Metoprolol succinate-HCTZ sustained release matrix tablet development.
Journal name: World Journal of Pharmaceutical Research
Original article title: Development and evaluation of metoprolol succinate microparticle-hydrochlorothiazide sustain release matrix tablet
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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Prajakta A. Ahire, Harshada Deoghare, Rajendra Surawase, Avish Maru
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Development and evaluation of metoprolol succinate microparticle-hydrochlorothiazide sustain release matrix tablet
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Doi: 10.20959/wjpr20166-6428
Download the PDF file of the original publication
Summary of article contents:
Introduction
The study conducted by Ahire et al. focuses on the development and evaluation of a sustained release matrix tablet combining Metoprolol succinate and Hydrochlorothiazide using ethyl cellulose-based microparticles. Metoprolol succinate is an antihypertensive agent, and Hydrochlorothiazide is used in combination to enhance therapeutic efficacy. The primary aim of this research is to create a drug delivery system that effectively maintains therapeutic drug levels while reducing the frequency of administration, thereby improving patient compliance.
Importance of Sustained Release Systems
A significant aspect of the study is the utilization of sustained release systems through the formulation of microparticles. These systems offer numerous advantages for drugs with narrow therapeutic windows or those that are eliminated from the body quickly. The sustained release characteristics of the developed microparticles allow for a more uniform drug distribution throughout the gastrointestinal tract, thus minimizing the risk of gastric irritation and ensuring that the drug concentrations remain within the therapeutic range. The study demonstrates that the microparticles produced via solvent evaporation showed desirable properties, confirming their potential role in sustained drug delivery.
Preparation Techniques and Optimization
The research highlights a meticulous preparation process using the solvent evaporation method to create the microparticles of Metoprolol succinate. This method forms a water-in-oil-in-water (w/o/w) emulsion, which is essential for the encapsulation of the drug in the polymer matrix. The study emphasizes the influence of different polymer ratios on the encapsulation efficiency and drug release rates. The optimization of the formulation leads to a drug-polymer ratio of 1:3 being identified as the most effective, resulting in microparticles that demonstrated enhanced sustained release capabilities.
Evaluation of Physical Properties
In addition to drug release characteristics, the study evaluates the physical properties of the microparticles, such as particle size, yield percentage, and micromeritic studies. These evaluations indicate good flow properties, which are essential for the subsequent tableting process. The effects of different excipients on the formulation are also assessed, identifying optimal concentrations for enhancing disintegration time and dissolution rates. The study's results indicate a successful correlation between optimized processing parameters and improved tablet performance.
Conclusion
In conclusion, the research by Ahire et al. highlights the effective formulation of sustained release matrix tablets that combine Metoprolol succinate and Hydrochlorothiazide through the use of ethyl cellulose microparticles. The findings showcase the successful application of the solvent evaporation technique and the significance of optimizing formulation parameters to achieve desirable drug release profiles. Overall, the study contributes to the understanding of sustained release systems and their potential to enhance therapeutic outcomes in antihypertensive medication administration. The optimized formulation demonstrated stability over two months under specific storage conditions, affirming its potential for future clinical applications.
FAQ section (important questions/answers):
What is the main focus of the study conducted?
The study focuses on developing and evaluating Metoprolol succinate microparticle-Hydrochlorothiazide sustained release matrix tablet, emphasizing its formulation, characteristics, and release behavior.
How are the microparticles prepared in this study?
Microparticles are prepared using the solvent evaporation method involving creating an emulsion with drug and polymer solutions, leading to the formation of solid microspheres after solvent evaporation.
What advantages does the combination therapy offer?
Combination therapy can reduce dose-related risks, minimize side effects, and enhance therapeutic outcomes compared to monotherapy, particularly when using antihypertensive agents like Metoprolol and Hydrochlorothiazide.
What methods are used to evaluate the microparticles?
Micromeritic properties, percentage yield, drug loading efficiency, and in vitro drug release studies are among the evaluation methods used to assess microparticle quality and performance.
What was the optimal drug to polymer ratio found?
The study found that a drug to polymer ratio of 1:3 for Metoprolol succinate and ethyl cellulose yielded the best sustained release characteristics among various formulations tested.
What conclusion can be drawn from the study's results?
The study concludes that the solvent evaporation technique is effective for microencapsulating Metoprolol succinate, producing stable sustained release formulation suitable for antihypertensive therapy.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Metoprolol succinate-HCTZ sustained release matrix tablet development.”. 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) Drug:
The word 'Drug' refers to an active substance administered to induce a therapeutic effect, typically in treating diseases or conditions. In the context of the study, Metoprolol succinate and Hydrochlorothiazide are highlighted as antihypertensive agents, showcasing their importance in pharmacology and drug delivery systems for maintaining health.
2) Table:
The term 'Table' pertains to the structured presentation of data and information, usually comprised of rows and columns. In this study, tables are utilized to summarize formulations, compositions, and evaluation results, aiding clarity and comprehension of experimental outcomes, facilitating quick reference for researchers and readers.
3) Study (Studying):
The word 'Study' signifies systematic investigation, particularly into drug formulations and their results. In the research, it encapsulates the examination of Metoprolol succinate microparticles and their sustained release characteristics, contributing original knowledge to pharmaceutical sciences through rigorous analysis and data collection.
4) Medium:
The term 'Medium' often denotes a substance through which activities occur, especially in scientific experiments. In this study, it references the dissolution media used during drug release tests, demonstrating how the drug interacts with its environment, crucial for understanding bioavailability and release kinetics.
5) Water:
'Water' serves as a universal solvent in pharmaceutical formulations and is used extensively in various methods described, including the preparation of microparticles and the dissolution medium. Its role is critical as it enhances solubility and facilitates chemical reactions and drug release processes in the gastrointestinal tract.
6) Surface:
'Surface' refers to the outer layer or boundary of microparticles in this research. The investigation into surface morphology reveals crucial information about the physical characteristics and behavior of the microparticles in the body, influencing drug release rates and patient response to the medication.
7) Manur:
Manur is indicative of the geographic location where the research was conducted, specifically related to Loknete Dr. J.D. Pawar College of Pharmacy. This local context may contribute to the educational environment and availability of resources, impacting the studies’ feasibility and relevance to regional healthcare needs.
8) Nashik:
'Nashik' is a city in India where the research institution is located. It provides context about the cultural and administrative backdrop of the research facility, potentially influencing local healthcare practices and access to pharmaceutical education, ultimately affecting the types of studies and developments undertaken.
9) Nature:
The term 'Nature' often relates to the inherent characteristics of materials, such as the physical and chemical properties of the microparticles discussed. Understanding the nature of drug carriers and excipients is essential for optimizing drug delivery systems and ensuring effective and safe therapeutic outcomes.
10) Maru:
'Maru' refers to a specific individual, presumably a team member involved in the research or administration at Loknete Dr. J.D. Pawar College of Pharmacy. This highlights the importance of collaboration and mentorship in academic research endeavors, fostering an environment conducive to scientific exploration and discovery.
11) Biodegradable:
The term 'Biodegradable' describes materials capable of being broken down by natural processes, relevant to the study regarding the use of ethyl cellulose. This property is significant for drug delivery systems, minimizing environmental impact and enhancing safety and tolerability in patients as the materials degrade in the body.
12) Observation:
'Observation' involves closely monitoring results or behaviors during experiments. In this context, observations of drug release rates and microparticle characteristics are fundamental to understanding the effectiveness of the formulations, contributing valuable insights that guide further research and the development of optimized drug delivery systems.
13) Discussion:
The word 'Discussion' refers to the section of a research paper where findings are interpreted and implications are explored. Here, it is vital for contextualizing results in light of existing literature, addressing limitations, and suggesting future research avenues, thereby advancing the understanding of drug formulation strategies.
14) Irritation:
'Irritation' pertains to adverse reactions that may be caused by some drugs when they reach particular sites in the body. The significance of minimizing gastric irritation through controlled release formulations is emphasized, showcasing the importance of regional drug delivery systems in improving patient tolerance and adherence.
15) Crushing:
'Crushing' in this study refers to the mechanical process of breaking down microparticles to evaluate drug loading and entrapment efficiency. This is crucial for assessing the bioavailability of the drug, determining how much of the active ingredient is retained within the carrier and available for therapeutic action.
16) Balaji:
'Balaji' denotes a specific drug supplier mentioned within the context of the study. It reflects the significance of collaborations and partnerships with suppliers in the pharmaceutical industry, aiding researchers in accessing high-quality materials essential for experimental integrity and success in formulation development.
17) Ajanta (Ajamta):
'Ajanta' refers to a pharmaceutical company that provided the drug samples for the study. The mention highlights the critical role of industry partnerships in academic research, facilitating access to vital materials and enhancing the relevance of the research being conducted in real-world applications.
18) Blood:
The word 'Blood' relates to the physiological system that transports drugs to their site of action once administered. Understanding the pharmacokinetics and therapeutic ranges in relation to blood concentration is fundamental for developing effective drug delivery systems that ensure both efficacy and safety for patients.
19) Wall:
'Wall' typically refers to the outer structure of microparticles in this context. The characteristics of the polymeric wall are crucial for controlling the rate of drug release, impacting the overall performance of the drug delivery system and the pharmacological effects experienced by the patient.