proposed as preventive effect of rutin on oxaliplatin- induced painful peripheral neuropathy based on their antioxidant properties (Azevedo et al., 2013). Rutin as parent compound was not detected in plasma and absolute systemic bioavailability is negligible, following oral administration due to first pass metabolism (Day et al., 1998; Jaganath et al., 2006). Thus, looking to need of a study related to pharmacokinetic profile of rutin after intramuscular administration along with in vivo evaluation of its anti-inflammatory activity in animals, present study was planned to generate data related to disposition and in vivo anti-inflammatory efficacy of rutin in rodent model which would be useful for future research on therapeutic application of rutin. Annals of Phytomedicine 8(1): 185-192, 2019 Annals of Phytomedicine: An International Journal http://www.ukaazpublications.com/publications/index.php Print ISSN : 2278-9839 Online ISSN : 2393-9885 DOI: 10.21276/ap.2019.8.1.25