Formulation and evaluation of modified release tablet of donepezil hydrochloride
Journal name: World Journal of Pharmaceutical Research
Original article title: Formulation and evaluation of modified release tablet of donepezil hydrochloride
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. Patel Bhavik N., Patel Devyani B., Dr. Patel Chhagan N.
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Formulation and evaluation of modified release tablet of donepezil hydrochloride
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
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Summary of article contents:
Introduction
The research focuses on the development and evaluation of a sustained release matrix tablet of Donepezil hydrochloride, aimed at providing stable and therapeutically effective plasma levels over a 24-hour period while minimizing side effects. Donepezil hydrochloride is a second-generation cholinesterase inhibitor primarily used in the treatment of Alzheimer’s disease. The study emphasizes the advantages of sustained release formulations over immediate release forms, particularly in terms of improved patient compliance due to less frequent dosing and more consistent plasma drug levels.
Importance of Sustained Release Formulations
Sustained release dosage forms are designed to release drugs continuously at predetermined rates, thus allowing for better control of plasma drug levels. This formulation approach not only reduces the frequency of dosing but also decreases side effects, enhances efficacy, and provides a constant delivery system. The study highlighted the transition from immediate release to sustained release formulations as a means to overcome the spikes in plasma drug levels and associated adverse effects. Donepezil Hydrochloride, with its long plasma half-life, serves as a promising candidate for this type of formulation, as it can maintain therapeutic levels more effectively.
Methodology: Development Techniques
The study utilized both direct compression and wet-granulation methods for tablet preparation. Initially, natural polymers such as Guar gum, Xanthan gum, Karaya gum, and Pectin were evaluated through direct compression; however, these did not yield sufficient sustained release. Consequently, the wet-granulation technique was employed, which involved mixing Donepezil HCl with selected polymers and excipients, followed by drying, lubricating, and compressing the resulting granules into tablets. The formulation design also employed a 3² full factorial design to systematically evaluate the impact of polymer concentration and binder ratio on drug release profiles.
Results and Evaluation of Formulations
The evaluation of the matrix tablets revealed significant differences between formulations prepared by both methods. The optimized formulation, designated E7, contained Guar gum and PVP-K30, demonstrating favorable in vitro drug release profiles. The study measured various properties, including weight variation, hardness, friability, and drug content, to ascertain the quality of the tablets. Key findings indicated that the E7 batch not only exhibited a cumulative drug release of 100% at 24 hours but also achieved a similarity factor (f2) of 76.22 when compared to marketed sustained release formulations, affirming its potential efficacy.
Conclusion
The research successfully developed a sustained release matrix tablet of Donepezil hydrochloride using Guar gum as a release-modifying agent. With an optimized formulation (E7) showcasing a desirable drug release profile and high similarity factor, this study meets its primary objective of enhancing patient compliance and therapeutic effectiveness. The findings underscore the importance of formulation techniques and the selection of excipients in developing advanced drug delivery systems for chronic conditions like Alzheimer's disease, paving the way for further research and clinical application.
FAQ section (important questions/answers):
What is the purpose of this research on Donepezil hydrochloride?
The research aimed to develop a sustained release matrix tablet of Donepezil hydrochloride that maintains effective plasma levels over 24 hours while minimizing side effects and improving in-vitro drug release compared to existing formulations.
Which natural polymers were used in the tablet formulation?
The formulation utilized natural polymers such as Guar gum, Xanthan gum, Karaya gum, and Pectin to control the drug release in the sustained release matrix tablet.
How were the matrix tablets prepared and evaluated?
Matrix tablets were prepared using wet granulation technique, followed by evaluation of physicochemical properties, including thickness, hardness, friability, drug content, and in-vitro drug release to assess performance.
What was the significance of the similarity factor (f2) in this study?
The similarity factor (f2) measures the similarity in dissolution profiles between the optimized formulation and marketed formulations. A higher value indicates better release similarity; batch E7 achieved a high similarity factor of 76.22.
What were the key findings about the optimized formulation?
The optimized formulation, batch E7, demonstrated a 100% drug release in 24 hours, showcasing effective sustained release characteristics while maintaining stability under accelerated conditions.
Why is sustained release formulation beneficial for patients?
Sustained release formulations reduce dosing frequency and increase patient compliance by maintaining consistent therapeutic plasma levels, which can enhance overall treatment efficacy and reduce side effects.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Formulation and evaluation of modified release tablet of donepezil hydrochloride”. 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 term 'drug' refers to a chemical substance used for the diagnosis, treatment, or prevention of a disease. In the context of this study, Donepezil hydrochloride is the drug of focus, specifically formulated for sustained release to effectively manage Alzheimer's disease while minimizing side effects.
2) Table:
In the research, 'table' denotes the various matrix tablet formulations created through different methods such as direct compression and wet granulation. Each table outlines specific formulation components, sizes, and evaluations, contributing to the understanding of design optimization for delivering Donepezil hydrochloride.
3) Similarity:
The term 'similarity' pertains to the comparison of dissolution profiles between the newly formulated tablets and existing marketed formulations. The similarity factor (f2) is a statistical measure that indicates how closely the release pattern matches, targeting consistency in therapeutic efficacy with reduced side effects.
4) India:
India is significant as the geographical location of the research, indicating that the pharmaceutical formulations and techniques utilized are influenced by regional standards, regulations, and access to materials. The research was conducted at the Shri Sarvajanik Pharmacy College in Gujarat, India.
5) Study (Studying):
The word 'study' represents the systematic investigation carried out to evaluate the formulation, development, and optimization of a sustained release matrix tablet of Donepezil hydrochloride. This comprehensive approach includes material selection, preparation methods, and evaluation of release mechanisms over a specified duration.
6) Water:
Water is crucial in this context as it serves as a solvent and medium in the preparation and evaluation processes. The binder solution specifically utilizes water to create a uniform mass in granulation, and water is a primary component during dissolution testing for drug release.
7) Swelling:
Swelling refers to the process by which polymers in the tablet absorb water and expand, significantly impacting the drug release mechanism. In the study, swelling contributes to controlling the release rate of Donepezil hydrochloride, thereby enhancing therapeutic effectiveness through sustained release.
8) Surface:
The term 'surface' relates to the outer area of tablet formulations, where interactions between the drug and excipients occur. Surface properties can influence the dissolution characteristics and, consequently, the drug release profile, making it a critical factor in tablet design.
9) Patel:
Patel refers to Dr. Patel Bhavik N., the lead author of the research. His expertise and leadership in the study are vital for ensuring the rigorous scientific methodology employed in formulating and evaluating the sustained release matrix tablets.
10) Medium:
In pharmaceutical contexts, 'medium' describes the environment in which drug release and dissolution occur. The medium can affect how the drug is released from the tablet. In this study, the dissolution medium is adjusted to simulate physiological conditions for accurate testing.
11) Shri (Sri, Sr):
The prefix 'Shri' denotes respect and is used to address institutions and authorities in India. It is part of the college name, 'Shri Sarvajanik Pharmacy College,' where the research was conducted, emphasizing the institution's role in advancing pharmaceutical education and research.
12) Transformation (Transform, Transforming):
Transformed describes the change in properties or states during the preparation and evaluation processes of the tablets. This can refer to the change observed in the excepients and the active pharmaceutical ingredient as they undergo granulation and compaction to form a cohesive tablet.
13) Gujarat:
Gujarat is the Indian state where the research was situated. Its relevance lies in the availability of local resources, expertise in pharmaceutical development, and the promotion of regional educational institutions that support cutting-edge pharmaceutical research and innovation.
14) Powder:
In this study, 'powder' describes the form of the drug and excipients prior to tablet formulation. The properties of the powders, such as particle size and flow characteristics, directly influence the efficiency of the granulation process and, ultimately, the quality of the final tablets.
15) Blood:
The term 'blood' relates to the physiological system targeted by Donepezil hydrochloride, as it ultimately aims to attain therapeutic plasma levels for efficacy in treating Alzheimer’s disease. Monitoring drug plasma concentrations is vital for ensuring therapeutic effectiveness while managing potential side effects.
16) Sign:
In this context, 'sign' may refer to indications or symptoms that guide the treatment of Alzheimer's disease with Donepezil. Furthermore, statistical significance in the study results signifies the importance of the findings regarding formulation efficiency and releases profiles.
17) Discussion:
The term 'discussion' represents the segment of the research where findings are interpreted and contextualized within the broader field of pharmaceutical development. It highlights the implications of the results obtained from various trials conducted during the study.
18) Relative:
Relative in this context may indicate the comparison of the newly formulated tablets to existing formulations concerning drug release profiles, efficacy, and side effects. Such comparisons help in establishing the performance of new formulations against established standards.
19) Disease:
Disease refers specifically to Alzheimer's disease in this study. The focus on developing a sustained release tablet form of Donepezil hydrochloride targets the management of this neurodegenerative condition and aims to improve the patient's quality of life by providing effective medication.
20) Glass:
Glass may refer to the physical state of the matrix polymers before they interact with water. The transition from a glassy state to a rubbery state in polymer matrices signifies the absorption of moisture and the beginning of the drug release process.
21) Life:
The word 'life' refers to the aspect of improving the quality of life for patients suffering from Alzheimer’s disease through effective treatment options. The study ultimately aims to develop pharmaceutical solutions that enhance therapeutic benefits and patient compliance.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Formulation and evaluation of modified release tablet of donepezil hydrochloride’. Further sources in the context of Science might help you critically compare this page with similair documents:
Statistical analysis, Experimental design, Stability study, Physicochemical properties, Sustained release, Fourier transform infrared spectroscopy, Preliminary screening, Stability Studies, Pharmaceutical technology, Tablet compression machine, Granules, Wet granulation method, In Vitro Dissolution Study, Direct compression method, Xanthan gum, Controlled release dosage form, Optimized formulation, Polynomial equation, Dissolution profile, Drug content, In vitro drug release, Wet granulation technique, Dissolution media, Regression coefficient, Guar gum, Content uniformity, Fickian diffusion, Response surface plot, Direct compression technique, Matrix tablet, Hydrochloric Acid, Degree of Freedom, Thickening agent, Similarity factor, Drug release mechanism, Dissolution Rate Studies, Sustained release matrix tablet, Humidity chamber, Pectin, Dependent variable, Independent variable, USP Type II, Anomalous non Fickian.