Reactonz

Why Effervescent Tablet?

Effervescent Technology

Effervescence is defined as the evolution of bubbles of gas from a liquid as the result of a chemical reaction. Effervescent tablet formulations generally include an agent that is capable of releasing CO2 (sodium carbonate and sodium bicarbonate) and an agent that induces releases of CO2 (adipic acid, malic acid, tartaric acid, ascorbic acid, fumaric acid, maleic acid, succinic acid, or citric acid). Majority of effervescent tablet formulations are using Sodium bicarbonate as an agent to release CO2 and Citric Acid to induce releasing the CO2 (Figure 1)

When citric acid and sodium bicarbonate are together comes in contact with water, the effervescent reaction occurs which results in carbon dioxide gas to be released and the tablet dissolved in couple of minutes. Indeed, the effervescent reaction is one the strongest reactions in pharmaceutical industry for tablet disintegration which is due to the pressure of CO2 gas inside the tablet results in complete dissociation and dissolving of tablet ingredients. The ingredients which are used in effervescent tablets are water soluble or they have carefully selected form insoluble ingredients salts which turn into soluble form during dissolution process of effervescent tablet.

As evident in figure, 1 mol of citric acid will react with 3 mol of sodium bicarbonate, that’s why sodium bicarbonate will be used up during effervescent reaction process.

 

 

The Merits of effervescent tablet
  1. Easy to use
  2. A national study into the medicine-taking habits of Australians on 2018, estimated more than 9 million of the population is taking a prescribed medicine every day, with 8 million taking two or more prescribed medicines in a week [1]. On the same year, a survey conducted on 2,000 Australians adults demonstrated that more than 63% of participants are using at least one complementary medicine every day [2].

    The problem intensifies, due the fact that many new pharmaceutical products are manufactured in larg-sized formats, so they can incorporate the required ingredients for the therapeutic outcome along with necessary ingredients for dissolving and absorption of tablets by our body.

    Effervescent tablets are a good choice for people who don’t like tablets and capsules or who have difficulty with swallowing tablets. This is more important for peoples who are taking multiple tablets per day.

     

  3. Increased liquid intake
  4. Effervescent tablets provide the nutritional benefits intended, but in addition to this, they also increase liquid intake. This can be especially beneficial if you are dehydrated or having health issue and not ingesting as much fluid as usual. Effervescent tablets can be a great choice of rehydrating as well as earning the advantages you are taking the tablets for whether this is a dietary supplement or medicine.

     

  5. Pleasant tasting
  6. Effervescent tablets formulations also combine other ingredients such as flavours and sweeteners which help improve the taste. The addition of flavours and sweeteners can help to improve compliance and make taking medications an easier and more pleasant experience.

     

  7. Reduces the side effects of normal tablets and capsules on digestive system
  8. By swallowing normal tablets and capsules, they will start a journey in our digestive system toward disintegration, dissolving, absorption and elimination. From the moment we are swallowing a medicine, the process of disintegration and release of the components are initiated. As matter of fact, normal tablet and capsules will release their ingredients at a specific site of action in our body, which causes the high concentration of medicines at a specific location in our digestive system. This may result in localized sever acidic or basic condition over our tissues and subsequent irritation, gastric refluxes and chronic ulcers.

    Tablets or capsules that stay in the esophagus may release chemicals that can irritate the lining of the esophagus. This may cause ulcers, bleeding, perforation, and narrowing (strictures) of the esophagus. The risk of these types of injuries is greater in persons with medical conditions involving the esophagus.

    One of the most common irritants to the lining of the stomach is that caused by oral medicines. These medicines either weaken the ability of the stomach lining to resist acid made in the stomach or sometimes lead to inflammation of the stomach lining (gastritis), ulcers, bleeding, or perforation of the lining [3] (Figure 2).

     

     

     

    Effervescent tablets pose a unique advantage of dissolving in plenty of water before administration which eradicate the chance of medicine localization in any part of our digestive system. Also effervescent formulations can incorporate buffering and neutralizing ingredients, which can provide neutralized solution for acidic and basic medicines and avoid localized change on our body tissues. Figure 3 shows the comparison between an acidic medicines digestion when in form of effervescent and normal tablet in change of acidity of stomach.

     

    Reactonz - why effervescent tablet - 3

     

  9. Higher bioavailability and faster action
  10. Bioavailability refers to the extent and rate at which the drug enters systemic circulation (blood stream), thereby accessing the site of action.

    Superior bioavailability-The bioavailability of effervescent attracted scientific attention in recent years due to the fact that the active ingredients are already dissolved, and the higher absorption in our blood stream is expected. In fact, studies compared the concentration of medicines in form of normal tablet and effervescent tablets in blood sample of human showed that the effervescent tablets has significantly higher absorption comparing with normal tablet [4,5] . This has opened new avenue for development of novel formulation for higher efficacy medicines in pharmaceutical industry.

    Fast onset of action – The scientific society also evaluated the time for onset of action of medicines in effervescent products versus normal tablets. This has been shown in various published studies that the time that medicines are entered into in blood stream is significantly shorter and the lag time for medicines absorption from digestive system is considerably shorter [6,7]. Shorter time to enter into blood stream provide faster onset of action.

    Converting medicines to soluble form- Effervescent technology also provide a unique avenue for converting conventional low absorbed medicines to the medicines with higher absorption and efficacy. Many medicines contains insoluble active ingredients which has a poor bioavailability once entered to our body. Due to effervescent reaction these medicines can be converted to the soluble form which results in highly bioavailable medicines for our body [8,9].

     

    Reference:
    [1] Wylie C., et.al., A national study on prescribed medicine use in Australia on a typical day, Pharmacoepidemiol Drug Safety, 2020.
    [2] Steel A. et.al., Complementary medicine use in the Australian population: Results of a nationally-representative cross-sectional survey, Scientific Reports, 2018.
    [3] Jaspersen D., Drug-Induced Oesophageal Disorders, Pathogenesis, Incidence, Prevention and Management, Drug Safety, 2000.
    [4] Sakhaee K., et. al., Superior calcium bioavailability of effervescent potassium calcium citrate over tablet formulation of calcium citrate after Roux-en-Y gastric bypass, Surgery for Obesity and Related Disease, 2013.
    [5] Altomare E., et. al., Bioavailability of a new effervescent tablet of ibuprofen in healthy volunteers, European Journal of Clinical Pharmacology, 1997.
    [6] Watson R., et. al., Bioavailability of a new effervescent tablet of ibuprofen in healthy volunteers, Aliment Pharmacology Therapy, 1996.
    [7] Girolamo G., et. al., Relative bioavailability of new formulation of paracetamol effervescent powder containing sodium bicarbonate versus paracetamol tablets: a comparative pharmacokinetic study in fed subjects, Pharmacotherapy, 2007.
    [8] Kalepu S., et.al., Insoluble drug delivery strategies: review of recent advances and business prospects, Acta Pharmaceutica Sinica B, 2015.
    [9] Devi J., et. al., Preparation and evaluation of ibuprofen effervescent granules, Asian Journal of Pharmaceutical and Clinical Research, 2019.