Pharmacokinetics of once-daily and immediate-release dextromethorphan.
Journal name: World Journal of Pharmaceutical Research
Original article title: Pharmacokinetic evaluation of once-daily sustained release dextromethorphan hydrobromide (dm) and immediate release dm in healthy human 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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Dr. Socorrina Colaco, Ramesh N., Sekar Rajan and Subramania Nainar Meyyanathan
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Pharmacokinetic evaluation of once-daily sustained release dextromethorphan hydrobromide (dm) and immediate release dm in healthy human volunteers
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Doi: 10.20959/wjpr20181-10514
Copyright (license): WJPR: All rights reserved
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Summary of article contents:
Introduction
Dextromethorphan (DM) is a widely utilized antitussive agent, primarily effective for cough suppression. Since its introduction in the 1960s, DM has gained prominence in cough and cold remedies due to its efficacy and generally favorable safety profile. However, its short half-life necessitates frequent dosing, which poses challenges for patient adherence. To address this issue, the development of sustained-release (SR) formulations has become a focus, enabling better therapeutic management of the drug by reducing the frequency of administration while maintaining effective plasma concentrations.
Pharmacokinetic Evaluation of Sustained-Release Formulations
The study undertook a pharmacokinetic evaluation of newly developed sustained-release dextromethorphan hydrobromide tablets compared to immediate-release formulations in healthy volunteers. Utilizing a randomized, three-period crossover design, the research involved six male subjects administered either a single dose of immediate release or the SR formulations. A sensitive high-performance liquid chromatography (HPLC) method was developed for quantifying dextromethorphan in human plasma, allowing for the collection of crucial pharmacokinetic data linked to the different formulations.
HPLC Method Development and Validation
A rapid and sensitive HPLC method was successfully validated for detecting dextromethorphan in plasma samples, employing solid phase extraction for sample preparation. The validation process confirmed the method's specificity, precision, and accuracy. Calibration curves exhibited linearity from 110.00 to 3000.00 ng/mL, with the overall precision of quality controls within acceptable limits. This reliable methodology ensured accurate pharmacokinetic profiling during the study, thereby facilitating a deeper understanding of the pharmacokinetic parameters associated with both sustained-release and immediate-release formulations.
Differences in Pharmacokinetic Parameters
The results highlighted significant differences in pharmacokinetic parameters between the formulations. The peak concentration (Cmax) for the sustained-release (SR) tablets was markedly lower than that of the immediate-release (IR) tablets, while the time to reach peak concentration (Tmax) was significantly extended for the SR. These findings indicate that the sustained-release formulation successfully prolonged the presence of dextromethorphan in the plasma, thereby enhancing the potential for improved patient compliance and a reduced risk of overdose.
Conclusion
The presented study underscores the efficacy of the newly developed sustained-release dextromethorphan hydrobromide tablets in achieving prolonged therapeutic effects with minimized dosing frequency. The validated HPLC method demonstrates robustness for pharmacokinetic assessments, contributing to knowledge surrounding DM formulations. The favorable pharmacokinetic profile of the SR formulation holds promise for enhancing the medication's safety and convenience, directly benefiting patients through improved adherence and reduced risks associated with more frequent dosing regimens.
FAQ section (important questions/answers):
What is the purpose of this pharmacokinetic study?
The study aims to evaluate the pharmacokinetics of sustained-release dextromethorphan hydrobromide compared to immediate-release formulations in healthy volunteers.
How was the pharmacokinetic evaluation conducted?
It was conducted using a randomized three-period crossover design with six healthy volunteers after administering single oral doses of the drug.
What methods were used for drug quantification in the study?
A sensitive and rapid HPLC method was developed and validated for determining dextromethorphan hydrobromide concentrations in human plasma using solid phase extraction.
What were the significant results regarding Cmax and Tmax?
The Cmax of the sustained-release tablet was significantly lower, and the Tmax was significantly longer than that of immediate-release formulations, indicating effective sustained release properties.
What conclusions can be drawn from the study?
The newly-developed sustained-release formulation of dextromethorphan hydrobromide could improve patient safety and dosing convenience due to lower peak plasma concentrations.
Who contributed to the materials and facilities used in the research?
The materials were provided by Divi's laboratories and Cadila pharmaceuticals, and facilities were supported by Sri Sutter Mutt, Mysore.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Pharmacokinetics of once-daily and immediate-release dextromethorphan.”. 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 study refers to a structured investigation carried out to evaluate the pharmacokinetics of sustained-release dextromethorphan hydrobromide compared to immediate-release formulations. It’s essential for understanding how the drug behaves in the body over time and contributes to the development of more effective treatment options.
2) Drug:
Drugs encompass a wide range of therapeutic agents, including dextromethorphan hydrobromide. The study focuses on the development, analysis, and pharmacokinetics of these agents, contributing to the broader field of pharmaceutical sciences and medication efficacy.
3) Table:
The table, particularly in pharmacological studies, typically presents organized data such as pharmacokinetic parameters or comparison results between different drug formulations. It helps in simplifying complex data interpretation and is crucial for communicating findings effectively in scientific literature.
4) India:
India serves as the geographical context for the study, highlighting the local relevance of the research. The absence of sustained-release dextromethorphan products in its pharmaceutical market indicates opportunities for innovation and development in drug formulation catered to Indian healthcare needs.
5) Blood:
Blood plays a critical role in pharmacokinetic studies as it is the medium through which drugs are distributed, metabolized, and eliminated in the body. Blood plasma concentration measurements help determine the drug's therapeutic effect and potential side effects in healthy volunteers.
6) Water:
Water is essential in laboratory and clinical studies for sample preparation, including the dissolution of drugs or dilution of reagents. The use of purified water ensures that no impurities interfere with the pharmacokinetic analysis or other experimental results.
7) Quality:
Quality in this context refers to the validation of analytical methods and the accuracy of pharmacokinetic data. Ensuring the quality of results is paramount in pharmaceutical studies as it directly impacts drug safety, efficacy, and regulatory approval processes.
8) House:
The word 'house' pertains to the in-house preparation of the test formulations, indicating that the sustained-release dextromethorphan tablets were developed and manufactured within a specific pharmaceutical facility. This highlights the significance of local manufacturing expertise in drug development.
9) Pharmacology:
Pharmacology is the branch of medicine concerned with the study of drugs and their effects on biological systems. This study contributes to the field by examining the pharmacokinetics of dextromethorphan, which informs therapeutic applications and further research in drug delivery systems.
10) Science (Scientific):
Scientific relates to the systematic inquiry underpinning the research methodology and analysis of the dextromethorphan study. It emphasizes the rigor, reproducibility, and evidence-based conclusions essential for advancing pharmacological and medical knowledge.
11) Divi:
Divi refers to Divi's Laboratories, the company that provided the key ingredient, dextromethorphan hydrobromide, for the study. Collaborations with pharmaceutical companies are essential in research as they supply necessary compounds and support the development of new therapeutic formulations.
12) Male:
Male refers to the gender of the healthy volunteers participating in the study. The selection of a homogeneous group helps eliminate variability related to sex, ensuring that pharmacokinetic results can be accurately attributed to the drug's formulation rather than differences between genders.
13) Life:
Life signifies the fundamental objective of pharmacological research — to improve life quality through effective medications. The study's focus on pharmacokinetics aims to optimize treatment protocols, which could lead to better management of conditions like cough and anxiety.
14) Measurement:
Measurement indicates the process of quantifying specific pharmacokinetic parameters such as Cmax and Tmax. It is vital to ensure these metrics are defined accurately for comprehensive drug profiling and understanding the pharmacological profile of dextromethorphan.
15) Discussion:
Discussion refers to the section of the article where study results are interpreted and implications are drawn. This part is crucial for placing findings in the context of existing literature, acknowledging limitations, and suggesting future research avenues.
16) Relative:
Relative in this case highlights the importance of comparative analysis between the sustained-release and immediate-release forms of dextromethorphan. Understanding the relative pharmacokinetic profiles aids in assessing the benefits and drawbacks of different drug formulations.
17) Gujarat:
Gujarat indicates the specific region in India from where the internal standard Losartan potassium was sourced. Regional sourcing is important for ensuring standardized supplies in research and can reflect localized pharmaceutical capabilities and regulatory environments.
18) Mysore:
Mysore is mentioned as the location associated with the research facilitator, His Holiness Jagadguru Sri Sri Shivarathree Deshikendra Mahaswamigalavaru, reflecting the involvement of local institutions in supporting scientific research efforts within the pharmaceutical field.
19) Purity:
Purity refers to the quality of the substances used in the study, particularly regarding the dextromethorphan hydrobromide. High purity is vital for ensuring the reliability of research findings and confirming that results are due solely to the drug under investigation.
20) Nature:
Nature may refer to the intrinsic qualities and behaviors of drugs, particularly in a pharmacokinetic context. Understanding the nature of how a drug acts within biological systems is fundamental to developing effective therapeutics and understanding their effects on patients.
21) Medium:
In this context, medium could also pertain to the means through which pharmacokinetic data is collected and analyzed. It indicates the tools and methodologies employed to evaluate drug metabolism and pharmacodynamics within human subjects.
22) Rajan:
Rajan refers to one of the authors associated with the study, indicating a collaborative effort in the research process. Author collaboration is essential in science to combine expertise and enhance the comprehensiveness of pharmacological investigations.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Pharmacokinetics of once-daily and immediate-release dextromethorphan.’. Further sources in the context of Science might help you critically compare this page with similair documents:
Statistical analysis, Oral administration, High performance liquid chromatography, Bioavailability, Stability study, Dosage form, Sustained release, Healthy volunteers, Declaration of Helsinki, Solid-phase extraction, Calibration curve, Pharmacological profile, Sustained release tablet, Dosing regimen, Serum sample.