Log-linear PK-PD model of dexibuprofen in healthy Indian males.
Journal name: World Journal of Pharmaceutical Research
Original article title: A simple non-invasive comparative log linear pk-pd model of dexibuprofen tablets in indian healthy human male volunteers
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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Punnamchand Loya & Madhusudan N. Saraf
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: A simple non-invasive comparative log linear pk-pd model of dexibuprofen tablets in indian healthy human male volunteers
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
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Summary of article contents:
Introduction
The study aimed to develop a simple pharmacokinetic-pharmacodynamic (PK-PD) model for dexibuprofen, a non-steroidal anti-inflammatory drug (NSAID), using healthy male volunteers. The investigation focused on understanding the relationship between the drug's plasma concentration and its efficacy in inhibiting inflammation induced by methyl nicotinate.
Relationship Between Concentration and Efficacy
The pharmacodynamic evaluation showed a significant correlation between the plasma concentration of dexibuprofen and the percentage inhibition of inflammation. After administering a 400 mg dose of dexibuprofen, the maximum observed inhibition was approximately 90%, occurring around 2.5 hours post-dosing. This indicates that effective plasma levels of dexibuprofen must be maintained to achieve significant anti-inflammatory effects.
Methodology for Assessment
A non-invasive method using Laser Doppler Flowmetry (LDF) was utilized to measure skin blood flow changes in response to dexibuprofen after methyl nicotinate application. This approach provided real-time assessment of the drug’s efficacy, showcasing its feasibility for use in human volunteers. The study followed strict ethical guidelines and involved a controlled experimental design to ensure reliable results.
Development of a Predictive Model
The investigation led to the establishment of a log-linear PK-PD model for dexibuprofen, which was found to be effective in predicting the drug's therapeutic outcomes. This model demonstrates a strong relationship between the concentration of the drug and its pharmacodynamic effects, which can be applied not only to dexibuprofen but also to other similar NSAIDs.
Conclusion
The findings confirm that a simple, non-invasive PK-PD modeling approach is effective for evaluating dexibuprofen's pharmacological effects in healthy volunteers. This model serves as a predictive tool for understanding the drug's clinical performance and helps inform dosing strategies for future formulations, enhancing the understanding of dexibuprofen's therapeutic profile.
FAQ section (important questions/answers):
What was the aim of the study on dexibuprofen?
The study aimed to develop a simple PK-PD model for dexibuprofen, investigating its pharmacokinetics and pharmacodynamics in Indian male volunteers after oral administration to predict clinical performance of NSAID formulations.
How was dexibuprofen administered to the volunteers?
Dexibuprofen was administered orally as a single dose of 400 mg tablets after an overnight fast to twelve healthy male volunteers participating in a randomized crossover study.
What method was used to measure the pharmacodynamic effects?
The pharmacodynamic effects were measured by assessing the inhibition of methyl nicotinate-induced erythema using a Laser Doppler Flowmeter (LDF) for up to 12 hours post-administration.
What were the key findings from the pharmacokinetic study?
The observed maximum concentration (Cmax) of dexibuprofen was around 30 µg/ml, achieving this level within about 1.83 hours after administration, indicating effective absorption of the drug.
What does the log-linear PK-PD model indicate?
The log-linear PK-PD model suggests a straightforward relationship between plasma concentration of dexibuprofen and its pharmacodynamic effects, enabling better predictions for therapeutic efficacy.
How long did dexibuprofen's effect last?
Dexibuprofen significantly inhibited methyl nicotinate-induced inflammation for up to 8 hours, requiring plasma concentrations to exceed 4 µg/ml for effective inhibition.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Log-linear PK-PD model of dexibuprofen in healthy Indian males.”. 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) Inflammation:
Inflammation is a biological response to harmful stimuli such as pathogens, damaged cells, or irritants. It plays a key role in the body's healing process but can also lead to chronic conditions. Understanding inflammation is crucial in pharmacology for developing treatments like dexibuprofen, which aims to reduce pain and swelling.
2) Blood:
Blood is a vital fluid in the body responsible for transporting oxygen, nutrients, hormones, and waste products. In pharmacokinetic studies, blood samples are used to measure drug concentration, helping establish the relationship between drug efficacy and plasma levels, essential for effective treatment outcomes.
3) Drug:
A drug is a chemical substance used to treat, cure, prevent, or diagnose diseases. In this study, dexibuprofen serves as a non-steroidal anti-inflammatory drug (NSAID) used to manage pain and inflammation. Understanding a drug's pharmacokinetics and pharmacodynamics is crucial for effective clinical application.
4) Water:
Water is a fundamental solvent in biological systems, crucial for dissolving nutrients, facilitating cellular reactions, and maintaining homeostasis. In pharmacological studies, it serves as a vehicle for drug administration, affecting absorption and distribution in the body, thereby influencing the efficacy of drugs like dexibuprofen.
5) Pharmacological:
Pharmacological refers to the study of drug actions, effects, and mechanisms on biological systems. This encompasses pharmacodynamics and pharmacokinetics, essential for understanding the therapeutic effects of drugs like dexibuprofen, which inhibit inflammation and pain through specific biological interactions.
6) Dysmenorrhea (Dysmenorrhoea):
Dysmenorrhoea is a medical term for painful menstrual periods. It is a common condition managed with NSAIDs like dexibuprofen. Understanding dysmenorrhoea is important in pharmacology, allowing for the development of effective treatments targeting pain relief and improving the quality of life for affected individuals.
7) Pharmacology:
Pharmacology is the science of how drugs interact with biological systems. It encompasses the study of drug mechanisms, effects, therapeutic applications, and side effects. Research in pharmacology, such as the study of dexibuprofen, informs safe and effective medication development, contributing to improved patient care.
8) Discussion:
Discussion refers to the section in scientific research where results are interpreted and implications are explored. It is critical for synthesizing findings, addressing limitations, and proposing future research directions. In this context, it helps understand the significance of dexibuprofen's effects on inflammation.
9) Activity:
Activity in pharmacology pertains to the effectiveness of a drug in eliciting a desired biological response. The activity of dexibuprofen in reducing inflammation is a central focus of this study, linking its pharmacokinetic and pharmacodynamic properties to therapeutic outcomes.
10) Ulcer:
An ulcer is a sore that develops on the lining of the stomach or other organs, often due to inflammation or irritation. NSAIDs like dexibuprofen can pose a risk of gastrointestinal ulcers. Understanding this risk is essential for safe prescribing and patient management.
11) Post:
Post refers to a period following an event, commonly used in clinical studies to denote timeframes after drug administration. For example, post-drug administration blood samples are collected to determine the pharmacokinetics of dexibuprofen, helping establish its therapeutic efficacy and safety in patients.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Log-linear PK-PD model of dexibuprofen in healthy Indian males.’. Further sources in the context of Science might help you critically compare this page with similair documents:
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