Enhancing losartan potassium solubility via solid dispersion with β-CD.
Journal name: World Journal of Pharmaceutical Research
Original article title: Enhancement of dissolution rate and solubility of losartan potassium by using solid dispersion method β-cyclodextrin as carrier
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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Dr. M. Sunitha Reddy, CH.Soujanya, MD. Fazal ul Haq
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Enhancement of dissolution rate and solubility of losartan potassium by using solid dispersion method β-cyclodextrin as carrier
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
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Summary of article contents:
Introduction
Losartan potassium, an antihypertensive agent, is noted for its poor solubility and low dissolution rate, which adversely affects its therapeutic efficacy. This study aimed to enhance the solubility and dissolution rate of losartan potassium by employing the solid dispersion method using β-cyclodextrin as a carrier. By optimizing the formulation through various drug-to-polymer ratios and techniques such as hot melt extrusion and lyophilization, the study seeks to improve the bioavailability of losartan potassium which is critical for effective treatment in patients with hypertension.
Solid Dispersion Technique
The solid dispersion method incorporates a poorly water-soluble drug with a hydrophilic carrier to enhance solubility and dissolution rates. In this study, eight different formulations of losartan potassium were created using varying ratios of the drug to β-cyclodextrin. Methods such as lyophilization, which involves co-dissolving the components in a solvent and subsequently sublimating it to yield a molecular dispersion, and hot melt extrusion, where the drug and carrier are mixed and processed at elevated temperatures, were employed. The formulations were evaluated based on flow properties and mechanical characteristics, leading to the preparation of orodispersible tablets aimed at improving the drug's performance.
Evaluation of Formulated Tablets
The formulated orodispersible tablets underwent rigorous evaluation across several parameters including thickness, weight variation, hardness, friability, and drug content. The tablets were produced via direct compression technique, and among the various formulations, F4 and F8 exhibited the highest drug release percentages of 93.83% and 97.10%, respectively, within 45 minutes. The compatibility between the drug and the excipients was confirmed through Fourier Transform Infrared (FTIR) spectroscopy, revealing no significant incompatibilities, which underlines the stability of the optimized formulations.
Kinetic Analysis and Stability Studies
To better understand the release characteristics of the optimized formulations, kinetic modeling was applied. The results showed that the drug release followed a zero-order kinetics pattern, indicating a consistent release rate over time. The formulations were subjected to accelerated stability studies under controlled conditions for three months, yielding satisfactory results. Parameters such as weight variation, friability, and drug content remained stable throughout the stability assessment period, suggesting that the formulations maintained their integrity and effectiveness over time.
Conclusion
In summary, the application of the solid dispersion method using β-cyclodextrin significantly improved the solubility and dissolution rate of losartan potassium, thus enhancing its potential bioavailability and therapeutic efficacy. Among the formulations tested, F8 showed the best performance in terms of drug release dynamics. The promising results deriving from both the in vitro dissolution studies and stability tests indicate that the solid dispersion approach could be an effective strategy for formulating other poorly soluble drugs, ultimately aiding in the development of more effective therapeutic agents for hypertensive patients.
FAQ section (important questions/answers):
What method was used to enhance losartan potassium's solubility?
The study employed the solid dispersion method using β-cyclodextrin as a carrier to enhance the solubility and dissolution rate of losartan potassium.
What were the key formulations tested in the study?
Eight solid dispersion formulations were tested, utilizing different drug-to-polymer ratios, specifically 1:2, 1:3, and 1:4, created via lyophilization and hot melt extrusion methods.
Which formulation showed the best drug release results?
Formulation F8 achieved the highest drug release at 97.10% within 45 minutes, using the hot melt extrusion method, compared to F4 and the pure drug.
How were the prepared tablets evaluated for quality?
The tablets were evaluated based on hardness, disintegration, weight variation, friability, and in vitro dissolution tests, ensuring they met established I.P quality control parameters.
What techniques were used for solid dispersion preparation?
The solid dispersion formulations were prepared using two techniques: lyophilization, which involves sublimation, and hot melt extrusion, which processes materials via a twin screw extruder.
What was the outcome of the stability studies?
Stability studies indicated that formulations F4 and F8 maintained their quality parameters such as weight variation, friability, hardness, and drug content after three months of storage.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Enhancing losartan potassium solubility via solid dispersion with β-CD.”. 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 keyword 'Drug' refers to medicinal substances used to enhance health and treat diseases. In the context of the document, Losartan potassium is a drug used for hypertension. Its effectiveness is limited due to poor solubility, prompting research to improve its bioavailability through solid dispersion methods utilizing β-cyclodextrin as a carrier.
2) Table:
The term 'Table' pertains to the physical dosage form of the drug, specifically orodispersible tablets, which are capable of dissolving in the mouth. The study emphasizes the preparation and evaluation of these tablets to enhance drug delivery and bioavailability, showcasing their significance in pharmaceutical formulations.
3) Science (Scientific):
The word 'Science' denotes the systematic study of the structure and behavior of the physical and natural world through observation and experimentation. This research article exemplifies pharmaceutical science, specifically the study of drug formulation and delivery methods aimed at improving the therapeutic efficacy of losartan potassium.
4) Water:
In this study, 'Water' serves as a critical solvent in drug solubility tests, evaluating the solubility of losartan potassium in different aqueous and non-aqueous solutions. The solubility of a drug in water is vital for its bioavailability, impacting how well it can be absorbed into the bloodstream after administration.
5) Powder:
The term 'Powder' refers to the physical form of losartan potassium used in the formulation process. The drug's powder state is crucial for subsequent preparation and testing of solid dispersions and orodispersible tablets, impacting the effectiveness of the drug's release and solubility in gastrointestinal fluids.
6) Study (Studying):
The keyword 'Study' indicates a systematic investigation aimed at discovering or confirming facts. This article describes an experimental study conducted to evaluate the enhancement of solubility and dissolution rate of losartan potassium through various solid dispersion techniques, with an emphasis on improving its pharmacological outcomes.
7) Pur (Pūr):
The word 'Poor' describes the inadequate solubility and dissolution characteristics of losartan potassium, categorized as a class II drug, which leads to suboptimal bioavailability. The study addresses this issue by employing solid dispersion methods to improve the drug's solubility, highlighting a common challenge in pharmaceutical formulation.
8) India:
The term 'India' is referenced as the geographical context of the research, where the study was conducted by authors affiliated with the Jawaharlal Nehru Technological University in Hyderabad. It underscores the importance of local research contributions to global pharmacological advancements and the challenges faced in drug formulation in the region.
9) Transformation (Transform, Transforming):
The word 'Transformation' signifies the change in physical form or chemical structure of the drug through various methods, such as solid dispersion. In this study, it refers to the conversion of losartan potassium into more soluble forms, enhancing its therapeutic effectiveness and stability through improvements in solubility and dissolution rates.
10) Substance:
In the document, 'Substance' refers to the chemical components involved in the study, including losartan potassium and β-cyclodextrin. It indicates the focus on how the interactions between drug substances and carriers can significantly affect drug properties, including solubility, stability, and overall therapeutic performance.
11) Toxicity:
The term 'Toxicity' relates to the potential harmful effects a drug may have at higher doses. The study notes that increasing the drug's release rate can reduce the required dosage of losartan potassium, thereby potentially decreasing the risk of toxicity. This aspect is critical in developing safer medication alternatives.
12) Crushing:
The keyword 'Crushing' refers to the force required to break a tablet, which is indicative of its mechanical strength and stability. In this research, tablet hardness is measured to ensure that the tablets can withstand handling without breaking, thus ensuring consistent drug delivery and performance during administration.
13) Quality:
The term 'Quality' pertains to the standards and attributes of the formulated orodispersible tablets, including their hardness, disintegration time, friability, and drug content. Maintaining quality is essential for ensuring the safety, efficacy, and regulatory compliance of pharmaceutical products, which is a focus of this study's evaluations.
14) Medium:
The word 'Medium' denotes the dissolution medium used during in vitro release testing, specifically phosphate buffer at pH 6.8. The choice of dissolution medium is critical as it simulates physiological conditions, allowing for accurate predictions of the drug's behavior, bioavailability, and release profile in the gastrointestinal tract.
15) Blood:
In this context, 'Blood' relates to the circulation system where drug absorption and bioavailability ultimately take place post-administration. Improving the solubility and dissolution of losartan potassium through the study's methods aims to enhance the amount of drug reaching systemic circulation, thereby effectively managing hypertension.
16) Post:
The term 'Post' refers to the subsequent processes following tablet compression, such as evaluation of mechanical properties and dissolution testing. It indicates the importance of assessing the quality and efficiency of the final dosage form after preparation, highlighting steps to ensure that the product meets therapeutic requirements.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Enhancing losartan potassium solubility via solid dispersion with β-CD.’. Further sources in the context of Science might help you critically compare this page with similair documents:
Pharmaceutical industry, Bioavailability, Solubility Test, Biavailability, Therapeutic Effectiveness, Dissolution rate, Stability Studies, Carr's Index, Angle of repose, Hausner ratio, Patients compliance, Quality control parameter.