Enhancing aceclofenac solubility via recrystallization with polar solvents

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Journal name: World Journal of Pharmaceutical Research
Original article title: Enhancement of solubility of aceclofenac by recrystallization method using polar solvents
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:

Gajanan V. Pulgamwar, Ram S. Pentewar, M. A. Saleem, R. V. Sugave, A.V. Moholkar and M. S. Digge


World Journal of Pharmaceutical Research:

(An ISO 9001:2015 Certified International Journal)

Full text available for: Enhancement of solubility of aceclofenac by recrystallization method using polar solvents

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 research focuses on the enhancement of solubility of Aceclofenac, a non-steroidal anti-inflammatory drug (NSAID), through a recrystallization method utilizing polar solvents. The study investigates different solvents such as ethanol and methanol, as well as various additives like Hydroxypropylmethyl cellulose (HPMC), Polyvinyl pyrrolidone (PVP), and others to create different crystal forms. The obtained crystals were subjected to thorough characterization using techniques such as scanning electron microscopy, X-ray diffraction, and differential scanning calorimetry. The results indicated that the modified crystals exhibited improved solubility compared to untreated Aceclofenac.

Impact of Recrystallization on Crystal Properties

The recrystallization process significantly influenced the physical properties of Aceclofenac crystals. Crystals obtained from ethanol exhibited prismatic and rod shapes, while those from methanol showed hexagonal and thin pole forms. Importantly, the X-ray diffraction analysis revealed distinct crystal modifications, demonstrating various forms including orthorhombic, triclinic, monoclinic, and hexagonal configurations. By altering the recrystallization solvent and conditions, it was possible to manipulate both the morphology and crystallinity of the resulting aceclofenac crystals, thus affecting their solubility and dissolution behavior.

Enhancement of Solubility and Dissolution

The solubility of Aceclofenac crystals developed through recrystallization was found to be 1.5 to 1.9 times higher in distilled water compared to the pure drug. Several solubility studies were performed, revealing that the newly formed crystals, particularly those developed with additives, showed superior solubility profiles. The study also detailed a dissolution test that compared the release rates of drug from both pure and modified crystals, illustrating a marked increase in bioavailability of the recrystallized forms. This enhanced solubility has critical implications in the formulation of improved pharmaceutical products, particularly for those with challenges related to drug solubility.

Characterization Techniques Employed

The crystals formed were characterized utilizing a variety of methods. Techniques such as photomicrography and scanning electron microscopy were employed to assess morphological properties. Powder X-ray diffractometry was used to determine the crystallographic structures and confirm the presence of distinct crystal forms. Additionally, differential scanning calorimetry provided insights into the thermal behavior of both the pure drug and modified crystals. The characterization demonstrated that the recrystallization method not only impacted the physical appearance but also preserved the chemical integrity of Aceclofenac, ensuring that the modified forms remained therapeutically effective.

Conclusion

The study successfully demonstrates that the recrystallization of Aceclofenac using polar solvents can significantly enhance the solubility and dissolution rate of the drug. By leveraging different solvents and additives, the research produced several modified crystal forms with superior physical characteristics and bioavailability. The findings underscore the potential of recrystallization techniques in pharmaceutical applications, providing a promising avenue for improving the solubility of poorly water-soluble drugs, thereby enhancing their therapeutic effectiveness. The implications of these advancements may lead to better patient compliance and more efficient drug formulation strategies in the future.

FAQ section (important questions/answers):

What is the focus of the research on Aceclofenac?

The research aims to enhance the solubility of Aceclofenac through the recrystallization method using polar solvents and various additives, improving its pharmaceutical properties.

What solvents were used in the recrystallization of Aceclofenac?

Ethanol and methanol were the primary solvents used for recrystallizing Aceclofenac, with observation of different crystal shapes produced from each solvent.

How were the recrystallized Aceclofenac crystals characterized?

The crystals were evaluated using photomicrography, scanning electron microscopy, X-ray powder diffractometry, FT-IR spectroscopy, and thermal analysis techniques.

What was the result of the solubility tests on crystal forms?

The newly developed Aceclofenac crystals showed a solubility increase of 1.5 to 1.9 times in distilled water compared to untreated Aceclofenac.

What is the significance of crystal modifications in this study?

Different crystal modifications obtained through recrystallization can significantly influence the solubility, dissolution rate, and potentially the bioavailability of Aceclofenac.

What methods improved the effectiveness of Aceclofenac solubility?

The inclusion of additives during the recrystallization process was shown to enhance solubility and dissolution rates, thus leveraging modifications to the drug's physical properties.

Glossary definitions and references:

Scientific and Ayurvedic Glossary list for “Enhancing aceclofenac solubility via recrystallization with polar solvents”. 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 context, 'drug' refers to aceclofenac, a pharmaceutical compound that requires improvement in solubility for better bioavailability and effectiveness as a medication. The study focuses on enhancing the physical properties of aceclofenac to facilitate its use in solid dosage forms, improving patient adherence and therapeutic outcomes.

2) Water:
Water is emphasized in the text as a solvent used in solubility studies. It represents a polar solvent that can affect the solubility of aceclofenac crystals. The interaction of aceclofenac with water molecules is crucial for its bioavailability, making it a significant aspect of the recrystallization study.

3) Table:
The term 'table' denotes the presentation format used to summarize data and findings in a clear manner. It contains organized information such as the results of solubility studies, calibration curves, and crystallographic data, facilitating a better understanding of the crystal properties and experimental outcomes.

4) Study (Studying):
The word 'study' signifies the systematic investigation into the solubility enhancement of aceclofenac via recrystallization. It encompasses various methodologies, results, and analyses that contribute to the understanding of how different solvents and additives influence the drug’s crystallinity and solubility.

5) Arrangement:
Arrangement relates to the geometric organization of molecules within the crystal lattice structure of aceclofenac. This term underscores the importance of molecular arrangement in determining the physical properties of the crystals, influencing their melting point, solubility, and overall efficacy as a pharmaceutical compound.

6) Substance:
In this document, 'substance' refers to aceclofenac as a specific chemical entity being analyzed. The study investigates how different substances, such as solvents and additives, interact with the drug to enhance its solubility and dissolution profiles, which are essential traits for effective pharmacotherapy.

7) Gelatin:
Gelatin is an additive explored in the recrystallization methods used in the study. Its role pertains to how it can impact the crystallization process and potentially modify the solubility and other physicochemical properties of aceclofenac, contributing to improved formulations in pharmaceutical applications.

8) India:
India is identified as the location of the research institutions and authors involved in the study. It reflects the geographic context in which this pharmaceutical research is happening and may also indicate the regulatory environment and market dynamics affecting drug formulations in the region.

9) Glass:
The term 'glass' appears in relation to laboratory equipment, particularly sintered glass funnels used for filtering during crystal collection. This material is essential for ensuring the precision of the experimental setup and reliable results in the characterization and purification of the substance under study.

10) Powder:
The term 'powder' refers to the form in which aceclofenac is typically found before recrystallization. Understanding the properties of the powder form is crucial since the study aims to enhance its solubility, which is vital for the drug's efficacy in solid oral dosage forms.

11) Road:
The word 'road' is part of the address of one of the associated institutions, Channabasweshwar Pharmacy College, which signifies the physical location where the research is conducted. It may also figuratively represent the journey of research and development in pharmaceutical sciences.

12) Pole:
In the context of the crystals, 'pole' refers to a specific shape obtained from recrystallization in the study. The terminology describes the morphological characteristics of aceclofenac crystals, which can influence their solubility and flow properties that are critical for the formulation of pharmaceuticals.

13) New Delhi:
New Delhi is included as the location of one of the suppliers mentioned in the study. Its mention highlights the regional suppliers' role in pharmaceutical research and may indicate the prevalence of various chemicals and materials necessary for conducting experimental investigations.

14) Measurement:
Measurement is the process of quantifying properties such as solubility, particle size, and melting point, which are vital in the context of the study. Accurate measurements underpin the experiment's reliability and validate the enhancements observed in aceclofenac due to recrystallization.

15) Discussion:
Discussion refers to the section of the study where results are interpreted. It includes the exploration of findings, comparisons to existing literature, and implications of the research. This is crucial for advancing knowledge in the field of enhancing drug solubility through crystallization methods.

16) Karnataka:
Karnataka is another Indian state mentioned in the study, indicating the geographic diversity of the institutions involved in conducting pharmaceutical research. This aspect points to the collaborative nature of academic and research efforts across different regions in India in the field of pharmacy.

17) Toxicity:
Toxicity is a critical factor concerning the safety of aceclofenac as a drug. The study indirectly addresses toxicity by focusing on enhancing solubility and bioavailability, aiming to optimize therapeutic effects while minimizing adverse reactions, highlighting the dual focus on efficacy and safety in pharmaceutical development.

18) Gujarat:
Gujarat is mentioned as the origin of one of the suppliers of aceclofenac in the study. Like other geographic terms, it identifies the supplier's location, reflecting the interconnected supply chain within the Indian pharmaceutical sector that supports research and formulation efforts.

19) Heating:
Heating is a significant technique in recrystallization, influencing the solubility of aceclofenac in solvent systems. The controlled application of heat allows for the dissolution of the drug, facilitating the formation of larger, purer crystals upon cooling, which is crucial for improving solubility and performance.

20) Surface:
Surface refers to the outer layer of the aceclofenac crystals, which interacts with solvents and affects solubility. The characteristics of the crystal surface, such as smoothness or roughness, can influence drug release rates, highlighting its importance in the design of effective pharmaceutical formulations.

21) Reason:
Reason embodies the rationale behind the research approach taken in the study. It reflects the motivations for pursuing recrystallization techniques to enhance the solubility of aceclofenac, which is known for its poor water solubility, aiming for better therapeutic efficacy and patient outcomes.

22) Medium:
Medium commonly describes the solvent system used for dissolving substances during solubility testing. In this study, it emphasizes the importance of the chosen medium's properties on aceclofenac's solubility and crystallinity, indicating strategic considerations in pharmaceutical preparations.

23) Delhi:
Delhi, similar to New Delhi, underscores the importance of location in the sourcing of materials used in the experimental procedures. It acts as a central hub in India for pharmaceutical research and development, showcasing the urban dynamics affecting scientific progress in the industry.

24) Field:
Field signifies the broader area of pharmaceutical science and research within which this study takes place. It encompasses the techniques of recrystallization and solubility enhancement, reflecting ongoing efforts to advance drug formulations and improve patient care through research.

25) Digge:
Digge is one of the co-authors involved in the study, signifying collaboration in research. His involvement highlights the collective effort of multiple researchers in addressing the challenges surrounding aceclofenac's solubility and demonstrates the collaborative spirit prevalent in academic investigations.

26) Vapi:
Vapi is mentioned as the location of the supplier of aceclofenac in the study. This geographic reference emphasizes the importance of local industrial players in providing the necessary substances for pharmaceutical research and reflects the agile supply chain critical for successful experimentation.

27) Gold (Golden):
Gold refers to the material used in the preparation of the electron microscopy sample stubs. The use of a conductive layer like gold is crucial for obtaining high-resolution images of the crystals, which aids in the characterization of their morphology and structural properties in scientific studies.

28) Pur:
The descriptor 'poor' highlights the challenges faced in drug formulation, specifically addressing the issue of aceclofenac's poor water solubility. The study aims to overcome this difficulty by investigating recrystallization methods to enhance solubility and thereby improve bioavailability and overall therapeutic efficacy.

Other Science Concepts:

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Discover the significance of concepts within the article: ‘Enhancing aceclofenac solubility via recrystallization with polar solvents’. Further sources in the context of Science might help you critically compare this page with similair documents:

Methods of preparation, Particle size, Particle size distribution, Scanning Electron Microscopy, Compressibility index, Hausner's ratio, Differential scanning calorimetry, Melting point, Infrared spectroscopy, Calibration curve, Angle of repose, Active pharmaceutical ingredient, Differential scanning calorimeter, Thermogravimetric analysis, Polar solvent, Additives, Water content.

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