Development and evaluation of floating bilayer tablet of baclofen
Journal name: World Journal of Pharmaceutical Research
Original article title: Development and evaluation of floating bilayer tablet of baclofen
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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Ritul B. Gabani, Dr. H. M. Tank and Nikunj Gabani
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Development and evaluation of floating bilayer tablet of baclofen
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Doi: 10.20959/wjpr20168-6744
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Summary of article contents:
Introduction
This study focuses on the development and evaluation of a floating bilayer tablet formulation of baclofen, a medication used primarily for muscle spasticity. The formulation comprises two distinct layers: an immediate release layer and a sustained-release layer. The immediate release layer is designed to ensure the rapid delivery of baclofen to achieve effective plasma concentrations, while the sustained-release layer allows for prolonged drug release over several hours. The incorporation of gas-generating agents like sodium bicarbonate and citric acid in the sustained-release layer enables the tablets to float in the gastric environment, improving bioavailability and retention time.
Role of Polymers in Sustained Release
One crucial aspect of the formulation is the selection of polymers, specifically hydrophilic natural polymers such as xanthan gum, guar gum, and pectin. Among these, xanthan gum exhibited the best performance in sustaining drug release over a 24-hour period, achieving a maximum drug release of 99.10%. The study demonstrated that the concentration of xanthan gum directly affects the drug release profile; as the concentration increased, the rate of drug release initially improved but later decreased at higher concentrations due to the formation of a more viscous gel matrix surrounding the drug. This illustrates the importance of optimizing polymer concentration in controlled-release formulations.
Importance of Superdisintegrants
In the formulation, various superdisintegrants were assessed, including crospovidone, sodium starch glycolate (SSG), and croscarmellose sodium. Crospovidone was identified as the most effective for the immediate release layer, achieving the fastest disintegration time of 15.10 minutes, compared to longer times for SSG and croscarmellose sodium. The selection of an appropriate superdisintegrant is vital for ensuring that the immediate release layer dissolves quickly, facilitating the rapid release of the active pharmaceutical ingredient (API) into the gastrointestinal tract.
Evaluation and Optimization of Formulations
The study employed a 3² factorial design to systematically evaluate the effect of varying the amounts of xanthan gum and sodium bicarbonate on the floating characteristics and drug release profiles of the tablets. The analysis resulted in nine formulations, with batch F5 demonstrating the most optimal characteristics, including a cumulative drug release of 98.90% over 24 hours and a total floating time of 24 hours. These results reaffirmed the importance of experimental design in optimizing formulation parameters to meet therapeutic needs.
Conclusion
Ultimately, this research successfully developed a floating bilayer tablet formulation of baclofen that enhances drug delivery through a gastroretentive system. The use of suitable polymers and superdisintegrants played a critical role in achieving desired drug release profiles and maintaining tablet buoyancy. The findings suggest that formulations designed in accordance with systematic optimization strategies can improve patient compliance and therapeutic effectiveness. Through this work, the potential for better management of conditions requiring baclofen therapy is significantly advanced, highlighting the importance of formulation science in pharmaceutical development.
FAQ section (important questions/answers):
What is the objective of developing a bilayer tablet of baclofen?
The objective is to create a floating bilayer tablet that offers both immediate and sustained release of baclofen, utilizing gas-generating agents for gastric retention and various natural polymers for controlled release.
What materials were used in the formulation of the tablets?
Key materials included baclofen, xanthan gum, crospovidone, sodium bicarbonate, citric acid, and various excipients to enhance drug release and stability in tablet formulations.
How was the release of baclofen evaluated in this study?
The release was evaluated through in vitro dissolution studies, assessing cumulative drug release over time in a controlled environment, using parameters such as buoyancy and disintegration time.
Why is baclofen suitable for a sustained release formulation?
Baclofen has a short half-life and is well-absorbed in acidic conditions, making it an ideal candidate for sustained release to improve therapeutic effectiveness while minimizing fluctuations in plasma concentration.
What results were achieved in the final optimized formulation?
The optimized formulation, batch F5, showed a cumulative drug release of 98.90% over 24 hours, with excellent buoyancy time and stability, confirming its potential for gastro-retentive delivery.
What polymers are effective for sustained drug release in this study?
Xanthan gum was found to be the most effective hydrophilic polymer for sustained drug release, yielding better drug retention and release profiles in the bilayer tablet formulation.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Development and evaluation of floating bilayer tablet of baclofen”. 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:
In the context of the study, the term 'Drug' refers specifically to Baclofen, a muscle relaxant used to treat conditions such as spasticity. The research focuses on formulating a floating bilayer tablet of Baclofen, highlighting its properties, effectiveness, and stability in sustained release and immediate release forms for improved patient compliance and therapeutic outcomes.
2) Table:
The word 'Table' relates to both the physical dosage form prepared in the experiment and the tabular data presented throughout the study. It emphasizes the organization and structured presentation of results, such as formulation compositions, evaluation parameters, or in vitro dissolution data, facilitating easy interpretation and comparison of experimental outcomes.
3) Study (Studying):
'Study' indicates the comprehensive research and experimental procedures undertaken to develop the floating bilayer tablet of Baclofen. This term encapsulates the outlined objectives, methods, results, and analyses that aim to provide novel insights into drug delivery systems, enhancing understanding of formulation techniques and implications for clinical applications.
4) Powder:
In pharmaceutical sciences, 'Powder' represents the form in which active pharmaceutical ingredients and excipients are processed before tableting. This term pertains to the particle size, flow properties, and compressibility of the powdered materials, which are critical in ensuring uniformity and efficacy in the eventual formulation of the floating bilayer tablets.
5) Medium:
'Medium' refers to the dissolution medium used in the experiments, predominantly 0.1 N HCl or simulated gastric fluids. The choice of medium is vital for mimicking physiological conditions, enabling accurate assessments of the drug release profile and buoyancy properties, thus determining the potential effectiveness of the final dosage form in a real-world setting.
6) Gujarat:
Gujarat is the region in India where the Manavar College of Pharmacy is located, the institution responsible for conducting this study. Its mention not only contextualizes the research geographically but also highlights the regional capabilities and contributions to pharmaceutical sciences, particularly in drug formulation and development research.
7) Maruti:
'Maruti' refers to one of the suppliers of excipients and chemicals used during the formulation process. The identification of specific material suppliers is pertinent to the study as it underscores the sourcing of quality ingredients necessary for producing effective pharmaceutical formulations, thus ensuring consistency and efficacy in the final products.
8) Glass:
The term 'Glass' relates to various lab equipment such as beakers and test tubes used during the experiments, and also to the Thiele tube mentioned, which is specifically utilized for melting point determination. It signifies the importance of appropriate laboratory materials for achieving accurate measurements and maintaining sterility in pharmaceutical development.
9) Heap:
'Heap' may refer to the heap of powdered materials during the pouring and mixing phases of tablet formation. Conceptually, it pertains to the physical state of powders and the methods employed to assess the flowability and angle of repose, both critical for ensuring proper mixing and eventually successful tablet compression.
10) Measurement:
'Measurement' encompasses the various quantitative analyses performed throughout the study, such as weight, hardness, disintegration time, and drug release profiles. Accurate measurements are essential for evaluating the properties and performance of the formulated tablets, guiding the optimization process of the floating bilayer drug delivery systems.
11) Discussion:
The term 'Discussion' pertains to the section of the study where findings are interpreted, compared with existing literature, and implications are drawn. This critical part of research enables insights into the relevance of data, future research directions, and practical applications of the developed formulations in clinical settings.
12) Drowsiness:
'Drowsiness' refers to a common side effect of Baclofen that can lead to patient noncompliance. The study addresses this issue by aiming to develop a sustained release formulation, potentially minimizing side effects and improving usability for patients experiencing muscle spasticity through better pharmacokinetics and adherence.
13) Dividing:
The term 'Dividing' provides context to the formulation of bilayer tablets, which includes the immediate release and sustained release layers. This concept emphasizes the strategic separation in the drug release profile within the tablet, crucial for achieving desired therapeutic effects over desired periods while ensuring effective plasma concentration.
14) Relative:
'Relative' contextually refers to the comparison of Baclofen's bioavailability when administered via different routes, highlighting the relevance of dosage forms. Understanding the relative effectiveness helps inform formulation choices aimed at optimizing drug delivery systems that maintain therapeutic levels over extended periods while addressing patient needs.
15) Heating:
'Heating' indicates processes used during the melting point determination or preparation stages. The significance of controlled heating in pharmaceutical formulations is crucial, as it affects the melting behavior of excipients and active ingredients, which can subsequently impact the physical properties and the stability of the final dosage forms.
16) Pouring:
'Pouring' in this context refers to the handling of powdered ingredients during tablet preparation. This step is critical in mixing processes and influences the uniformity of the formulation. Proper pouring techniques are necessary to ensure a homogenous blend of active and inactive components, vital for effective drug delivery.
17) Surface:
'Surface' relates to the physical characteristics of the tablets, including texture and morphology, which can influence the adhesive properties and release rates. Understanding and controlling surface characteristics are important in the formulation process, as they affect the tablet's interaction with the dissolution medium and consequently its performance.
18) Company:
The word 'Company' pertains to the entities such as manufacturers or suppliers of materials used in the formulation. It emphasizes the collaborative nature of pharmaceutical research, as quality and reliable sourcing can dramatically impact the development and performance of the drug formulations within the study.
19) Sama (Shama):
'Sama' refers to one of the manufacturers providing certain excipients used in the study. Identifying specific suppliers highlights the importance of sourcing quality materials for pharmaceutical formulations, where product quality directly affects the efficacy and consistency of the developed dosage forms.
20) Tank:
'Tank' is relevant in the context of the hardening of tablets and possibly pertains to equipment used in the manufacturing process for batching and stability testing. Proper handling and methodology in tank operations are vital in ensuring that pharmaceutical products meet the desired quality standards and specifications.
21) Life:
'Life' in this context may allude to the concept of 'drug life' or shelf-life, which is an important consideration in formulation sciences. The study's relevance lies in extending the effective therapeutic duration of Baclofen through innovative formulations that allow better patient management and drug availability over time.
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