Original Article
QBD-DRIVEN STABILITY INDICATING RP-HPLC METHOD DEVELOPMENT AND VALIDATION
FOR THE ESTIMATION OF NINTEDANIB ESYLATE
SANJAY DINKAR SAWANT , JYOTI BHAGWAN TANGDE
*
Department of Pharmaceutical Chemistry, Sinhgad Technical Education Society’s, Smt. Kashibai Navale College of Pharmacy, Pune,
Maharashtra, India
*
Corresponding author: Jyoti Bhagwan Tangde;
*
Email: jyotitangde@gmail.com
Received: 05 Nov 2024, Revised and Accepted: 16 Dec 2024
ABSTRACT
Objective: The present research work focuses on evaluation of Nintedanib esylate (NTB) with development and validation of Reverse Phase High-
Performance Liquid Chromatography (RP-HPLC) method pertaining to quality by design-based force degradation study.
Methods: A two-level, two-factorial design has been used with predetermined design specifications using design expert software. The RP-HPLC
method was developed with isocratic mode using a C-18 column at a 392 nm detection wavelength.
Results: The calibration curve was found to be linear with R² = 0.9996. Retention Time (RT) was obtained at 6.14; Limit of Detection (LOD) and
Limit of Quantitation (LOQ) were found to be 1.4121 μg/ml and 4.2790 μg/ml, respectively. Relative Standard Deviation (RSD) for intraday
precision was 1.799% and for interday precision 1.563%, respectively. Degradation studies found out the drug is susceptible to acidic, oxidative,
and photolytic conditions, while the drug was found to be stable in thermal and alkaline conditions.
Conclusion: The resulting method holds potential for application in routine analysis of nintedanib esylate in capsule formulation in compliance
with International Council for Harmonization (ICH) guidelines.
Keywords: Degradation, Design expert, Factorial design, ICH guidelines, Nintedanib esylate
© 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.2025v17i2.53110 Journal homepage: https://innovareacademics.in/journals/index.php/ijap
INTRODUCTION
Nintedanib (NTB) is chemically ethane sulfonic acid; methyl (3Z)-3-
[({4-[N-methyl-2-(4-methylpiperazin-1-yl) acetamido] phenyl} amino)
(phenyl) methylidene]-2-oxo-2, 3-dihydro-1H-indole-6 [1]. NTB is an
oxindole derivative having methyl ester, which undergoes ester
hydrolysis in vivo [2]. It is a BCS-II drug with poor solubility and high
permeability [3], commonly used in the treatment of pulmonary
fibrosis and Non-Small Cell Lung Cancer (NSCLC) [4]. NTB is a tyrosine
kinase inhibitor and acts by inhibiting platelet-derived growth factor
receptors, fibroblasts, and vascular growth factors, also interferes with
cell proliferation and cell differentiation [5]. This drug was first
approved by the US FDA in october 2014 for the treatment of
Idiopathic Pulmonary Fibrosis (IPF). It has been found to improve the
patient's quality of life by slowing down the forced vital capacity [6].
The National Institute for Health and Care Excellence (NICE) endorses
nintedanib in IPF, where the forced vital capacity anticipates 50-80%.
However, data conducted from Asia in 2023 indicates 50% of people
stop taking NTB in IPF within 12 mo because of its adverse effects [7].
Quality by Design (QbD) is a systematic approach that begins with a
predetermined design specification and emphasizes the product and
process understanding with quality risk management [8]. Over the
last decades, the QbD approach has been involved in
pharmaceuticals with the issuing of ICH Q8 (R2) guidelines. ICH Q8
(R2) guidelines state the implementation of structured and
organized methods for the determination of factors affecting the
process. It is also known as Design of Experiments [9, 10]. The
Analytical Quality by Design (AQbD), according to ICH Q14
highlights the summary of performance characteristics for intended
purposes. AQbD ensures the robustness and cost-effectiveness of the
method, which is applicable throughout the product lifecycle [11,
12]. The current study utilizes the QbD approach with a 2-level, 2-
factorial design for RP-HPLC method development and for stability
studies of nintedanib esylate using design expert software.
The analytical methods reported for NTB to date include the RP-
HPLC method [13, 14], HPLC stability-indicating method [15], QbD-
based impurity studies by LC-MS [16], stability-indicating RP-HPLC
method [17], Ultra High Performance Liquid Chromatography
coupled Mass Spectrometry (UHPLC-MS/MS) [18], stability study by
RP-HPLC [19], HPLC-UV in rat plasma [20], RP-HPLC in rat plasma
[21], and High-Performance Thin Layer Chromatography coupled
Mass Spectrometry (HPTLC MS-MS) [22, 23]. Literature survey
reveals that only two stability studies have been reported so far. Out
of which, Pasquini et al. have performed QbD-based simultaneous
estimation of nintedanib and related impurity profiling. While
Purnachand et al. have performed a simple stability study for
nintedanib. None of these methods focuses on the implementation of
QbD analysis for stability parameters. Therefore, a new RP-HPLC
method with a forced degradation study based on a two-level, two-
factorial quality-by-design approach for the evaluation of NTB has
been attempted.
Fig. 1: Structure of NTB esylate
MATERIALS AND METHODS
Materials
NTB (purity 99.96%), a yellow, crystalline solid powder, was
obtained as a gift sample from Chemsar Research Centre, Pune,
India. Nintedanib (Ofev) 100 mg as a capsule dosage form
manufactured by Boehringer Ingelheim Ltd. was purchased from a
International Journal of Applied Pharmaceutics
ISSN- 0975-7058 Vol 17, Issue 2, 2025