Sustained release nifedipine capsule: formulation and evaluation.
Journal name: World Journal of Pharmaceutical Research
Original article title: Formulation, characterization and evaluation of sustained release nifedipine capsule.
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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Kanika Arora,Meenu Nagpal, Upendra K. Jain, R. C. Jat, Dr.Suman Jain
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Formulation, characterization and evaluation of sustained release nifedipine capsule.
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 sustained release formulation of Nifedipine using the hydrophobic polymer Ethyl Cellulose. Nifedipine, a calcium channel blocker, is characterized by poor solubility and a short biological half-life, which complicates its effectiveness when administered orally. The aim was to enhance the drug’s solubility and achieve a controlled release over a 12-hour period.
Formulation Development
Five different formulations of Nifedipine matrix granules were prepared using various ratios of Ethyl Cellulose and the drug. These granules were subsequently filled into hard gelatin capsules. The characterization of these formulations included evaluating their particle size distribution, flow properties, and dissolution profiles. Among the formulations, F3—comprising a drug to polymer ratio of 1:3—demonstrated the most promising sustained release, showing 89.57% drug release over 12 hours while maintaining matrix integrity.
Release Kinetics
The optimized formulation was subjected to kinetic modeling to determine the mechanism of drug release. It was found that the Higuchi model best described the release profile, indicating that the drug diffused through the matrix. The formation of molecular dispersion of Nifedipine in the matrix was essential, as it shifted the dissolution step from being rate-limiting to allowing diffusion through channels formed by lactose erosion, facilitating a more controlled drug release.
Drug-Excipient Compatibility
Compatibility studies using Fourier Transform Infrared Spectroscopy (FTIR) indicated no significant interactions between Nifedipine and the excipients used, confirming that the drug's efficacy would not be compromised during formulation. This compatibility supports the stability and performance of the developed sustained release formulation.
Conclusion
The findings of this study provide evidence that Ethyl Cellulose can effectively modulate the release of poorly soluble drugs like Nifedipine in sustained release matrices. The successful formulation of Nifedipine granules not only enhances the drug’s solubility but also enables sustained release, encouraging better patient adherence through reduced dosage frequency and lower side effects. Hence, the utilization of Ethyl Cellulose in oral drug delivery systems presents a viable method for improving therapeutic outcomes for drugs with solubility challenges.
FAQ section (important questions/answers):
What is the purpose of using ethyl cellulose in Nifedipine capsules?
Ethyl cellulose is employed to create a sustained release formulation of Nifedipine, ensuring a prolonged drug delivery over 12 hours, thereby improving therapeutic efficacy and minimizing dose frequency.
How many different formulations of Nifedipine matrix granules were prepared?
Five formulations of Nifedipine matrix granules were prepared with varying drug-to-polymer ratios of 1:1, 2:1, 3:1, 4:1, and 5:1 using ethyl cellulose.
What were the results of the dissolution study for formulation F3?
Formulation F3 showed an impressive drug release of 89.57% over 12 hours, indicating it was the most promising sustained release formulation among those tested.
What technique was used to prepare the Nifedipine granules?
The Nifedipine granules were prepared using the wet granulation technique, which facilitated uniform mixing of the drug and polymers while ensuring good flow properties.
What method was used to evaluate drug-excipient compatibility?
Fourier Transform Infrared Spectroscopy (FT-IR) was used to assess drug-excipient compatibility, confirming there were no chemical interactions between Nifedipine and other ingredients.
What is the significance of lactose in these formulations?
Lactose acts as a soluble filler or pore former, enhancing drug release by creating channels within the matrix during dissolution, thus achieving sustained drug delivery.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Sustained release nifedipine capsule: formulation and evaluation.”. 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 refers to a substance used for medical treatment, intended to alter physiological functions, relieve symptoms, or cure diseases. In this context, nifedipine is highlighted as a poorly water-soluble drug. The study focuses on its delivery mechanism through sustained-release formulations, impacting therapeutic efficacy and patient compliance.
2) Water:
Water is a vital solvent in pharmaceutical formulations, influencing solubility and bioavailability of drugs. It plays a crucial role in sustainable drug release systems, especially for hydrophilic and poorly soluble compounds. The formulation utilizes water indirectly by involving various solvents, ultimately affecting the drug's dissolution and therapeutic effectiveness.
3) Transformation (Transform, Transforming):
Transform denotes changing the state or form of a substance. In pharmaceuticals, transforming drug solubility and release kinetics is critical. This research aims to transform nifedipine's low solubility into an accessible form by utilizing ethyl cellulose matrices, enhancing drug release profiles and therapeutic outcomes for better patient adherence.
4) Methane:
Methane is a simple hydrocarbon solvent referenced in pharmaceutical processes. It is used in various laboratory conditions and methodologies. Although the main focus is on dichloromethane or ethanol as solvents in formulations, methane effects on solubility assessment in certain conditions can indirectly affect pharmacokinetics of specific drugs.
5) Channel:
Channel refers to pathways created within matrices to facilitate drug release. In the context of the study, lactose acts as a pore former, creating channels that allow controlled drug diffusion over time. This mechanism is essential for achieving sustained release of nifedipine, ensuring its therapeutic efficacy and stability.
6) Gelatin:
Gelatin is a substance derived from collagen, typically used to form capsules. It serves as a delivery system for drugs, protecting active ingredients and enhancing stability. In this study, gelatin capsules contain nifedipine granules, showcasing an effective method for oral drug delivery and patient consumption ease.
7) Science (Scientific):
Scientific refers to a structured approach based on systematic and empirical methodologies to investigate drug formulations and their properties. The research presented utilizes scientific principles to assess the effectiveness of sustained-release systems for nifedipine, aiming to improve therapeutic delivery and patient health outcomes through rigorous testing and evaluation.
8) Glass:
Glass is often used in laboratory equipment, particularly in volumetric flasks and containers for preparing and analyzing pharmaceutical solutions. Its inert nature allows for accurate measurement and analysis of drugs, ensuring the integrity of samples. The study uses glassware for quantitative assessments of nifedipine release in various dissolution tests.
9) Discussion:
Discussion refers to the section where results are analyzed and interpreted in context. It provides insights into the significance of findings, like the efficacy of ethyl cellulose in achieving drug release stability. Within this study, discussion facilitates understanding the implications of sustained nifedipine release on therapeutic treatments and patient adherence.
10) Toxicity:
Toxicity defines the degree to which a substance can harm humans, emphasizing the importance of determining safety profiles in drug formulation. The study considers the potential toxicity of nifedipine, ensuring the sustained-release formulation minimizes adverse effects while maximizing therapeutic benefits, thus enhancing safer medication management for patients.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Sustained release nifedipine capsule: formulation and evaluation.’. Further sources in the context of Science might help you critically compare this page with similair documents:
Loss on drying, Bioavailability, Physicochemical properties, Analytical grade, Particle size distribution, Sustained release, Fourier transform infrared spectroscopy, Hausner's ratio, Whatman filter paper, Sample preparation, Uniformity of weight, Patient compliance, Therapeutic index, Wet granulation method, Carr's Index, UV-visible spectrophotometer, FT-IR spectra, Higuchi model, Drug release study, Angle of repose, Flow properties, Partition coefficient, Drug content, Dissolution study, Preformulation studies, Bulk density, Tapped density, Ethyl cellulose, FT-IR spectroscopy, In vitro drug release, Wet granulation technique, Dissolution media, Poorly Water Soluble Drug, Kinetic model, Simulated Gastric Fluid, Conventional dosage form, Separating funnel, KBr disk method, Release behavior, Release kinetic.