Overview, Advantage And Disadvantage Of Pharmaceutical Effervescent Tablets

Effervescent tablets are designed to break in contact with liquid such as water or juice, often causing the tablet to dissolve into a solution. The benefit of effervescent tablets is that they dissolve completely and evenly meaning that localized concentrations of the ingredients cannot occur. This means not only a better taste but also less chance of irritation and a more efficient means of ingesting the ingredients.

Effervescent tablet

Effervescence consists of a soluble organic acid and an alkali metal carbonate salt, one of which is often the active pharmaceutical ingredient (API). CO2 is created by the reaction between carbonate or bicarbonate and a weak acid such as citric acid or tartaric acid. Carbon dioxide is formed if this mixture comes into contact with water. They have good stomach and intestinal tolerance. The tablet disintegration should complete within a few minutes (15 minutes).

Components Of Pharmaceutical Effervescent Tablets

The main acid used is citric acid. The other acids of adipic, tartaric, malic and fumaric are also used. Alkali sources are potassium carbonate and bicarbonate, and sodium carbonate and bicarbonate. When considering low cost, high solubility and intensity of reaction, sodium carbonate is preferred.

Effervescent tablets are formulated by mixing these agents along with excipients; water soluble lubricants, colors, flavorings, sweeteners, binders and diluents then compressing them into tablets. (PVP) is used as an effervescent binder. Its form is as dry powder or wet forms of aqueous or hydroalcoholic solutions. Mannitol and PEG 6000 are other effective binder.

To obtain excellent flowability, production is made by direct compression method. To achieve agglomeration of the particles, monohydrate citric acid is released in the fusion method (at 54°C). Using a nonreactive solution, such as ethanol or isopropanol, granulation is achieved. 0.1–0.5% water is enough for an active solution.

The rate of effervescence can be modified with the use of a plasticizer. Basically, increasing the amount of plasticizer prolongs the rate of effervescence. Also, by controlling the hydrophobicity and hydrophilicity of binders used in the hot melt extrusion process, one can modify the effervescence. Increasing hydrophobic binder amounts reduces the rate of effervescence.

If a slight excess of either acidic or alkaline agents is used, they will enhance the effervescence rate compared to both the agents used in the same quantity. Further, these effervescent tablets can be coated to have drug release at the desired site in gastrointestinal tract (GIT).

API is either present in the effervescent granule mixture, or if it is having poor solubility, then it is converted into the salt form during the dissolution process. Effervescent tablets do not need disintegrants incorporated into their formulations as the evolution of in situ CO2 facilitates the disintegration process.

Dyes or lake pigments can be added to produce colored solutions or products. During production, hygroscopic materials are used to absorb moisture. Lubricants are used to prevent adhesion of the tablets. Sucrose is added as a hygroscopic material and causes the tablet to increase bulk. Aspartame and sucralose are the other sweeteners.

Mechanism Of Effervescent Tablets

These delivery systems utilize matrices prepared with swellable polymers such as methocel or poly saccharides and effervescent components or matrices containing chambers of liquid that gasify at body temperature. Flotation of a drug delivery system in the stomach can be achieved by incorporating a float.

Acid neutralizes a carbonated salt in an autocatalytic reaction. At the end, carbon dioxide gas is released which produces the fizzing. To initiate the reaction, water is important. If there is no water in the medium, acid or carbonate cannot dissociate and the reaction cannot be initiated. After the reaction begins, more water is generated.

Manufacture Of Pharmaceutical Effervescent Tablets

Effervescent granules are manufactured in low humidity areas. Effervescent granules are mixed in a V-type blender or a ribbon blender. Wet granulation is performed by using 0.1%–1% (weight by weight basis) of water and then immediately, granules are transferred to the drying oven. Care should be taken that all of the equipment used does not contain traces of water or moisture as it can destroy the effervescent mixture.

After drying, the granulation is sized, mixing them with water-soluble lubricants, and then compressed into tablets. Strict control of humidity in all of the manufacturing areas is a must [65°F–75°F, 10% relative Humidity (RH)]. Any packaging material used for an effervescent tablet should protect the tablet from external shear as well as entrap a small amount of air within it since moisture present in entrapped air can lead to physical and/or chemical degradation of the tablet.

Advantages Of Effervescent Tablets

1. Rapid drug action and it easily dissolve

2. Significant differences in absorption kinetics

(gastric emptying rate, rapid tablet dissolution)

3. Facilitate drug intake, for example vitamins

4. Easy alternative to regular tablets for 5hise who fund it hard to swallow

5. Increased liquid intake

6. Good stomach and intestinal tolerance

7. More portability

8. Improved therapeutic effect

9. Improved palatability

10. Superior stability

11. More consistent response

12. Incorporation of large amounts of active ingredients

13. Accurate dosing

Disadvantages Of Effervescent Tablets

1. It is only intended for immediate release, not for sustained or controlled release

2. Unpleasant taste of some active ingredients,

3. Relatively expensive to produce due to large amounts of more or less expensive excipients and special production facilities.

4. Not suitable for patient with cardiovascular health disease because if the sodium content

5. Bitter tasting active pharmaceutical ingredient may be difficult to formulate as effervescent tablets

Search This Blog

DrugXpert Blog