Analytical methods for the determination of leflunomide - a short review
Journal name: World Journal of Pharmaceutical Research
Original article title: Analytical methods for the determination of leflunomide - a short review
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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Shah Kruti V., Chauhan Sanjay P., Suhagia B. N.
World Journal of Pharmaceutical Research:
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Full text available for: Analytical methods for the determination of leflunomide - a short review
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
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Summary of article contents:
1) Introduction
Leflunomide (LEF) is a disease-modifying antirheumatic drug (DMARD) primarily utilized in the treatment of moderate to severe rheumatoid arthritis and psoriatic arthritis. It plays a significant role in managing symptoms associated with these conditions, reducing joint damage, and promoting improved physical functionality. Marketed under the brand name Arava® by Sanofi-Aventis, Leflunomide was approved for clinical use in 1998. Following oral administration, Leflunomide is rapidly converted to its active metabolite, Teriflunomide (A771726), which contributes to its therapeutic effects by inhibiting dihydro-orotate dehydrogenase—thereby impacting the synthesis of pyrimidines, vital for cellular growth and proliferation.
2) Analytical Methods for Leflunomide
The determination of Leflunomide in pharmaceutical formulations and biological samples employs several instrumental analytical techniques. The review discusses various methods, including UV-Visible Spectroscopy, Reverse Phase High-Performance Liquid Chromatography (RP-HPLC), Liquid Chromatography-Mass Spectrometry (LC-MS/MS), and Ultra-Performance Liquid Chromatography (UPLC). Each of these techniques offers unique advantages and has seen application in drug development, quality control, and pharmacokinetic studies. Notably, HPLC has employed different reversed-phase columns and mobile phase compositions, adapted for quantification accuracy in measuring Leflunomide and its metabolites.
3) Spectrophotometric Methods
Among the analytical methods, spectrophotometric techniques have been employed to assess Leflunomide's concentration in various formulations. Studies, such as that from Abbas et al. (2006), have showcased differential derivative spectroscopy to measure Leflunomide amidst its degradates. Five distinct methods were evaluated, demonstrating high accuracy across various concentrations. These methods highlight the versatility of UV-Visible spectroscopy in pharmaceutical analysis, enabling accurate measurements even in the presence of degradation products, underscoring the importance of developing robust methods for drug analysis.
4) Chromatographic Methods
Chromatographic methods, particularly RP-HPLC, have been pivotal in accurately quantifying Leflunomide in tablet forms and biological matrices. Yeniceli et al. (2006) established a reliable RP-HPLC method employing an internal standard to mitigate retention time fluctuations while validating parameters such as linearity, precision, and recovery. The study ensured specificity even in degraded samples, which is essential for quality assurance in pharmaceutical manufacturing. Additionally, more advanced techniques like LC-ESI-MS/MS have been reported for monitoring Teriflunomide in plasma samples, emphasizing the increasing sophistication in analytical methodologies for effective drug monitoring and therapeutic assessment.
5) Conclusion
The reviewed literature emphasizes the critical role of precise and validated analytical methods for Leflunomide in ensuring drug efficacy and safety in clinical applications. While various spectrophotometric and chromatographic approaches have proven effective for drug determination, there remains a need for the exploration of additional methods such as spectrofluorimetry and HPTLC. Moreover, expansion into combination formulations and degradation kinetics studies could enhance existing analytical frameworks. Continuous development in analytical techniques is essential to meet quality standards in the pharmaceutical industry, ensuring the reliability of drug formulations and therapeutic outcomes.
FAQ section (important questions/answers):
What is Leflunomide and its primary use?
Leflunomide is a disease-modifying antirheumatic drug (DMARD) used to treat moderate to severe rheumatoid arthritis, helping to reduce symptoms, joint damage, and improve physical functioning.
What are the common analytical methods for Leflunomide?
Common analytical methods include UV-Visible Spectroscopy, RP-HPLC-UV, LC-MS/MS, LC-ESI-MS/MS, and UPLC-PDA, which are used for its determination in pharmaceutical formulations and biological samples.
How is Leflunomide administered and metabolized in the body?
Leflunomide is taken orally as a prodrug and rapidly converts to its active metabolite, Teriflunomide, which inhibits pyrimidine synthesis and various protein kinases.
What are the marketed formulations of Leflunomide?
Marketed formulations of Leflunomide include Arava®, Cleft®, Lefra®, Lefumide®, Lisifen®, and Rumaleft®, available in various tablet strengths.
What is the significance of method validation in drug analysis?
Method validation ensures that analytical methods for drug quantification are reliable, reproducible, and meet predefined acceptance criteria, which is crucial for quality assurance in pharmaceuticals.
What challenges exist in Leflunomide's analytical method development?
Challenges include the need for more methods using spectrofluorimetry and HPTLC, as well as a lack of information regarding combination preparations involving Leflunomide.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Analytical methods for the determination of leflunomide - a short review”. 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) Table:
In the context of scientific research, a table presents data in a structured format, allowing for easy comparison and analysis of results. In the text, tables are used to summarize validation parameters, method comparisons, and other key findings related to Leflunomide and its analytical determination, enhancing clarity and understanding.
2) Drug:
A drug is a chemical substance used for medical purposes, primarily to diagnose, cure, treat, or prevent diseases. In this paper, Leflunomide is highlighted as a disease-modifying antirheumatic drug (DMARD) used to treat rheumatoid arthritis, showcasing its pharmacological importance in modern medicine.
3) Sah:
Shah refers to the lead author, Shah Kruti V., of the review article. Authors' names are essential in academic publications as they attribute credit for the research and findings. Shah's work contributes to the understanding of analytical methods for Leflunomide determination in pharmaceutical sciences.
4) Measurement:
Measurement refers to the quantitative evaluation of substances or properties, crucial in scientific research. In the context of analytical methods for Leflunomide, measurement techniques like HPLC and spectrophotometry are discussed for their roles in determining drug concentrations in pharmaceutical preparations and biological samples.
5) Water:
Water serves as a solvent and is often used in analytical chemistry methods, including chromatography and preparation of buffers. In the analysis of Leflunomide, water is mentioned in the context of mobile phases and buffers, critical for sample preparation and maintaining reaction conditions during measurements.
6) Rheumatoid arthritis:
Rheumatoid arthritis is an autoimmune disorder characterized by chronic inflammation of joints. Leflunomide is specifically mentioned as a treatment for this condition, emphasizing the drug's relevance in managing symptoms and preventing joint damage, which outlines its therapeutic importance in rheumatology.
7) Study (Studying):
A study involves systematic investigation to discover or validate facts and theories. This article presents various studies that analyze Leflunomide's stability, analytical methods, and pharmacological effects. These studies underscore the importance of research in enhancing drug safety and efficacy in treatment regimens.
8) Performance:
Performance pertains to the functioning or effectiveness of analytical methods in measuring drug concentrations. The text evaluates the performance of various analytical techniques used for Leflunomide, discussing precision, accuracy, recovery rates, and sensitivity, which are critical in ensuring reliable results in pharmaceutical analyses.
9) Gujarat:
Gujarat is a state in India where the research institution, Dharamsinh Desai University, is located. The geographical context is essential in academic publications as it often reflects the research environment, available resources, and cultural perspectives, influencing studies in pharmaceutical sciences like Leflunomide evaluation.
10) Disease:
A disease refers to a pathological condition of a bodily part or system resulting from various causes, manifesting through characteristic symptoms. The article focuses on Leflunomide's application in treating rheumatoid arthritis, identifying it as a significant intervention in managing chronic diseases and improving patient quality of life.
11) Pharmacological:
Pharmacological relates to the study of drug action on biological systems. In the text, the pharmacological properties of Leflunomide are examined, particularly its mechanisms of action as an immunosuppressive agent, highlighting the compound's roles in treatment strategies for autoimmune conditions.
12) Pharmacology:
Pharmacology is the branch of medicine concerned with the uses, effects, and mechanisms of drugs. The article provides insights into pharmacological aspects of Leflunomide, discussing how its metabolites and mechanisms contribute to therapeutic effects, pivotal for understanding drug development and clinical applications.
13) Toxicology:
Toxicology is the study of the adverse effects of substances on living organisms. Although the primary focus of the article is on analytical methods, toxicological studies are essential in evaluating the safety of drugs like Leflunomide, ensuring that their therapeutic benefits outweigh potential risks in patients.
14) Substance:
A substance generally refers to a particular kind of matter with uniform properties. In the context of this research, 'substance' refers to Leflunomide and its metabolites, which are studied for their pharmaceutical relevance, stability, and analytical determination using various methods discussed in the article.
15) Activity:
Activity describes the functional effect of a drug within biological systems. In this case, the pharmacological activity of Leflunomide, particularly its metabolite Teriflunomide, is assessed regarding its immunosuppressive properties, crucial for effectively managing autoimmune diseases such as rheumatoid arthritis.
16) Chauhan (Chauhān):
Chauhan references another author, Sanjay P. Chauhan, contributing to the collective expertise and credibility of the research team. The collaboration among authors enriches the study's findings on Leflunomide, demonstrating a multidisciplinary approach to pharmaceutical research and development.
17) Quality:
Quality refers to the standard of a product or method in terms of performance and reliability. The article discusses the importance of method validation in ensuring the quality of pharmaceutical products containing Leflunomide, highlighting analytical techniques that guarantee consistency and safety in medicinal formulations.
18) Company:
Company refers to the pharmaceutical firms involved in the marketing and production of drugs like Leflunomide. Specifically, Sanofi-Aventis is mentioned, emphasizing the role of companies in the drug development process, including the importance of quality control and analytical methods in ensuring efficacy and safety.
19) Medium:
Medium often refers to the solvent used in chemical reactions or the physical environment in which experiments are conducted. In this article, the choice of medium, such as buffers and solvents in chromatographic methods, is critical for achieving accurate measurements and maintaining the stability of compounds being analyzed.
20) Joshi (Jōśī, Jośī):
Joshi is another author involved in the study, contributing to the research on Leflunomide's analytical methods. The inclusion of multiple authors showcases a collaborative effort in the scientific community, enriching the insights and findings presented regarding the stability and validation of Leflunomide analysis.
21) Food:
Food typically pertains to substances consumed for nutritional purposes, but in this context, it represents the regulatory aspect of drug safety governed by organizations like the FDA. The mention of the FDA highlights the importance of food and drug safety standards in the approval and use of pharmaceuticals, including Leflunomide.
22) Post:
Post can refer to a stage following an event or action, often used in research to denote procedures that occur after data collection. In this article, it might refer to post-analysis considerations, including the implications of study results for drug efficacy and the need for further research or validation.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Analytical methods for the determination of leflunomide - a short review’. Further sources in the context of Science might help you critically compare this page with similair documents:
Pharmaceutical preparation, Analytical method, Oral administration, Pharmaceutical industry, High performance liquid chromatography, Anti-inflammatory properties, Stability study, Dosage form, Drug development, Retention time, Clinical pharmacology, Mobile phase, Correlation coefficient, Internal standard, Multiple reaction monitoring, Method development, Sensitivity, Pharmaceutical formulation, Method validation, Spectrophotometric method, UV-Visible spectroscopy, Biological samples, Chromatographic method.