Effervescent tablets dosage forms

Chemical stability, disintegration rate, dissolution profile, friability, and hardness are the major stability attributes for the tablet dosage form. An unoptimized tablet formulation may become soft or very hard after storage, with altered dissolution profiles, and as a result, its dissolution profile and bioavailability may not be appropriate. If effervescent products are not properly formulated, manufactured, and packaged, the premature acid-base reaction will cause the product s self-destruction. 

Uses. Aspirin has analgesic, antiinflammatory, and antipyretic activity. It is used for the reHef of less severe types of pain, such as headache, neuritis, acute and chronic rheumatoid arthritis, and toothache. Aspirin can be purchased in a variety of OTC and prescription dosage forms made and formulated by many companies. Tablets, ie, buffered, plain, or enteric-coated, are the most familiar in the United States, but other forms such as powder and effervescent formulations are of considerable importance in other parts of the world. 

Tablets are solid dosage forms that are compressed or prepared by a sintering proeess, including sublingual, buccal, chewable, effervescent, and compressed tablets. Some of these ean be easily compoimded an example of a tablet triturate is as follows ...

Buccal dosage forms can be of the tablet, patch, gel, or ointment type and can be employed for local or systemic delivery. For local deliveiy, conventional dosage forms such as solutions and various types of tablets (immediate release, effervescent, etc.) are more suitable. These forms generally have uncontrolled drug release with subsequent variable absorption and short residence times, and may not provide sufficient bioavailability. Novel dosage forms such as adhesive tablets, patches, gels, and... 

Effervescent tablets (compressed effervescent powders) do not represent a solid dosage form, because they are dissolved in water immediately prior to ingestion and are, thus, actually, liquid preparations. 

Solid dosage form includes capsules, granules, effervescent granules, powders, tablets, insufflations, suppositories (pessaries, bougies and ear cone) etc. 

Lee, R. E., Effervescent tablets. Key facts about a unique effective dosage form, Tablets Capsules, available http //www.amerilabtech.com/EffervescentTablets KeyFacts.pdf, accessed Aug. 6, 2004. 

Nishimura, K. Sasahara, K. Araj, M. Nitanai, T. Ikegami, Y. Morioka, T. Nakajima, E. Dosage form design for improvement of bioavailability of levodopa VI formulation of effervescent enteric-coated tablets. J. Pharm. Sci. 1984, 73, 942-946. 

Tablets manufactured with OraSolv technology should contain an effervescence couple along with microparticles of drug within a rupturable coat. The tablets manufactured are compressed at a low hardness that promotes fast disintegration. The dosage forms need to be packaged in foil-foil aluminum blisters with a dome shape that impact physical protection and impermeability to moisture. This constitutes the PakSolv Techonology. ...

Effervescent dosage forms have several drawbacks when compared with aqueous solutions and plain tablets. For example, they are relatively expensive to produce due to the use of large amounts of more or less... 

The bioavailability of acetylsalicylic acid from three different dosage forms—two types of effervescent tablets with different buffering properties and tablets of a conventional type— was studied in healthy volunteers. Complete absorption was found for all the preparations studied. Both effervescent tablets were rapidly absorbed. The buffering properties did not influence the rate of absorption.f ... 

El-Banna, H.M. Minina, S.A. The construction and uses of factorial designs in the preparation of solid dosage forms. Part 1 effervescent acetylosalicylic acid tablets. Pharmazie 1981, 36, 417-A20. 

Mohrle, R. Effervescent tablets. In Pharmaceutical Dosage Forms, 2nd Ed. Lieberman, H.-A., Lachman, L., Schwartz, J.B., Eds. Marcel Dekker, Inc. New York, 1989 Vol. 1. Schmidt, P.C. Christin, I. Brausetabletten—eine fast vergessene arzneiform. Pharmazie 1990, 45, 89-101. 

Excipients such as mannitol can affect small intestinal transit, which in turn can affect the absorption of certain drugs. Oral solutions are rarely likely to fall short of bioequivalence relative to solid oral formulations, although during the development of a ranitidine effervescent oral solution dosage form containing sodium acid pyrophosphate (SAPP), a marked decrease in absorption was observed in the extent of ranitidine absorption from the liquid formulation relative to the conventional oral tablet. The formulation contained 150 mg ranitidine with 1132 mg SAPP together with 1.5 MBq hndium chloride solutions. Small intestinal transit time was decreased to 56% in the presence of the excipient. The rapid small intestinal transit associated with an excipient of a solution dosage form resulted in a decreased extent of ranitidine absorption. " ... 

Many solid-dosage forms of potassium chloride exist including tablets prepared by direct compression and granulation effervescent tablets coated, sustained-release tablets " sustained-release wax matrix tablets micro-capsules pellets and osmotic pump formulations. ... 

All solid dosage forms to exacting weight and hardness specifications, including mono- and two-layer tablets, effervescent tablets, etc. 

To overcome insufficient stability in liquid state, dispersible tablets and effervescent dosage forms provide a dry alternative to liquid but are not without inherent issues (large volume of diluent, bicarbonate ingestion, sodium and/or potassium content not suitable for renally impaired patients, difficult taste masking). 

Ideally, if there is no appropriate dosage form for a drug, another drug with the same therapeutic spectrum but adequate formulation, such as liquid, effervescent, dispersible tablets, is recommended in accordance with the prescriber. 

The production of effervescent tablets is first of all a conventional solid dosage form manufacturing process, which has to be taken into consideration, due to the special characteristics of the product and some unusual features. 

Effervescent granulation is an important step in the production of fizzy dosage forms that, most of the time, cannot be avoided to achieve the desired characteristics of the effervescent tablets. It is also very critical because it can affect the stability of the final dosage forms. 

The first effervescent preparations were described over two centuries ago in the official compendia they were in powder form for use as cathartic salts. Later, in 1815, a patent described a combination of neutral salt or powder which possesses all the properties of the medicinal spring of Seidlitz in Germany, under the name of Seidlitz Powders, which contains sodium potassium tartarate, sodium bicarbonate, and tartaric acid, in the proportions 3 1 1, respectively (1). Effervescent granules and tablets have become more and more popular as the dosage form because they are readily soluble and easy to consume just by drinking the glass of water where they are dissolved. 

As far as other exdpients, such as diluents or binders, are concerned there is a very little freedom for the formulator to experiment, because of the large dimension of the tablet required for effervescent systems. In addition, compressibility caimot be enhanced by additional binders for effervescent dosage form, because of the larger size of the tablet. 

Mohrle R. Effervescent tablets. Lieberman HA, Lachman L, eds. Pharmaceutical Solid Dosage Forms. Vol. 1. New York Marcel Dekker, 1980 225-258. http //www.desiccantcity.com/CASE HISTORIES/Historyl l.htm. 

---