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THE PHARMA REVIEW (JUNE 2008) |
Development and Validation
of New RP-HPLC Method with UV-Detection for the
Determination of Carvedilol in Human Serum
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Mogallapalli L V Setti,
Vijaya Ratna J |
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Abstract: Carvedilol
is mainly used as an antihypertensive drug and it also
possesses antioxidant and antiproliferative effects. A
simple and sensitive analytical method was developed for
carvedilol in human serum by using high performance
liquid chromatography (HPLC). The method employs a
liquid- liquid extraction for isolation and sample
concentration followed by reversed phase liquid
chromatography (RPLC) analysis using ultraviolet (UV)
detection at 241 nm. Analytes were extracted from serum
samples that were previously mixed with sodium hydroxide
solution into an n- hexane, dichloromethane (7:3)
solvent system. The mobile phase consisted of
acetonitrile: orthophosphoric acid (37:63). The filtered
mobile phase components were pumped from the respective
reservoirs at a flow rate of 1.0 mL/min. Celecoxib was
used as internal standard. Serum samples containing the
carvedilol and internal standard, celecoxib were eluted
through a C18 column. Retention times of carvedilol and
celecoxib are 9.12 min and 11.49 min, respectively. The
limit of detection of the drug in serum is 5 500 ng/ml.
The extraction recovery of carvedilol is more than 75%.
The intra day and inter day coefficient of variation and
percent error values of the assay method were less than
5 %. Such a method would be ideally suitable for the
estimation of carvedilol in pharmacokinetic studies
after administration of carvedilol formulations.
Introduction
Carvedilol, (+)-1-(Carbaz ol-4-yloxy)-3-{[
2-(o-methoxyphenoxy)ethyl] amino}- 2-propanol (Figure
1), is a b receptor blocker and is an antihypertensive
drug with a multiple action spectrum, and it also has
vasodilating properties that are attributed mainly to
its blocking activity at a1 receptors. Carvedilol is
used in the treatment of mild to moderate hypertension
and angina pectoris. Carvedilol undergoes extensive
first pass metabolism that results in an absolute
bioavailability of about 25%.
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