"Telmisartan tablet formulation optimized using 23 factorial design."
Journal name: World Journal of Pharmaceutical Research
Original article title: Formulation of telmisartan tablets employing î²cd, crospovidone, poloxamer - optimization by 23 factorial design
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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V. Ramesh, Rukesh Kumar Jat and K. P. R Chowdary
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Formulation of telmisartan tablets employing î²cd, crospovidone, poloxamer - optimization by 23 factorial design
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
Telmisartan is an antihypertensive medication that belongs to Class II of the Biopharmaceutical Classification System (BCS), characterized by low solubility and variable oral bioavailability. This study aims to enhance the dissolution rate of telmisartan in tablet formulations, thereby maximizing its therapeutic efficacy. The investigation utilizes β-cyclodextrin (βCD), crospovidone, and Poloxamer 188 as excipients, employing a 2^3 factorial design for optimization. The ultimate goal is to achieve a dissolution rate of not less than 85% (NLT 85%) within 10 minutes post-administration.
Optimization of Tablet Formulation
The study adopts a 2^3 factorial design to determine the optimum combinations of βCD, crospovidone, and Poloxamer 188, as well as their respective levels in the formulation. Two levels are established for each factor — for βCD, a drug to excipient ratio of 1:1 and 1:5; for crospovidone, percentages of 2% and 30% of drug content; and for Poloxamer 188, 0% and 2% inclusions. Eight formulations (F1 to Fabc) are prepared and directly compressed, followed by evaluations of their performance. The polynomial equation developed from the dissolution data reveals that specific combinations of these excipients can significantly influence the dissolution performance, highlighting the significance of systematic optimization methods in pharmaceutical formulations.
Dissolution and Disintegration Characteristics
The results demonstrate substantial variability in disintegration and dissolution rates across different formulations. Certain tablet formulations, particularly Fbc and Fb, exhibited rapid disintegration within one minute, achieving over 99% dissolution within 10 minutes. Conversely, increasing βCD levels correlated with delayed disintegration times, while higher crospovidone concentrations notably enhanced dissolution rates. The study also noted that the dissolution kinetics of the tablets adhered primarily to first-order kinetics, allowing for the estimation of specific dissolution rate constants, thereby facilitating a comprehensive understanding of how formulation variables impact drug release.
Statistical Analysis Using ANOVA
To assess the significance of the formulation variables, an Analysis of Variance (ANOVA) is conducted on the dissolution rate constant values. The results consistently reveal that the factors βCD, crospovidone, and Poloxamer 188, along with their interactions, significantly affect the dissolution of telmisartan tablets (P < 0.01). The evaluation identifies that specific combinations, particularly those with balanced levels of the excipients, are crucial for optimizing the dissolution profile. This statistical approach affirms the reliability of the 2^3 factorial design in facilitating the identification of effective formulation strategies.
Conclusion
The study successfully established a method for optimizing telmisartan tablet formulations using β-cyclodextrin, crospovidone, and Poloxamer 188 by means of a 2^3 factorial design. The polynomial equation derived from the analysis indicates that an optimal formulation achieving NLT 85% dissolution within 10 minutes requires a βCD ratio of 1:3, crospovidone at 26.22% of drug content, and Poloxamer 188 at 1%. The optimized tablet formulation fulfills the dissolution target with an impressive 86.15% in 10 minutes, validating the efficacy of factorial design in deriving pharmaceutical formulations catering to precise therapeutic needs.
FAQ section (important questions/answers):
What is the main objective of formulating Telmisartan tablets?
The main objective is to enhance the dissolution rate of Telmisartan, as it has poor aqueous solubility. This is essential to maximize its therapeutic efficacy in treating hypertension.
Which excipients were used in the Telmisartan tablet formulation?
The formulation included β-cyclodextrin (βCD), crospovidone, and Poloxamer 188 to improve the dissolution rate of Telmisartan tablets.
What design method was applied to optimize the tablet formulation?
A 2^3 factorial design was employed to systematically evaluate various combinations of the selected excipients and their effect on the dissolution rate.
What were the main findings regarding dissolution rates?
Formulations F b and F bc achieved over 99% dissolution in 10 minutes, while higher βCD levels resulted in lower dissolution rates, indicating the significance of formulation variables.
How was the dissolution rate of the tablets measured?
Dissolution rates were assessed using a paddle stirrer method in phosphate buffer at pH 6.8, and samples were analyzed at specified time intervals for Telmisartan content.
What was the optimized formulation for desired dissolution levels?
The optimized formulation used βCD at a 1:3 ratio, crospovidone at 26.22%, and Poloxamer 188 at 1%, achieving 86.15% dissolution in 10 minutes.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “"Telmisartan tablet formulation optimized using 23 factorial design."”. 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 the context of the study, 'Drug' refers to Telmisartan, an antihypertensive medication with poor solubility affecting its bioavailability. The research focuses on improving its formulation through various excipients to enhance its therapeutic efficacy, which is crucial for effective hypertension management in patients.
2) Table:
'Table' pertains to the format used for presenting the formulations and results within the research. Tables concisely organize complex data, facilitating easier interpretation of the physical parameters, dissolution rates, and optimization results for the telmisartan tablets, thus aiding the reader's understanding of experimental findings.
3) Study (Studying):
'Study' signifies the systematic investigation undertaken to explore the optimization of Telmisartan tablet formulations. It encompasses methodology, experimentation, analysis, and conclusions aimed at enhancing the dissolution rate. Scientists often conduct similar studies to advance pharmaceutical formulations, ensuring medications are effective and safe for patient use.
4) Pur (Pūr):
'Poor' describes the aqueous solubility of Telmisartan, indicating a significant barrier to its bioavailability. The study endeavors to address this issue by employing various excipients to increase the dissolution rate and, consequently, the drug's therapeutic efficacy, which is vital for the overall effectiveness of antihypertensive treatments.
5) Rajasthan (Rājasthān):
'Rajasthan' designates the geographical location of Shri Jagdishprasad Jhabarmal Tibrewala University, where the research was conducted. The region's educational institutions contribute to advancements in pharmaceutical sciences, enhancing the local and national capacity for drug development and formulating innovative health solutions for diverse medical challenges.
6) India:
'India' is the country where the study originates. As a rapidly advancing nation in the pharmaceutical sector, India plays a significant role in drug development and formulation. The research reflects the country's commitment to improving healthcare through innovative solutions to medication challenges, particularly in managing chronic conditions.
7) Shri (Śri, Śrī, Śṝ, Sṛ, Sṝ):
'Shri' is a title of respect in Indian culture, often used before names. In this context, it precedes the name of the university, enhancing its formal recognition and stature. This reflects academic tradition and acknowledges the institution's dedication to delivering quality education and research in pharmacy.
8) Measurement:
'Measurement' in this study revolves around quantifying key parameters such as drug content, hardness, dissolution rates, and other physical attributes of the Telmisartan tablets. Accurate measurements are vital for ensuring that the formulations meet regulatory standards and effectively deliver the desired therapeutic effects in patients.
9) Discussion:
'Discussion' refers to the section in the research where the authors interpret the findings, compare results with previous studies, and explore the implications of their work. This critical analysis fosters a deeper understanding of the optimization processes used, providing insights that inform future pharmaceutical development efforts.
10) Relative:
'Relative' pertains to comparing the dissolution rates and other measurement results of different tablet formulations. Establishing relative performance is crucial in pharmacology as it helps identify the most effective formulations that can be developed further for clinical applications, ensuring optimal drug delivery systems are achieved.
11) Quality:
'Quality' addresses the standard of the formulated Telmisartan tablets in terms of their physical characteristics, safety, and efficacy. Ensuring high quality is imperative during drug development to adhere to pharmacopoeial guidelines and regulatory requirements, thereby guaranteeing patient safety and effective treatment outcomes.
12) Nature:
'Nature' conveys the characteristics or properties of the excipients and active ingredients used in the tablet formulations. Understanding the nature of materials such as βCD and crospovidone is essential for predicting how they interact, which is crucial for optimizing the performance of the final pharmaceutical product.
13) Powder:
'Powder' refers to the form of the Telmisartan drug utilized in the tablet formulations. The study involves careful preparation processes, including blending and compressing the powdered ingredients to ensure uniformity and efficacy in the final product, affecting dissolution and bioavailability significantly.
14) Kumar (Kumār):
'Kumar' is a common surname in India, likely referring to one of the authors involved in the research study. The inclusion of authors' names emphasizes collaboration and contributions from different individuals in academia, highlighting the collective effort in advancing pharmaceutical sciences and delivering actionable research outcomes.
15) Glass:
'Glass' pertains to the glass mortar used for powdering the tablets during the measurement of drug content. This laboratory tool is crucial for ensuring homogeneous mixing and preparation of drug samples for analysis, which is fundamental for accurate and reproducible results in pharmaceutical research.
16) Water:
'Water' is mentioned as the test fluid for disintegration studies. As a universal solvent, its properties are vital for simulating physiological conditions in vitro. Proper disintegration in water indicates the tablet's ability to dissolve in the gastrointestinal tract, ultimately impacting drug release and absorption.
17) Pose:
'Pose' relates to the challenges posed by poor solubility of drugs like Telmisartan. Addressing these challenges requires innovative formulation strategies, as highlighted in the study, which seeks to overcome limitations that hinder effective drug delivery, ensuring that patients receive the full therapeutic benefits of their medications.
Other Science Concepts:
Discover the significance of concepts within the article: ‘"Telmisartan tablet formulation optimized using 23 factorial design."’. Further sources in the context of Science might help you critically compare this page with similair documents:
ANOVA, Disintegration time, Friability test, Dissolution rate, Direct compression method, Polynomial equation, Dissolution efficiency, Dissolution profile, Drug content, Phosphate buffer, Poloxamer-188, Roche friabilator, Optimization, First order kinetic.