Zolpidem tartrate solid dispersion sublingual tablet evaluation
Journal name: World Journal of Pharmaceutical Research
Original article title: Formulation and comparitive in-vitro evaluation of zolpidem tartrate solid dispersion sublingual tablet
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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Original source:
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Tharini L. and Satish C. S.
World Journal of Pharmaceutical Research:
(An ISO 9001:2015 Certified International Journal)
Full text available for: Formulation and comparitive in-vitro evaluation of zolpidem tartrate solid dispersion sublingual tablet
Source type: An International Peer Reviewed Journal for Pharmaceutical and Medical and Scientific Research
Doi: 10.20959/wjpr20178-8802
Download the PDF file of the original publication
Summary of article contents:
1) Introduction
The study focuses on enhancing the solubility of the anti-psychotic drug Zolpidem tartrate through the formulation of solid dispersion sublingual tablets (SDSL). By utilizing solid dispersion methods, specifically with different polymers such as PEG-6000, PEG-4000, and Poloxamer-188, researchers aimed to maintain an optimal plasma concentration of the drug. The research investigates both pre-compression and post-compression parameters, alongside in vitro drug release profiles, to identify the most effective formulation for rapid disintegration and drug absorption.
2) Importance of Solid Dispersion in Drug Formulation
Solid dispersion significantly enhances drug solubility and bioavailability, especially for poorly soluble drugs like Zolpidem tartrate. Various ratios of Zolpidem tartrate with PEG and Poloxamer polymers were prepared using the melting and solvent evaporation methods. The study found that the formulation with Poloxamer-188 at a 1:5 ratio prepared via solvent evaporation method exhibited the highest dissolution rate. This highlights the critical role of solid dispersions in overcoming solubility issues associated with certain pharmaceutical compounds, thus paving the way for improved therapeutic efficacy.
3) Sublingual Drug Delivery Advantages
The study emphasizes the sublingual route of drug delivery as a beneficial method for the administration of Zolpidem tartrate. With this route, drugs are rapidly absorbed into the systemic circulation, bypassing the hepatic first-pass metabolism. This not only expedites the onset of action but also increases bioavailability. Sublingual tablets of Zolpidem are particularly useful for the short-term treatment of insomnia due to their quick action, enhancing patient compliance and satisfaction compared to traditional oral formulations.
4) Formulation Optimization and Stability
Formulation F6, utilizing 5% Croscarmellose sodium as a superdisintegrant, emerged as the optimal choice among the tested combinations, showcasing superior disintegration times and drug release profiles. Stability studies conducted for three months under ICH guidelines revealed that the formulation maintained its integrity, with no significant changes in physical appearance or drug content. This stability is crucial for ensuring the efficacy and safety of pharmaceuticals throughout their shelf-life.
5) Conclusion
The research concludes that solid dispersion sublingual tablets of Zolpidem tartrate can effectively improve the drug's solubility and bioavailability, facilitating faster therapeutic effects for patients experiencing insomnia. Formulation F6 demonstrates the best performance in terms of drug release and stability, suggesting it could serve as a viable alternative to existing marketed formulations. The findings underscore the significance of utilizing innovative formulation technologies to enhance drug delivery systems in pharmaceutical applications.
FAQ section (important questions/answers):
What are sublingual tablets and how do they work?
Sublingual tablets are designed to dissolve under the tongue, allowing rapid absorption into the bloodstream. This method bypasses the gastrointestinal tract and first-pass metabolism, leading to quicker onset of action for medications like Zolpidem tartrate.
What is the purpose of using solid dispersions for Zolpidem tartrate?
Solid dispersions are utilized to enhance the solubility of Zolpidem tartrate, which has low water solubility. This formulation increases drug dissolution rates and improves bioavailability, ensuring effective treatment for insomnia.
Which formulation showed the best drug release for Zolpidem tartrate?
The optimized formulation, F6, containing 5% Croscarmellose sodium, showed the best release profile, achieving 99.87% drug release in 30 minutes, demonstrating its effectiveness for rapid absorption.
What excipients were used in the sublingual tablets' formulation?
The formulation included Crospovidone, Croscarmellose sodium, Sodium starch glycolate as superdisintegrants, with MCC and directly compressible Mannitol as diluents, Magnesium stearate as lubricant, and Aspartame for sweetness.
How stable were the optimized formulations during the study?
The optimized formulations maintained stability over a three-month period according to ICH guidelines. Evaluations showed consistent hardness, drug content, and dissolution properties, affirming their suitability for use.
What were the primary benefits of the prepared Zolpidem tartrate tablets?
The prepared tablets provided enhanced solubility and rapid dissolution, allowing for quicker onset of action in treating insomnia. The use of solid dispersion technology significantly improved their pharmacokinetic properties.
Glossary definitions and references:
Scientific and Ayurvedic Glossary list for “Zolpidem tartrate solid dispersion sublingual tablet evaluation”. 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 this study, 'drug' refers specifically to Zolpidem tartrate, an anti-psychotic medication used primarily for treating insomnia. The formulation aims to enhance its solubility and bioavailability through innovative delivery methods, such as solid dispersion sublingual tablets, thus emphasizing the importance of drug formulation in pharmacotherapy.
2) Table:
The 'table' in this context primarily refers to the sublingual tablets developed in the study for the delivery of Zolpidem tartrate. Tables outline important information such as formulation components, ratios, and results of pre-compression and post-compression tests, showcasing the organization and clarity necessary in scientific research for data presentation.
3) Water:
Water is crucial to this research as it serves as a solvent in various experimental procedures, including drug dissolution studies. It acts as a medium for testing solubility and release profiles of Zolpidem tartrate, affecting how the drug interacts with different excipients and how well it can be absorbed into the bloodstream.
4) Study (Studying):
The term 'study' denotes the structured investigation conducted to formulate and evaluate the sublingual tablets of Zolpidem tartrate. It encompasses methodologies to test solubility, drug release, and stability, laying the groundwork for future applications in pharmaceuticals through rigorous testing and validation of findings in drug formulation and delivery systems.
5) India:
India is significant in this research context as the location where the study and formulation development occurred. The involvement of institutions like Hillside College of Pharmacy and PES College of Pharmacy in Bengaluru reflects India's growing emphasis on pharmaceutical research and development, particularly in the production of innovative drug formulations catering to local healthcare needs.
6) Post:
The term 'post' pertains to the post-compression parameters evaluated after the formulation of the tablets. This includes tests for hardness, friability, thickness, and weight variation. Such assessments are critical to ensure the quality and efficacy of the tablets, indicating that the medication will perform reliably in clinical settings.
7) Karnataka:
Karnataka is the Indian state where the research institutions involved in this study are situated. It highlights the region’s active role in pharmaceutical education and innovation, serving as a center for developing novel drug delivery systems, research collaborations, and contributing to advancements in healthcare and drug formulation technologies.
8) Medium:
The term 'medium' refers to the environments used in several experiments, particularly the dissolution medium. In this study, a phosphate buffer of pH 6.8 serves as the medium for evaluating the drug's release profile. The choice of medium is vital in simulating physiological conditions to predict how the drug will behave in vivo.
9) Dish (Dis):
In the experimental context, a 'dish' typically relates to the dish used in wetting tests or drug dissolution experiments. The design and material of the dish are significant for ensuring accurate measurements and results, as it interacts with the tablets and dissolution medium, impacting the outcome of the evaluations.
10) Powder:
'Powder' pertains to the state of the drug or various excipients during formulation and evaluation phases, including preparation of physical mixtures. The consistency, size, and properties of the powder are important for ensuring proper blending, flow, and compression characteristics, significantly affecting the quality of the final tablet formulation.
11) Calculation:
'Calculation' refers to the quantitative assessments done during the study, such as determining drug content, percentage yields, and absorbance readings. Accurate calculations are essential for data analysis and validating the effectiveness and performance of the tablet formulations, ensuring they meet the required pharmacological standards.
12) Discussion:
The term 'discussion' refers to the section where results are analyzed and interpreted in relation to existing knowledge. It allows researchers to contextualize their findings, compare them with previous studies, and highlight the implications for future research. This critical evaluation forms the backbone of scientific inquiry and innovation.
13) Transformation (Transform, Transforming):
'Transform' indicates the changes made to Zolpidem tartrate through processes like solid dispersion to enhance its solubility and absorption characteristics. The transformation of drug solubility profiles plays a fundamental role in developing effective pharmaceuticals, influencing therapeutic outcomes by improving bioavailability for patients requiring medication.
14) Surface:
'Surface' relates to the active surface area of the drug within the formulation, impacting its solubility and dissolution rates. In pharmaceutical formulations, increased surface area often enhances drug release, which is a focal point in developing effective delivery systems for Zolpidem tartrate sublingual tablets.
15) Life:
'Life' refers to the biological aspect of drug activity, particularly its pharmacokinetics and dynamics within a living organism. Understanding drug life, including onset of action and duration, is crucial for assessing therapeutic effectiveness, enhancing patient outcomes, and guiding dosage regimen developments in insomnia treatments with Zolpidem tartrate.