Dual therapy bilayered tablets: diclofenac sodium and esomeprazole.
Journal name: World Journal of Pharmaceutical Research
Original article title: Formulation and evaluation of bilayered tablets of diclofenac sodium and esomeprazole magnesium- a dual therapy for peptic ulcer
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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Pasam Jyothirmayi, Sonti Madhavi and E. Pratap
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Formulation and evaluation of bilayered tablets of diclofenac sodium and esomeprazole magnesium- a dual therapy for peptic ulcer
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Doi: 10.20959/wjpr201612-7416
Copyright (license): WJPR: All rights reserved
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Summary of article contents:
Introduction
The development of bilayered tablets represents an innovative approach in pharmaceutical formulation, allowing the combination of two distinct active pharmaceutical ingredients (APIs) into a single dosage form. The presented study focuses on formulating and evaluating bilayered tablets of Diclofenac Sodium, a nonsteroidal anti-inflammatory drug (NSAID), and Esomeprazole Magnesium, a proton pump inhibitor (PPI), targeting the effective management of peptic ulcers and pain relief. The formulation is designed to utilize a sustained release layer for Diclofenac Sodium coupled with an immediate release layer for Esomeprazole Magnesium, thereby addressing both therapeutic needs in one tablet.
Bilayer Tablet Concept
Bilayer tablets are a type of modified release formulation that comprises two different layers of active substances, each designed to release at different rates. The structure allows for the immediate release of one drug while controlling the release of the second drug over an extended period. This form enhances the convenience of medication for patients who require both medications simultaneously, reducing the frequency of dosing and improving patient compliance. In this formulation, Diclofenac Sodium is formulated as a sustained release component, while Esomeprazole Magnesium serves as the immediate release component. Their synergistic effect can effectively mitigate the side effects typically associated with NSAIDs, particularly the risk of gastrointestinal damage.
Characterization of Granules
The preformulation studies assessed both drugs' properties, including solubility, melting point, and interaction with excipients. It was noted that Esomeprazole Magnesium displayed maximum solubility in methanol, while Diclofenac Sodium was freely soluble in the same solvent. The compatibility of the drug with excipients was established using Fourier-transform infrared spectroscopy (FTIR), indicating no undesirable interactions. Flow properties of the granules were evaluated through parameters such as bulk density, tapped density, and angle of repose, suggesting good flow characteristics essential for uniform tablet compression.
In Vitro Dissolution Studies
Dissolution studies conducted on the bilayered tablets revealed that the immediate release layer of Esomeprazole Magnesium achieved nearly complete release (98-99%) within the first 45 minutes. In contrast, the sustained release layer of Diclofenac Sodium demonstrated a controlled release pattern, with varying times to achieve maximum release depending on the specific formulation. Formulation DF-7, which utilized a combination of HPMC and Xanthan gum, exhibited the most prolonged release, confirming that combining polymers can effectively manage drug release profiles.
Conclusion
The study successfully outlines the formulation and evaluation of bilayered tablets containing Diclofenac Sodium and Esomeprazole Magnesium for dual therapy of peptic ulcers and pain relief. The combination of immediate and sustained release mechanisms within a single dosage form not only enhances therapeutic efficacy but also improves patient adherence to medication regimens. This formulation strategy demonstrates the potential to mitigate NSAID-induced gastric mucosal damage while providing pain management, thus addressing a significant clinical challenge in treating conditions like rheumatoid arthritis and postoperative pain. This innovative approach emphasizes the importance of developing modified release systems for enhanced patient care and therapeutic outcomes.
FAQ section (important questions/answers):
What is the purpose of formulating bilayer tablets?
The primary aim is to combine Diclofenac sodium as a sustained release layer and Esomeprazole magnesium as an immediate release layer to effectively treat peptic ulcers and minimize gastrointestinal side effects.
What techniques were used to create the bilayer tablets?
The sustained release layer of Diclofenac sodium was prepared using the wet granulation technique with specific polymers, while the immediate release layer of Esomeprazole magnesium employed wet granulation with super disintegrants.
What parameters were evaluated for the formulated tablets?
Bilayered tablets were assessed for hardness, friability, thickness, weight variation, disintegration time, and cumulative drug release, ensuring the formulations met the required standards for effective drug delivery.
How did the drug release profiles behave during testing?
The immediate release layer of Esomeprazole magnesium exhibited rapid release, while Diclofenac sodium showed sustained release over time, with the formulations designed to achieve optimal therapeutic effects within 12 hours.
What was the significance of using two different polymers?
Combining HPMC and xanthan gum allowed for more effective control over the release of Diclofenac sodium, managing its release profile and improving overall drug delivery and patient compliance.
What was the conclusion of the study?
The study concluded that bilayer formulations enhance patient compliance and therapeutic outcomes in pain management, significantly reducing the risks of gastrointestinal adverse effects through the simultaneous delivery of both medications.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Dual therapy bilayered tablets: diclofenac sodium and esomeprazole.”. 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 that can alter physiological functions in the body. In this study, Diclofenac sodium and Esomeprazole magnesium are the active pharmaceutical ingredients used to treat peptic ulcers and pain. Their effectiveness in formulation helps improve patient adherence and therapeutic outcomes.
2) Table:
A table, in pharmaceutical terms, refers to a solid dosage form containing a mixture of active ingredients and excipients compressed into a specific shape. In this study, bilayered tablets are utilized to deliver both anti-inflammatory and anti-ulcer medications, optimizing release profiles for therapeutic efficacy.
3) Powder:
Powder is a fine, dry, solid particle that may be used as a form for drug delivery. In this study, the powdered raw materials are processed to form granules and tablets, influencing dissolution characteristics and bioavailability of the drugs involved in the formulation.
4) Krishna (Krsna):
Krishna refers to Krishna District in Andhra Pradesh, India, where the research was conducted at Vikas College of Pharmacy. This geographical reference highlights the regional context in which the study and pharmaceutical formulations are developed, emphasizing local healthcare needs and education.
5) Water:
Water is a common solvent and critical excipient in pharmaceutical formulations. It is used to dissolve active ingredients and excipients during the granulation processes. In this study, the role of water ensures that the mixture achieves the desired consistency for tablet formation and effective drug release.
6) Ulcer:
An ulcer is a sore that develops on the lining of the stomach or duodenum, often due to an imbalance of digestive fluids. This study focuses on dual therapy for managing gastric and duodenal ulcers, providing a clinical background for the formulation of the bilayered tablets.
7) Study (Studying):
A study refers to the systematic investigation to gather knowledge or evaluate hypotheses. In this context, the study aims to formulate and evaluate the efficacy of bilayered tablets combining Diclofenac sodium and Esomeprazole magnesium for improved management of peptic ulcers and pain relief.
8) India:
India is a country where the research was conducted, indicating the local healthcare challenges and the need for effective drug formulations. The socio-economic context of India influences the pharmaceutical development practices aimed at improving treatment options for various medical conditions.
9) Post:
Post denotes the period following a specific event. In this study, it relates to post-operative pain management where effective formulations can alleviate pain and prevent complications like ulcers, emphasizing the importance of tailored pharmacological therapies in surgical recovery.
10) Pain:
Pain is a distressing sensory and emotional experience, often associated with tissue damage. The study investigates effective therapeutic strategies utilizing the combination of Diclofenac sodium for pain relief and Esomeprazole magnesium to prevent gastrointestinal irritation, aiming for holistic patient care.
11) Machilipatnam:
Machilipatnam is a city in Andhra Pradesh, India, which is mentioned as part of the location of Krishna University. This geographical detail emphasizes where the educational and research efforts take place, contributing to the local development of pharmaceutical science.
12) Swelling:
Swelling refers to the increase in size or volume of a mass or body part, often related to drug release in formulations. In this study, swelling indices of bilayer tablets illustrate how the sustained-release layer may affect drug liberation in gastrointestinal conditions.
13) Salt (Salty):
In chemistry, a salt is a product formed from the neutralization reaction of an acid and a base. In this research, the term represents Esomeprazole magnesium, a salt form utilized for better solubility and absorption, crucial for its efficacy in treating ulcers.
14) Life:
Life represents the biological context in which drugs impact health and vitality. The study aims to enhance the quality of life for patients suffering from conditions like peptic ulcers by ensuring effective medication delivery through innovative pharmaceutical formulations.
15) Rheumatoid arthritis:
Rheumatoid arthritis is a chronic inflammatory disorder affecting joints, leading to pain and disability. The study addresses the need for effective pain management strategies, highlighting combinations of medicines that can help manage symptoms without aggravating other health issues such as ulcers.
16) Discussion:
Discussion involves analyzing the results and implications of a study. In this research, it reflects on findings from the formulation and evaluation of bilayered tablets, considering the significance of drug interactions and therapeutic effectiveness for patient care.
17) Developing:
Developing refers to the process of creating or improving pharmaceutical formulations. In this context, developing bilayered tablets involves innovative methods to combine immediate and sustained-release properties, enhancing therapeutic outcomes for managing ulcers and associated pain.
18) Swallowing:
Swallowing is the act of moving food or medication from the mouth to the stomach. The ease of swallowing is a crucial consideration in tablet formulation, especially for patients requiring long-term treatment, emphasizing the need for acceptable dosage forms.
19) Irritation:
Irritation refers to the discomfort caused by medications, particularly in gastrointestinal contexts. The study focuses on using Esomeprazole magnesium to counteract the gastric irritation often induced by NSAIDs like Diclofenac sodium, aiming to improve patient tolerability.
20) Substance:
A substance is a form of matter with specific properties. In the research, substances refer to the active pharmaceutical ingredients and excipients used in tablet formulations, each contributing to the overall stability, effectiveness, and bioavailability of the medication.
21) Dividing:
Dividing indicates the separation of components in a formulation. In the context of this study, it emphasizes the bilayer structure of tablets that allows for differentiated release profiles of active ingredients, maximizing therapeutic effectiveness while minimizing side effects.
22) Bleeding:
Bleeding is a potential serious side effect associated with NSAID use, particularly in gastrointestinal contexts. The study aims to develop formulations that mitigate such risks through concurrent administration of protective agents like Esomeprazole magnesium in treating pain.
23) Madhavi:
Madhavi is one of the authors of the study, highlighting the collaborative effort in conducting research on the formulation and evaluation of bilayered tablets. The contribution of researchers like Madhavi exemplifies the teamwork involved in advancing pharmaceutical sciences.
24) Quality:
Quality in pharmaceuticals refers to the standard of the active ingredients and manufactured products. Ensuring high quality in formulations like the bilayered tablets is fundamental for safety, effectiveness, and regulatory compliance, thereby impacting patient care and treatment outcomes.
25) Surface:
Surface relates to the outer boundary of a material. In tablet formulation, the surface characteristics can influence the drug’s release profile and bioavailability, making it an important factor in developing effective pharmaceutical products.
26) Purity:
Purity indicates the absence of contaminants in a substance. In pharmaceuticals, maintaining the purity of active ingredients is essential to ensure that drug formulations are safe and effective, directly impacting their therapeutic efficacy and patient safety.
27) Nature:
Nature refers to the intrinsic characteristics of substances, including their chemical and physical properties. Understanding the nature of the active ingredients in this study aids in optimizing their formulation and efficacy, especially concerning drug interactions and release mechanisms.
28) Shomti (Somti, Shonti, Sonti):
Sonti is another author contributing to the research, signifying collaboration among researchers in the formulation study. The presence of co-authors like Sonti underscores the importance of teamwork in advancing pharmaceutical research and innovation.
29) Food:
Food plays a significant role in drug absorption and metabolism. In this study, understanding the interactions between food and the formulated drugs is crucial, particularly regarding the administration recommendations for medications to ensure optimal therapeutic outcomes.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Dual therapy bilayered tablets: diclofenac sodium and esomeprazole.’. Further sources in the context of Science might help you critically compare this page with similair documents:
Granulation process, Immediate release, Therapeutic efficacy, Drug Absorption, Gastric irritation, Non steroidal anti inflammatory drug, Sustained release, Diclofenac sodium, Hausner's ratio, Friability test, Calibration curve, Proton Pump Inhibitor, Patient compliance, Wet granulation method, Carr's Index, Content uniformity test, Dissolution test, Angle of repose, Solubility studies, Flow properties, Dissolution profile, Partition coefficient, Preformulation studies, Bulk density, Tapped density, Floating lag time, FT-IR spectroscopy, Wet granulation technique, Drug-excipient compatibility, Drug release, Cumulative drug release, Modified Release Dosage Form, Gastrointestinal toxicity, Maximum absorbance, Oral drug delivery system, Biopharmaceutics Classification System, Sustained release tablet, Fixed Dose Combination, Post Compression Parameter, Hydrophilic matrix, Combination product, Bilayered tablet, Anti-ulcer agent, Release kinetic, NSAID-induced gastrointestinal injury.