Review of sublingual risperidone minitablets via melt-granulation.
Journal name: World Journal of Pharmaceutical Research
Original article title: An extensive review on sublingual minitablet of respiridone and evaluation by melt-granulation method
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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G. Hariharaputhraayyanar and B. Manoj
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: An extensive review on sublingual minitablet of respiridone and evaluation by melt-granulation method
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Doi: 10.20959/wjpr20241-30911
Copyright (license): WJPR: All rights reserved
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Summary of article contents:
Introduction
The research article discusses the formulation and evaluation of sublingual minitablets containing the antipsychotic drug risperidone using the melt granulation method. Risperidone is primarily utilized for the treatment of mental health disorders such as schizophrenia, bipolar disorder, and autism spectrum disorder. Due to its short half-life and extensive metabolism in the liver, conventional oral delivery methods often require frequent dosing, which can compromise patient compliance. This study aims to enhance the bioavailability and patient adherence to medication regimens by developing a twice-daily sublingual tablet formulation.
Melt Granulation Method
One of the key concepts discussed is the melt granulation technique, a process that solves the challenges associated with handling fine, poorly compressible materials commonly found in pharmaceuticals. Unlike traditional wet granulation, where a solvent is used, melt granulation utilizes a heated binder—typically a low-melting-point polymer or lipid—to agglomerate dry powders. This method not only simplifies the granulation process but also eliminates the need for drying steps, resulting in a more efficient manufacturing process. The article highlights how this technique can lead to improved dissolution profiles and enhanced bioavailability of active pharmaceutical ingredients (APIs), specifically in developing formulations for moisture-sensitive compounds.
Physicochemical Studies
Another significant aspect of the research involves conducting physicochemical studies to assess the compatibility between risperidone and various excipients through Fourier-transform infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC). These tests are essential to understand the interactions between the drug and excipients like silicified microcrystalline cellulose, polyethylene glycols (PEG), and polyvinyl alcohol (PVA). The results of these studies help optimize the formulation, ensuring that the drug remains stable and effective throughout its shelf life. Compatibility assessments are crucial for refining the formulation by identifying suitable excipients that enhance tablet properties such as dissolution and mechanical strength.
Optimization of Formulation
The paper also details the optimization of the formulation by varying the ratios of PEG and mannitol to improve the flow and compression properties of the granules used in the tablet formulation. The blend of excipients, including superdisintegrants, diluents, and flavorings, plays a vital role in achieving desired tablet characteristics, such as rapid disintegration time and an improved mouthfeel. This optimization process involves systematic experimentation to evaluate the effects of different combinations of binders and excipients on the final product's performance, showcasing the intricate balance required in pharmaceutical formulations to address both efficacy and patient experience.
Conclusion
The development of sublingual minitablets for risperidone via the melt granulation method indicates a promising stride towards enhancing patient compliance in psychiatric treatment. The combination of improved bioavailability through rapid dissolution and patient-friendly administration positions this formulation as a significant advancement over traditional oral dosage forms. The ongoing research emphasizes the need for meticulous characterization and optimization of formulations in ensuring effective therapeutic outcomes while minimizing the challenges associated with conventional delivery methods. Overall, this study offers valuable insights into modern pharmaceutical practices aimed at improving drug delivery systems for a diverse patient population.
FAQ section (important questions/answers):
What is Risperidone used for in treatment?
Risperidone is an antipsychotic medication primarily used to treat schizophrenia, bipolar disorder, and autism spectrum disorder. It helps manage symptoms associated with these conditions, improving overall patient compliance.
What is melt granulation in pharmaceutical formulation?
Melt granulation is a process where a low melting point binder is used to agglomerate pharmaceutical powders. This technique enhances flow properties and facilitates tablet formation without the need for solvents, streamlining the formulation process.
What are the benefits of sublingual tablets for Risperidone?
Sublingual tablets of Risperidone promote rapid disintegration and dissolution, leading to faster absorption into the bloodstream. This method improves bioavailability, making them particularly beneficial for patients with swallowing difficulties.
What excipients were used in the formulation of Risperidone tablets?
The formulation included polyethylene glycol (PEG), mannitol, silicified microcrystalline cellulose (MCC), hydroxyethyl cellulose, and Croscarmellose sodium. These excipients enhance solubility, stability, and disintegration properties of the tablets.
How was drug-polymer compatibility assessed in the study?
Drug-polymer compatibility was evaluated using Fourier-Transform Infrared Spectroscopy (FTIR), which identifies interactions and ensures that the components do not adversely affect each other's properties during formulation.
What was the goal of the research conducted on Risperidone?
The research aimed to design and evaluate sublingual tablets of Risperidone using the melt granulation method to enhance bioavailability and patient adherence through improved drug delivery systems.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Review of sublingual risperidone minitablets via melt-granulation.”. 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:
A drug is a substance used to diagnose, cure, treat, or prevent diseases. In this context, risperidone is highlighted as an antipsychotic drug used for conditions such as schizophrenia and bipolar disorder. The formulation and delivery methods significantly influence the drug's bioavailability and therapeutic efficacy in patients.
2) Science (Scientific):
Sciences refers to the systematic study of various phenomena and principles in different fields such as physics, chemistry, biology, and pharmacology. This multidisciplinary approach is vital in pharmaceutical research, driving innovations in drug formulation and improving patient healthcare outcomes.
3) Water:
Water is an essential solvent in pharmaceutical formulations, affecting dissolution and absorption rates of drugs. In the context of the research, maintaining a suitable water activity level is important for granulation processes, ensuring that tablets dissolve efficiently for optimal drug delivery, particularly for patients with swallowing difficulties.
4) Sugar:
Sugar serves both as a sweetening agent and a component to aid tablet disintegration. In the study, different sugar ratios were analyzed to enhance the mouthfeel and solubility of risperidone sublingual tablets, improving patient compliance, especially for populations needing quick and effective drug delivery.
5) Table:
In this context, the term 'table' refers to tablet dosage forms in pharmaceutical sciences. Tablets are solid dosage forms that deliver drugs in a controlled manner. The review are studying the formulation of sublingual tablets, which offer rapid disintegration and faster absorption compared to traditional dosage forms.
6) Gelatin:
Gelatin is a natural polymer often used as a gelling agent and film-former in pharmaceutical formulations. Its properties make it suitable as a meltable binder in sublingual tablet preparation, which can enhance the disintegration and dissolution of medications, leading to improved patient outcomes.
7) Tamilnadu (Tamil-nadu):
Tamil Nadu is a state in southern India where the research was conducted at the Adhiparasakthi College of Pharmacy. The state's rich cultural and educational legacy plays a critical role in advancing pharmaceutical sciences through innovative research and development in drug formulations, improving healthcare within the region.
8) Powder:
Powder refers to the finely divided solid particles used in granulation processes to prepare tablets. In this research, the consolidation of powdered materials through melt granulation is crucial to form stable and effective sublingual tablets while ensuring uniform drug distribution throughout the formulation.
9) Study (Studying):
The study outlines systematic research to develop and evaluate risperidone sublingual minitablets. It examines various formulation methods, including melt granulation, to achieve rapid drug dissolution and absorption, ultimately aiming to enhance patient compliance and therapeutic effectiveness for those with psychotic conditions.
10) Tamil:
Tamil refers to the language and cultural identity prevalent in Tamil Nadu, India. The use of regional languages in scientific communication can help in disseminating research findings to local communities, strengthening education and awareness regarding advancements in pharmaceutical sciences among indigenous populations.
11) Nadu:
Nadu, meaning 'land' or 'country' in Tamil, forms part of various place names in India, including Tamil Nadu. Its significance in this context lies in highlighting the geographical and cultural background of the research, facilitating recognition of the local contributions to the pharmaceutical sciences and education.
12) Melmaruvathur:
Melmaruvathur is a town in Tamil Nadu, India, notable for its educational institutions, including the Adhiparasakthi College of Pharmacy where the research was conducted. This location fosters significant advancements in the field of pharmacology and serves as a hub for pharmaceutical education.
13) Chennai:
Chennai is the capital of Tamil Nadu and a major educational and economic center in southern India. Its universities and research institutions, including those focusing on pharmaceuticals, attract students and professionals, contributing to advancements in drug delivery systems and pharmaceutical sciences.
14) Heating:
Heating is a crucial process in melt granulation, where materials are subjected to elevated temperatures to facilitate the melting of binders and the formation of granules. This process improves the flow properties of powders, essential for producing high-quality sublingual tablets that disintegrate effectively.
15) Surface:
The surfaces of pharmaceutical tablets significantly affect their interactions with biological environments. Analyzing the surface properties can reveal insights into the disintegration and dissolution rates of sublingual tablets, ensuring effective release profiles and optimal drug absorption in the body.
16) India:
India is a diverse country with a robust pharmaceutical industry and significant research contributions to global pharmaceutical sciences. The study of risperidone sublingual tablets in India underscores the country's commitment to healthcare advancements and improving patient outcomes through innovative drug formulations.
17) Pur:
In pharmacology, 'poor' may refer to poor metabolizers or low bioavailability in drug formulations. Understanding patient variations, such as metabolism rates or swallowing difficulties, is crucial to developing effective delivery systems like sublingual tablets that improve drug absorption and therapeutic outcomes.
18) Pharmacology:
Pharmacology is the branch of medicine that focuses on the study of drug action on biological systems. This research highlights the importance of understanding pharmacokinetics and pharmacodynamics in developing drug formulations, ensuring that the sublingual delivery systems effectively release the active drug in patients.
19) Raghavendra:
Raghavendra is a common name in India and might refer to authors or researchers in scientific literature. Mentioning authors such as Raghavendra signifies their contributions to the field, enhancing the credibility and depth of research in formulations and the pharmaceutical sciences.
20) Swallowing:
Swallowing presents a challenge for certain patient populations, such as the elderly or those with psychological disorders. The formulation of sublingual tablets aims to address this issue by providing an easy-to-administer alternative, improving compliance and ensuring effective medication delivery in various conditions.
21) Transformation (Transform, Transforming):
The term 'transform' in pharmaceutical contexts can refer to the process of changing drug formulations to improve efficacy or delivery methods. In this research, transforming conventional oral medications to sublingual tablets enhances patient compliance and provides faster drug absorption for effective therapeutic intervention.
22) Toxicity:
Toxicity relates to the degree to which a substance can harm living organisms. In drug research, understanding the toxicity profile of active ingredients, like risperidone, is crucial in formulation development to ensure patient safety and minimize adverse effects while providing therapeutic benefits.
23) Swelling:
Swelling refers to the increase in size or volume of granules or tablets due to absorption of moisture or the action of superdisintegrants. This property is important for evaluating the disintegration and dissolution behavior of sublingual tablets, enhancing drug release efficiency.
24) Relative:
Relative properties or characteristics in pharmaceutical formulations are essential to understand when optimizing drug delivery. Comparing the efficacy, bioavailability, and patient compliance of sublingual tablets relative to traditional dosage forms can inform better formulation practices and enhance patient therapeutic experiences.
25) Venkata (Vemkata):
Venkata is another common name in India, often seen in academic and research contexts. Authors with this name contribute to advancements in pharmaceutical sciences, further enriching the research landscape and highlighting collaborative efforts in drug development and formulation optimization.
26) Mishra (Misra):
Mishra, as a surname commonly found in India, may represent a researcher or contributor in the field of pharmaceutical sciences. The involvement of individuals like Mishra emphasizes the significance of collaborative research in achieving advancements in drug formulation and delivery systems.
27) Sharman (Sarma, Sarman, Sharma):
Sharma is a prevalent surname in India, commonly associated with scholars and professionals in various fields. The mention of researchers like Sharma underscores the collaborative nature of scientific research in pharmacology, contributing to developments in pharmaceutical technology and effective drug delivery systems.
28) Medium:
In the context of drug formulation, 'medium' refers to the environment in which dissolution testing occurs, influencing the release characteristics of the drug. The study utilized phosphate buffer as a dissolution medium to accurately assess the solubility and bioavailability of the formulated tablets.
29) Nibha:
Nibha is a common name in India and may refer to contributors or researchers in the pharmaceutical sciences. The acknowledgment of individuals like Nibha enhances the collaborative nature of research, promoting diverse perspectives and insights into drug formulation and delivery mechanisms.
30) Gunda (Gumda):
Gunda, often a surname, may be associated with researchers involved in pharmaceutical studies. The presence of authors like Gunda signifies contributions to the advancement of healthcare through research, helping to refine drug formulations and optimize therapeutic strategies for patients.
31) Kumar:
Kumar is a widely used surname in India, often representing scholars or professionals in various sectors, including pharmacology. The contributions of individuals like Kumar highlight the importance of collaborative research efforts in advancing pharmaceutical sciences and improving patient care.
32) Glass:
Glass can refer to glassware commonly used in laboratory settings for drug formulation and analysis. In pharmaceutical research, glass containers and apparatus are essential for handling substances, ensuring precise measurements, and conducting experiments crucial to understanding drug behaviors and properties.
33) Anna:
Anna refers to a common name in India that may represent individuals contributing to scientific research. The presence of scientists or researchers named Anna emphasizes the diversity in academic contributions and collaboration in advancing pharmaceutical sciences and innovative drug delivery systems.
34) Miṇi (Mini):
Mini may refer to mini-tablets, a specific dosage form aiming for rapid disintegration and absorption. The development of mini-tablets, especially sublingual forms, offers advantages in dosing accuracy, ease of administration, and therapeutic effectiveness, particularly for patients with specific swallowing difficulties.
35) Food:
Food has implications in pharmacology, particularly regarding drug interactions and absorption. Meal timing, composition, and food-drug interactions can significantly influence the bioavailability of drug formulations, making it crucial to consider these factors in developing and prescribing medications.
36) Seth:
Seth is often a surname that may represent a researcher in pharmaceutical sciences. The contributions of individuals like Seth highlight the importance of collaborative efforts in research, promoting innovation and improvements in formulation and delivery methods for drugs.
37) Line:
Line can refer to production lines in pharmaceutical manufacturing where drug formulations are mass-produced. Implementing efficient processes along the production line, such as melt granulation, enhances product quality, reduces costs, and improves the efficiency of drug delivery systems.
38) Life:
Life refers to the state of living organisms. In pharmacology, the impact of drug formulations on patients' quality of life is a critical consideration, as it influences treatment adherence and overall healthcare outcomes. Effective drug delivery methods can significantly enhance patients' everyday functioning.
39) Oil:
Oils can signify lipids used in pharmaceutical formulations, particularly in melt granulation techniques. These oils may serve as active components or excipients, influencing the solubility, absorption, and release profiles of drugs, ultimately contributing to the effectiveness of various dosage forms.
Other Science Concepts:
Discover the significance of concepts within the article: ‘Review of sublingual risperidone minitablets via melt-granulation.’. Further sources in the context of Science might help you critically compare this page with similair documents:
Bioavailability, Compatibility studies, Oral bioavailability, Dose Optimization, Taste-masking, In vitro drug release, Active pharmaceutical ingredient, Risperidone, Pharmaceutical application.