Effervescent Tablets

Mohammad Vakar*, Shaikh Imran Kalam, Dr. G.J. Khan, M Sohil M Shabbir, Aman Shaikh, Shaikh Md. Moiz

JIIU’s Ali Allana College of Pharmacy Akkalkuwa, Dist-Nandurbar -425415, Maharashtra, India

Correspondence: mohammadvakar7271@gmail.com 

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INTRODUCTION

The term "effervescent" refers to the fizzing, foaming, and bubbling that happen when components dissolve in water or aqueous solutions. Gases can be introduced into liquids either through pressurization or by chemical reactions occurring in place. (1) Effervescent technology has become increasingly significant and is now being utilized alongside traditional extraction methods. Solid medications can be taken orally in the form of powders, tablets, capsules, or cachets. Each of these dosage forms represents a single unit of medication, hence they are classified as solid unit dose forms.(2). Tablets and capsules make up more than two-thirds of the total production and expenditure in the global pharmaceutical market. Tablets, in particular, represent the classic form of solid dosage. In fact, over 70% of all medications are dispensed as tablets, establishing them as the most commonly utilized dosage form. This prevalence can be attributed to their ease of use, accurate dosing, and stability, making them a preferred choice for both manufacturers and patients alike. (3) 

The tablet quickly dissolves by releasing carbon dioxide into the water. This effervescent reaction produces carbon dioxide, which improves the absorption of active ingredients by enabling them to move through the paracellular pathway. (4) These dosage forms are beneficial for such patients because the effervescent formulation bypasses direct contact with the gastrointestinal tract..(5) The onset of effects is delayed because liquid dosage forms are absorbed more rapidly than tablets. Both the supplement and pharmaceutical industries are experiencing an increase in the use of effervescent pills.6)  

PROPERTIES

Anhydrous citric acid and sodium bicarbonate are also utilized as effervescent agents. The mixture should comprise 10% to 20% effervescent agents. Figure 1 shows an effervescent tablet in a glass of water. Specially formulated tablets include carbon tablets and effervescent tablets.

 PLEASANT TEST  COMPARED TO REGULAR  TABLETS ^(7.8.9)

Effervescent tablets are favored for their rapid dissolution in liquids such as water or fruit juice, resulting in a more pleasant taste compared to standard tablets. These effervescent forms promote optimal absorption and maximize the benefits of the active ingredients, whereas traditional tablets dissolve more slowly and less completely.

 More Evenly Distributed

 This enhances the flavour of effervescent tablets, minimizes discomfort, and allows for the incorporation of effervescent agents, unlike regular tablets that dissolve slowly and can irritate the gastrointestinal tract. In addition to delivering the desired nutritional benefits, effervescent tablets also promote increased fluid intake.

Increased Liquid Intake

Boosting fluid intake is especially beneficial during dehydration when consumption is typically reduced. Whether used for oral hydration or medicinal purposes, effervescent tablets offer an effective way to rehydrate and enjoy the advantages of nutritional supplements.

Easy Alternative to Regular Tablets

Effervescent tablets serve as a practical alternative to regular tablets, especially for those who struggle with swallowing due to age or health issues. Older adults who regularly take medications or supplements often find it challenging to swallow traditional tablets. Effervescent tablets can ease this difficulty, making them particularly valuable for individuals with sore throats or medical conditions that complicate swallowing. Thus, effervescent tablets provide an effective solution for those facing swallowing challenges.

 To Sum Up

The rising popularity of effervescent tablets is easy to see. Their uniform and rapid dispersion makes them a more effective option for taking vitamins or medications compared to traditional tablets. Effervescent tablets are especially favored by individuals using supplements, as they taste better, can be mixed with water or other liquids, and are easier to swallow for those who may have difficulty. The reaction between an acid and sodium bicarbonate, resulting in the formation of sodium citrate, water, and carbon dioxide, further illustrates their efficiency.

Figure 1: Mechanism of Effervescence 

ENFUNDAMENTALOF   EFFERVESCS

Effervescence occurs when a soluble organic acid reacts with an alkali metal carbonate salt, which often includes the active pharmaceutical ingredient (API). When this combination is exposed to water, it produces carbon dioxide. Common examples of acids and alkalis used in this process include citric acid, as well as malic, fumaric, and tartaric acids.

ADVANTAGES ( 11.12 )

Quick onset of effects. o No need to swallow tablets. o Excellent tolerance in the stomach and intestines. o Enhanced mobility. o More pleasant taste. o Improved stability. o More consistent reaction. o High concentration of active ingredients. o Precise dosing. o Better treatment outcomes.

In remote areas where parenteral options are costly or where skilled medical professionals are unavailable, effervescent tablets can serve as an alternative.

DISADVANTAGES ^{( 12 )}

Some active ingredients have an unpalatable taste. o Larger tablets require special packaging materials. o They tend to be more expensive compared to larger tablets that need specific packaging supplies.

Complete dispersion may take longer. Certain active substances may also have an  o unpleasant flavor.

FORMULATION  ^{( 13 )}

 It typically includes a blend of acids and/or acid salts, carbonates, and hydrogen carbonates, along with the active ingredients. When this mixture is mixed with water, it generates carbonic acid gas.

 DRUGS THAT ARE FORMULATED AS EFFERVESCENT TABLETS 

Substances that may cause stomach discomfort or are difficult to digest: When taken as an effervescent, calcium carbonate dissolves in water and is quickly absorbed by the body. This helps prevent constipation caused by low stomach acid and excessive gas buildup.

Antibiotics and amino acids are examples of drugs sensitive to pH levels. Effervescent formulations can help buffer the aqueous solution, raising the stomach's pH and preventing the inactivation or degradation of the active ingredient caused by the stomach's low pH.

Substances that require high dosages: A standard effervescent tablet typically weighs five grams and measures about an inch in diameter. It can contain approximately two grams of water-soluble ingredients.

EXCIPIENTS

Grease serves as an excipient in effervescent formulations. A lubricant for these products should be non-toxic, tasteless, and water-soluble. For example, a blend of 4% polyethylene glycol (PEG) 6000 and 0.1% sodium stearyl fumarate has proven effective for vitamin C tablets produced through direct compression. Other water-soluble lubricants recommended for effervescent tablets include sodium acetate, common salt, and D, L-leucine, used in very small amounts. Additionally, surfactant lubricants such as sodium lauryl sulfate and magnesium are utilized. Ant enthusiasts often use polyurethane or polytetrafluoroethylene discs to prevent the grains from sticking together.

Surfactants

Aiming to enhance the speed at which medications dissolve and become hydrated.

Sweeteners

Saccharin, sucrose, and other natural sweeteners are utilized to enhance flavor.

Sweeteners often incorporate flavors to mask any unpleasant tastes by creating a more appealing effect.

Colors: A water-soluble dye is added to provide an attractive appearance.

Typical Production Process for Carbonated Products:

The effervescent formulation is made up of three key components:

•       Acid source

•       Active ingredient

•       Bicarbonate or carbonate-based alkaline substance.

Table 1. Components of Effervescent Formulation.

 EVALUATION OF EFFERVESCENT TABLET  ^{(14.15.16.17)}

PRE-COMPRESSION PARAMETERS:

 1) Angle of repose (θ):

The angle of repose is the steepest angle at which the surface of a pile of powder can rest against a horizontal plane. It can be used to calculate the frictional force in loose powders or grains and serves as an indicator of the powder's flow characteristics.

tan-1 (H/R) tan θ = H / R θ

 H is the height of the pile if θ is the angle of repose. 

 R is the base radius of the pile. 

The powder mixture was poured into a funnel secured to a stand at a specified height (H). The angle of repose was determined by measuring the height and radius of the resulting powder mound. This angle represents the steepest incline that a powder pile can maintain against a horizontal surface. It indicates the frictional force within loose powders or granules and effectively reflects their flow properties.

tan θ = H / R θ = tan-1 (H/R) 

where θ is he angle of repose,

 H is the pile's height, and R is the pile's base radius.

The powder mixture was permitted to flow through a funnel secured to a stand at a designated height (H). The angle of repose was calculated by measuring the height and radius of the resulting powder pile, ensuring that the particles slid and rolled over each other as they moved through the funnel's edges. This process illustrates the relationship between the angle of repose and the flow characteristics of the powder.

TABLE 2

2)     Flow Rate :

The flow rate of the powder refers to the speed at which a specific mass moves through a funnel of appropriate diameter. A timer was used to measure the duration it took for the entire granule mass to exit through the opening. The flow rate was then determined using the following formula:

Flow Rate = Granule Weight / Time Duration.

3)     Bulk Density :

The bulk density of a powder was determined by dividing its mass by its bulk volume, measured in cm³. For each formulation, the bulk density was calculated by taking the sample weight in grams and dividing it by the final volume of the sample in cm³ within the cylinder. The formula used for this calculation is:

M / Vp = Df

 where Df  represents the bulk density, 

M is the sample weight in grams, and 

Vp is the final volume of the granules in cm³.

4)     Tapped density : 

The tapped density was determined by dividing the mass of the powder by its tapped volume, measured in cm³. For each formulation, the tapped density was calculated by taking the sample weight in grams and dividing it by the final tapped volume in cm³ within the cylinder. The formula used for this calculation is: M / Vp =Do

where Do represents the tapped density.

 Here, M is the sample weight in grams, and Vp  is the final volume of the granules in cm³.  Bulk density is similar to Do

5)     Carr’s Index : 

Each formulation's Carr's index was determined using the following equation: 

Compressibility percentage = Df-Do × 100 /Df 

 Df  stands for bulk density, fluff, or poured bulk. 

Do = Consolidated or Tapped Bulk Density. 

EVALUATIONS  OF   EFFERVESCENT  TABLETS:

Physicochemical  Evaluation of the Effervescent Tablets

The following physicochemical tests were conducted to evaluate the tablets.

Weight Variation  

Weight Variation: Twenty tablets were randomly selected and weighed individually. The weights of these tablets were compared to the calculated average weight. According to this process, the variation should not exceed the pharmacopoeial limits, which allow for a deviation of ± 5% from the mean weight for more than two tablets.

Friability Test  

To assess the friability of the tablets, I used a friabilator. The tablets were placed in a sturdy cylinder that rotated at 25 rpm, dropping them six inches at a time for four minutes to expose them to a combination of shock and abrasion. Afterward, the tablets were reweighed. Following the removal of any dust with a soft muslin cloth, they were weighed again. This process allowed for the calculation of the friability percentage. I consider a friability of less than 1% to be optimal.

Thickness 

The thickness of the effervescent tablets is measured using a sliding caliper scale. A tray is filled with twenty randomly selected effervescent tablets, and then the total thickness of the tablet's crown is measured.

Hardness ^{( 18 )}

Tablet hardness, also referred to as tablet crushing strength, is assessed using a hardness test. This test measures the force needed to break the tablet.

Hardness Tester Figure No.2

Friability  ^{( 19 )}

Twenty effervescent tablets are placed in the Roche friabilator after being weighed. As the friabilator spins at 25 rpm, the tablets are dropped from a height of six inches. Afterward, the tablets are weighed again and crushed into a powder.

Friabilator Figure No.4

Disintegration time ^{( 20 )}

The pH of a solution in standardized water at the same volume and temperature is measured using a digital pH meter. An effervescent tablet is placed in a beaker containing 200 milliliters of

water heated to between 1500 and 2500 degrees Celsius. The pH is recorded once the effervescent tablet has completely dissolved.

Solution pH  ^{( 20 )}

The pH of a solution in standardized water at the same volume and temperature is assessed using a digital pH meter. An effervescent tablet is added to a beaker containing 200 milliliters of water heated to between 1500 and 2500 degrees Celsius. The pH is measured once the tablet has completely dissolved.

Drug content ⁽²¹⁾

To determine the drug content, dissolve the effervescent tablet in 200 milliliters of water. Use a UV spectrophotometer to measure the absorbance of this solution, which will indicate the amount of medication in the tablet.

Measurement of CO2 content  ^{( 21)}

Weight variations are calculated after dissolving one effervescent tablet in 100 milliliters of 1N sulfuric acid solution. The resulting weight difference indicates the concentration of CO2 (in milligrams) per tablet. The averages of these measurements are then computed.

Evaluation of the water content

10  tablets of the combination are dried with activated silica gel in a desiccator for four hours. A water content of 0.5% or less is established as an acceptable limit.

APPLICATIONS  OF  EFFERVESCENT  TABLETS ^{( 21,22 )} 

The medication is administered as planned. Effervescent osmotic pump tablets were utilized for controlled release, and there were also effervescent cosmetic tablets available.

The concentration of effervescent agents plays a crucial role in determining the floating time within floating drug delivery systems.

Using effervescent tablets enhances compatibility, simplifies dose administration, increases fluid intake for patients, promotes faster and better absorption, and addresses the challenges associated with taking large doses of medication.

CONCLUSION 

Effervescent tablets can be produced using three methods: dry, wet, and compression. The wet method is the most commonly used for creating effervescent granules. The formulations are evaluated for hardness, friability, weight variation, and disintegration time.

Known as carbon tablets, effervescent tablets are designed to dissolve in water and release carbon dioxide. They are produced by compressing powdered ingredients into a dense mass, which is then sealed in a blister pack or a container with a desiccant in the cap. These tablets are used by mixing them with water to create a solution. Additionally, powdered materials can be granulated and marketed as effervescent granules or packaged as effervescent powders. Typically, the powdered materials are granulated prior to tablet production.

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