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