Formulation and evaluation of zolmitriptan rapimelts

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Journal name: World Journal of Pharmaceutical Research
Original article title: Formulation and evaluation of zolmitriptan rapimelts
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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Original source:

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Author:

Balagani Pavan Kumar and Manubolu Sindhuri


World Journal of Pharmaceutical Research:

(An ISO 9001:2015 Certified International Journal)

Full text available for: Formulation and evaluation of zolmitriptan rapimelts

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

This study focuses on the formulation and evaluation of controlled release Zolmitriptan rapimelts, a novel dosage form designed to improve the management of migraine. The tablets were prepared using direct compression, with HPMC K15M polymer utilized to create micromatrices that allow for controlled drug release. Key parameters evaluated included drug content, moisture content, and in vitro drug release profiles, with physicochemical compatibility assessed through Fourier Transform Infrared (FTIR) analysis to ensure there were no adverse interactions between the drug and excipients.

Controlled Release Mechanism

The research primarily explores the controlled release of Zolmitriptan, a second-generation triptan effective in alleviating migraine symptoms. The study demonstrated that using different formulations of HPMC as polymers could modulate the rate of drug release. The kinetics of the release behavior adhered to the Korsmeyer-Peppas and Higuchi models, indicating a Fickian diffusion mechanism. The optimal formulation, FHC3, achieved a cumulative drug release of 96.68% over 24 hours, showcasing the potential for improved bioavailability in migraine treatment.

Importance of Orally Disintegrating Tablets (ODTs)

The growing demand for orally disintegrating tablets (ODTs) is driven by their convenience and patient compliance, especially for individuals struggling to swallow conventional tablets. The rapimelts developed in this study are tailored to disintegrate rapidly in saliva, thereby enhancing the patient's experience, particularly for populations with dysphagia such as the elderly and children. The formulation included superdisintegrants that facilitated faster disintegration and improved taste masking, showcasing a dual benefit of enhanced absorption and improved palatability.

Evaluation of Formulation Parameters

Throughout the study, thorough evaluation of the various formulation parameters was performed, including thickness, hardness, friability, and wetting time, in addition to disintegration and dispersion times. All these parameters fell within acceptable limits, indicating the physical stability and effectiveness of the tablets. The formulations were assessed for drug content uniformity, with results demonstrating consistent active ingredient distribution across multiple batches, thereby validating the reliability of the manufacturing process.

Conclusion

The successful formulation of Zolmitriptan rapimelts using the mass extrusion method exhibits a promising avenue for enhancing migraine treatment through superior bioavailability, controlled release, and patient compliance. The findings of this study highlight the compatibility of Zolmitriptan with various excipients and the optimization of tablet properties conducive to patient-centered drug delivery. The results advocate for further development of this innovative dosage form, potentially offering a more effective solution for managing migraine episodes.

FAQ section (important questions/answers):

What is the purpose of the Zolmitriptan rapimelts study?

The study aimed to prepare controlled-release Zolmitriptan rapimelts in tablet form, enhancing drug release characteristics using HPMC K15M polymer for improved bioavailability and patient compliance.

What advantages do orally disintegrating tablets (ODTs) provide?

ODTs are beneficial for patients with dysphagia, including pediatric and geriatric populations. They offer convenience by disintegrating rapidly in the mouth, improving drug absorption and patient compliance.

How were the micromatrices for the rapimelts prepared?

Micromatrices were prepared using a mass extrusion method, combining Zolmitriptan with HPMC K15M polymer, resulting in a uniform extrudable mass before being cut into smaller micromatrices.

What properties were evaluated in the micromatrices?

Micromatrices were evaluated for drug content, moisture content, in vitro drug release, and flow properties including bulk and tapped density, angle of repose, and Carr's index.

What was the optimal formulation for Zolmitriptan rapimelts?

The optimal formulation was FHC3, which demonstrated 96.72% drug content and 96.68% cumulative drug release, showcasing excellent drug release properties suitable for rapimelts.

Which release kinetic models best fit the drug release data?

The analysis indicated that formulations fit primarily into the Higuchi model, while some followed first-order kinetics. The n values indicated Fickian diffusion as the drug release mechanism.

Glossary definitions and references:

Scientific and Ayurvedic Glossary list for “Formulation and evaluation of zolmitriptan rapimelts”. 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 is a chemical substance used in the diagnosis, treatment, or prevention of disease. In this research, Zolmitriptan is the focal drug being formulated into a controlled release system to enhance bioavailability and efficacy in treating migraines.

2) Pavan:
Pavan refers to Balagani Pavan Kumar, a primary author and researcher in this study. His contributions are pivotal in the development and evaluation of Zolmitriptan rapimelts, showcasing the importance of individual researchers in advancing pharmaceutical science.

3) Table:
Tables present organized data clearly and concisely. In this study, various tables summarize formulations, drug release profiles, and evaluations of micromatrices, enabling quicker analysis and comparison of essential results in pharmaceutical research.

4) Water:
Water is a critical solvent and medium in drug formulation and evaluation processes. It is often used to dissolve drugs or act as a medium in dissolution studies, essential for assessing the release profile of Zolmitriptan in the developed rapimelts.

5) Powder:
Powder forms represent a critical physical state of both the drug and excipients in pharmaceuticals. This study involves creating micromatrices and rapimelts from powders, emphasizing the significance of powder characteristics on drug formulation and delivery.

6) Study (Studying):
A study is an extensive investigation aimed at exploring specific hypotheses or research questions. This study focuses on formulating and evaluating Zolmitriptan rapimelts, examining their effectiveness and assessing various physical and chemical properties.

7) Surface:
Surface characteristics impact dissolution and absorption of drugs. The study emphasizes the significance of surface area of micromatrices in facilitating drug release, thus enhancing the bioavailability of the formulated Zolmitriptan.

8) Medium:
Medium refers to a substance in which reactions or processes occur. In pharmaceutical studies, it often is the liquid used in dissolution tests, affecting the solubility and bioavailability of drugs like Zolmitriptan.

9) Science (Scientific):
Science is the systematic study of the structure and behavior of the physical and natural world. This research exemplifies pharmaceutical science, utilizing scientific principles to formulate effective drug delivery systems, improving treatment options for migraines.

10) Indian:
Indian refers to the context in which this research is conducted and published. The study reflects contributions to pharmaceutical science in India, highlighting local advancements in drug formulation and healthcare.

11) India:
India is the geographical and cultural context of this study. The study showcases Indian pharmaceutical research and universities, emphasizing the country's ongoing contributions to global healthcare through innovative drug delivery systems.

12) Kumar:
Kumar refers to Balagani Pavan Kumar, a primary researcher involved in the study. His work in the formulation and evaluation of Zolmitriptan rapimelts demonstrates the contributions of individuals within academia to pharmaceutical advancements.

13) Swallowing:
Swallowing difficulties affect patient compliance with traditional oral dosage forms. The study addresses this issue by developing orally disintegrating tablets, providing an innovative solution for patients who struggle with swallowing conventional tablets.

14) Substance:
Substances in pharmaceuticals can range from active ingredients to excipients. This study involves several substances to create micromatrices and rapimelts, essential for formulating effective drug delivery systems.

15) Krishna (Krsna):
Krishna is part of the institutional reference, specifically Gokula Krishna College of Pharmacy, where the research was conducted. Such affiliations highlight the importance of educational institutions in fostering pharmaceutical innovation.

16) Gokula (Go-kula):
Gokula refers to Gokula Krishna College of Pharmacy. The college plays a critical role in pharmaceutical education and research in India, contributing to the development of novel drug delivery systems showcased in this study.

17) Nausea:
Nausea is a common symptom associated with migraines, which Zolmitriptan aims to alleviate. Addressing nausea as part of migraine treatment contributes to developing effective therapies that improve patient quality of life.

18) Patel:
Patel is mentioned as part of the collaborative authorship, embodying the collaborative nature of scientific research. This highlights the teamwork necessary for conducting comprehensive research studies in pharmaceuticals.

19) Shri (Sri, Sr):
Shri is a respectful title used in India, acknowledging the individuals associated with the research. It signifies the respect afforded to the management and contributors to the study, which is important in academic settings.

20) Measurement:
Measurement is essential in scientific research to ensure accuracy and reliability of results. In this study, various measurements are taken, from drug content to dissolution rates, ensuring the formulations meet required standards.

21) Transformation (Transform, Transforming):
Transformation refers to the process of changing something into a different state. In this study, it characterizes the process of developing Zolmitriptan from a traditional formulation into fast-disintegrating rapimelts.

22) Vomiting:
Vomiting can be a recurring issue for migraine sufferers; effective treatments must address it. Zolmitriptan aims to mitigate both pain and associated symptoms like nausea and vomiting, improving overall treatment efficacy.

23) Quality:
Quality in pharmaceuticals refers to the standard of the formulation and its effectiveness. The research focuses on maintaining high quality of micromatrices and rapimelts to ensure they deliver the intended therapeutic effects.

24) Pain:
Pain is a primary symptom of migraines. The formulation of Zolmitriptan rapimelts targets this pain directly, underscoring the purpose of the study in addressing a prevalent and debilitating health condition.

25) Dish (Dis):
Dish is likely metaphorically referring to a container for a scientific experiment. In pharmaceutical contexts, dishes are utilized for conducting various in vitro studies, underscoring the importance of experimental settings in research.

26) New Delhi:
New Delhi represents a significant cultural and political center in India. The mention of New Delhi could imply a broader context of the research, potentially influencing pharmaceutical policies and healthcare advancements nationally.

27) Discussion:
Discussion in research presents an analysis of results and their implications. This section allows researchers to interpret findings, relate them to existing literature, and propose future directions for studies.

28) Shrinivasa (Shri-nivasa, Srinivasa):
Srinivasa is part of the acknowledgment for management personnel who facilitated the research. Recognizing contributions from leaders highlights collaborative efforts in achieving research objectives within academic institutions.

29) Mahapatra (Maha-patra):
Mahapatra likely refers to Anjan Kumar Mahapatra, another contributor in the context of the research. Co-authors reinforce the collaborative spirit pivotal in the pharmaceutical sciences.

30) Container:
A container in pharmaceutical research refers to any receptacle used to hold substances during experiments or formulations. Proper choice of containers ensures accurate measurements and protects materials during research.

31) Observing:
Observing is a fundamental activity in scientific research where data and phenomena are recorded. In this study, observing various parameters during the evaluation of Zolmitriptan formulations is crucial for deriving conclusions.

32) Jagannatha (Jagannath, Jagat-natha):
Jagannath may refer to Jagannath Sahoo, another potential researcher or contributor to the study. Establishing diverse authorship illustrates the collective effort required in pharmaceutical development.

33) Merchant:
Merchant refers to Hamid A. Merchant, contributing to the study. The diversity of researchers includes varied expertise, enhancing the quality and thoroughness of research outputs in pharmacy.

34) Relative:
Relative refers to comparisons made between formulations or evaluation metrics in research. This comparative analysis is fundamental for understanding the effects of different formulation variables on drug release and efficacy.

35) Sandhya (Shandhya, Samdhya):
Sandhya likely alludes to Sandhya S. Murthy, potentially a researcher involved in the study. Highlighting varied authors emphasizes the collaborative effort required for successful pharmaceutical research.

36) Shravan:
Shravan refers to Shravan Kumar Y., indicating his involvement in the study. His collaboration illustrates the collective effort and expertise needed in pharmacological research and development.

37) Heating:
Heating is a significant process in the formulation of certain drug systems. In this study, heating techniques may be employed to create stable micromatrices, affecting drug release properties.

38) Vijaya:
Vijaya likely refers to Vijaya Ratna, signifying his contribution to the research. Collaboration among various researchers emphasizes the interdisciplinary nature of challenges addressed in pharmaceutical formulations.

39) Bitter:
Bitter represents the taste profile of certain drugs, including potentially Zolmitriptan. Addressing bitterness through formulation methods can improve patient compliance, particularly for orally disintegrating tablets.

40) Nature:
Nature typically signifies the inherent qualities or characteristics of substances. In the research context, understanding the nature of Zolmitriptan and excipients ensures appropriate interactions during formulation development.

41) Avani:
Avani may refer to Avani R. Gosai, possibly another contributing author. Each contributor adds unique perspectives and skills necessary for addressing complex challenges in pharmaceutical development.

42) Ratna:
Ratna may signify Vijaya Ratna, a researcher in the study. The inclusion of various researchers reflects the collaborative efforts crucial to advancements in drug formulation.

43) Delhi:
Delhi, as a major city in India, serves as a backdrop for the research community. Its status indicates the concentration of academic institutions and resources available for pharmaceutical research.

44) Joshi (Josi):
Joshi refers to H. Joshi, indicative of a researcher involved in these findings. Collaborations among researchers enhance the depth and breadth of pharmaceutical studies.

45) Patil:
Patil signifies Sanjay B. Patil, emphasizing the extensive cooperation fundamental in research endeavors. The collaborative approach enriches the study and diverse insights contribute to findings.

46) Shetti:
Setti likely refers to Varahala Setti, highlighting his contributions to the research. Acknowledging various authors underscores the multifaceted teamwork required in developing effective drugs.

47) Jacob:
Jacob refers to a potential collaborator in the research. The mention of diverse authors demonstrates the importance of collective expertise in achieving meaningful pharmaceutical innovations.

48) Miṇi (Mini):
Mini refers to the scale of formulation techniques like mini-matrices used in the research. Miniaturization in drug formulation offers benefits in bioavailability and patient compliance, essential for optimal therapeutic outcomes.

49) Rama:
Rama signifies the contributions of individuals who participated in the research. Such acknowledgment highlights the collaboration necessary for addressing the complexities of pharmaceutical sciences.

50) Food:
Food underscores the relevance of formulations that can be ingested easily and are suitable for patient consumption. Developing palatable medicinal forms enhances adherence to therapy, especially in pediatrics and geriatrics.

51) King:
King may signify an author or figure related to pharmaceutical influence. The mention of revered figures emphasizes respect and the historical context of advancements in the pharmaceutical sciences.

52) Sign:
Sign represents markers used to denote beneficial outcomes or conditions within research contexts. Observing signs like dosage effectiveness or formulations success becomes essential for evaluating study results.

53) Ter:
Ther is short for therapy, referencing the therapeutic use of Zolmitriptan for treating migraines. Effective therapy development is crucial for enhancing patient quality of life and supporting broader healthcare objectives.

Other Science Concepts:

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Discover the significance of concepts within the article: ‘Formulation and evaluation of zolmitriptan rapimelts’. Further sources in the context of Science might help you critically compare this page with similair documents:

Hardness, Dysphagia, Effectiveness of formulation, Bioavailability, Moisture content, Dose administration, Drug stability, Controlled release, Sustained release, Weight variation, Fourier transform infrared spectroscopy, Hausner's ratio, First Pass Metabolism, FTIR Analysis, Carr's Index, Direct compression method, Taste-masking, Mechanical strength, Dissolution studies, Angle of repose, Melting point determination, Evaluation parameter.

Concepts being referred in other categories, contexts and sources.

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