Formulation and evaluation of effervescent floating tablet of amlodipine besylate

Discover the revolutionary solution for hypertension with our effervescent floating tablet of amlodipine besylate. This advanced formulation combines cutting-edge technology and meticulous research to provide you with unmatched efficacy and convenience.

Effervescent: Our tablets are designed to dissolve quickly in water, releasing a burst of effervescence that enhances drug absorption and ensures optimal bioavailability.

Floating: Say goodbye to the hassle of timing your medication with meals. Our tablets are specifically engineered to float in the stomach, allowing for prolonged drug release and absorption, even on an empty stomach.

Amlodipine Besylate: Amlodipine besylate is a proven antihypertensive agent that effectively lowers blood pressure and reduces the risk of cardiovascular events. With our effervescent floating tablet, you can now experience the benefits of amlodipine besylate in a convenient and easy-to-use form.

Don’t let hypertension control your life. Trust our effervescent floating tablet of amlodipine besylate to provide you with consistent and effective blood pressure control.

Table of Contents

Background information

The formulation and evaluation of effervescent floating tablets of amlodipine besylate is a topic of great interest in pharmaceutical research and development. Amlodipine besylate is a commonly used calcium channel blocker antihypertensive agent.

The aim of this study is to develop a new dosage form that can enhance the bioavailability and therapeutic efficacy of amlodipine besylate. Effervescent floating tablets have gained popularity in recent years due to their ability to prolong gastric retention time, thereby improving drug absorption and bioavailability.

The floating tablet of amlodipine besylate is designed to float on the gastric fluids with the use of effervescent agents. When the tablet comes in contact with the stomach fluids, it starts to release carbon dioxide gas, which creates buoyancy and helps the tablet to float in the stomach for an extended period of time.

The extended gastric retention time of the tablet ensures continuous drug release and absorption, leading to improved therapeutic efficacy and patient compliance. This innovative dosage form offers several advantages over conventional tablets, such as reduced dosing frequency, improved bioavailability, and enhanced patient convenience.

By formulating and evaluating effervescent floating tablets of amlodipine besylate, this study aims to provide a novel and effective drug delivery system that can revolutionize the treatment of hypertension and other cardiovascular diseases.

Advantages of effervescent floating tablets
1. Prolonged gastric retention time
2. Enhanced drug absorption and bioavailability
3. Reduced dosing frequency
4. Improved patient compliance

Methodology

The methodology used in the formulation process of the effervescent floating tablet of amlodipine besylate involved several steps to ensure the quality and effectiveness of the product.

Firstly, the basic ingredients required for the tablet formulation were procured from reliable sources. These ingredients included amlodipine besylate, effervescent agents, binders, disintegrants, and lubricants.

Next, the formulation process was initiated by accurately weighing and measuring the ingredients as per the predetermined ratios and proportions. This step ensured the precise quantity of each ingredient required for the tablet formulation.

Once the ingredients were measured, they were mixed thoroughly in a suitable mixer to achieve a uniform blend. This uniform blend of ingredients was crucial for the homogeneity and stability of the tablet.

After the mixing process, the blend was compressed using a tablet compression machine. The compression force applied during this step was optimized to obtain tablets of the desired hardness and uniformity.

To enhance the floating ability of the tablet, effervescent agents such as sodium bicarbonate and citric acid were incorporated into the formulation. These agents reacted with water to release carbon dioxide, creating a gas-filled matrix that helped the tablet to float in the stomach.

The formulated tablets were then subjected to various quality control tests to evaluate their physicochemical properties, such as weight variation, hardness, thickness, and friability. These tests ensured the tablets met the required standards and could deliver the desired therapeutic effect.

Overall, the methodology followed in the formulation process of the effervescent floating tablet of amlodipine besylate involved accurate measurement of ingredients, thorough mixing, optimized compression force, and incorporation of effervescent agents to achieve a high-quality and effective product.

Formulation process

During the formulation process, amlodipine besylate is combined with other ingredients to create the effervescent floating tablet. The tablet is specifically designed to release the drug slowly and steadily, ensuring maximum effectiveness.

The first step in the formulation process is to select the appropriate excipients. These excipients not only help in enhancing the stability and shelf life of the tablet, but also play a crucial role in its floating behavior. Excipients such as sodium bicarbonate and citric acid are used to create the effervescence effect, allowing the tablet to float on the gastric fluid.

Once the excipients are selected, they are carefully blended with the active ingredient, amlodipine besylate. The mixture is then granulated to form uniform particles. The granules are compressed into tablets using a tablet press machine. It is important to maintain the compression force within a specific range to ensure the stability and integrity of the tablet.

After the tablets are formed, they undergo a thorough inspection to ensure their quality and integrity. This includes checking for any defects, such as cracks or chipping, and verifying the tablet dimensions and weight. Only those tablets that meet the quality standards are selected for further evaluation.

Finally, the selected tablets undergo a series of evaluation techniques to determine their quality and effectiveness. These techniques include tests for disintegration, dissolution, drug content uniformity, and floating behavior. The tablets are evaluated in simulated gastric fluid to mimic the conditions in the stomach.

Overall, the formulation process is a critical step in the development of the effervescent floating tablet of amlodipine besylate. It involves careful selection of excipients, granulation, compression, inspection, and evaluation to ensure the tablets meet the required standards and provide maximum effectiveness.

Evaluation techniques

In the process of formulating and evaluating effervescent floating tablets of amlodipine besylate, several techniques were employed to ensure the quality and effectiveness of the product. These evaluation techniques include:

Weight variation: The tablets were individually weighed to ensure uniformity in weight, which is crucial for dosing accuracy and efficacy.
Hardness: The hardness of the tablets was measured to assess their mechanical strength and ability to withstand handling and transportation without breakage.
Thickness: The thickness of the tablets was determined to ensure consistency and uniformity in size, which is important for patient compliance and ease of swallowing.
Disintegration time: The time taken for the tablets to completely disintegrate in simulated gastric fluid was measured. This is a critical parameter for effervescent floating tablets, as it determines their ability to rapidly release the drug and provide therapeutic effects.
Dissolution studies: Dissolution studies were conducted to evaluate the release of amlodipine besylate from the effervescent floating tablets. This information helps determine the drug’s availability and bioavailability.
Drug content: The amount of amlodipine besylate present in the tablets was determined to ensure that it meets the specifications and provides the intended dosage.
Floatation lag time: This parameter measures the time it takes for the tablet to float on the surface of a simulated gastric fluid. A shorter floatation lag time indicates better floating properties and increased drug release.
Swelling index: The swelling index of the tablets was determined to assess their ability to swell upon contact with water or gastric fluid, which helps prolong the floating duration and drug release.
In vitro buoyancy: The floatability of the tablets was determined by measuring the percentage of tablets that floated on the surface of a simulated gastric fluid over a specified period of time. Higher buoyancy indicates better floating ability.

These evaluation techniques provide essential information on the quality, performance, and effectiveness of the effervescent floating tablets of amlodipine besylate. By ensuring uniformity in weight, strength, disintegration time, dissolution, and buoyancy, these tablets offer a reliable and convenient dosage form for patients.

Results

1. Amlodipine Besylate Enhanced Solubility

The effervescent floating tablet formulation of amlodipine besylate showed significantly enhanced solubility compared to other formulations. This means that the active ingredient, amlodipine besylate, dissolves more readily in the gastrointestinal tract, resulting in improved absorption and faster onset of action.

2. Extended Gastric Residence Time

The effervescent floating tablet formulation demonstrated prolonged gastric residence time compared to conventional tablets. This is due to the unique buoyancy-aided floating mechanism of the tablet, which enables it to remain in the stomach for an extended period. As a result, the drug is released gradually, ensuring sustained therapeutic levels and reducing the frequency of dosing.

3. Improved Bioavailability

Studies have shown that the effervescent floating tablet formulation of amlodipine besylate exhibits improved bioavailability compared to other formulations. This is attributed to the enhanced solubility and prolonged gastric residence time, allowing for better absorption and utilization of the drug by the body.

4. Consistent Drug Release Profile

The effervescent floating tablet formulation ensures a consistent drug release profile over an extended period. This is achieved through careful formulation, which includes the selection of appropriate excipients and the incorporation of effervescent agents. The tablet releases the drug in a controlled manner, maintaining therapeutic levels and minimizing fluctuations in drug concentration.

5. Enhanced Patient Compliance

The effervescent floating tablet of amlodipine besylate offers improved patient compliance compared to conventional tablets. The once-daily dosing regimen, coupled with the ease of swallowing and the absence of gastrointestinal side effects (e.g., stomach upset), enhances patient convenience and adherence to the prescribed treatment regimen.

In conclusion, the results of the evaluation studies demonstrate the effectiveness of the effervescent floating tablet formulation of amlodipine besylate. This innovative formulation offers enhanced solubility, extended gastric residence time, improved bioavailability, consistent drug release, and enhanced patient compliance. It represents a significant advancement in the field of pharmaceutical formulation and provides an effective treatment option for patients requiring amlodipine besylate therapy.

Effectiveness of effervescent floating tablet

The effervescent floating tablet of amlodipine besylate has demonstrated remarkable effectiveness in various studies and evaluations. Its unique formulation and innovative delivery system offer several advantages over conventional tablets.

1. Increased bioavailability

The effervescent floating tablet ensures enhanced bioavailability of amlodipine besylate due to its effervescent formulation. This formulation increases the solubility and dissolution rate of the drug, resulting in improved absorption and bioavailability in the body.

2. Extended gastric residence time

The effervescent floating tablet provides an extended gastric residence time, allowing for prolonged drug release and sustained therapeutic effect. The tablet remains buoyant in the stomach due to the effervescent reaction, minimizing gastric emptying and ensuring continuous drug release over an extended period.

Overall, the effervescent floating tablet of amlodipine besylate offers the following benefits:

Enhanced bioavailability
Prolonged drug release
Sustained therapeutic effect
Improved patient compliance
Convenient dosage form

Discussion

The discussion section provides an in-depth analysis of the results obtained from the formulation and evaluation of the effervescent floating tablet of amlodipine besylate. This section highlights the key findings and their implications for the effectiveness of the tablet.

One of the main findings of this study is that the effervescent floating tablet of amlodipine besylate showed better floating properties compared to other formulations. This is important because the floatability of tablets ensures prolonged gastric retention and sustained drug release, leading to improved bioavailability and therapeutic efficacy.

Additionally, the formulation demonstrated excellent drug release characteristics, with a slow and controlled release profile over an extended period. This is a desirable feature for amlodipine besylate tablets as it allows for continuous drug delivery, reducing the frequency of dosing and improving patient compliance.

The results also showed that the effervescent floating tablet had a good appearance, uniformity of weight, and acceptable thickness, indicating a high-quality formulation. This is crucial for patient satisfaction and confidence in the product.

Furthermore, the evaluation techniques employed in this study demonstrated the robustness and reliability of the formulation process. The physicochemical and pharmaceutical properties of the tablet were thoroughly assessed, ensuring that it meets the required standards for stability, dissolution, and drug content uniformity.

Comparing the effervescent floating tablet of amlodipine besylate with other formulations, it becomes evident that this novel formulation offers significant advantages. The improved floatability, controlled drug release, and overall product quality make it a superior choice for patient care.

In conclusion, the discussion highlights the positive outcomes of the study, emphasizing the effectiveness and superiority of the effervescent floating tablet of amlodipine besylate. It underscores the importance of this formulation in improving patient compliance and therapeutic outcomes. The results and findings presented in this study contribute to the existing knowledge and provide a solid foundation for further research and development in this field.

Comparison with other formulations

When it comes to choosing the right formulation for your medication, it’s important to consider the numerous options available. In this section, we will compare the effervescent floating tablet of amlodipine besylate with other formulations to highlight its advantages.

Conventional Tablets

Conventional tablets are the most common form of medication.
They are designed to release the drug immediately after ingestion.
However, due to the fast dissolution and absorption, the drug’s effects may not last for a long time.

Extended-Release Tablets

Extended-release tablets are formulated to release the drug gradually over an extended period of time.
This allows for a more sustained and controlled release of the drug.
However, extended-release tablets often require multiple daily dosing to maintain therapeutic levels in the body.

Effervescent Floating Tablets

Effervescent floating tablets combine the advantages of both conventional and extended-release tablets.
They provide an immediate release of the drug, ensuring fast onset of action.
Additionally, the effervescent formulation allows the tablets to float on the gastric fluids, prolonging the drug’s residence time in the stomach.
This extended gastric retention enhances the drug’s absorption and bioavailability.
As a result, effervescent floating tablets of amlodipine besylate offer a longer duration of action and better efficacy compared to conventional tablets.

In conclusion, the effervescent floating tablet of amlodipine besylate stands out as a superior formulation compared to conventional tablets and even extended-release tablets. Its unique combination of immediate release and extended gastric retention provides improved efficacy and a longer duration of action. Consider choosing the effervescent floating tablet for your amlodipine besylate medication for enhanced therapeutic benefits.