Sustained-release matrix pellets of diltiazem HCl formulation.
extrusion and spheronization
Journal name: World Journal of Pharmaceutical Research
Original article title: Formulation and evalution of sustained released matrix pellets of diltiazem hcl by
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: extrusion and spheronization
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Giram P.S. and Bare A.R and Puranik P.K.
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Formulation and evalution of sustained released matrix pellets of diltiazem hcl by
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
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Summary of article contents:
Introduction
The study focuses on the formulation and evaluation of sustained-release matrix pellets of Diltiazem HCl, an antihypertensive drug, employing the extrusion-spheronization technique. The investigation aims to enhance therapeutic efficiency and patient compliance by creating a dosage form that can release the active ingredient steadily over a prolonged period. The study utilized a combination of hydrophobic and hydrophilic polymers, particularly Ethylcellulose (EC) and Hydroxypropyl Methylcellulose (HPMC K15M), to formulate the sustained-release pellets without the need for coating. Various parameters were tested, including binder concentration, plasticizer effects, and the nature of wetting agents, to optimize the formulation.
Extrusion and Spheronization Technique
Extrusion-spheronization is an advanced method for pelletization, allowing for the creation of small, spherical granules containing the active pharmaceutical ingredient (API). The process involves several stages: dry mixing, wet granulation, extrusion to form rod-shaped particles, and further rounding of these particles in a spheronizer. The method emphasizes the influence of various parameters, such as the binder concentration and spheronization speed. The study revealed that the optimal concentration of HPMC K15M as a binder was crucial in achieving good pellet morphology and drug release characteristics, maximizing the benefits of the extrusion-spheronization approach.
Drug-Polymer Interaction Analysis
To ensure compatibility between Diltiazem HCl and the selected polymers, Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC) were utilized for drug-polymer interaction studies. FTIR analysis indicated no significant interactions, as there were no substantial shifts in characteristic peaks of the drug when mixed with the polymers. Similarly, the DSC thermograms revealed that mixing the drug with the matrix-forming polymers did not alter the thermal behavior of Diltiazem HCl, confirming its compatibility with Ethylcellulose and HPMC K15M. This suggests that the formulations developed during the study can maintain the drug's efficacy and stability.
Evaluation of Formulation Characteristics
The evaluation of the pellets focused on several important characteristics, including flow properties, morphological features, friability, and drug content. The flow properties of the pellets were satisfactory, exhibiting an angle of repose and Hausner ratio indicative of good flowability, which is essential for the manufacturing process. Morphological assessments showed that the optimal batch exhibited desirable sphericity and size distribution. The friability tests confirmed that the pellets had suitable mechanical strength with a loss percentage below the acceptable limit. Moreover, drug content uniformity was achieved, ensuring that the pellets delivered the correct dosage of Diltiazem HCl.
Conclusion
The study successfully developed sustained-release matrix pellets of Diltiazem HCl using the extrusion-spheronization technique, demonstrating that combining EC and HPMC K15M in a 3:1 ratio, along with 2% triethyl citrate as a plasticizer, significantly affects drug release profiles. The optimized formulation exhibited a 92.7% drug release over 12 hours, meeting the standards set by the USP. This research illustrates the potential of extrusion-spheronization as a promising method for creating effective controlled-release pharmaceutical formulations, ultimately contributing to enhanced therapeutic outcomes in managing hypertension. The authors express gratitude for the support received from Wockhardt Pvt Ltd and the faculty at Government College of Pharmacy, Aurangabad.
FAQ section (important questions/answers):
What is the aim of the study on Diltiazem HCl?
The study aims to prepare sustained release matrix pellets of Diltiazem HCl using the extrusion-spheronization technique, focusing on formulating pellets without coating for increasing drug release duration.
What polymers were used in the formulation of pellets?
Ethylcellulose, a hydrophobic matrix-forming polymer, and HPMC K15M, a hydrophilic matrix-forming polymer, were used in a ratio of 3:1 to achieve sustained drug release.
How was the drug-polymer interaction studied?
Drug-polymer interaction was studied using Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC), confirming compatibility without significant interaction.
What was the optimization process for pellets manufacturing?
The optimization involved adjusting variables like binder concentration, spheronization speed, and time, utilizing a 32 factorial design to study their effects on drug release.
What was the result of the in vitro drug release study?
The optimized batch of pellets (F7) showed a 92.7% drug release at 12 hours, indicating effective sustained release characteristics.
What are the concluded benefits of the study?
The study concluded that the combination of EC, HPMC K15M, and TEC efficiently sustained drug release, making the extrusion-spheronization technique a promising approach for Diltiazem HCl without coatings.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Sustained-release matrix pellets of diltiazem HCl formulation.”. 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 this research, 'Drug' refers to Diltiazem HCl, an antihypertensive medication studied for its release profile in matrix pellets. The goal is to develop a sustained release formulation that maintains therapeutic levels over time, enhancing patient compliance while minimizing adverse effects through optimized drug delivery systems.
2) Table:
Tables are employed throughout the study to organize experimental data, formulations, and results clearly. They facilitate quick reference for comparisons of batch characteristics, such as drug release percentages and physical properties, enabling readers to easily understand and evaluate the findings and design of the study.
3) Study (Studying):
The term 'Study' encapsulates the comprehensive investigation into the formulation and evaluation of sustained release matrix pellets of Diltiazem HCl. It outlines the methodologies, experimental designs, results, and conclusions drawn about drug delivery systems, emphasizing the advancements being made in pharmaceutical research for improved efficacy.
4) Water:
Water is utilized as a solvent in various processes, including dissolving excipients and forming binder solutions. It plays a crucial role in determining the consistency of the wet mass during the extrusion-spheronization process, thereby affecting the final characteristics and quality of the produced pellets.
5) Powder:
'Powder' refers to the solid state of the pharmaceutical ingredients before they are processed into pellets. Its characteristics, such as particle size and flowability, have significant implications for the mixing, extrusion, and spheronization processes, impacting the overall efficacy and uniformity of the final formulation.
6) India:
'India' indicates the geographical location where the research was conducted, specifically referring to the institutions and manufacturers involved. The regional context may also reflect the pharmaceutical industry's landscape in India, as well as regulatory guidelines that influence the development and commercialization of drug formulations.
7) Surface:
Surface characteristics of the pellets, including morphology and smoothness, are critical for drug release behavior, flowability, and stability. Understanding surface properties helps in predicting how the formulation will interact in physiological environments, impacting the bioavailability and therapeutic effectiveness of the drug once administered.
8) Medium:
'Medium' usually refers to the dissolution or solvent environment where the drug release study is conducted. In this context, it would denote the specific conditions, such as the type of fluid used for releasing the drug from the pellets, which are crucial for accurately assessing release kinetics.
9) Transformation (Transform, Transforming):
'Transformed' indicates changes in the state of materials during the production process. In this study, the powder mixture is transformed into wet mass, then extruded and spheronized. This transformation is essential in determining the final physical properties and drug release behavior of the pellets.
10) Channel:
'Channel' relates to calcium channel blockers, a class of medications that Diltiazem HCl belongs to. Understanding how Diltiazem HCl interacts with calcium channels is vital in treating conditions like hypertension, as these interactions directly influence the drug's therapeutic effects and efficacy in cardiovascular diseases.
11) Nature:
'Nature' refers to the inherent properties of the drug and excipients, such as solubility, hydrophilicity, and compatibility. The study emphasizes the importance of analyzing these attributes to optimize formulation strategies, ensuring stable and effective release profiles that meet therapeutic needs over extended periods.
12) Observation:
Observation encompasses the careful monitoring and recording of changes or behaviors noted during experiments. In this study, it includes tracking pellet characteristics, drug release rates, and formulation stability, providing essential data that guide the interpretation of results and formulation optimization.
13) Discussion:
The discussion section interprets the experimental findings, exploring implications, correlations, and significance. It contextualizes the results within existing literature, allowing for a comprehensive understanding of how the study contributes to current knowledge on sustained drug release systems and potential applications.
14) Developing:
Developing refers to the process of creating and optimizing sustained release formulations. This involves evaluating various factors such as polymer ratios, processing techniques, and release mechanisms, all essential for formulating an effective matrix pellet system that meets therapeutic demands and improves patient compliance.
15) Irritation:
Irritation pertains to the local adverse effects that some drugs may cause in the gastrointestinal tract. The study aims to formulate pellets that reduce irritation potential compared to conventional tablets, thereby improving patient experience. This is particularly crucial for drugs with known irritant properties.
16) Swelling:
'Swelling' describes the ability of hydrophilic polymers like HPMC to absorb water and expand during the dissolution process. This property is significant because it influences the control of drug release rates; a controlled swelling behavior is necessary for achieving sustained therapeutic effects.
17) Activity:
'Activity' refers to the pharmacological effects or actions exerted by Diltiazem HCl when released from the pellets. Evaluating the activity ensures that the drug behaves as intended within the body, providing effective therapeutic outcomes without undesirable side effects, thereby validating the formulation strategy.
18) Relative:
'Relative' is used to compare outcomes in terms of efficacy, stability, or release profiles among different formulations or experimental conditions. Understanding relations between factors helps researchers optimize formulations, ensuring the produced pellets achieve desired specifications and therapeutic goals.
19) Quality:
'Quality' pertains to the physical and chemical characteristics of the pellets, including consistency, shape, hardness, and drug content. Ensuring high quality is pivotal for regulatory compliance and effective functionality, influencing how well the formulation performs in real-world therapeutic settings.
20) Desire:
'Desire' indicates the objective of achieving specific pharmacokinetic profiles and formulation characteristics in the developed pellets. It underscores the aim of obtaining a sustained release of Diltiazem HCl over intervals that align with patient needs and therapeutic guidelines, highlighting the study's goals.
21) Filling (Filled):
'Filled' refers to the process of dosing the matrix pellets with the active pharmaceutical ingredient. This step is crucial for ensuring uniformity and achieving the required dosage, impacting both the efficacy of the therapy and the quality control measures throughout the manufacturing process.
22) Blood:
'Blood' signifies the transport medium in the body for delivering drugs to target tissues. The study considers how sustained release formulations can maintain therapeutic levels of Diltiazem HCl in the bloodstream, ultimately improving treatment outcomes in hypertension and related cardiovascular conditions.
23) Food:
'Food' relates to dietary factors that can influence drug absorption, metabolism, and bioavailability. Understanding interactions between the formulation and food intake is critical for optimizing dosing regimens and ensuring consistent therapeutic effects, minimizing variability in drug delivery and patient response.
24) Line:
'Line' may suggest a guideline or pathway, such as defining parameters for research or showing a trend in data analysis. In this context, it can also refer to the hypothetical relationships explored during experiments, contributing to the study's conclusions and future research directions.
25) Life:
'Life' encompasses the biological lifespan of the drug's therapeutic effect, which is influenced by formulation design. The goal of developing sustained release pellets is to prolong the drug's action in the body, enhancing the quality of life for patients by minimizing dosing frequency.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Sustained-release matrix pellets of diltiazem HCl formulation.’. Further sources in the context of Science might help you critically compare this page with similair documents:
Cold water, Drug Absorption, Mechanical properties, Sustained release, Morphological study, Morphological properties, Hausner's ratio, Differential scanning calorimetry, Melting point, Pharmaceutical Research, Pharmaceutical technology, Angle of repose, Melting point determination, In vitro drug release, Drug release rate, Binder, Different concentration.