Multilayer tablets of naproxen and esomeprazole: design and studies.
layer by layer tablet technology
Journal name: World Journal of Pharmaceutical Research
Original article title: Design, preparation, evaluation, compatibility and invitro studies of naproxen and esomeprazole multilayer tablets
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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Subtitle: layer by layer tablet technology
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Irin Dewan, Sadiya Afrose Jahan, Mahjabeen Gazi, Joydeb Nath, Md. Asaduzzaman, Maksud Al- Hasan
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Design, preparation, evaluation, compatibility and invitro studies of naproxen and esomeprazole multilayer tablets
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Copyright (license): WJPR: All rights reserved
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Summary of article contents:
Introduction
The study focuses on developing a novel multilayer tablet formulation combining naproxen, a nonsteroidal anti-inflammatory drug (NSAID), and esomeprazole, a proton pump inhibitor, through a layer-by-layer tableting method. This approach aims to achieve both immediate and delayed drug release, allowing for enhanced therapeutic outcomes and improved patient compliance. The formulation utilizes various polymers as enteric coating agents to prevent the premature release of naproxen in the acidic environment of the stomach while ensuring the immediate release of esomeprazole to mitigate gastric acidity.
Layer by Layer Technology
One of the key concepts presented in this study is the "layer by layer" technology used in tablet formulation. This method involves the sequential addition of layers, with the naproxen core being coated with esomeprazole. The multilayer design allows for the integration of immediate release and controlled release dosing in a single tablet. The study highlighted the advantages of this technology, including the ability to avoid incompatibility between different active pharmaceutical ingredients (APIs), optimize pharmacokinetic profiles, and enhance the drug's stability. The results demonstrated that this innovative formulation method can facilitate the creation of fixed-dose combinations that improve patient adherence.
Physicochemical Stability of Esomeprazole
Another significant aspect explored in the research is the physicochemical stability of esomeprazole within the multilayer tablet. Esomeprazole is known to degrade rapidly in acidic conditions; therefore, the formulation's design incorporated an enteric coating that protects the drug from being released in the stomach. The study evaluated various polymers for their efficacy in creating an optimal enteric environment, ultimately identifying formulations that significantly reduced drug release in acidic media while allowing a substantial release in alkaline conditions. This controlled release mechanism was crucial to ensure that esomeprazole effectively suppresses gastric acid secretion prior to the administration of naproxen.
Drug Release Kinetics
The study also examined the kinetics of drug release from the formulated tablets, utilizing various models such as zero-order, first-order, and Higuchi equations to analyze release mechanisms. The findings indicated that the drug release from the multilayer tablets followed a non-Fickian diffusion mechanism, suggesting that the release rate was influenced by both the drug concentration and the formulation components. The mean dissolution times calculated for the various formulations provided insight into how different combinations of polymers affected the drug release profiles, emphasizing the importance of formulation optimization in achieving desired therapeutic effects.
Conclusion
The research highlights the successful development of a multilayer tablet combining naproxen and esomeprazole, elucidating the considerable benefits of the layer by layer technology in pharmaceutical formulations. The study confirms that this innovative approach not only enhances the stability and bioavailability of the drugs but also offers significant improvements in patient compliance and therapeutic efficacy. By effectively addressing the challenges associated with NSAID-induced gastric damage, this combination product represents a promising advancement in the realm of targeted drug delivery systems. Future work could focus on further refining the formulation parameters and conducting clinical evaluations to validate the findings in practical scenarios.
FAQ section (important questions/answers):
What was the purpose of the study on naproxen and esomeprazole?
The study aimed to design and prepare a combination product of naproxen and esomeprazole tablets using layer by layer tableting technology for optimal release profiles and improved patient compliance.
What materials were used for the enteric coating?
Enteric coatings utilized shellac, cellulose acetate phthalate, methacrylic acid copolymers, polyvinyl acetate phthalate, and hypromellose phthalate to ensure delayed action of naproxen and protect esomeprazole.
What advantages do multilayer tablets provide in drug delivery?
Multilayer tablets allow for controlled and immediate drug release, avoid incompatibility between active ingredients, reduce costs, enhance stability, and provide improved pharmacokinetic profiles for effective therapies.
How does the combination of naproxen and esomeprazole benefit patients?
This combination helps provide pain relief from naproxen while reducing the risk of gastric ulcers, thus improving patient compliance and safety.
What tests were performed to evaluate the tablet formulations?
The formulations were tested for flow properties, hardness, thickness, friability, disintegration time, and dissolution studies to assess their effectiveness and compatibility.
What were the findings regarding drug release mechanisms?
The analysis indicated that drug release followed various kinetics, with most formulations aligning with zero-order release, suggesting drug release was independent of concentration and involved diffusion and erosion.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Multilayer tablets of naproxen and esomeprazole: design and studies.”. 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:
A drug is a chemical substance used to diagnose, treat, or prevent diseases. In the context of the study, drugs like naproxen and esomeprazole are analyzed for their therapeutic effects and interactions. The study focused on developing a drug delivery system that combines both medications to enhance efficacy and reduce gastrointestinal side effects.
2) Table:
Table in this context refers to the tablet formulation created for delivering naproxen and esomeprazole. The study employs layer-by-layer technology to create a multi-layer tablet, optimizing the release profiles of the drugs. The physical attributes of these tablets—such as size, hardness, and dissolution time—are crucial for their effectiveness.
3) India:
India is significant in this research as many of the excipients and polymers used in the tablet formulation were sourced from Indian suppliers. Moreover, the pharmaceutical industry in India plays a vital role globally, and studies conducted there contribute to advancing drug delivery technologies and healthcare solutions for various ailments.
4) Water:
Water is an essential solvent used in the preparation of drug formulations, particularly during the granulation and coating processes. It serves as a medium for dissolving excipients and facilitates drug layering. The quality of water impacts the solubility and stability of the compounds within the tablets.
5) Study (Studying):
The study refers to the extensive research and experimentation conducted to develop a dual-layer tablet for the simultaneous delivery of naproxen and esomeprazole. This research investigates the formulation, preparation methods, and evaluation of the tablet's performance, focusing on its release kinetics and compatibilities.
6) Surface:
Surface in this study pertains to the physical characteristics of the tablets, particularly the smoothness and coating quality of the layers. The surface properties influence how the tablet interacts with the gastrointestinal tract, affecting drug release and absorption rates, subsequently impacting therapeutic outcomes.
7) Post:
Post refers to the phase of the study dealing with the evaluation of the tablets after they have been manufactured. This includes assessing the physical properties, drug release profiles, and overall performance of the multi-layer tablets, which are critical for ensuring the quality and efficacy of the final product.
8) Powder:
Powder is a term used for the solid state of the active pharmaceutical ingredients and excipients before compression into tablets. The powder characteristics, such as flowability and particle size, influence the granulation process and the final tablet quality, highlighting the importance of optimizing these parameters in tablet formulation.
9) Ulcer:
An ulcer is a sore that develops on the lining of the stomach or intestines, often caused by prolonged use of NSAIDs like naproxen. The study aims to create a formulation that reduces the risk of gastric ulcers while providing effective pain relief, addressing the critical need for safer drug delivery options.
10) Cina:
China is relevant in this study because many manufacturing equipment and excipients used, such as fluid bed dryers and coating machines, originated from Chinese suppliers. The globalization of pharmaceutical manufacturing emphasizes partnerships across borders for advancing drug formulation technologies and improving patient care.
11) Colouring (Coloring):
Coloring refers to the application of colorants in the final tablet formulation. This enhances the aesthetic appeal of the tablets, making them more recognizable and acceptable to patients. Moreover, coloring agents may provide protective qualities to the tablet surface, shielding it from environmental factors that could degrade the active ingredients.
12) Medium:
Medium is a term that describes the dissolution conditions used during the drug release study, which typically involves different pH buffers to mimic the gastro-intestinal environment. The choice of medium is vital as it impacts the dissolution behavior of the tablet, helping to predict therapeutic efficacy in actual patient scenarios.
13) Discussion:
Discussion denotes the analytical part of the study where findings are interpreted and implications are drawn. It involves evaluating the results in the context of existing literature, offering insights into the application of the formulated tablets for clinical use, and exploring potential modifications for future research.
14) Toxicity:
Toxicity pertains to the harmful effects a drug can have on the body, especially concerning the gastrointestinal system in this study. The combination of naproxen and esomeprazole aims to minimize toxicity while providing effective pain management, addressing the critical need for safer NSAID options in treatment regimes.
15) Reason:
Reason in this context refers to the justification for combining naproxen and esomeprazole into a single tablet formulation. The study aims to provide an effective treatment for pain while reducing the risk of gastric damage caused by NSAIDs, addressing patient compliance issues with co-therapy for ulcer prevention.
16) Sugar:
Sugar may refer to the excipients that have sugar-like properties used in tablet formulations, such as binders or fillers. While not a direct focus of the study, sugars can enhance the palatability of the tablets or help in the formulation’s overall stability and release characteristics.
17) Pain:
Pain is the primary condition targeted by the formulation of naproxen—a nonsteroidal anti-inflammatory drug (NSAID) that provides analgesic effects. The study seeks to optimize the delivery of naproxen in combination with esomeprazole to ensure effective pain management while minimizing adverse gastrointestinal effects.
18) Hand:
Hand can sometimes refer to the handling and manipulation of materials during the tablet formulation process. In this context, it emphasizes the precision required in the preparation phases and the careful attention to avoid contamination or degradation risks for the active ingredients and excipients.
19) Life:
Life pertains to the overall quality of life improvements that can arise from effective pain management with reduced side effects from medications. The goal of this study ultimately aims to enhance patient experiences and adherence to treatment regimens for chronic pain conditions through innovative drug formulations.
20) Rheumatoid arthritis:
Rheumatoid arthritis is a chronic inflammatory disorder that can cause joint pain and damage. The relevance of this condition in the study arises from the need for effective pain relief therapies, as NSAIDs like naproxen are commonly prescribed for managing symptoms associated with rheumatoid arthritis, emphasizing the importance of safe formulations.
21) Accumulation (Accumulating, Accumulate):
Accumulation in the study context refers to the build-up of drug concentrations in the body or specific tissues, which can lead to toxicity. The formulated tablet aims to manage the release rate and maintain therapeutic levels without unnecessary accumulation, ensuring efficacy alongside safety in chronic treatment applications.
22) Inflammation:
Inflammation is a key physiological process implicated in conditions that naproxen treats. The study emphasizes the importance of combining drugs such as naproxen with esomeprazole, focusing on their roles in managing inflammation while also considering the gastrointestinal side effects commonly associated with NSAIDs.
23) Performance:
Performance relates to how well the formulated tablets release their active ingredients within specified timeframes under controlled conditions. The study rigorously evaluates tablet performance to ensure they meet desired dissolution profiles, ensuring therapeutic effectiveness and patient compliance in pain management strategies.
24) Observation:
Observation refers to the systematic assessment of the formulation process, including monitoring physical and chemical properties during and after tablet preparation. The authors documented various observations throughout experimentation, crucial for validating the stability and effectiveness of the multilayer drug delivery system developed in the study.
25) Transformation (Transform, Transforming):
Transform pertains to the technological advancements and changes in pharmaceutical manufacturing processes that have aided in producing complex dosage forms. This study reflects the transformation of traditional tablet formulations into innovative multilayer systems that enhance drug delivery and minimize adverse effects, representing progress in drug development.
26) Bleeding:
Bleeding is a serious adverse effect associated with the prolonged use of NSAIDs, such as naproxen. The study carries significant implications for the reduction of gastric bleeding risks through the combination of esomeprazole, focusing on creating a safer treatment option while still effectively managing pain and inflammation.
27) Disease:
Disease refers to any abnormal condition affecting bodily functions, including chronic conditions treated with naproxen. The study aims to provide effective therapeutic solutions for diseases that require pain management without the adverse effects of conventional NSAID treatment paradigms, addressing gaps in current pharmaceutical care.
28) Nature:
Nature relates to the inherent qualities or attributes of the drugs used in the study, such as their chemical properties and mechanisms of action. Understanding the nature of naproxen and esomeprazole allows researchers to optimize the formulation, ensuring compatibility and effective drug delivery in a combined dosage form.
29) Salt (Salty):
Salt refers to ionic compounds typically used as pharmaceutical excipients in drug formulation. In this study, the term includes esomeprazole as magnesium salt, emphasizing its importance for stability and absorption under specific pH conditions, ultimately enhancing the efficacy of the formulated multi-layer tablets.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Multilayer tablets of naproxen and esomeprazole: design and studies.’. Further sources in the context of Science might help you critically compare this page with similair documents:
Physical appearance, Therapeutic effect, Adverse effect, Granulation process, Drug Absorption, Drug delivery system, Combination therapy, Controlled release, Disintegration time, Gastric ulcer, Compressibility index, Nonsteroidal anti-inflammatory drug, Long-term safety, Clinical safety, Proton Pump Inhibitor, Patient compliance, Gastric mucosa, Carr's Index, FTIR Spectroscopy, UV Spectrophotometer, Phosphate buffer, Gastric acid secretion, Fixed Dose Combination, Pharmacokinetic profile, Mathematical Model, Controlled Release Delivery System.
Concepts being referred in other categories, contexts and sources.