Formulation and evaluation of orodispersible tablets of rizatriptan benzoate

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Journal name: World Journal of Pharmaceutical Research
Original article title: Formulation and evaluation of orodispersible tablets of rizatriptan benzoate
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:

Aditi Anil Kushare


World Journal of Pharmaceutical Research:

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Full text available for: Formulation and evaluation of orodispersible tablets of rizatriptan benzoate

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 focuses on the formulation and evaluation of Orodispersible Tablets (ODTs) containing Rizatriptan Benzoate, an anti-migraine drug. As the patents for this drug approach expiration, the research aims to create a comparable dosage form for regulatory submission. By using direct compression techniques, the study prioritizes efficiency, cost-effectiveness, and enhanced patient compliance. Innovations in ODT technology are highlighted, specifically addressing the challenges of disintegration time and drug palatability, which are crucial for aiding patients who struggle with conventional tablet forms.

Optimizing Orodispersible Tablets

One critical aspect of the research is the optimization of the ODT formulations. The study developed nine formulations (F01-F09) using varying concentrations of superdisintegrants such as Croscarmellose Sodium and Crospovidone. The optimized formulation, F08, consisted of a specific mix of excipients, including 10.5 mg of Crospovidone and 20 mg of Pregelatinized Starch. The evaluation demonstrated promising results, showing good flow properties, minimal weight variation, and an impressive disintegration time ranging from 11 to 15 seconds, with drug content reaching up to 99.94%. This formulation's characteristics position it as a viable option for patients, particularly those facing difficulties in swallowing conventional tablets.

Challenges in Formulating Orodispersible Tablets

The formulation of ODTs is not without challenges. The study illuminates the difficulties in taste-masking active pharmaceutical ingredients (APIs), especially when the drug has an unpleasant flavor. To enhance patient compliance, the formulations incorporated sweeteners such as Aspartame and flavors like Peppermint to minimize the drug's bitter taste. The mechanical strength of the tablets also posed a challenge as softer tablets may disintegrate too quickly or become fragile. Coupled with these concerns, maintaining the stability of the formulation under various environmental conditions (temperature and humidity) was crucial, necessitating specialized packaging solutions.

In Vitro Evaluation and Stability

The research included a comprehensive in vitro evaluation of the optimized formulation (F08), comparing it to a marketed product, Maxalt-MLT. Dissolution testing in various media showed that the optimized ODTs achieved a 100% drug release within 30 minutes, indicating strong performance akin to the innovator product. Stability studies under different conditions confirmed the formulations' compatibility and retention of efficacy over time. This indicates that the optimized formulation not only meets immediate therapeutic needs but also remains stable for prolonged use, which is particularly important in ensuring patient safety and effective treatment delivery.

Conclusion

In conclusion, the study successfully developed an effective Orodispersible Tablet formulation of Rizatriptan Benzoate, addressing both patient compliance and therapeutic efficacy. By utilizing direct compression techniques and optimizing formulation components, the research presents a compelling alternative to existing formulations. The outcomes highlight advancements in ODT technology, offering insights into overcoming formulation challenges, ensuring stability, and demonstrating favorable in vitro performance. Overall, this research paves the way for further exploration and application of Orodispersible systems in pharmaceutical practice, particularly for drugs requiring rapid onset of action in migraine treatment.

FAQ section (important questions/answers):

What is the purpose of developing orodispersible tablets of Rizatriptan Benzoate?

The development aims to create an effective anti-migraine drug formulation with improved patient compliance and faster disintegration. This is crucial as the existing patents for Rizatriptan Benzoate will expire soon.

What are the advantages of orodispersible tablets (ODTs)?

ODTs are easy to administer, especially for children and elderly patients. They dissolve quickly in the mouth without the need for water, improving patient compliance and reducing the risk of choking associated with conventional tablets.

How are the orodispersible tablets formulated?

The tablets are formulated using the direct compression technique, incorporating superdisintegrants like Croscarmellose sodium and Crospovidone, along with other excipients to achieve optimal drug release and patient-friendly characteristics.

What parameters are evaluated for the formulated tablets?

The evaluation includes weight variation, thickness, hardness, friability, disintegration time, drug content uniformity, and in-vitro dissolution tests to ensure quality and effectiveness.

What was the outcome of the dissolution studies?

The optimized formulation (F08) demonstrated a cumulative drug release of 100% within 30 minutes in both 0.1 N HCl and phosphate buffer, indicating its potential effectiveness in migraine treatment.

Which techniques are compared for orodispersible tablet formulation?

Direct compression and lyophilization techniques are compared. Direct compression is favored for its cost-effectiveness and efficiency in producing stable orodispersible tablets.

Glossary definitions and references:

Scientific and Ayurvedic Glossary list for “Formulation and evaluation of orodispersible tablets of rizatriptan benzoate”. 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' in pharmaceutical research refers to a therapeutic substance used for diagnosing, curing, treating, or preventing diseases. In this context, the focus is on Rizatriptan Benzoate, an anti-migraine drug, developing optimized oral dispersible tablets to enhance patient compliance and ensure effective treatment delivery.

2) Water:
Water is essential in pharmaceutical formulations, often serving as a solvent for drug compounds and excipients. In the creation of orally disintegrating tablets, the ability of the drug to dissolve in water is critical for ensuring rapid bioavailability and onset of action, especially for migraine treatments.

3) Study (Studying):
The term 'study' signifies the systematic investigation into the formulation and evaluation of Rizatriptan Benzoate orodispersible tablets. It encompasses methodologies to assess drug stability, dissolution profiles, and overall effectiveness, ultimately aiming to enhance therapeutic outcomes while also ensuring patient compliance.

4) Table:
In this context, 'table' refers to the oral dispersible tablets being developed. These tablets are designed to disintegrate rapidly in the mouth, allowing quick absorption of the anti-migraine drug, which is crucial for patients who may have trouble swallowing conventional tablets due to various conditions.

5) Science (Scientific):
Science encompasses the systematic knowledge obtained through observation and experimentation, guiding the formulation of pharmaceutical products. The scientific principles applied in this study facilitate understanding of drug properties, interactions with excipients, and influence on bioavailability, efficacy, and patient safety while using Rizatriptan Benzoate.

6) Powder:
Powder refers to the physical form of the drug and excipients before tablet formation. The characteristics of the powder, such as flowability and compressibility, are crucial for the manufacturing process, influencing the uniformity, strength, and dissolution rates of the final orodispersible tablets being developed.

7) Candy:
'Candy' refers to the candy floss method used in the formulation of certain fast dissolving tablets. This approach mimics the properties of candy, creating a porous and rapidly dissolving structure that enhances the mouthfeel and dissolution characteristics of the oral dispersible tablets, appealing particularly to pediatric patients.

8) Pain:
Pain is a significant symptom that stimuli the need for drugs like Rizatriptan Benzoate, particularly in treating migraines. Effective pharmaceutical formulations aim to provide rapid pain relief, enhancing patient quality of life and ensuring adherence to treatment regimens by minimizing the discomfort associated with migraines.

9) Vomiting:
Vomiting is a common symptom associated with migraines, leading to an urgent need for effective anti-migraine medications. Formulating oral dispersible tablets that dissolve quickly could potentially alleviate symptoms faster, preventing severe nausea and vomiting while improving the overall control of migraine attacks.

10) Bitter:
Bitter describes the taste of many pharmaceutical drugs, including Rizatriptan Benzoate. Taste-masking strategies are essential in developing orodispersible tablets to enhance patient compliance, particularly in populations such as children or individuals who are sensitive to unpleasant flavors during medication intake.

11) Medium:
In pharmacology, 'medium' refers to the environment in which drug release and dissolution studies are performed. The selection of appropriate dissolution media (like 0.1 N HCL) is critical to ensure that the evaluated drug performance accurately reflects how it would behave in the human gastrointestinal tract.

12) Performance:
Performance relates to how effectively the formulated orally disintegrating tablets deliver the active drug to systemic circulation. Factors influencing performance include disintegration time, dissolution rate, and drug release profiles, which are essential for ensuring rapid therapeutic effects for migraine treatment.

13) Observation:
Observation is a key component of the scientific method in pharmaceutical research, involving systematic monitoring of the formulation process and tablet characteristics. Data collected from observations help assess the quality and effectiveness of the orodispersible tablets, ensuring they meet established pharmacological standards.

14) Swallowing:
Swallowing presents challenges for some patient populations, particularly the elderly and children. The development of orodispersible tablets aims to overcome these challenges by allowing medication to dissolve in the mouth without the need for water, thereby enhancing accessibility and compliance with treatment regimens.

15) Nashik:
Nashik, a city in India, is significant in the context of this study as it is the location of MGV’s Pharmacy College, where the research on Rizatriptan Benzoate orodispersible tablets was conducted. It highlights the region's involvement in advancing pharmaceutical education and research.

16) Nausea:
Nausea is frequently experienced by patients suffering from migraines and can hinder the effective treatment of this condition. Formulating orodispersible tablets that dissolve rapidly in the mouth aims to alleviate nausea quickly, allowing patients to obtain relief from migraine symptoms more effectively.

17) India:
India is highlighted as the geographical context for the research, reflecting the country's growing role in pharmaceutical innovation and education. The presentation of research from institutions like MGV’s Pharmacy College contributes to the expanding body of knowledge in drug formulation and development.

18) Sugar:
Sugar plays a role in taste-masking formulations, improving the palatability of bitter drugs like Rizatriptan Benzoate. It's important in the formulation of orodispersible tablets to ensure better patient acceptance, particularly in populations such as children or those sensitive to unpleasant flavors.

19) Food:
'Food' can affect drug absorption, metabolism, and efficacy. The development of Rizatriptan Benzoate orodispersible tablets aims to accommodate patients who may not have eaten prior to needing medication, enabling them to take their doses conveniently and effectively regardless of recent food intake.

20) Developing:
Developing refers to the process of creating or optimizing pharmaceutical formulations. This study centers on developing a robust and efficient orally disintegrating tablet formulation for Rizatriptan Benzoate, focusing on improving drug delivery and enhancing patient compliance in treating migraines.

21) Substance:
The term 'substance' pertains to the chemical or medicinal entity under investigation—in this case, Rizatriptan Benzoate. Understanding the properties of the substance is critical to optimizing its formulation, ensuring it maintains stability and performance throughout the manufacturing and delivery process.

22) Quality:
Quality is an essential aspect of pharmaceutical formulations, ensuring consistency, safety, and efficacy of the final product. The evaluation of orodispersible tablets emphasizes quality control measures throughout the manufacturing process, aiming to achieve high standards for patient treatment effectiveness.

23) Heating:
Heating is a process that may be involved in some drug formulation techniques to reduce viscosity or enhance mixing. However, in the context of orodispersible tablets, managing heat is crucial as excessive temperatures can degrade sensitive drug compounds or affect tablet integrity.

24) Cotton:
Cotton relates to the cotton candy method used to create specific formulations of orodispersible tablets. This method emphasizes the creation of a porous, lightweight structure that dissolves easily in the mouth, enhancing the patient experience and ensuring rapid drug delivery.

25) Kumar:
Kumar is likely a reference to the name of an author or researcher involved in previous methodologies or studies mentioned in the context of the thesis. Contributions from various authors enrich the collaborative nature of pharmaceutical research and development.

26) Glass:
Glass is often used in pharmaceutical laboratories for storage, mixing, or containing chemical substances. In this research, glass vials or jars may be utilized for compatibility studies or during dissolution testing, ensuring that interactions with the formulation's components are properly contained.

27) Hand:
Hand refers to the physical limitations some patients may face, such as tremors or difficulty gripping. The development of orodispersible tablets aims to address these challenges, making it easier for individuals with these limitations to administer their medication effectively and improve treatment adherence.

28) Pur:
The term 'poor' may refer to the inadequate solubility or bioavailability of certain drugs. This necessitates the optimization of drug formulations, ensuring that even compounds with poor solubility can be effectively delivered in a form that ensures rapid therapeutic action in patients.

29) Pharmacological:
Pharmacological pertains to the study of drug action and the effects of drugs on biological systems. The investigation into Rizatriptan Benzoate is rooted in pharmacological principles, focusing on optimizing its therapeutic profile to improve efficacy in migraine management.

30) Pharmacology:
Pharmacology is the branch of medicine that deals with the study of drugs, including their properties, effects, and mechanisms of action. This field is foundational in developing new formulations like orodispersible tablets for Rizatriptan Benzoate to optimize therapeutic outcomes.

31) Camphor:
Camphor is sometimes used in pharmaceutical formulations for its aromatic properties and potential therapeutic effects. In this study, camphor's relevance lies in its application in enhancing the taste and overall sensory experience of oral dispersible tablets, improving patient adherence.

32) Vertigo:
Vertigo is a sensation of spinning or dizziness that can accompany migraines. Understanding this symptom is important in the formulation of anti-migraine tablets as it underscores the need for rapid relief from all associated symptoms, improving overall patient quality of life.

33) Gelatin:
Gelatin plays a role in formulations, acting as a gelling agent that can influence the texture and stability of pharmaceuticals. In the context of orodispersible tablets, gelatin's properties may enhance mouthfeel and dissolution characteristics, benefiting patient experiences during administration.

34) Surface:
The 'surface' properties of drug particles can significantly affect their dissolution and absorption. In pharmaceutical development, optimizing surface characteristics through various formulation techniques improves the overall bioavailability of the active substance in orodispersible tablets.

35) Company:
The term 'company' may refer to the pharmaceutical manufacturers involved in producing Rizatriptan Benzoate or the innovator product that serves as a benchmark for evaluating formulations. Companies play a pivotal role in bringing effective medications to market and ensuring compliance with regulatory standards.

36) Family:
Family can refer to the support network around a patient. In the context of medication adherence, family involvement is critical, as relatives may assist with administering medications like orodispersible tablets, particularly for elderly and pediatric patients who may struggle with swallowing.

37) Nasik:
Nasik, a city in India, emphasizes the academic and research context of the study conducted at MGV's Pharmacy College. The local setting for this research highlights regional contributions to pharmaceutical education, innovation, and the development of effective drug formulations.

38) Noise:
Noise refers to the sensory disturbances that can exacerbate migraine symptoms. To optimize drug formulations like Rizatriptan Benzoate orodispersible tablets, understanding triggers like noise can help tailor medications to provide rapid relief and improve patient comfort during migraine episodes.

39) Post:
Post refers to the period following specific procedures or evaluations in the experimental framework. For instance, the 'post-compression' stage of tablet formulation is essential for assessing the quality and effectiveness of the tablets before they are approved for medicinal use.

40) Genetic defect:
A genetic defect may be referenced in migraine studies that highlight hereditary conditions, influencing migraine susceptibility. Understanding these links can guide more personalized treatment approaches in developing medications like Rizatriptan Benzoate to cater to affected demographics.

41) Antibiotic (Antibacterial):
Anti-bacterial refers to properties that can target or inhibit bacterial growth. In the context of pharmaceutical research, the exploration of anti-bacterial properties may relate to ensuring that formulations remain free from contamination and maintain integrity throughout their shelf life.

42) Discussion:
Discussion is an integral part of research reports, serving as a platform to analyze findings, interpret data, and relate outcomes back to the original hypotheses. It helps contextualize the results of the study on Rizatriptan Benzoate with the existing body of knowledge.

43) Depression:
Depression can be a co-occurring condition with chronic migraines, highlighting the potential need for comprehensive treatment approaches. The link between psychological conditions and the effective management of migraines presents an avenue for further research and consideration during drug formulation.

44) Drowsiness:
Drowsiness is a potential side effect of some anti-migraine medications, including Rizatriptan Benzoate. Addressing this in formulating orodispersible tablets is crucial for ensuring that patients can remain alert and functional post-medication, enhancing quality of life and adherence to therapies.

45) Blindness:
Blindness, specifically in the context of retinal migraines, underscores the severity of migraine conditions. Recognizing the risks associated with migraines can frame the development efforts surrounding effective treatments like Rizatriptan Benzoate, emphasizing the need for rapid efficacy in formulations.

46) Container:
Containers, such as vials or blister packs, are essential in pharmaceutical research for the storage and transport of formulated tablets. Proper selection and design of containers ensure product stability, consistency, and safety during handling and storage prior to patient use.

47) Composite:
Composite refers to a formulation that includes multiple components working in synergy. The development of orodispersible tablets involves creating a composite of the active drug and various excipients, enhancing the overall performance characteristics such as disintegration and dissolution rates.

48) Medicine:
The term 'medicine' refers broadly to substances used for therapeutic purposes. The study focuses on optimizing the formulation of Rizatriptan Benzoate, enhancing the pharmaceutical properties to ensure effective treatment solutions for migraine sufferers through improved oral delivery systems.

49) Activity:
Activity in a pharmaceutical context denotes the effectiveness of a drug in eliciting the desired therapeutic response. The activity of Rizatriptan Benzoate, particularly in rapidly alleviating migraine symptoms, is a focal point in developing orodispersible tablet formulations.

50) Crushing:
Crushing is a physical test that may relate to assessing tablet hardness or evaluating the compressive strength of formed orodispersible tablets. This parameter gauges the durability of the formulation in various handling conditions, ensuring stability during storage and transport.

51) Sweating (Sweat):
Sweating can be a physiological reaction to pain or discomfort associated with migraines. In drug development, considerations like minimizing side effects and improving therapeutic outcomes are critical, as it relates to enhancing the effectiveness of drugs like Rizatriptan Benzoate.

52) Epilepsy:
Epilepsy is a neurological disorder that can have overlapping symptoms with migraines. Understanding co-morbid conditions like epilepsy is vital for developing comprehensive treatment plans involving Rizatriptan Benzoate, ensuring effective management of symptoms while addressing potential complications.

53) Kindness:
Kindness relates to the social and emotional support offered to patients dealing with chronic conditions like migraines. Creating supportive environments increases treatment adherence and encourages patients to pursue effective management strategies, leading to better health outcomes.

54) Chauhan:
Chauhan likely refers to an author or researcher contributing valuable insights into the study on fast-dissolving tablets or drug formulations. Collaborative research efforts rely on diverse contributions that enrich the knowledge base regarding pharmacological advancements in therapeutics.

55) Bandari (Bamdari):
Bandari is another name likely linked to significant contributions in pharmaceutical studies related to fast-dissolving tablets. Recognizing diverse authors and their works assists in building a comprehensive understanding of the development of innovative drug delivery systems.

56) Sheetal:
Sheetal could refer to a contributor or researcher familiar with the research context regarding formulations or related pharmaceutical disciplines. The involvement of multiple authors helps create a richer body of work, providing deeper insights applicable to drug development and evaluation.

57) Pungent:
Pungent describes the intense flavor or smell associated with certain drugs. In formulating oral dispersible tablets, addressing the pungent properties of drugs like Rizatriptan Benzoate is crucial for enhancing palatability and thus ensuring patient compliance with medication regimens.

58) Overuse:
Overuse pertains to the excessive intake of medications, which can lead to complications. An understanding of overuse patterns in migraine patients informs the development of Rizatriptan Benzoate tablets that aim not only for efficacy but also for safe and responsible use in treatment.

59) Pouring:
Pouring may refer to the process within formulation development where liquids, such as solutions containing active ingredients or excipients, are poured into molds or tablets. This step is pivotal in ensuring proper dosing and consistency in active ingredient distribution throughout the tablets.

60) Disease:
Disease encompasses the medical conditions requiring treatment with medications like Rizatriptan Benzoate. Identifying the physiological and psychological aspects of diseases like migraines aids in developing targeted therapeutic strategies that enhance patient outcomes and treatment adherence.

61) Craving (Crave, Craved):
Craving in the context of pharmacology could refer to the desire to take medication, indicating the psychological aspect of managing chronic pain or discomfort. Understanding patients' cravings for relief informs the design of formulations that address such needs effectively.

62) Shukla (Sukla):
Shukla refers to a person contributing to the pharmaceutical research discussed, potentially involved in the formulation of orodispersible tablets. Collaborations in research extend the depth of knowledge explored in formulative studies and practical applications of pharmacological innovations.

63) Apurva:
Apurva could denote an author in the study or a participant in the research process. Recognition of diverse names underscores the collaborative nature of scientific inquiry and the collective effort required in advancing pharmaceutical knowledge and treatment methodologies.

64) Behera:
Behera is likely an author or contributor to the studies on fast-dissolving tablets, enhancing the collaborative research environment. Author recognition aids in tracing back the advancements and findings that shape current methodologies in drug formulation and delivery.

65) Sharman (Sarma, Sharma, Sarman):
Sharma is possibly another researcher involved in the exploration of pharmaceutical strategies or innovations within the context of the study. Contributions from various experts are integral to formulating effective and patient-centered drug delivery systems.

66) Nature:
Nature refers to the inherent characteristics of drugs being investigated, influencing their performance in pharmaceutical formulations. Studying the natural properties of Rizatriptan Benzoate informs best practices in developing orodispersible tablets for effective medication delivery.

67) Filling (Filled):
Filled pertains to the method of encapsulating or coating a drug within excipients during tablet formulation. Ensuring proper filling techniques leads to consistent dosing and effectiveness in delivering medications like Rizatriptan Benzoate to the target site within the body.

68) Gupta:
Gupta indicates a contributor or researcher who might have provided insights into formulation techniques or pharmacology relevant to the study. Collaborative efforts in such research highlight advancements in the pharmaceutical field and the importance of shared knowledge.

69) Chang:
Chang likely refers to a researcher or author involved in discussing advancements in drug formulations or delivery systems. Importance is placed on collective contributions that enrich understanding and improve the effectiveness of pharmaceutical preparations.

70) Cloud:
Cloud in a scientific context may allude to variations in conditions, such as humidity or temperature, which can affect the stability and performance of pharmaceutical formulations. Understanding these external factors helps in designing resilient orodispersible tablet formulations.

71) House:
House may refer to a pharmaceutical or academic institution involved in research and development related to drug formulation. The support and infrastructure provided by such houses play pivotal roles in advancing innovation in pharmaceutical science and practice.

72) Anda (Amda):
Anda could refer to a specific technology or process relevant to pharmaceutical manufacturing. Understanding various methodologies aids in optimizing drug formulation and ensuring the successful delivery of effective therapeutic regimens for managing migraine treatments.

73) Giri:
Giri may denote an author or researcher contributing insights on tablet formulations or drug delivery systems. Acknowledging individual contributions emphasizes the collaborative and multifaceted approach needed in advancing pharmaceutical research.

74) Papa:
Papa highlights the familial aspect of patient support systems, where family involvement can significantly influence adherence to medication regimens. The presence of supportive family members can enhance the overall effectiveness and compliance of patients in managing health conditions.

75) Sah:
Shah could refer to another author or researcher in the field of pharmaceutical sciences. Recognizing various names involved enriches the context of the research, showcasing collaboration that enhances the quality of findings in drug formulation studies.

[Note: The above list is limited to 75. Total glossary definitions available: 83]

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Ideal characteristics, Sublimation process, Environmental condition, Bioavailability, Patient population, Solid dosage form, Stability study, Controlled release, Dosage form, Average weight, Patient safety, Weight variation, Hygroscopic nature, Disintegration time, Compressibility index, Tablet compression, Friability test, Compatibility studies, Pharmacological response, Melting point, Pharmaceutical Research, Novel drug delivery system, Drug properties, Migraine, Dissolution rate, Patient compliance, Weight variation test, Formulation Development, Taste-masking, Mechanical strength, Melting point determination, Direct compression, FDA, Neuroleptics, Hardening process.

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