Aspirin solubility enhancement via solid dispersion with various polymers.
Journal name: World Journal of Pharmaceutical Research
Original article title: Evaluation of enhancement of solubility of aspirin by solid dispersion techniques using different polymers concentration
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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Rohan R. Shirsat and Sheeja Koliyote
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Evaluation of enhancement of solubility of aspirin by solid dispersion techniques using different polymers concentration
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
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Summary of article contents:
Introduction
Aspirin (acetylsalicylic acid, ASA) is a widely used therapeutic drug known for its analgesic, antipyretic, and anti-inflammatory properties. Despite the availability of newer non-steroidal anti-inflammatory drugs (NSAIDs), aspirin remains effective, especially for the treatment of cardiovascular diseases and prevention of specific cancers. However, high and frequent dosing is often necessary due to aspirin's poor solubility and extensive pre-systemic metabolism, leading to associated gastrointestinal side effects. The present study investigates the enhancement of aspirin's solubility and dissolution rate through solid dispersion techniques using polyethylene glycols (PEG) 1500 and 6000 as carriers.
Enhancement of Solubility through Solid Dispersion Techniques
The study systematically compares the solubility of aspirin with varying concentrations of PEG 1500 and PEG 6000 by employing different solid dispersion methods, such as kneading, solvent evaporation, and fusion methods. Results show that solid dispersions significantly improved the saturation solubility of aspirin compared to the pure drug. In particular, the optimal condition was achieved with a 1:4 ratio of aspirin to PEG 6000 prepared via the fusion method, which resulted in a marked increase in solubility from 13.86 mg/mL (pure aspirin) to 36.56 mg/mL.
Dissolution Studies and Drug Release Profiles
In vitro dissolution studies indicated that solid dispersions exhibited superior drug release profiles when compared to physical mixtures. The solid dispersions created with PEG 6000 demonstrated the fastest drug release rates, highlighting the effectiveness of PEG as a solubilizing agent. This finding is significant as it confirms that using a PEG carrier can enhance both the solubility and dissolution of poorly soluble drugs like aspirin, which could lead to improved clinical efficacy and reduced dosing frequency.
Characterization of Solid Dispersions
The characterization of the solid dispersions was performed using Fourier Transform Infrared (FT-IR) spectroscopy and Differential Scanning Calorimetry (DSC) analysis. FT-IR results indicated that there were no significant interactions between aspirin and the chosen carriers, while DSC revealed a shift in the melting point, suggesting a change to an amorphous form for the solid dispersion with PEG 6000. This change underscores a reduction in crystallinity, which is often linked with improved solubility and bioavailability of solid dispersions.
Conclusion
The study concludes that solid dispersions utilizing hydrophilic polymer carriers significantly enhance the solubility and dissolution rate of aspirin. The use of PEG 6000 in particular has shown to be beneficial, achieving the best results when formulated at a 1:4 ratio via the fusion method. Overall, the research emphasizes the potential of solid dispersion techniques to improve the pharmacokinetic profiles of poorly soluble drugs, thus fostering better therapeutic outcomes with lower doses and minimized side effects.
FAQ section (important questions/answers):
What was the main goal of the study on aspirin?
The study aimed to evaluate the enhancement of aspirin's solubility and dissolution rate using solid dispersion techniques with different polymer concentrations, specifically PEG 1500 and PEG 6000.
What methods were used to prepare solid dispersions of aspirin?
Solid dispersions of aspirin were prepared using three methods: kneading, solvent evaporation, and fusion, with varying drug-to-carrier ratios.
How was the solubility of aspirin measured in the study?
Saturation solubility studies were conducted in pH 6.8 phosphate buffer, measuring how much aspirin dissolved over time and comparing solid dispersions to the pure drug.
What were the findings related to drug release from solid dispersions?
The study found that solid dispersions, especially those with PEG 6000, showed significantly improved dissolution rates compared to the pure drug and physical mixtures.
What characterization techniques were employed in the research?
The solid dispersions were characterized using solubility tests, FT-IR spectroscopy, and differential scanning calorimetry (DSC) to analyze drug interactions and crystalline properties.
What conclusion was drawn about the use of PEGs in this study?
The study concluded that using PEGs in solid dispersions significantly improved aspirin's solubility, dissolution rate, and systemic availability, particularly with PEG 6000 by the fusion method.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Aspirin solubility enhancement via solid dispersion with various polymers.”. 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:
The term 'Drug' refers to a chemical substance used for medical purposes, primarily to diagnose, treat, or prevent diseases. In this context, aspirin is the drug studied for its solubility and dissolution enhancement by using various solid dispersion techniques. Understanding drug properties is crucial in pharmaceutical research for effective treatment formulations.
2) Study (Studying):
The term 'Study' indicates a systematic investigation or analysis conducted to understand specific phenomena, which in this case refers to evaluating the enhancement of aspirin's solubility. The context of the research involves diverse methodologies aimed at improving drug performance, which is vital in developing effective pharmaceutical therapies.
3) Water:
Water is a crucial solvent in pharmaceutical studies, especially for testing solubility and dissolution. In the research, double distilled water is utilized for preparing buffers and conducting experiments to analyze the solubility and dissolution characteristics of aspirin solid dispersions. Its role underscores the importance of a reliable solvent in drug formulation processes.
4) Table:
The term 'Table' refers to a structured format used to present data clearly and concisely. In the research, tables are utilized to summarize experimental results, such as drug content percentages and solubility levels of various formulations. This clarity helps in comparing different methods and outcomes, facilitating effective communication of findings.
5) Heating:
Heating is a process used in the preparation of pharmaceutical solid dispersions. In the research, heating methods are applied to melt polymers like PEG to disperse the drug effectively. The significance lies in altering the physical state of substances, influencing solubility and bioavailability, critical for enhancing drug delivery systems.
6) India:
India is the geographical context where the research is conducted, highlighting its location in the pharmaceutical landscape. The significance lies in understanding local regulatory environments, access to research materials, and potential market implications for developed drugs, reinforcing the relevance of regional settings in pharmaceutical studies and innovations.
7) Disease:
The term 'Disease' refers to a pathological condition that impairs normal functioning, which in this context includes various health issues treated with aspirin. Understanding disease mechanisms is crucial for developing effective therapies. The research supports the goal of improving drug formulations to enhance treatment outcomes for common diseases, such as cardiovascular complications.
8) Cancer:
Cancer represents a group of diseases characterized by uncontrolled cell growth. In the study, aspirin's anti-cancer potential is highlighted, emphasizing its significance as a therapeutic agent. The research focuses on improving the drug's bioavailability through enhanced solubility, potentially contributing to more effective cancer treatment strategies and patient outcomes.
9) Powder:
The term 'Powder' refers to the physical form of the drug or carrier in pharmaceutical formulations. In this research, powders are created from solid dispersions using various methods. The powdered form is crucial for enhancing solubility and improving dissolution profiles, which are essential for the efficacy and absorption of the drug.
10) Glass:
In the context of this research, 'Glass' refers to laboratory glassware used for mixing, storing, and analyzing compounds. Its relevance lies in providing an inert material that does not interact with chemicals, ensuring accurate experimental results and preventing contamination, which is vital in pharmaceutical research to uphold data integrity.
11) Discussion:
The term 'Discussion' encapsulates the analysis and interpretation of experimental results in the research. It allows authors to contextualize findings within existing literature, assess implications, and propose future directions. The significance lies in promoting understanding and guiding further research based on observed interactions and outcomes in drug solubility studies.
12) Substance:
The term 'Substance' refers to a specific chemical entity, such as aspirin or its carriers (PEG 1500, PEG 6000). In this research, the understanding of substances and their interactions is essential for enhancing drug formulation. Proper handling and characterization of substances are critical to developing effective pharmaceutical applications and therapeutic strategies.
13) Toxicity:
Toxicity signifies the degree to which a substance can harm organisms. In the context of the research, it emphasizes the importance of selecting carriers (like PEG) that are low in toxicity to ensure safe and effective drug formulations. Understanding toxicity is vital for developing drugs with minimal adverse effects on patients.
14) Field:
The term 'Field' pertains to the area of study or specialization, which in this case is pharmaceutical research. The relevance lies in encompassing various disciplines such as drug formulation, pharmacology, and bioavailability studies. This term underscores the extensive nature of research aimed at developing effective therapeutic interventions and improving patient care.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Aspirin solubility enhancement via solid dispersion with various polymers.’. Further sources in the context of Science might help you critically compare this page with similair documents:
Fusion method, Bioavailability, Anti-inflammatory properties, Gastrointestinal side effects, Differential scanning calorimetry, Analgesic properties, Dissolution rate, Antipyretic properties, In vitro dissolution studies, Differential scanning calorimetry (DSC), Solid Dispersion, Polyethylene Glycol, In Vitro Dissolution Study, Dissolution characteristics, Aqueous solubility, Drug content, UV spectroscopic method, Solubility Enhancement, Solid Dispersion Technique, Kneading Method, PEG 6000, Physical Mixture, Solvent Evaporation Method, Saturation Solubility Studies, Phosphate buffer solution, Cumulative release, IR spectroscopy, High dose, Weight ratio, Solvent evaporation, Enhancement of solubility, PEG 1500, Saturation solubility study, Fourier transmitted Infrared (FT-IR) spectroscopy, Pure Drug, Anti-thrombotic properties, Over the counter drug, Pharmaceutical carrier, Fourier transmitted Infrared spectroscopy, Crystallinity and Stability.