Original Article
DEVELOPMENT AND VALIDATION OF DEFERASIROX-RELATED SUBSTANCE METHOD IN
SOLID DOSAGE FORMS USING HPLC
RUJUTA TRIVEDI
1*
, BHANUBHAI SUHAGIA
2
1
Department of Pharmacy, Dharmsinh Desai University, Nadiad-387001, Gujarat, India.
2
Faculty of Pharmacy, Dharmsinh Desai
University, Nadiad-387001, Gujarat, India
*
Corresponding author: Rujuta Trivedi;
*
Email: rujuta.trivedi@yahoo.co.in
Received: 19 Dec 2024, Revised and Accepted: 07 Feb 2025
ABSTRACT
Objective: A simple, sensitive, and reproducible Reverse-Phase High-Performance Liquid Chromatography (RP-HPLC) method was developed to
quantitatively determine related substances in bulk and pharmaceutical dosage forms of Deferasirox (DFS). The method's performance was
validated according to the present International Council on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for
Human Use (ICH) guidelines for specificity, limit of detection (LOD), limit of quantification (LOQ), linearity, accuracy, precision, and Robustness. The
developed method can be used for routine analysis of the determination of DFS in the presence of degradation products and impurities.
Methods: Chromatographic separation was achieved on Shimadzu shim pack GIS (150*4.6) mm5μm using isocratic elution mode, which included
0.1 % Formic acid in Water: Acetonitrile in gradient mode as mobile phase at a flow rate of 1.0 ml/min. And column temperature of 40 °C. Detection
was performed at a wavelength of 254 nm coupled with an Ultra Violet (UV) detector. The Injection volume was 10 μl. The drug was exposed to
various stress conditions in degradation studies, such as acidic, basic, oxidative, hydrolytic, photolytic, and thermal degradation.
Results: The retention time of DFS was 8.1 min. The resolution of DFS and four impurities was greater than 2.0 for all pairs of components. The high
correlation coefficient (r2>0.9990) values indicated clear correlations between the investigated compound concentrations and their peak areas
within the test ranges. The Repeatability and intermediate precision expressed by the Relative Standard Deviation (RSD) were less than 10%. The
accuracy evaluated by performing recovery studies via a spike method was 50-150%. Stress Degradation studies were carried out; however, no
significant degradation was observed in any of the stress degradation conditions, implying a chemically stable drug formulation and the method
used to measure stability is robust to minor variations; hence, the product is likely to maintain its quality and efficacy throughout its shelf life.
Conclusion: Hence, a suitable, reliable, accurate, precise, and economical HPLC method was developed, which is ideal for analyzing DFS in both bulk
and commercial formulations.
Keywords: Deferasirox, Related substances, Impurity, Validation, Forced degradation, High-performance liquid chromatography
© 2025 The Authors. Published by Innovare Academic Sciences Pvt Ltd. This is an open access article under the CC BY license (https://creativecommons.org/licenses/by/4.0/)
DOI: https://dx.doi.org/10.22159/ijap.2025v17i2.53465 Journal homepage: https://innovareacademics.in/journals/index.php/ijap
INTRODUCTION
Iron is essential in all living organisms and involves many
physiological processes, such as oxygen transport and energy
transduction. It is estimated that more than a quarter of the human
population is affected at some stage of their life by abnormalities of
iron metabolism, particularly iron deficiency anemia. Similarly,
millions of people suffer from iron overload, including hereditary
hemochromatosis and Thalassemia Intermedia (TI), which are
caused by increased iron absorption. Excess iron is toxic in these and
other iron-loading conditions, causing increased morbidity and
mortality due to tissue damage. DFS is an oral iron chelator. Its
primary use is to reduce chronic iron overload in patients receiving
long-term blood transfusions for conditions such as beta-
thalassemia and other chronic anemia [1-6].
Iron chelators, such as deferoxamine or deferasirox, are commonly
used to treat iron overload disorders. If the iron chelator or its
impurities degrade, the degradation products may become toxic or
cause harmful side effects. For example, impurities might lead to
adverse patient reactions, such as liver damage, kidney issues,
gastrointestinal discomfort, and increased toxicological burden due
to unintended or harmful by-products from degradation or
contamination. A reliable method can be developed and validated to
identify and quantify these impurities; manufacturers can ensure
that their product is safe for patient use.
Regulatory agencies such as the FDA, EMA, and ICH have stringent
guidelines for the development, validation, and testing of drugs,
particularly in the case of impurities. The ICH Q3A and Q3B
guidelines (on impurities in new drug substances and products)
provide detailed standards for identifying, quantifying, and
controlling impurities. Proper method development and validation
of the analytical technique (such as HPLC, GC, or UV
spectrophotometry) help ensure compliance with regulatory
standards. This is essential for obtaining approval for the drug and
maintaining it in the market [9]. By creating specific impurities,
researchers can validate analytical methods for their ability to
detect, quantify, and separate these impurities from the API. This
ensures that the method is robust and reliable. For regulatory
approval, methods must be validated to demonstrate their accuracy,
precision, specificity, sensitivity, and Robustness [10]. Various
factors such as experimental design and analysis conditions such as
matrix type, column type, mobile phase, elution modes, detection
wavelengths, and therapeutic category influence the separation and
identification of the impurities and degradation products [11].
Hence, an attempt was made to develop an RP-HPLC method that is
simple, rapid, accurate, precise, specific, economical, sensitive, and
stable, indicating the estimation of DFS and related substances in
bulk and pharmaceutical tablet formulation.
Deferasirox is a white to slightly yellow powder. It is the first oral
medication approved in the USA for this purpose. It was approved by the
United States Food and Drug Administration (FDA) in November 2005
[7]. It is approved in the European Union by the European Medicines
Agency (EMA) for children 6 years and older for chronic iron overload
from repeated blood transfusions. Its low molecular weight and high
lipophilicity allow the drug to be taken orally, unlike deferoxamine,
which must be administered by intravenous infusion. Along with
deferiprone, DFS seems capable of removing iron from cells (cardiac
myocytes and hepatocytes) and iron from the blood. Chemically it is 4-
[3,5-bis(2-hydroxyphenyl),4-[3,5-bis(2-hydroxyphenyl)-1,2,4-triazol-1-
yl] benzoic acid 4-[3,5-bis(2-hydroxyphenyl)-1,2,4-triazol-1-yl] benzoic
acid [8]. The structure of DFS is shown in fig. 1.
International Journal of Applied Pharmaceutics
ISSN- 0975-7058 Vol 17, Issue 2, 2025