Gatifloxacin aqueous injection: mixed solvency formulation development.
Journal name: World Journal of Pharmaceutical Research
Original article title: Formulation development and evaluations of an aqueous injection of gatifloxacin by novel mixed solvency technique
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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Gayakwad PS, Gavit AJ, Rajput PV,Bari MM, Barhate SD, Maheshwari RK
World Journal of Pharmaceutical Research:
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Full text available for: Formulation development and evaluations of an aqueous injection of gatifloxacin by novel mixed solvency technique
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
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Summary of article contents:
Introduction
The study investigates the application of the mixed solvency technique to enhance the aqueous solubility of gatifloxacin, a poorly water-soluble synthetic fluoroquinolone antibiotic. Gatifloxacin is utilized to treat bacterial infections, and improving its solubility is crucial for formulating effective dosage forms, particularly aqueous injections. The study also aims to minimize the concentration of individual solubilizers to reduce potential toxicity while maximizing the solubilization effect through the use of blends of hydrotropic agents and co-solvents.
Synergistic Enhancement of Solubility
One of the key concepts explored in this research is the synergistic enhancement of solubility through mixed solvency. Mixed solvency leverages the combined solubilizing power of various solubilizers, such as hydrotropes (nicotinamide, sodium benzoate, and sodium citrate) and co-solvents (propylene glycol, PEG-400, and ethanol). The results indicated a significant increase in gatifloxacin solubility, with blends yielding solubility levels ranging from 22.79 mg/ml to 82.05 mg/ml, compared to distillation water's 1.19 mg/ml. The optimal blend achieved an enhancement ratio of 68.95-fold, demonstrating the technique's effectiveness in improving the solubility of poorly water-soluble drugs.
Characterization and Stability Assessment
The study also emphasizes the importance of characterizing solubilized products through various techniques, including ultraviolet (UV) and infrared (IR) spectroscopy. This characterization is essential to understand the interaction between gatifloxacin and the solubilizers, ensuring that no detrimental changes occur in the drug's structure. Additionally, the research assesses the physical and chemical stability of the developed formulations under different storage conditions. Formulations were rigorously evaluated for color changes, turbidity, crystal growth, pH, and particulate matter, indicating that certain formulations were stable over time and varying temperatures.
Sterility and Dilution Testing
Ensuring the sterility of the developed aqueous injections is critical for their safety. The study employed the direct inoculation method to test for microbial growth, confirming the effectiveness of the sterilization process as none of the formulations showed signs of contamination. Furthermore, dilution studies demonstrated that formulations maintained stability for up to 24 hours in normal saline and 5% dextrose solutions, which is beneficial for practical applications in clinical settings.
Conclusion
The findings from this research highlight the potential of the mixed solvency technique as a viable strategy for formulating aqueous injections of poorly water-soluble drugs like gatifloxacin. The ability to synergistically enhance solubility while minimizing the individual concentrations of toxic solubilizers presents a significant advancement in pharmaceutical formulation. The study underscores the importance of exploring innovative approaches in drug solubility enhancement, which could lead to safer and more effective treatments. Overall, the application of mixed solvency could greatly benefit pharmaceutical industries by allowing for the efficient development of stable and less toxic drug formulations.
FAQ section (important questions/answers):
What is the main objective of this research on gatifloxacin?
The main objective is to explore the mixed solvency technique for improving the aqueous solubility of gatifloxacin, a poorly water-soluble drug, and to reduce the concentration of individual solubilizers in the formulation.
How does the mixed solvency approach enhance drug solubility?
Mixed solvency utilizes combinations of various water-soluble solubilizers and co-solvents, resulting in additive or synergistic effects that significantly enhance the solubility of poorly soluble drugs without needing high concentrations of individual agents.
What are the key findings regarding gatifloxacin solubility?
The study found that solubility of gatifloxacin increased from 1.19 mg/ml in distilled water to as high as 82.05 mg/ml using optimized blends of hydrotropic agents and co-solvents.
What methods were used to determine solubility and stability?
The study employed UV spectrophotometry for solubility analysis, alongside stability testing for physical properties like color change, crystal growth, turbidity, and pH over varying storage conditions.
What findings were reported about the stability of formulations F4 and F6?
Formulations F4 and F6 remained physically stable without color change or crystal growth after 4 weeks under specified storage conditions, indicating their suitability for further development.
What implications does this research have for pharmaceutical industries?
This research suggests that the mixed solvency approach allows for effective formulation of poorly soluble drugs, reducing toxicity concerns while enabling large-scale production, making it a beneficial technique for pharmaceutical manufacturing.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Gatifloxacin aqueous injection: mixed solvency formulation development.”. 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 gatifloxacin, which is the focus of the study. Gatifloxacin is a poorly water-soluble synthetic fluoroquinolone antibiotic used for treating bacterial infections. The investigation aims to enhance its solubility and develop an aqueous injection, demonstrating the practical implications of pharmaceutical research in drug formulation.
2) Table:
In the context of the research, 'table' is used to organize data such as solubility determinations, properties of mixed solvent solutions, and stability testing results. Organized tables help in visually presenting complex data, allowing readers to easily compare different formulations and their characteristics based on the study's findings.
3) Water:
'Water' is crucial as it is the primary solvent used in the solubility enhancement studies for gatifloxacin. The investigation explores the use of various solubilizers and mixed solvency techniques to improve the aqueous solubility of gatifloxacin, ultimately leading to a more effective injectable formulation for medical use.
4) Gayakwad:
Gayakwad refers to the lead author of the study, highlighting the individual's contribution in the field of pharmaceutical research. The acknowledgment of authorship is essential in academic publications, showcasing the collaborative effort involved in conducting the research and developing innovative techniques for drug solubility enhancement.
5) Study (Studying):
'Study' encompasses the entire research project, focusing on the development and evaluation of an aqueous injection of gatifloxacin. It details methodologies, results, and conclusions aimed at improving drug solubility, thereby underscoring the importance of systematic research in advancing pharmaceutical formulations and addressing challenges with poorly soluble drugs.
6) Medium:
In the research context, 'medium' often refers to the growth medium for sterility testing, such as fluid thioglycolate medium and soybean-casein digest medium. These media are essential for assessing the sterility of the prepared formulations, ensuring that the injections are safe for patient use without microbial contamination.
7) India:
India is the geographical context of the research, specifically mentioning the Shree Sureshdada Jain Institute of Pharmaceutical Education and Research in Maharashtra. The location highlights the significance of pharmaceutical research conducted in India, contributing to the global knowledge base and addressing local healthcare challenges through innovative drug formulation strategies.
8) Substance:
'Substance' refers to the various solubilizers and co-solvents employed in the mixed solvency technique to enhance the solubility of gatifloxacin. The research emphasizes the role of different substances in forming effective blends, showcasing their combined synergistic effects to improve drug formulation efficiency and reduce individual toxicities.
9) Education:
'Education' reflects the academic setting where the research takes place, emphasizing the importance of pharmaceutical education in training professionals like researchers and formulators. The foundation of rigorous educational programs equips individuals with the knowledge and skills necessary to innovate and address challenges in pharmaceutical sciences.
10) Jalgaon:
Jalgaon is the district where the Shree Sureshdada Jain Institute of Pharmaceutical Education and Research is located. Mentioning this locale provides insight into the regional development of pharmaceutical education and research infrastructure, illustrating how local institutions contribute to the advancement of science and healthcare solutions within India.
11) Surface:
'Surface' refers to properties studied in the formulations, such as surface tension of mixed solvent solutions. Understanding surface properties is significant in pharmaceutical formulations as they impact drug behavior, interactions, and overall stability of injectable preparations, which are critical for ensuring the efficacy of the medical product.
12) Shri (Śri, Śrī, Śṝ, Sṛ, Sṝ):
The term 'Shree' is part of the name of the educational institution mentioned in the research. It holds cultural and honorific significance within Indian contexts, conveying respect and reverence towards the institute, which plays a pivotal role in fostering research and education in the pharmaceutical field.
13) Maharashtra (Mahārāṣṭra, Maha-rashtra):
Maharashtra is the state in India where the research was conducted. The mention of Maharashtra underscores the region's contributions to pharmaceutical education and innovation, highlighting its role as a hub for educational initiatives, research institutions, and healthcare advancements within the broader Indian context.
14) Transformation (Transform, Transforming):
'Transform' relates to the potential of the mixed solvency technique to change the solubility profile of gatifloxacin. This term encapsulates the goal of the research to fundamentally alter the solubility characteristics of poorly soluble drugs, thereby enhancing their therapeutic potential and usability in clinical settings.
15) Toxicity:
Toxicity is a critical concern in pharmaceutical research, especially related to the solubilizers used in drug formulations. The study aims to minimize toxicity by employing lower concentrations of various solubilizers through mixed solvency techniques, ensuring safety for patients while maintaining therapeutic efficacy, which is crucial in drug design.
16) Filling (Filled):
'Filled' refers to the process of completing the packaging of the aqueous injections, ensuring they are properly sealed and sterilized before distribution. Each step in the filling process is pivotal for maintaining the integrity and sterility of the pharmaceutical product, which is vital for patient safety.
17) Delhi:
Delhi is referred to in the context of the laboratory equipment used in the research, highlighting that some materials and instruments, such as autoclaves for sterilization, are sourced from vendors located in the national capital. This indicates the connectivity and logistics involved in conducting scientific research in India.
18) Glass:
'Glass' is significant due to its use as a material for the vials used to package the gatifloxacin injections. Glass is preferred in pharmaceutical applications for its inert nature, preventing interactions with the drug, and ensuring product integrity, which is vital for maintaining the medication's efficacy and stability.
19) Life:
The term 'life' in the context refers to the shelf life of the formulated aqueous injection of gatifloxacin, indicating how long the product remains effective and safe for use. Understanding shelf life is crucial in pharmaceuticals to ensure optimal patient safety, efficacy, and quality during the medication's storage and usage.
20) Sign:
'Sign' is relevant in the context of indicating results and observations in the study, such as color changes or the presence of turbidity in formulations. These signs are critical for assessing the physical stability of the formulations throughout the study and play a vital role in quality control in pharmaceutical manufacturing.
21) Observation:
'Observation' is essential in experimental research, involving the careful monitoring of changes and effects throughout the study, including physical and chemical stability assessments of the formulations. Systematic observations facilitate the understanding of the behavior of the drug formulations and ensure their safety and efficacy upon use.
22) Measurement:
'Measurement' pertains to the quantification of various physical properties and solubility parameters in the study. Accurate measurements are fundamental in pharmaceutical research to validate findings, ensure consistency, and determine the requisite concentrations of solubilizers, which is key to developing effective drug formulations.
23) Discussion:
'Discussion' reflects the analytical interpretation of results obtained from the research. This section provides insights into the implications of findings regarding solubility enhancement and formulation stability, facilitating a comprehensive understanding of the study's contribution to the field of pharmaceuticals and potential future research directions.
24) Rajput:
Rajput is one of the co-authors of the research, showcasing the team effort involved in conducting the study. The acknowledgment of contributors emphasizes the collaborative nature of scientific inquiry and the diverse expertise brought together to achieve the research objectives effectively.
25) Powder:
'Powder' alludes to the potential for formulating gatifloxacin as a dry powder for injection in future research. This method presents an alternative to liquid formulations, which may address stability issues and offers advantages in storage and transportation, ultimately improving the product's shelf life and usability.
26) Bari (Barī):
Bari is cited as a co-author in the study, highlighting the collaborative efforts in conducting the research. Mentioning co-authors is essential to acknowledge their contributions and share credit for the innovative research conducted in enhancing the solubility of poorly soluble drugs.
27) Wall:
'Wall' may pertain to the aseptic area preparation methodology, emphasizing hygiene and sterile conditions during the formulation process. Maintaining a clean environment is critical in pharmaceutical manufacturing to prevent contamination and ensure the safety and effectiveness of the final product.
28) Line:
The term 'line' can refer to the methodology of drawing conclusions from the data collected and the systematic approach taken throughout the study. Clear lines of reasoning are essential in scientific discourse to logically present findings and support the broader implications of the research on drug formulation.