Formulation and development of matrix tablet of thiocolchicoside
Journal name: World Journal of Pharmaceutical Research
Original article title: Formulation and development of matrix tablet of thiocolchicoside
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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Punam Agrahari, Dr. Navjot Singh and Shradha Shende
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Formulation and development of matrix tablet of thiocolchicoside
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Doi: 10.20959/wjpr202114-22352
Copyright (license): WJPR: All rights reserved
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Summary of article contents:
Introduction
The formulation and development of matrix tablets for Thiocolchicoside were explored in this research. Thiocolchicoside is recognized for its muscle-relaxing, anti-inflammatory, and analgesic properties, yet it suffers from low bioavailability (approximately 25%), a short half-life (approximately 3-4 hours), and associated side effects. The goal of the study was to enhance the drug's release profile and bioavailability by creating a sustained-release dosage form using matrix tablets. The use of Hydroxypropyl methylcellulose (HPMC) as a polymer was paramount in achieving this objective.
Optimization of Polymer Concentration
A significant concept in this study was the optimization of the polymer concentration to enhance the matrixing properties and sustain the drug's release. Various formulations (H-1 to H-5) were developed using different concentrations of HPMC, evaluated for their physico-chemical properties, and assessed for their sustained-release capabilities. The findings indicated that the formulation H-3 demonstrated the best drug release profile, achieving a cumulative release of 93.15% over 24 hours. The systematic optimization process underscores the importance of polymer selection and concentration in developing effective matrix tablets.
Drug-Excipient Compatibility
Another crucial aspect of the research involved studying the compatibility between Thiocolchicoside and the excipients used in the formulation. Compatibility was assessed through physical observations and Fourier Transform Infrared Spectroscopy (FT-IR) analysis over one month under varying storage conditions. The results indicated no significant incompatibility, suggesting that the selected excipients did not adversely affect the stability of the drug. This compatibility analysis is vital for ensuring the safety and efficacy of the formulated dosage form.
Evaluation of Tablet Characteristics
The evaluation of various characteristics of the matrix tablets, such as hardness, thickness, weight variation, and friability, was thoroughly conducted. The study confirmed that the physical properties of the tablets remained optimal across formulations. Additionally, the swelling behavior of the matrices was measured, and it was found that the swelling index increased consistently, indicating that the tablets could expand and help maintain the drug release profile. These evaluations are crucial to ensure uniformity and reliability in drug delivery.
Conclusion
In conclusion, this research demonstrated that matrix tablets of Thiocolchicoside can be effectively formulated using HPMC without any adverse interactions with the drug. The systematic optimization processes highlighted the potential to improve the release profile and bioavailability of the drug significantly. The study paves the way for future research in sustained-release formulations, indicating that hydrophilic polymers like HPMC could be key components in the design of effective oral drug delivery systems. The successful integration of various evaluation techniques ensures a robust approach to developing and assessing new pharmaceutical formulations.
FAQ section (important questions/answers):
What is thiocolchicoside and its therapeutic effects?
Thiocolchicoside is a muscle relaxant with anti-inflammatory and analgesic effects. It acts as a competitive antagonist of GABA A receptors and has potential side effects, particularly convulsions, hence caution is needed in susceptible individuals.
What challenges does thiocolchicoside face regarding bioavailability?
Thiocolchicoside has a bioavailability of about 25% due to first-pass metabolism and a short half-life of 3-4 hours, leading to the need for improved drug delivery formulations.
What formulation method was used for the matrix tablets?
Matrix tablets of thiocolchicoside were prepared using the non-aqueous wet granulation method, optimizing the polymer concentration for better drug release properties and maintained matrixing capability.
How was drug release from the formulation evaluated?
The drug release from thiocolchicoside matrix tablets was evaluated using dissolution studies in pH 6.8 phosphate buffer, demonstrating a release profile of approximately 93.15% for the optimized formulation.
Which polymer was used for the matrix tablet formulation?
Hydroxypropyl methylcellulose (HPMC) was used as the main polymer, providing effective matrix formation for sustained release of thiocolchicoside without interfering with its therapeutic properties.
What was the outcome of the stability testing for the formulations?
Stability testing of the formulations indicated no observed color changes or physical incompatibility over a 30-day period, suggesting robustness of the matrix tablet formulations.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Formulation and development of matrix tablet of thiocolchicoside”. 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:
Drugs are chemical substances that affect physiological functions in living organisms. They serve various purposes, including diagnosis, treatment, or prevention of diseases. Understanding the properties and interactions of different drugs is critical in pharmaceutical research for developing effective therapies and ensuring safety during patient care.
2) Study (Studying):
In the context of pharmaceuticals, a study encompasses systematic research designed to evaluate the efficacy, safety, and properties of drugs. It involves various methodologies, including in vitro and in vivo experiments. Studies are essential for understanding drug behavior, interactions, and potential impacts on health, forming the basis for clinical applications.
3) Swelling:
Swelling pertains to the increase in size or volume of the matrix tablet when immersed in a solvent, such as phosphate buffer. It indicates the hydration ability of the matrix'material and plays a critical role in controlling drug release kinetics, allowing for sustained therapeutic effects through gradual release from the swollen polymer matrix.
4) Table:
In a pharmaceutical context, a table refers to a collection of data, generally organized in rows and columns. Tables are crucial for presenting experimental results, comparing formulations, and summarizing findings within research studies. They help in visualizing quantitative data, such as drug release rates and physical characteristics of tablets.
5) Water:
Water is a universal solvent and critical component in drug formulations. It is often used in the preparation of pharmaceutical dosage forms, like matrix tablets, as it aids in dissolution, solubility, and the swelling of polymers. Its role in drug release mechanisms is pivotal, influencing the rate and extent of therapeutic effects.
6) Observation:
Observation is a fundamental part of scientific research where researchers closely monitor and record changes or phenomena encountered during experiments. In pharmacological studies, observation aids in gathering data about the physical and chemical properties of drugs or formulations, contributing to the understanding of their behaviors and interactions in biological systems.
7) Life:
In pharmaceuticals, 'life' refers to the pharmacokinetics of a drug, including parameters such as half-life and bioavailability, which determine its efficacy and safety. Understanding these factors is essential in formulating drugs that provide adequate therapeutic effects while minimizing side effects, ultimately impacting patient compliance and treatment success.
8) Measurement:
Measurement in pharmaceutical research involves quantifying various parameters, such as drug concentration, release rates, and physical properties of formulations. Accurate measurements are critical for ensuring quality control, standardization, and reproducibility of results, which ultimately validate the therapeutic effectiveness and safety of pharmaceutical products.
9) Discussion:
Discussion is a section in scientific papers that interprets and analyzes results, relating them to existing literature and theoretical frameworks. It provides insights into the implications of findings, strengths and limitations of the study, and suggestions for future research, guiding the scientific community in understanding drug formulations and their potential applications.
10) Powder:
Powder refers to the physical state of solid drugs or excipients before they are formulated into dosage forms like tablets. The characteristics of powders, including particle size and flowability, significantly influence the granulation processes, tablet formulation, and overall drug release properties, making powder characterization a crucial step in pharmaceutical development.
11) Filling (Filled):
Filling in pharmaceutical terms refers to the process of placing powders or granules into dosage forms. It involves ensuring the uniform distribution of drug and excipients throughout the formulation, which is crucial for ensuring consistency in tablet properties and reliable drug release profiles, impacting overall therapeutic effectiveness.
12) India:
India is a significant hub for pharmaceutical research and manufacturing, home to numerous pharmaceutical companies and educational institutions. The country plays a vital role in global drug production, contributing to advancements in drug formulations, including matrix tablets, and supporting the development of effective therapies that meet international health standards.
13) Heap:
Heap refers to a mound or pile of granules or powders in pharmaceutical research. The concept of heap is related to studies of bulk density and flow properties, which are critical for maintaining consistency in dosage forms. Understanding heap behavior aids in optimizing processes like mixing, granulation, and tablet formation.
14) Pur:
Poor describes the unfavorable conditions that can occur with drug formulations, such as low bioavailability or inadequate stability. Addressing poor performance in drug delivery systems is essential, as it can lead to suboptimal therapeutic outcomes. Research focused on improving these aspects is vital to enhance patient compliance and drug efficacy.
15) Substance:
Substance refers to any material with specific physical properties and chemical composition, including drugs and excipients used in formulations. Understanding the characteristics and behavior of different substances is crucial for ensuring effective drug delivery systems and can impact the therapeutic efficacy and safety of the resulting product.
16) Inference:
Inference is the drawing of conclusions based on empirical data observed during experiments. In the context of drug studies, inferences are made about the drug's stability, efficacy, and compatibility based on results from formulation tests or clinical trials. It is a key component in hypothesis testing and subsequent research directions.
17) Activity:
Activity in pharmaceuticals describes the performance and effects of a drug in biological systems. This includes its therapeutic effects, mechanism of action, and potential side effects. Evaluating a drug's activity is essential for assessing its clinical significance and determining the appropriate use in treatment regimens.
18) Relative:
Relative refers to the comparative relationship between drug characteristics or responses in relation to other drugs or formulations. Understanding relative differences in properties such as solubility, pharmacokinetics, and bioavailability helps researchers improve drug design and tailor therapies for specific patient needs, ultimately enhancing treatment outcomes.
19) Surface:
Surface refers to the outer layer or boundary of a solid dosage form, like a tablet. The characteristics of the surface, including roughness and porosity, influence drug release rates and absorption in the gastrointestinal tract. Understanding surface properties is crucial for optimizing formulation designs that ensure effective drug delivery.
20) Reason:
Reason refers to the justification behind the choice of methods or formulations in pharmaceutical studies. It encompasses the logic applied in selecting specific polymers, excipients, or drug delivery systems. Identifying the reasoning helps to validate approaches in formulating effective medications that meet therapeutic needs.
21) Glass:
Glass is commonly used as a packaging material for pharmaceutical products, ensuring protection from moisture and environmental degradation. Its transparent nature allows for visibility and verification of contents. Glass containers are essential in maintaining the stability and shelf life of drug formulations throughout their intended storage period.
22) Kala:
Kala refers to a region or specific location; in this context, it is pertinent to the sourcing of raw materials or drugs for pharmaceutical studies. Understanding the geographical location can play a key role in the supply chain of compounds like Thiocolchicoside and relates to regional practices in pharmaceutical manufacturing.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Formulation and development of matrix tablet of thiocolchicoside’. Further sources in the context of Science might help you critically compare this page with similair documents:
Half life, Bioavailability, Organoleptic properties, Micromeritic properties, Compatibility studies, Granules preparation, Compression method, Weight variation test, UV-visible spectrophotometer, Swelling Index, Statistical model.