HPLC development, determination, and validation for ezetimibe dosage.

| Posted in: Scientific

Journal name: World Journal of Pharmaceutical Research
Original article title: Hplc method development, method determination and method validation of dosage form of ezetimibe
The WJPR includes peer-reviewed publications such as scientific research papers, reports, review articles, company news, thesis reports and case studies in areas of Biology, Pharmaceutical industries and Chemical technology while incorporating ancient fields of knowledge such combining Ayurveda with scientific data.
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Original source:

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Author:

N. Suneel Kumar, B. Thirupathi Rao, P. Muralikrishna and CH. Narasimha Rao


World Journal of Pharmaceutical Research:

(An ISO 9001:2015 Certified International Journal)

Full text available for: Hplc method development, method determination and method validation of dosage form of ezetimibe

Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research

Doi: 10.20959/wjpr20183-10632


Download the PDF file of the original publication


Summary of article contents:

Introduction

Ezetimibe is a pharmaceutical compound used to lower cholesterol levels by inhibiting cholesterol absorption in the small intestine. It is often prescribed alone or in combination with statins for patients who do not respond adequately to statin therapy alone. The study presented in the World Journal of Pharmaceutical Research focuses on developing, determining, and validating a stability-indicating HPLC analytical method for Ezetimibe in tablet formulation. The primary aim of the research is to establish a method that is simple, rapid, and sensitive for the quantification of Ezetimibe in pharmaceutical products.

Method Development and Validation

The analytical method employs High-Performance Liquid Chromatography (HPLC) with a mobile phase consisting of 0.1% orthophosphoric acid and acetonitrile in a 50:50 ratio, operating at a flow rate of 1 mL/min. Utilizing a Zorbax SB-C18 reverse-phase column, the researchers optimized chromatographic conditions to achieve reliable separation of Ezetimibe. The method validation included assessments of linearity, precision, and specific parameters such as Limit of Detection (LOD) and Limit of Quantification (LOQ), with LOD at 0.1 µg/ml and LOQ at 0.2 µg/ml, showcasing the method's efficacy for quality control in pharmaceutical contexts.

System Suitability and Performance Metrics

Key system suitability parameters were established, demonstrating the method's reliability. The ideal Relative Standard Deviation (RSD) was found to be under 2.0%, and the theoretical plates exceeded 5000, indicating high efficiency in the chromatographic separation. The performance of the method was demonstrated through method precision and intermediate precision studies, revealing a very low overall RSD of 0.67%. These results confirmed that the method is robust and suitable for regulatory compliance according to ICH guidelines.

Forced Degradation Studies

Forced degradation studies were conducted to assess the stability of Ezetimibe under various adverse conditions, including acidic, alkaline, oxidative, thermal, and photolytic environments. The findings indicated that no significant degradation occurred under these conditions, with peak purity values well within acceptance criteria. This further validates the specificity of the HPLC method and ensures that it can be reliably used for Ezetimibe determination in the presence of potential impurities or degradation products.

Conclusion

In conclusion, the developed HPLC method for Ezetimibe demonstrated high sensitivity, specificity, and stability, making it an effective tool for routine quality control of the drug in pharmaceutical formulations. All validation parameters adhered closely to established acceptance criteria, asserting the method's suitability for intended use. The study highlights the importance of method validation in ensuring the quality and safety of pharmaceutical products, as well as contributing to the ongoing efforts in pharmaceutical analysis to maintain efficacy in cholesterol management therapies.

FAQ section (important questions/answers):

What is the objective of the study on Ezetimibe?

The objective is to develop, determine, and validate a stability-indicating method for Ezetimibe dosage forms, specifically for assay and content uniformity of tablet formulations.

What method was used for analyzing Ezetimibe?

A simple, sensitive, and rapid HPLC method was developed, using a mobile phase of 0.1% orthophosphoric acid and acetonitrile in a 50:50 ratio at a flow rate of 1 mL/min.

What were the results of the HPLC method's validation?

The HPLC method exhibited good linearity (r² = 0.9999), with LOD and LOQ values of 0.1 µg/ml and 0.2 µg/ml, respectively, and overall %RSD of method precision was 0.67.

What are some key characteristics of Ezetimibe?

Ezetimibe is a cholesterol absorption inhibitor with a molecular formula of C24H21F2NO3. It is a white crystalline powder, insoluble in water but soluble in organic solvents like ethanol and acetone.

What equipment was used for HPLC analysis in the study?

A Waters 2695 HPLC system equipped with a Photodiode Array Detector (PDA) and Empower Software was utilized for the analysis of Ezetimibe.

How was the system suitability for the method established?

System suitability was established by evaluating % RSD, peak asymmetry, and theoretical plates, ensuring all parameters met predefined acceptance criteria for reliable results.

Glossary definitions and references:

Scientific and Ayurvedic Glossary list for “HPLC development, determination, and validation for ezetimibe dosage.”. This list explains important keywords that occur in this article and links it to the glossary for a better understanding of that concept in the context of Ayurveda and other topics.

1) Study (Studying):
The term 'study' in this context refers to the systematic investigation aimed at developing and validating a high-performance liquid chromatography (HPLC) method for the drug Ezetimibe. It encompasses experimental design, data collection, and analytical techniques used to ensure the reliability and accuracy of the analytical method for pharmaceutical applications.

2) Kumar:
Kumar is one of the authors of the research, indicating his significant contribution to the study. His involvement likely includes experimental design, data analysis, and manuscript preparation, reflecting both his expertise in the field of pharmaceutical analysis and his role in academic research at Dravidian University.

3) Drug:
In the context of this research, 'drug' specifically refers to Ezetimibe, a medication used to lower cholesterol levels. The study focuses on developing a reliable analytical method for this drug, which is crucial for quality control in pharmaceuticals, ensuring its efficacy and safety in therapeutic applications.

4) Water:
'Waters' is in reference to the manufacturer of the HPLC system used in the study. This mention emphasizes the reliance on high-quality equipment to achieve accurate analytical results, reinforcing the importance of utilizing reputable brands in pharmaceutical research.

5) Relative:
'Relative' often pertains to relative standard deviation (% RSD) in this study, a statistical measure employed to assess precision in the analytical method. A low % RSD indicates good repeatability and reliability of the method, confirming its suitability for routine quality control of Ezetimibe formulations.

6) Table:
'Table' refers to a systematic arrangement of data presented in the study. Tables compile results from the validation process, including system suitability parameters and degradation profiles. This organized presentation allows for easier comparison and evaluation of the analytical method's performance against established criteria.

7) Andhra (Amdhra):
'Andhra' references the state of Andhra Pradesh in India, where the research was conducted at Dravidian University. This geographical context emphasizes the regional origin of the study and highlights the contributions of Indian institutions to global pharmaceutical research and development.

8) India:
India serves as the nation where the research and validation of the HPLC method for Ezetimibe took place. As a country known for its pharmaceutical industry, India contributes significantly to drug development and quality assurance, underscoring the importance of this study in ensuring medication safety.

9) Performance:
'Performance' relates to the efficacy and efficiency of the developed analytical method in measuring Ezetimibe accurately. The study emphasizes the method's reliable performance for routine quality control, vital for maintaining the standards of pharmaceutical products and protecting public health.

10) Observation:
'Observation' is crucial in scientific research, referring to the results and findings derived from conducting the study and experiments. It underscores the systematic approach taken to analyze data and validate method parameters, ensuring that conclusions drawn about the HPLC method's reliability are well-founded.

11) Purity:
'Purity' in this context pertains to the assessment of the Ezetimibe sample's integrity, ensuring that it is free from impurities. The study's validation ensures that the method accurately reflects the drug's quality, which is essential for therapeutic effectiveness and patient safety.

12) Discussion:
'Discussion' refers to the section of the research where findings are interpreted, implications are analyzed, and comparisons to previous work are made. This aspect of the study is crucial for understanding the method's relevance, limitations, and potential for application in quality control processes.

13) Narasimha (Narasingha, Nara-simha):
Narasimha is another author on the research team, perhaps indicating his role in the analytical procedures or statistical evaluations conducted within the study. Collaborators like Narasimha enhance the research's academic rigor through diverse expertise and experience in pharmaceutical sciences.

14) Tirupathi:
'Tirupathi' identifies the location of SV University, another collaborating institution involved in the research. The mention of such institutions emphasizes the collaborative nature of academic research in India and the contribution of local universities to advancements in pharmaceutical analysis.

15) Substance:
'Substance' refers to Ezetimibe as the primary focus of the study. The term underscores the material being analyzed and the importance of validating methods for accurate measurement, which is critical for pharmaceutical formulation and regulatory compliance.

16) Activity:
'Activity' pertains to the processes and experiments conducted during the validation of the HPLC method. This term emphasizes the dynamic nature of research, encompassing the systematic steps taken to achieve results consistent with regulatory standards for pharmaceutical testing.

17) Quality:
'Quality' relates to the reliability and effectiveness of the analytical method developed for Ezetimibe. The study is focused on ensuring that the pharmaceutical product meets stringent quality criteria necessary for approval and safe use in the healthcare system.

18) Powder:
'Powder' refers to the form in which Ezetimibe was analyzed, indicating the compound's physical state for testing purposes. It highlights the necessity of preparing the substance correctly to ensure accurate results during the HPLC analysis and further implications for formulation development.

19) House:
'House' may refer to 'in-house' methodologies or protocols established within the research setting. This highlights the developed processes that allow for consistent analysis and validation of the method, contributing to the overall credibility and reproducibility of the research findings.

20) Hand:
'Hand' relates to practical techniques employed during the experiment, such as sonication or shaking. These hands-on methods are significant in preparing samples and solutions, ensuring the accuracy of results, and reflecting the essential nature of laboratory skills in pharmaceutical research.

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