Formulation and evaluation of sustained release tablet of acebrophylline
Journal name: World Journal of Pharmaceutical Research
Original article title: Formulation and evaluation of sustained release tablet of acebrophylline
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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Abhinav Shahi, Dharmendra Kumar
World Journal of Pharmaceutical Research:
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Full text available for: Formulation and evaluation of sustained release tablet of acebrophylline
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
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Summary of article contents:
Introduction
The development of extended release drug delivery systems (ERDDS) has gained significant attention in recent years, particularly for optimizing the biopharmaceutical properties and pharmacokinetics of various drugs. The purpose of these systems is to enhance therapeutic efficacy while minimizing side effects, enabling more controlled and sustained drug action. Acebrophylline, a bronchial muscle relaxant with mucosecretolytic and anti-inflammatory properties, is particularly beneficial for conditions such as chronic bronchitis and asthma. The study focused on formulating a sustained release tablet of Acebrophylline using various grades of Hydroxypropyl Methylcellulose (HPMC) as matrix formers through a wet granulation technique, which allows for controlled dosage delivery over extended periods.
Drug-Release Mechanism
In the experimental results, significant findings were reported regarding the drug release mechanisms of the formulated tablets. The research employed various kinetic models—Zero order, First order, Higuchi, Hixson-Crowell, and Korsemeyer-Peppas—to analyze the release patterns. Particularly, the formulation (F5) demonstrated notable linearity across different models, predominantly aligning with Higuchi's diffusion mechanism (r^2 = 0.999). This indicates that the drug release was primarily governed by diffusion processes, with some formulations also showing non-Fickian diffusion (anomalous release). These outcomes suggest that a combination of diffusion and erosion mechanisms controlled the rate of drug release from the tablets.
Stability and Compatibility Studies
The study also encompassed the evaluation of drug-excipient compatibility and stability under different environmental conditions. Compatibility assessments revealed no incompatibility among the active ingredient and excipients at controlled room temperatures and accelerated conditions. Stability testing for the optimized formulation (F5) at both 40°C/75% RH and 25°C/60% RH over a 90-day period confirmed that the tablet formulation maintained drug content and physical appearance without significant changes. These results solidify the formulation's stability, indicating effectiveness for sustained release over time.
Formulation and Evaluation Methodology
The formulation development utilized a wet granulation method involving a matrix comprising Acebrophylline and two variants of Methocel (K100 LV and K4M). The manufacturing process ensured that the resultant granules had ideal flow characteristics, demonstrated through various pre-compression evaluations such as bulk density, tapped density, and angle of repose. The tablets were subjected to rigorous in-process quality control for parameters including hardness, weight variation, thickness, and friability. Furthermore, in-vitro dissolution studies determined that batch F5 yielded the most controlled and efficient release profile, outperforming other trial batches in terms of cumulative drug release at various time intervals.
Conclusion
In conclusion, this study successfully developed a stable sustained release tablet formulation of Acebrophylline using Methocel K100 LV and Methocel K4M as retardants. The optimized formulation exhibited favorable drug release kinetics, strong stability under varying temperatures, and ensured compliance with pharmaceutical standards. These findings reinforce the potential of utilizing polymer-based matrices for the effective delivery of medications, particularly for conditions requiring consistent therapeutic levels over extended durations, thus improving patient adherence and overall treatment outcomes.
FAQ section (important questions/answers):
What is the purpose of developing sustained-release tablets for Acebrophylline?
The objective is to produce a sustained-release dosage form to optimize the biopharmaceutical and pharmacokinetic properties of Acebrophylline, ensuring prolonged therapeutic effect while minimizing side effects and enhancing patient compliance.
Which polymer was primarily used in the sustained-release formulation?
The primary polymers used were Methocel K100 LV and Methocel K4M, which served as matrix formers in the sustained-release tablet formulation.
What method was used to manufacture the Acebrophylline tablets?
The tablets were manufactured using the wet granulation technique, which is simple and cost-effective for producing sustained-release formulations.
How was the in vitro drug release of formulations evaluated?
In vitro drug release was assessed using USP Apparatus 2 with paddle stirrer in phosphate buffer pH 6.8, measuring the cumulative percentage of drug released over time.
What stability conditions were the optimized Acebrophylline tablets tested under?
Stability testing was conducted at 40°C/75% RH and at room temperature (25°C), over a period of 90 days to evaluate the product's stability.
What was concluded about the release mechanism of formulation F5?
Formulation F5 exhibited both diffusion and erosion mechanisms, indicating a controlled drug release profile and confirming the presence of anomalous diffusion.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Formulation and evaluation of sustained release tablet of acebrophylline”. 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 any substance that can be used for the diagnosis, cure, treatment, or prevention of diseases. In the context of the study, Acebrophylline is the active pharmaceutical ingredient being formulated into a sustained-release tablet to improve therapeutic outcomes and enhance patient compliance.
2) Table:
The word 'Table' in this context refers to the tabulated data used to present various parameters related to the formulation of the sustained-release tablets. Tables summarize experimental results, making it easier to compare different formulations and their respective physical and chemical characteristics.
3) Study (Studying):
The term 'Study' encompasses the systematic investigation and evaluation of the properties of Acebrophylline sustained-release tablets. It describes the entire process, including formulation development, preformulation studies, in vitro drug release testing, and stability testing, aiming to improve drug delivery mechanisms.
4) Medium:
In pharmaceutical formulations, 'Medium' often refers to the dissolution medium used during in vitro testing to assess drug release rates. In this study, a phosphate buffer pH 6.8 was employed as the dissolution medium, simulating physiological conditions within the gastrointestinal tract.
5) India:
'India' identifies the geographical location where the research was conducted, particularly highlighting the institutions involved in the study. It reflects the local context of the pharmaceutical industry and the significance of developing drug formulations that cater to the specific needs of the Indian population.
6) Container:
The term 'Container' refers to the packaging used to store the formulated sustained-release tablets. Proper containers are crucial for maintaining drug stability and protecting against environmental factors such as light, moisture, and temperature, which can affect the drug's efficacy over time.
7) Quality:
'Quality' pertains to the standard of the formulated sustained-release tablets in terms of their physical and chemical properties. Rigorous quality control tests are imperative to ensure that the tablets meet established specifications for safety, efficacy, and consistency in drug release.
8) Sahi:
'Shahi' refers to one of the authors of the study, Abhinav Shahi. His involvement and contributions to the research signify the collaborative effort in the formulation and evaluation of Acebrophylline sustained-release tablets, underscoring the importance of authorship in academic publications.
9) Blood:
The term 'Blood' is relevant in discussing pharmacokinetics, particularly how sustained-release formulations can influence drug levels in the bloodstream over time. Stabilizing drug concentrations in the blood is critical to minimizing side effects and ensuring therapeutic efficacy throughout the treatment course.
10) Observation:
'Observation' is a key element in the study, particularly related to the monitoring of tablet stability and performance during various tests. Detailed observations of physical and chemical changes in the drug formulation help assess compatibility and predict shelf life.
11) Performance:
The word 'Performance' relates to how well the sustained-release tablets of Acebrophylline function in delivering the drug over time. It encompasses evaluations of drug release rates, stability, and overall delivery efficacy, which are crucial for patient treatment outcomes.
12) Dharmendra (Dharma-indra):
'Dharmendra' is another author involved in the study, indicating a collaboration between researchers. His expertise may have contributed to the formulation process, data analysis, and interpretation of results, enhancing the research's integrity and depth.
13) Discussion:
'Discussion' refers to the section in scientific research where the authors interpret and analyze the experimental results. It is crucial for understanding the implications of the findings on the formulation process and how they contribute to the existing body of knowledge in drug delivery.
14) Substance:
The term 'Substance' is generally used to describe the active chemical component in the study, which is Acebrophylline. It is the core of the research, as the study focuses on the formulation and assessment of this specific pharmaceutical agent's efficacy and stability.
15) Activity:
'Activity' denotes the biological function or therapeutic effect of Acebrophylline in treating conditions like bronchitis. Understanding the pharmacological activity of the drug is essential for its successful formulation into a sustained-release system for optimal patient outcomes.
16) Surface:
'Surface' relates to the outer layer of the tablets or the interaction with the dissolution medium. The surface properties can significantly influence the drug release behavior, affecting the rate and mechanism of how the drug is released from the tablet matrix.
17) Powder:
The word 'Powder' refers to the physical state of the ingredients used in the formulation process. The characteristics of the powder, such as particle size and flowability, play a crucial role in the granulation and compression phases of tablet manufacturing.
18) Kumar (Kumār):
'Kumar' is mentioned as one of the authors of the research paper. His contributions represent the collaborative nature of scientific research, highlighting the sharing of knowledge and expertise necessary for successful pharmaceutical formulation and evaluation.
19) Glass:
In the pharmaceutical context, 'Glass' can refer to glassware used in laboratory settings for mixing, measuring, or storing substances. The use of appropriate glass containers is vital to ensure that there is no contamination or chemical reaction affecting the formulations.
20) Water:
'Water' is often used in pharmaceutical formulations as a solvent for various processes, including granulation and dissolution testing. The quality of water is critical in maintaining the integrity of the formulation and ensuring accurate results in drug release studies.
21) House:
'House' in this context may refer to a testing environment or facility where experiments and evaluations are conducted. It signifies the controlled setting required for observing and measuring the performance and stability of pharmaceutical formulations.
22) Pur (Pūr):
The term 'Poor' is typically used to describe suboptimal characteristics such as inadequate drug release, low bioavailability, or poor stability in the context of pharmaceutical formulations. Understanding the consequences of poor performance helps guide formulation improvements.
Other Science Concepts:
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Stability testing, Anti-inflammatory agent, Average weight, Disintegration time, Accelerated stability study, Compressibility index, Hausner's ratio, Pharmaceutical Research, Stability Studies, Wet granulation method, FDA guidelines, Angle of repose, In vitro drug release, Sustained release tablet, Accelerated stability.