Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Reexamination Certificate
2000-12-27
2003-07-08
Spear, James M. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
Reexamination Certificate
active
06589555
ABSTRACT:
FIELD OF THE INVENTION
The invention relates to a dry effervescent composition containing at least one vitaceutical, and optionally containing inulin and other active agents. The effervescent products optionally contain lubricants and essential oils and can generate magnesium malate, a therapeutic effector. The invention also encompasses methods of preparing the effervescent compositions of the invention.
BACKGROUND OF THE INVENTION
Many types of formulations are available for administering medicaments to a subject. Solid dosage forms which are swallowed, such as tablets and capsules are useful because they provide quick and easy administration routes as well as accurate dosages. Many medicinal compositions, including vitamins, nutritional supplements and medicines have unpleasant tastes. These compositions can be administered in the form of a tablet or capsule to avoid unpleasant taste. Solid dosage forms, however, must disintegrate in the gastrointestinal tract and the medicament must dissolve before it is absorbed. As a result, absorption tends to be slower than from a liquid suspension and may be incomplete. Additionally, some subjects have difficulty swallowing tablets and capsules. Another draw-back of solid dosage forms is that tablets and capsules can only have a maximal size which can easily be swallowed and thus the dosage cannot be increased above that size. If more medicament is required, multiple tablets or capsules must be administered.
Medicinals can also be administered as liquids, chewables or formulations which dissolve in the mouth. In these instances, it is desirable to add a component which masks the taste of the bitter medicinals. Fruit flavoring mixed with sugars are often used.
Soluble medicaments administered in aqueous suspensions can also be used for administering medicaments. Aqueous suspensions are useful because they provide good bio-availability of the medicament. These preparations, however, often have limited shelf-life and it is difficult to accurately measure the dose of a medicament being provided. It is also difficult to mask the bitter taste of medicaments in this type of formulation.
In order to avoid some of the problems associated with administration of medicaments in the forms of solid dosages or aqueous suspensions, effervescent formulations can be used. Effervescent formulations usually require components which mask the taste because these formulations are dissolved in water prior to ingestion. Some effervescent formulations have been prepared using citrus flavoring. Other taste-masking substances include clove oil with a supportive flavor component or calcium carbonate, such as those described in U.S. Pat. No. 5,837,286. Clove oil is capable of masking the bitter taste of medicinals, particularly analgesics, expectorants, anti-tussives, decongestants or combinations thereof.
Effervescent formulations are well-known to those of ordinary skill in the art. These formulations include those described in U.S. Pat. Nos. 3,495,001; 3,518,344; 4,083,950; 4,783,331; 4,942,039; 5,824,339; 5,834,019; 5,962,022; 5,919,483; 5,912,012, and 5,869,095, the entire contents of which are hereby incorporated by reference. In general, effervescent formulations include an acid/base component such as edible organic acids such as citric acid and a carbonate or bicarbonate, lubricants, sweeteners, excipients, clarity-enhancing components, surfactants, emulsifiers, sorbitol, and mannitol to enhance compressibility.
When the effervescent formulation is dissolved in water, the base liberates carbon dioxide to produce the effervescent or fizzy characteristics of the formulation. The use of effervescent formulations to administer medicaments provides the advantage that disintegration of the medicament in the gastrointestinal tract is accomplished easily. Some of the disadvantages of prior art effervescent formulations include a difficulty with maintaining stability of hydrophobic compounds, the bad taste associated with certain medicaments, and the quick time with which the effervescent formulation must be consumed once it is mixed with water.
Another problem associated with the use of effervescent compositions has been the inability to incorporate acid-sensitive drugs because these compositions will hydrolyze or decompose while in contact with the acid of the effervescent system. Thus, these compositions are not stable for reasonable periods of time. Additionally, hydrophobic particles within the drug contained within the effervescent composition tend to leach out of the effervescent composition when it is mixed with water and deposit along the bottom or sides of the glass. Loratadine is an example of a hydrophobic active agent which is difficult to formulate in an effervescent composition.
Additionally, effervescent compositions are not a preferred composition for formulating hygroscopic medicaments. Hygroscopic medicaments take up and absorb moisture. When hygroscopic compounds in effervescent formulations are exposed to moisture they are quickly inactivated.
SUMMARY OF THE INVENTION
The invention is directed to effervescent compositions having improved properties. One of the effervescent compositions of the inventions is an effervescent formulation containing an inulin. The inulin increases the effervescence time, which would allow a subject to ingest the effervescent drink over a longer period of time. This would allow the subject to drink the effervescent formulation in a relaxed manner as a regular drink. Thus, one aim of the formulations of the invention, is to provide a composition which can be enjoyed in the form of a drink which tastes good and is enjoyable. This drink overcomes the difficulty associated with other forms of administering medicine, such as reluctance to swallow pills, bad taste associated with medicaments, and general problems associated with inconvenience due to the frequency and quantity of taking pills. Additionally, it is desirable to maintain intestinal health for maximal nutrient absorption and assimilation. Inulin can help to improve and maintain intestinal health, reducing stomach distress, increasing mineral absorption, helping to multiply the native gut microorganisms and decreasing pathogenic bacteria in the gut to promote nutrient assimilation.
The invention in other aspects relates to an effervescent formulation which produces a therapeutic agent when mixed with water. Thus the therapeutic agent is formed “in situ.” The effervescent compositions, according to this aspect of the invention, are capable of generating magnesium malate which has a therapeutic effect in the treatment of muscle soreness and has been used to promote muscle relaxation. In other aspects, the invention relates to methods of treating or preventing muscle soreness and/or promoting muscle relaxation by administering an effervescent composition of the invention.
According to yet another aspect of the invention, an effervescent composition containing a hygroscopic compound such as glucosamine is provided. Glucosamine is an active agent which has been used for the treatment of osteoarthritis. Because glucosamine is hygroscopic and oxidizes when exposed to air for long periods of time, it is predominantly available in hard gelatin capsule forms. Some tablet forms are also available. The tablets, however, suffer from deterioration due to moisture and oxygen. The novel effervescent formulations of the invention containing glucosamine and or other hygroscopic compounds are useful for delivering glucosamine for therapeutic purposes because they contain ingredients which help prevent the oxidation and deterioration of glucosamine within the formulation. The effervescent formulations include ascorbic acid which selectively protects glucosamine against oxidation by preferentially being oxidized. The formulation also contains sorbitol and/or inulin, which because they are more hygroscopic than glucosamine, selectively protect the glucosamine against moisture. Additionally, some of the most common side-effects of glucosamine are stomach distress, diarrhea, and nause
Spear James M.
Wolf Greenfield & Sacks P.C.
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