Asian J. Pharm. Ana. 2011; Vol. 1: Issue 4, Pg 67-70 [AJPAna.]
67
ISSN- 2231–5667 (Print) www.asianpharmaonline.org
ISSN- 2231–5675 (Online) 0974-3618
REVIEW ARTICLE
An Analytical Approach of Doxofylline: A Review
Akhilesh Gupta
1
*, Vimal Yadav
1
, Jaydeep S. Yadav
1
and Swati Rawat
2,
1
Kunwar Haribansh Singh College of Pharmacy, Jaunpur (U.P.)
2
Shri Bhagwan College of Pharmacy, Aurangabad (M.S.)
*Corresponding Author E-mail: akhileshgupta81@rediffmail.com
ABSTRACT:
Doxofylline is chemically designated as 7-(1, 3 dioxolone-2-yl methyl) theophylline. Presence of a dioxolane group in
position C-7 differentiates it from theophylline. It is a new antibronchospastic drug recently introduced in therapy with
pharmacological properties like theophylline; a potent adenosine receptor antagonist. doxofylline do not affect gastric
acid secretion; either invivo or in-vitro; unlike theophylline. The lack of side effects with doxofylline indicates that the
drug can be used safely and effectively. Some analytical methods for quantitative determination of doxofylline in
pharmaceutical formulations like UV-Spectrophotometry, HPLC and LC-MS are reported. The present review deals
with the various analytical methods reported as well as adopted for the estimation of doxofylline.
KEYWORDS: Doxofylline, UV, HPLC, LC-MS.
INTRODUCTION:
Doxofylline is methyl xanthine derivatives
1
; it is a
bronchodilator and plays a direct role in bronchial
relaxation of bronchial smooth muscle. Doxofylline by
inhibiting the phosphodiesterase within the smooth muscle
cells and cause smooth muscle relaxation, thus achieving
suppression of asthma. Doxofylline is a novel
bronchodilator xanthine that differs from theophylline
because the presence of a dioxalane group in position C-7
2
.
Like theophylline, mechanism of action of doxofyllines is
related to the inhibition of phosphodiesterase activities.
However, differently from theophylline, doxofylline
appears to have decreased affinities toward adenosine A1
and A2 receptors which may account for the better safety
profile of the drug
3
. As per pharmacokinetic parameters it
absorbed rapidly. In healthy adults for the first 0.4 g oral,
time to peak plasma concentration (Tmax) was 1.22 hours,
the peak plasma concentration (Cmax) for a 0.9 g / ml.
The materials widely distributed in various organs, with the
highest content in the lungs
4
. The phony goods to and from
the form of metabolites in urine excretion, for the main
metabolite of - hydroxyethyl theophylline.
Received on 09.09.2011 Accepted on 18.10.2011
© Asian Pharma Press All Right Reserved
Asian J. Pharm. Ana. 1(4): Oct. - Dec. 2011; Page 67-70
The elimination half-life of the goods (t1 / 2) for 7.42 hours.
Eight healthy male volunteers for each of the 0.4 g of oral,
twice daily, for seven days, reaching a steady state Cmax
(13.00 ± 2.54) g / ml, Cmin (3.22 ± 1.99) g / ml, steady
Mean plasma concentration of (7.11 ± 1.72) g / ml.
Taking xanthine derivatives may cause nausea, vomiting,
abdominal pain, headache, insomnia, irritability,
tachycardia, period of contraction, shortness of breath, high
blood sugar, and proteinuria. Excessive use will emerge as a
serious arrhythmia
5
.
ANALYTICAL APPROACH FOR THE
DETERMINATION OF DOXOFYLLINE:
H R Joshi and coworkers
6
reported two methods for
determination of Doxophylline in solid dosage form. The
first method was based on UV-Spectrophotometric
determination of the drug. It involves absorbance
measurement at 274 nm (absorption maxima of
Doxophylline) in 0.1 N hydrochloric acid. Calibration curve
was linear with the correlation coefficient between 0.99 to
1.0 over a concentration range of 0.20 to 30 µg/ml for the
drug. The second method was based on HPLC separation of
the drug in reverse phase mode using Hypersil ODS C18
column (250 X 4.6mm). The mobile phase constituted of
Buffer: Acetonitrile (80:20) and pH adjusted to 3.0 with
dilute orthophosphoric acid was delivered at the flow rate
1.0 ml min-1. Detection was performed at 210 nm.
Separation was completed within 7 min. Calibration curve