Formulation and in-vitro evaluation of floating pulsatile tablet of lisinopril
Journal name: World Journal of Pharmaceutical Research
Original article title: Formulation and in-vitro evaluation of floating pulsatile tablet of lisinopril
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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Durga Bhavani K. and Poornima N. B.
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Formulation and in-vitro evaluation of floating pulsatile tablet of lisinopril
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Doi: 10.20959/wjpr202321-30446
Copyright (license): WJPR: All rights reserved
Download the PDF file of the original publication
Summary of article contents:
Introduction
Hypertension, a prevalent cardiovascular condition, presents a significant challenge in clinical management due to its complex pathophysiology and circadian variations in blood pressure. Lisinopril, an angiotensin-converting enzyme (ACE) inhibitor, is commonly used to treat hypertension and related disorders but is hindered by issues such as a short half-life and adverse side effects from conventional dosing. This study aims to develop Lisinopril Floating Pulsatile Release Tablets (FPRTs) to provide chronomodulated therapeutic effects, enhancing the medication's efficacy while minimizing side effects through a more tailored drug delivery system.
Floating Pulsatile Release Tablets
The formulation of Lisinopril FPRTs involves creating a rapid-release core tablet that utilizes superdisintegrants for improved disintegration and drug release. These core tablets are then compression-coated with hydrophilic polymers, including various grades of Hydroxypropyl Methylcellulose (HPMC) and Xanthan gum, to achieve the desired floating and pulsatile release characteristics. The optimized formulations aim to release the medication at specific times, aligning with the body's circadian rhythms and improving treatment outcomes for hypertension, particularly during morning surges in blood pressure.
Drug Release Characteristics
The in vitro evaluation of the FPRTs revealed that the optimized formulation, particularly FP8, exhibited favorable drug release kinetics that conformed to zero-order kinetics. This indicates a consistent release rate of Lisinopril over time, further supporting the pulsatile release mechanism designed to target specific therapeutic needs. This controlled release profile reinforces the potential for reduced side effects and enhanced patient compliance, as the medication can be tailored to be released when it is most effective.
Stability and Compatibility Studies
Compatibility studies demonstrated that both the drug and excipients did not interact adversely, ensuring formulation integrity. The physical and chemical compatibilities were confirmed through visual inspection and Fourier Transform Infrared (FTIR) spectroscopy. Stability studies conducted over a period of 45 days at elevated temperatures and humidity showed no significant changes in drug content or release profiles, validating the robustness of the FPRTs and their potential for long-term use.
Conclusion
The formulation and evaluation of Lisinopril FPRTs represent a significant advancement in hypertension management by aligning drug delivery with the body's biological patterns. The findings confirm that the optimized FP8 formulation demonstrates promising attributes including favorable drug release kinetics, stability, and compatibility, paving the way for more effective and patient-friendly treatments. Future research should focus on large-scale production, in vivo studies, and the exploration of alternative polymers to further enhance the versatility and efficacy of chronomodulated therapeutic systems in the treatment of hypertension.
FAQ section (important questions/answers):
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Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Formulation and in-vitro evaluation of floating pulsatile tablet of lisinopril”. 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:
药物是现代医学不可或缺的元素，广泛用于预防和治疗各种疾病。本文中提到的其他药物、特别是利辛普利，重点讨论了它们在治疗高血压及相关心血管疾病中的应用与挑战。
2) Table:
表是用于组织和展示数据的结构化方式。其在科研中不可或缺，通过精确呈现实验结果、配方比例与物理特性，使数据清晰易读，便于比较和分析，从而增强研究的可理解性和可信度。
3) Powder:
粉末是药物剂型中的一个重要形态，尤其是在制备快速释放核心片和浮动脉动释放片时。粉末的流动特性、颗粒大小和形态影响最终药物配制的均匀性和释放特性，这些参数对于确保药物有效性至关重要。
4) Bhavani:
Bhавани是本研究的主要作者之一，与其他研究者共同致力于利辛普利浮动脉动释放片剂的配方与评估。作为作者，她的贡献在于整合医学、药理学和科学研究，推动新药物治疗方法的开发。
5) Study (Studying):
研究在药物开发中发挥关键作用，涉及药物机制、配方和效果的深入分析。本文描述了一项对利辛普利的具体研究，旨在优化其释放特性，以提高对高血压患者的疗效，确保科学依据的治疗方案。
6) Swelling:
膨胀是描述药物释放特性和制剂行为的重要参数。本文评估膨胀行为，特别是在浮动脉动释放片中的表现，提供了对药物在胃肠道中的反应和效用的洞察。这是确保按需释放药物的关键因素。
7) Post:
在科学研究中，后续步骤至关重要，确保前期实验的成果得到验证和评估。文献强调了后处理（如药品稳定性测试、物理特性评估）的必要性，确保最终产品在临床应用中的安全性和有效性。
8) Life:
生命科学研究探索生物体的基本过程与机制。本文涉及药物对生命的影响，特别是如何通过改善药物释放科技来提升患者的生活质量，指出科学进步在改善健康领域的重要性。
9) Karnataka:
卡纳塔克邦是本项研究的实施地点，具体来说是拉吉夫甘地健康科学大学。该地区在医疗健康与药物研究方面有着丰富的资源和历史，是培养药学人才与推动创新的重要框架。
10) Science (Scientific):
科学方法是本文研究的基础，强调实验设计、数据分析和结论的逻辑性与严谨性。科学严谨的研究方法确保了研究结果的可信性，并为将来的临床应用提供理论基础。
11) Filling (Filled):
填充是药物制剂中的关键步骤，确保制剂内有效成分的均匀分布和释放。文献中提及的压缩成型技术和材料填充过程，直接影响到制剂的物理性能与最终治疗效果。
12) Surface:
表面特性在药物释放中具有重要影响，特别是在涉及涂层和粉末表面行为时。该文献探讨了浮动脉动释药片的涂层材料如何影响药物的释放速率与持续时间，表面交互作用对药物传递至关重要。
13) Medium:
溶液是许多药物释放测试的基础，比如在体外溶解度测试中使用的酸性溶液。研究围绕药物在不同介质中的行为，为合适的制剂设计和靶向释放提供了重要信息，影响药效评价。
14) Durga (Dur-ga):
杜尔加是研究的另一位作者，她与Bhавани共同努力推进浮动脉动释放片的开发。作为贡献者，她在药物制剂与药理学方面的专长促成了本文中创新治疗方案的形成与分析。
15) Pharmacological:
药理学是研究药物与生物体相互作用的科学，直接影响药品的效果与安全性。研究中强调了药理学在药物设计和释放机制分析中的重要性，确保有效治疗高血压的科学基础。
16) Performance:
性能评价是药物开发和研究中至关重要的一环，体现在药物的释放速率、药效及稳定性等方面。文章中通过多种测试评估了不同配方的性能，为最终推荐的药物提供了实证支持。
17) Discussion:
讨论部分是科研文献的重要组成，通常包括对研究结果的分析与解释。本文的讨论部分深入分析了利辛普利片剂的各项评估指标，阐明了其在治疗高血压方面的潜力及未来方向。
18) Reflecting:
反映过程指研究如何展现其目的和结果。文章反映了设计和评估浮动脉动释放片的复杂性，提供了重视患者需求与个性化治疗的重要见解，是现代药物开发的关键理念。
19) Medicine:
医学是探索与维护人类健康的综合性学科，本文聚焦于利用药物，如利辛普利，来改善临床疗效。在现代医疗中，药物研究和开发对提高患者健康状况具有重要现实意义。
20) Quality:
质量控制是药物开发和生产中不可或缺的一部分。研究确保其制剂的各种标准（如外观、稳定性和释放特性）达到要求，以提供安全且高效的治疗方案，反映了对患者健康负责任的态度。
21) Nature:
自然界中的现象及其规律是科学探索的基础。本文通过分析利辛普利的药动学特性与释放机制揭示了药物如何与生物体的自然过程相互作用，这是理解药理治疗的基础。
22) Field:
领域代表了特定的研究或专业范畴。该文中药物研发领域与医学相关性显著，展示了新药物技术如何在临床上实现应用，强调了跨学科合作的重要性。
23) Blood:
血压是高血压研究中的关键参数，利辛普利作为一种有效的治疗药物，其主要功能之一便是调节血压。在药物研发过程中，研究血液中的药物浓度变化直接关系到药效与安全性。
24) Pose:
提出的问题和研究假设在科学研究中至关重要。本文探讨了高血压治疗方案中的挑战，反映出临床医学中如何应对药物作用的复杂性，以寻找新的更有效的治疗方法。
Other Science Concepts:
Discover the significance of concepts within the article: ‘Formulation and in-vitro evaluation of floating pulsatile tablet of lisinopril’. Further sources in the context of Science might help you critically compare this page with similair documents:
Bioavailability, First Pass Metabolism, Patient compliance, Stability Studies, Dissolution studies, Preformulation studies, Hydrophilic polymer, Superdisintegrant, ICH Guideline, In vitro release kinetics, Physical characteristic.