Preparation and characterization of solid dispersion of furosemide

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Journal name: World Journal of Pharmaceutical Research
Original article title: Preparation and characterization of solid dispersion of furosemide
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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Author:

Purohit Nimesh Bhikhabhai


World Journal of Pharmaceutical Research:

(An ISO 9001:2015 Certified International Journal)

Full text available for: Preparation and characterization of solid dispersion of furosemide

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

Furosemide is a widely used loop diuretic, primarily indicated for the treatment of hypertension and pulmonary edema. Being classified as a class IV drug under the biopharmaceutical classification system, it exhibits poor solubility and oral bioavailability, which hampers its therapeutic effectiveness. This study aimed to enhance the solubility of furosemide through the preparation of solid dispersions (SD) using various hydrophilic polymers. The investigation explored two methods of preparation: physical mixing and solvent evaporation, with several combinations of drug-to-polymer ratios.

Solubility Enhancement through Solid Dispersion

One key concept illustrated in this study is the utilization of solid dispersion to improve the solubility of poorly soluble drugs like furosemide. Solid dispersion involves dispersing the drug in a water-soluble carrier, thereby increasing its surface area and reducing aggregation. The research demonstrated significant solubility improvement when furosemide was combined with polymers such as PEG 4000, PEG 6000, PEG 8000, and Poloxamer 407 in different drug-carrier ratios. Of all formulations, the solid dispersion with Poloxamer 407 at a 1:3 ratio prepared via the solvent evaporation method exhibited the highest solubility, showing a marked enhancement over the pure drug.

Preparation Methods: Physical Mixing vs. Solvent Evaporation

The study compared the efficacy of physical mixing and solvent evaporation methods for preparing solid dispersions. Results indicated that the solvent evaporation method provided superior solubility and dissolution rates compared to physical mixing. This was attributed to the better interaction and distribution of the drug within the polymer matrix in solvent evaporation, leading to a finer dispersion and reduced drug crystallinity. In vitro dissolution studies revealed that the tablets formulated through solvent evaporation released up to 97.41% of furosemide, showcasing a substantial improvement in drug availability compared to the physical mixtures.

Characterization Techniques for Solid Dispersions

Several characterization techniques were employed to validate the solid dispersions. The solubility of furosemide was significantly improved when prepared as solid dispersions, as quantified through solubility testing using UV spectrophotometry. Differential Scanning Calorimetry (DSC) and X-ray Diffraction (XRD) assessments were also conducted to evaluate thermal properties and crystallinity. Results indicated that, while pure furosemide maintained its crystalline structure, its presence in solid dispersion led to changes in thermal behavior, demonstrating effective incorporation into the polymer matrix without significant drug-polymer interaction.

Conclusion

This research illustrates the successful use of solid dispersion techniques to enhance the solubility and, consequently, the bioavailability of furosemide. By employing various polymers and preparation methods, it was found that the solvent evaporation approach offered a more effective dispersion of furosemide compared to physical mixing. The results underscore the importance of formulation strategies in improving the bioavailability of poorly soluble drugs and position solid dispersion as a viable technique in pharmaceutical development. The most promising formulation, demonstrated to have the best solubility profile, was identified as the combination of furosemide with Poloxamer 407 in a 1:3 ratio using the solvent evaporation method.

FAQ section (important questions/answers):

What is the main purpose of this study on furosemide?

The study aimed to develop solid dispersion tablets of furosemide to improve its poor solubility and thus enhance its bioavailability for effective treatment in hypertension and pulmonary edema.

How were solid dispersions of furosemide prepared in this study?

Solid dispersions were prepared using two methods: physical mixing and solvent evaporation, with different carrier-to-drug ratios and polymers such as PEG and Poloxamer 407.

What was the best formulation for furosemide solid dispersion tablets?

The best formulation was F11, which used Poloxamer 407 with a drug-to-carrier ratio of 1:3, prepared via solvent evaporation method, showing 97.41% drug release.

What techniques were used to characterize the solid dispersion?

Characterization included solubility testing, DSC studies, and X-ray diffraction to evaluate the solid dispersion’s physical properties and crystallinity.

What were the findings regarding the solubility of furosemide?

The solid dispersions significantly improved furosemide’s solubility compared to the pure drug, with the highest solubility noted for the formulation with Poloxamer 407.

How were the furosemide solid dispersion tablets evaluated for quality?

The tablets were evaluated based on hardness, friability, disintegration time, and in-vitro dissolution studies, all of which aligned with pharmacopoeial standards.

Glossary definitions and references:

Scientific and Ayurvedic Glossary list for “Preparation and characterization of solid dispersion of furosemide”. 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 substance used for medical treatment, especially for the diagnosis, prevention, or cure of diseases. In this context, furosemide is an active pharmaceutical ingredient classified as a diuretic used primarily in the management of hypertension and edema. Its solubility is critical for its bioavailability and therapeutic efficacy.

2) Study (Studying):
The term 'Study' is used to indicate a systematic investigation aimed at discovering or interpreting facts about a particular subject. In this context, it pertains to the systematic preparation and evaluation of solid dispersions of furosemide to improve its solubility, thereby enhancing its effectiveness as a pharmaceutical agent.

3) Water:
'Water' is a key solvent and medium for dissolving substances in pharmaceutical studies. It plays a critical role in the solubility testing of various compounds, including furosemide. The solubility levels assessed in both distilled water and acidic conditions reveal how effectively the drug can be absorbed in the human body.

4) Table:
The term 'Table' is used to refer to the dosage form created to deliver the drug to patients efficiently. In this study, solid dispersion tablets were crafted from furosemide to enhance its solubility. The efficacy, physical characteristics, and dissolution profiles of these tablets are meticulously evaluated during the research.

5) Indian:
'Indian' indicates the geographical and cultural context of the study, as it mentions the elements of research conducted within India. The use of locally sourced materials and compliance with Indian pharmacopoeial standards emphasizes the study’s relevance to Indian healthcare and pharmaceutical practices.

6) Kumar (Kumār):
'Kumar' typically signifies a male name in India and is a common surname. In the context of this text, it corresponds to a co-author involved in previous studies cited or referenced, displaying the collaborative effort of researchers in enhancing drug formulations and contributing to the scientific literature in pharmacology.

7) Substance:
The term 'Substance' in this context encompasses the various chemical compounds utilized in experimentation, including furosemide and the polymers mentioned. It highlights the importance of understanding the chemical and physical properties of substances while formulating solid dispersions that enhance drug solubility and bioavailability.

8) Surface:
'Surface' refers to the outer layer of solids or the interface where interactions occur. In this research, it is significant since increasing the drug's surface area using solid dispersion methods can lead to improved dissolution rates, directly impacting the efficacy of furosemide as a pharmaceutical product.

9) Science (Scientific):
'Science' denotes the systematic study of the structure and behavior of the physical and natural world through observation and experiments. This research reflects the principles of pharmaceutical science, aiming to discover innovative solutions to improve the solubility and bioavailability of poorly soluble drugs like furosemide.

10) Activity:
'Activity' in this scientific context refers to the pharmaceutical efficacy and therapeutic effects of furosemide. It is crucial to evaluate the in vitro activity of the drug post-formulation to ascertain how effectively it can fulfill its intended medical purposes, including diuresis and blood pressure management.

11) Gujarat:
'Gujarat' specifies the state in India where the research was conducted. This geographical identifier adds local relevance to the study by indicating the regional resources, academic institutions involved, and contextual practices associated with pharmaceutical development and healthcare provisions.

12) Medium:
The term 'Medium' points to the environment or substance in which experiments take place, especially regarding solubility studies. In this context, the dissolution medium used for testing furosemide's solubility is an important factor that influences the outcomes of the drug release evaluations.

13) Powder:
'Powder' refers to the physical state of the solid dispersions evaluated in the study. The preparation of furosemide in powdered form, achieved through methods like solvent evaporation, increases the surface area and potentially enhances solubility and dissolution rates, essential for effective drug delivery.

14) India:
'India' denotes the country in which the research occurred, contextualizing its significance within the Indian pharmaceutical landscape. The focus on enhancing drug formulations like furosemide underscores the necessity of addressing local health issues and improving the bioavailability of critical medications within the region.

15) Glass:
'Glass' typically refers to the material of laboratory equipment, such as flasks and mortars, used in the preparation and mixing of drug formulations. The use of glass containers is pertinent because it ensures chemical stability and prevents contamination during the solubility testing and other experiments.

16) Edema (Oedema):
'Edema' is a medical condition characterized by excess fluid accumulation in tissues, particularly relevant when discussing the therapeutic applications of furosemide, which is prescribed to alleviate such conditions. Understanding drug solubility affects how effectively it can manage and treat edema in patients.

17) Measurement:
'Measurement' involves obtaining quantitative data during scientific experiments, critical for assessing parameters like solubility and drug release rates. Accurate measurement is essential in this study to validate the formulations and ensure compliance with pharmacological standards to guarantee drug efficacy.

18) Discussion:
The term 'Discussion' refers to the section in research articles where findings are interpreted, and implications are delineated. It involves analyzing results and comparing them to existing literature, shedding light on the significance of improved furosemide solubility achieved through the methods employed in this study.

19) Similarity:
'Similarity' signifies the comparison standing between the new formulations and existing methodologies or drug profiles. In the context of this study, demonstrating similarity to established norms in drug formulation and release profiles empowers the research with credibility and relevance in the pharmaceutical domain.

20) Rishabha (Ṛṣabha, Ṛṣabhā):
'Rishabha' reflects a personal name likely associated with one of the authors or contributors to the referenced studies. The inclusion of author names emphasizes collaboration in enhancing drug formulations and fosters a sense of community in the scientific exploration of pharmaceutical sciences.

21) Relative:
'Relative' indicates a comparative aspect inherent in evaluating experimental outcomes against reference standards or other samples. In this context, it relates to how the solubility and dissolution rates of the solid dispersions developed are assessed against those of the pure drug to establish efficacy improvements.

22) Krishna (Kṛṣṇā, Kṛṣṇa):
'Krishna' is often a personal name, possibly linked to one of the contributors or authors in the referenced research. Such mentions honor collaboration and statistical contributions within the scientific community, fostering advancements in research methodologies and findings in drug formulation.

23) Sharman (Śarma, Sarmā, Sarma, Sharma, Śarman):
'Sharma' is a common surname in the Indian context, likely representing a co-author associated with similar studies. The inclusion of names underscores the collaborative nature of research efforts aimed at developing enhanced pharmaceutical formulations and addressing health-related challenges through scientific innovation.

24) Nature:
'Nature' pertains to the inherent characteristics and properties of substances involved in the study. Understanding the nature of furosemide, polymers, and their interactions is essential in developing solid dispersions that can effectively improve solubility and therapeutic performance.

25) Sagar (Sagár):
'Sagar' is a personal name that may correspond to an author or researcher within the context of the cited works. Its presence indicates the teamwork and multi-author contributions fundamental to the progress of research in drug delivery systems and formulation science.

26) Patel (Paṭel, Pāṭel):
'Patel' is another common surname in India, suggesting an author or collaborator in the study's development or referenced research. The acknowledgement of such individuals reflects the collaborative nature of scientific inquiry aimed at enhancing medication formulations and advancing pharmaceutical sciences.

27) Patil (Pāṭīl):
'Patil' denotes a common Indian surname, recognized in the context of authorship for research or studies referenced in this work. This highlights the significance of teamwork and shared efforts in clinical and pharmaceutical research initiatives focused on improving drug formulations.

28) Giri:
'Giri' may refer to an author or contributor in cited studies on improving drug solubility. Acknowledging individual researchers emphasizes the collaborative effort necessary to advance pharmaceutical science and address complexities in drug formulation and delivery systems effectively.

29) Chau (Chāū):
'Chau' is likely a reference to an author's name related to previous studies on similar subjects. The mention highlights the importance of collaboration in scientific endeavors, showcasing the intertextual relationships in research focused on enhancing drug solubility and bioavailability.

30) Pur (Pūr):
'Poor' indicates a condition faced by certain drugs, notably their low solubility and bioavailability. In the context of this study, recognizing furosemide as a 'poorly soluble drug' establishes the need for innovative methods like solid dispersions to enhance therapeutic effectiveness and patient health outcomes.

31) Inci (Iñci, Imci, Incī):
'Inch' pertains to measurement, particularly in relation to the equipment or dimensions described in experimental setups. While not directly tied to the study’s results, it highlights the meticulous nature of laboratory methodologies employed in formulating and testing the solid dispersions of furosemide.

Other Science Concepts:

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Discover the significance of concepts within the article: ‘Preparation and characterization of solid dispersion of furosemide’. Further sources in the context of Science might help you critically compare this page with similair documents:

X-ray diffraction, X-ray diffraction study, Solubility Test, Stability study, Dosage form, Disintegration time, Absorbance maxima, Tablet formulation, Furosemide, Oral bioavailability, Distilled water, Tablet dosage form, Solvent evaporation.

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