Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Reexamination Certificate
2000-08-16
2002-03-19
Dudash, Diana (Department: 1619)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
C424S489000, C424S479000, C514S054000
Reexamination Certificate
active
06358526
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to a method for making tablets, and more particularly, relates to a method for making tablets that are substantially free of excipients, where at least one therapeutic compound in the tablet serves as a compaction enhancing agent for the tablet. The present invention also relates to tablet compositions produced by the methods of the present invention.
BACKGROUND OF THE INVENTION
Tablet compositions are commonly used to deliver therapeutic compounds to a patient such as a human or animal. By “tablet” as used herein, it is meant solid particles, containing or including therapeutic compounds, that are compressed under pressure into any desirable shape, such as a pill or caplet.
Typically, tablets contain other ingredients, hereinafter referred to as “excipients,” that provide necessary physical or aesthetic properties to a tablet for delivery of the therapeutic compound. For example, with respect to physical properties, tablets generally need to have acceptable hardness, disintegration, dissolution rate for release of the therapeutic, friability, stability, and size to effectively deliver a therapeutic compound. With respect to aesthetics, it may be desirable for the tablet to contain additives that appeal to the human senses such as colorants, fragrances, texture modifiers, and/or flavorants. Specific types of excipients commonly used in tablet compositions include for example diluents, binders, lubricants, glidants, disintegrants, gelling agents, flavoring agents, and coloring agents. Many of these excipients are commonly added because the therapeutic compound alone may have poor compactability, and thus excipients are needed to achieve the desired tabletting performance.
A problem, however, in using excipients, is that the tablet may become too large to ingest due to the amount of excipients needed to effectively formulate the tablet. A solution to this problem would be to reduce the amount of therapeutic compound and excipients to reduce the overall weight of the tablet, however, multiple tablets would then be needed to deliver the appropriate amount of therapeutic compound. Another problem in using excipients is that, particularly in nutraceuticals, they do not adequately compensate for low density of many herbal products and as such, are in many cases unsatisfactory solutions to tabletting problems. Additionally, excipients often add cost to the tablet, and also may be objectionable to some consumers.
Tablet formulations in which it is especially desirable to reduce the amount of excipients are those used for the treatment of connective tissue to prevent, repair, or lessen ailments of the joints and cartilage tissue, such as observed with arthritis. For example, U.S. Pat. Nos. 5,364,845 and 5,587,363 both to Henderson (“Henderson”) disclose therapeutic compositions for the treatment and repair of connective tissue containing amino sugars such as glucosamine, and glycosaminoglycans such as chondroitin. The compositions disclosed in Henderson are used in the form of a powder (for large animals) or capsule (for small animals). Additionally, it is known that these same compositions can be supplied in tablet form, if excipients are used. For example, the commercially available product called “Osteo-Bi-flex” supplied by Rexall Sundown, provides in tablet form a composition containing glucosamine, chondroitin sulfate, and excipients, where the excipients make up at least 23 wt % of the tablet formulation.
U.S. Pat. No. 5,843,919 to Burger discloses a composition and method for the treatment of arthritis where the composition contains one or more glucosamines and one or more omega-3-fatty acids. Although Burger discloses that a tablet can be prepared, it is apparent that excipients would be needed as Burger discloses that the glucosamine is preferably dissolved in an oil containing the omega-3-fatty acid.
Other compositions, which may optionally be in the form of tablets, for treating ailments of the joints and connective tissues are disclosed in for example U.S. Pat. No. 5,605,891 to Prino et al., U.S. Pat. No. 5,840,715 to Florio, and U.S. Pat. No. 5,849,336 to Aoyagi et al. These patents however, provide no specific example of useful tablet formulations.
Amino sugars and glycosaminoglycans have also been used in compositions for treating skin. For example, U.S. Pat. No. 5,804,594 to Murad discloses a composition for the prevention and treatment of skin conditions that contain a sugar compound, an antioxidant, an amino acid, a transition metal component, a catechin based preparation, a glucosamine and chondroitin. Although tablet formulations are disclosed, it is taught that such compositions need to be prepared in the presence of carriers.
With respect to other therapeutics, it is known that a therapeutic alone may be compressible, without excipients. For example, U.S. Pat. No. 5,079,007 to Putnam discloses an implant containing a crystalline salt of cephalosporin, an amorphous salt of cephalosporin and from 0 to 10 weight percent excipients. Putnam teaches that the crystalline and amorphous cephalosporin forms are compressible alone to form a tablet, and that the ratio of the two components are adjusted to obtain the desired release characteristics of the implant. Putnam thus does not describe a method for making a tablet where one therapeutic compound serves as a compaction enhancing agent for a different therapeutic compound.
Thus, it would be desirable to develop a method of making tablets and tablet compositions produced therefrom that are substantially free of excipients, where at least one of the therapeutic compounds is a compaction enhancing agent for the other therapeutic compound.
SUMMARY OF THE INVENTION
The present invention provides a method of making tablets that are substantially free of excipients. The method of the present invention includes forming a compactable granular mixture comprising (i) at least about 3 weight percent of a compaction enhancing therapeutic compound, (ii) at least one other therapeutic compound that is different from the compaction enhancing therapeutic compound and (iii) less than about 15 weight percent of non-aesthetic excipients. The compactable granular mixture is compressed to form one or more tablets.
In a preferred embodiment of the present invention, the compaction enhancing therapeutic compound includes a glycosaminoglycan and the other therapeutic compound includes an amino sugar.
The present invention also provides a tablet composition containing from about 3 weight percent to about 99.5 weight percent of a compaction enhancing therapeutic compound; from about 0.5 weight percent to about 97 weight percent of at least one second therapeutic compound that is different from the compaction enhancing therapeutic compound; and less than about 15 weight percent excipients. The compaction enhancing therapeutic compound enhances the compaction of the second therapeutic compound and is preferably in intimate admixture with the second therapeutic compound.
DETAILED DESCRIPTION OF THE INVENTION
The present invention provides a method of making tablets that are substantially free of excipients. The tablets produced by the method of the present invention contain at least two therapeutic compounds, where at least one of the therapeutic compounds serves as a compaction enhancing agent for the other therapeutic compound. By being able to provide tablets that are substantially free of excipients, smaller tablets and/or tablets containing greater amounts of therapeutic compounds can be produced. Thus, tablets can be provided that are more easily ingested due to the smaller size, and/or eliminating the need for taking multiple tablets to obtain a desired dosage of a therapeutic compound.
By “substantially free” of excipients it is meant that the tablet contains less than about 15 weight percent, more preferably less than about 8 weight percent, and most preferably less than about 2 weight percent excipients, based on the total weight of the tablet on a dry basis (i.e., excluding moisture as he
Chang Kuei Tu
Holly Gerald T.
Mergens William J.
Dudash Diana
Haghighation Mina
Rexall Sundown
Woodcock & Washburn LLP
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