- A more gentle action on the patient’s stomach;
- Improved dissolution and nutraceutical remedy or pharmaceutical absorption;
- Opportunity for an improved taste;
- Increased therapeutic response;
Advantages of Effervescent Formulations
Incorporation of Large Amounts of Active Ingredients.
- In many cases, one effervescent tablet will equal three to ten conventional tablets in active dose amounts.
No Need to Swallow Tablets.
- The number of people who cannot swallow tablets or who dislike swallowing tablets and capsules is growing. And many products require the patient or customer to swallow several tablets at a time. The elderly, in particular, have difficulty swallowing tablets.
- With an effervescent dosage form, one dose can usually be delivered in just 3 or 4 ounces of water. That’s about the amount used when someone swallows a conventional tablet or capsule.
The Product is Typically Self Mixing and Flavourful.
Many times effervescent tablets can include flavourings so they taste much better than a mixture of a non-effervescent powder in water.
- Many studies have demonstrated that effervescent tablets and powders enhance absorption of a number of active ingredients compared to conventional formulations. That’s because the carbon dioxide created by the effervescent reaction can induce enhanced active-ingredient permeability due to an alteration of the paracellular pathway. The paracellular pathway is the primary route of absorption for hydrophilic active ingredients in which solutes diffuse into the intercellular space between epithelial cells.
- It is theorized that the carbon dioxide alters (widens) the intercellular space between cells, which leads to greater absorption of active ingredients (both hydrophobic and hydrophilic). The increased absorption of hydrophobic active ingredients could be due to the non-polar carbon dioxide gas molecules partition into the cell membrane, thus creating an increased hydrophobic environment, which would allow the hydrophobic active ingredients to be absorbed
|Those that are difficult to digest or disruptive to the stomach||A classic example is calcium carbonate, the most widely used form of calcium. In a normal tablet or powder, the calcium carbonate dissolves in the stomach acid and is carried into the digestive system for absorption. However, calcium carbonate releases carbon dioxide when it dissolves in the GI, which usually produces gas in the stomach. On Those that are difficult to digest or disruptive to the the other hand, as people age, they have less acid in the stomach. stomach, and thus a calcium carbonate tablet may pass through the stomach without dissolving. That, in turn, may lead to constipation. However, if the calcium carbonate is taken in an effervescent formulation, the calcium dissolves in water, is readily available for the body to absorb, and there is no risk of excessive gas in the stomach or of constipation.|
|Those that are pH-sensitive, such as amino acids and antibiotics||The low pH in the stomach can cause active ingredients to become denatured, lose activity, or cause them to remain inactive. Effervescent ingredients, how-ever, can buffer the water-active solution so that the stomach pH increases Those that are pH-sensitive, such as amino acids and (becomes less acidic) and thus pre-vent the degradation or antibiotics. inactivation of the active ingredient. This buffering effect (via carbonation) induces the stomach to empty quickly usually within 20 minutes into the small intestine. The result is maximum absorption of the active ingredient.|
|Those requiring a large Dose||A typical effervescent tablet (1 inch in diameter weighing 5 grams in total weight) can include more than 2,000 milligrams of water soluble active ingredients in a single dose. If the required dose is larger than that, the sachet (powder form) is commonly chosen as an alternative means of delivery|
As a product undergoes dissolution, the molecules on the surface are the first to enter into solution, creating a saturated layer or solution that envelops the surface of the solid nutraceutical or pharmaceutical particle.
This layer of solution is the diffusion layer. From this diffusion layer the molecules pass throughout the dissolving fluid and make contact with the biologic membranes, and absorption ensues. As molecules of the nutraceutical or pharmaceutical continue to leave the diffusion layer, the layer is replenished with dissolved molecules from the surface of the nutraceutical or pharmaceutical particles and the process of absorption continues.
If the dissolution of a given nutraceutical or pharmaceutical particle is rapid or if the nutraceutical or pharmaceutical is administered as a solution and remains present in the body as such, the rate at which the nutraceutical or pharmaceutical becomes absorbed depends mainly on its ability to traverse the membrane barrier. However, if the rate of dissolution for a nutraceutical or pharmaceutical particle is slow because of the physicochemical characteristics of the nutraceutical or pharmaceutical substance or the dosage form, dissolution itself is a rate-limiting step in absorption. Slowly soluble nutraceuticals or pharmaceuticals may not only be absorbed at a slow rate; they may be incompletely absorbed or in some cases largely unabsorbed following oral administration because of the natural limitation of time that they may remain within the stomach or the intestinal tract.
- The dissolution of a substance may be described by the modified Noyes-Whitney equation: Dc / dt= ksics-ct)
- Where; dc/dt is the rate of dissolution,
- k is the dissolution rate constant,
- S is the surface area of the dissolving solid
- C is the saturation concentration of nutraceutical or pharmaceutical in the diffusion layer (which may be approximated by the maximum solubility of the nutraceutical or pharmaceutical in the solvent, because the diffusion layer is considered saturated), and is the concentration of the nutraceutical or pharmaceutical in the dissolution medium at timet (C: – Cis the concentration gradient).
The rate of dissolution is governed by the rate of diffusion of solute molecules through the diffusion layer into the body of the solution. The equation reveals that the dissolution rate of a nutraceutical or pharmaceutical may be increased by increasing the surface area (reducing the particle size) of the nutraceutical or pharmaceutical, by increasing the solubility of the nutraceutical or pharmaceutical in the diffusion layer, and by factors embodied in the dissolution rate constant, k, including the intensity of agitation of the solvent and the diffusion coefficient of the dissolving nutraceutical or pharmaceutical. For a given nutraceutical or pharmaceutical , the diffusion coefficient and usually the concentration of the nutraceutical or pharmaceutical in the diffusion layer will increase with increasing temperature.
A classic example of this occurs with phenytoin sodium capsules, which have two distinct forms. The first is the rapid- release type, that is, Prompt Phenytoin Sodium Capsules, USP, and the second is the slow-dissolution type, that is, Extended Phenytoin Sodium Capsules, USP. The former has a dissolution rate of not less than 85% in 30 minutes and is recommended for use three to four times per day. The latter has a slower dissolution rate, for example, 15% to 35% in 30 minutes, which
lends itself to use in patients who can be dosed less frequently. Because of such differences in formulation for a number of nutraceutical remedy or pharmaceutical drug s and nutraceutical remedy or pharmaceutical drug products, it is generally advisable for a person to continue taking the same brand of medication, provided it produces the desired therapeutic effect. Patients who are stabilized on one brand of nutraceutical remedy or pharmaceutical drug should not be switched to another unless necessary. However, when a change is necessary, appropriate blood or plasma concentrations of the nutraceutical remedy or pharmaceutical drug should be monitored until the patient is stabilized on the new product.
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3. Nuernberg, B. and Brune, K. Buffering the stomach content enhances the absorption of diflunisal in man.
4. Hespe, W. Vershoor, J.S.C., and Olthoff, M. Bioavalability of new formations of amoxicillin in relation to its absorption kinetics. Arzneim. Forsch. 1987: 37: 372-375.
5. Eichman, J.D. and Robinson, J.R. Mechanistic studies on effervescent-induced permeability enhancement. Pharmaceutical drug research. 1998: 15(6): 925-930
6. Eichman, J.D. Mechanistic studies on effervescent-induced permeability enhancement. Pharmaceutical drug research. 1997: Ph.D dissertation. University of Wisconsin-Madison
7. Ansel’s Pharmaceutical drug Dosage Forms and Nutraceutical remedy or pharmaceutical drug Delivery Systems By Allen 9th Edition, published by Walters Kluwer.
1. Controlled release effervescent buccal discs of buspirone hydrochloride: in vitro and in vivo evaluation studies.
Effervescent and non-effervescent buccal disc of BS using HPMC were successfully prepared using direct compression method. Drug release rate from effervescent buccal discs was directly proportional to amount of effervescence forming agent. In vivo pharmacokinetic studies revealed that effervescent HPMC buccal discs give significantly higher bioavailability when compared to that of non-effervescent buccal discs. Hence, effervescent buccal discs can be used as an alternative to improve the drug permeation resulting in better bioavailability.
2. Effervescent dry powder for respiratory drug delivery
A new formulation was established for the use in the pulmonary route of administration. The new formulation contained effervescent and lubricant excipients. The active release mechanism increased drug dissolution and enhanced the dispersion of nanoparticles over the effervescent gas bubble interface. These carrier particles can be synthesized with an adequate particle size for deep lung deposition. Furthermore, effervescent carrier particles can be used to deliver a large range of substances to the lungs with possibly a faster release compared to conventional carrier particles.
3. Coenzyme Q10: Clinical Update and Bioavailability
The time to reach maximum plasma concentration, however, was significantly shorter for the fast-melting and effervescent formulations compared with the soft gel and powder-filled forms, suggesting that the fast-melting and effervescent formulations provided a more rapid delivery of CoQ10 to the blood while exhibiting a similar area under the curve value compared with current formulations