Drug – bio-affecting and body treating compositions – Solid synthetic organic polymer as designated organic active... – Ion exchange resin
Reexamination Certificate
1999-07-29
2001-08-28
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Solid synthetic organic polymer as designated organic active...
Ion exchange resin
C424S488000
Reexamination Certificate
active
06280717
ABSTRACT:
TECHNICAL FIELD
The present invention relates to a cation exchange resin preparation used for treatment of hyperpotassemia resulting from chronic and acute renal failure. More specifically, it relates to a cation exchange resin preparation which comprises a cation exchange resin and a gelling agent, and if desired, further comprises a binder, a corrigent of taste, a disintegrator and the like.
PRIOR ART
The cation exchange resin therapy is most popular for daily potassium control in hyperpotassemia resulting from chronic and acute renal failure. However, cation exchange resin preparations are powders which hardly dissolve in water and are peculiar to the palate, and a large daily dosage of 5 to 30 g is required. At oral administration, sandy feel remains in the mouth and throat, and the unpleasant feel and the like may lead to poor compliance. This clearly indicates the necessity of a composition of a cation exchange resin preparation with better feel of oral administration compared to conventional cation exchange resin preparations.
In order to improve the feel of oral administration of a strongly basic anion exchange resin (e.g. cholestyramine), there have been known so far a method of obtaining a dry syrup by fixing an anion exchange resin to a large amount of gum such as hydroxypropyl methylcellulose and methylcellulose (see, for example, Japanese Patent Unexamined Publication (KOKAI) No. (Sho) 63-290822/1988 and No. (Hei) 1-172324/1989), and a method of obtaining a tablet using a hydrophobic substance such as higher fatty acids, their metal salts or glycerol esters, and wax, together with a binder such as hydroxypropyl cellulose and methylcellulose (see, for example, Japanese Patent Unexamined Publication (KOKAI) No. (Hei) 2-286621/1990). However, these methods are limited to those for improving the feel of oral administration of anion exchange resins. In addition, the aforementioned methods require a large quantity of hydrophobic substances and the like to improve the feel of administration of the ion exchange resin preparations. This may cause problems in that manufacturing methods are inconvenient and doses are too large.
DISCLOSURE OF THE INVENTION
Accordingly, an object of the present invention is to provide a composition of an ion exchange resin preparation which can be prepared conveniently and give excellent feel of oral administration, although it contains only a small amount of additives such as a gelling agent. Another object of the present invention is to provide preparations which can easily be dispersed and suspended in water by stirring for only a few seconds before oral administration and will not cause aggregation for a while after the suspending. Further object of the present invention is to provide preparations which can rapidly be re-dispersed by stirring in a few seconds even after precipitation is formed by leaving the suspension to stand for a while.
The present inventors conducted various studies to solve the foregoing problems and found that preparations, which were obtained by kneading a small amount of a gelling agent and, if desired, a binder and the like into a cation exchange resin and extruding the mixture for granulation, achieved remarkably easier feel of oral administration compared to preparations consisting solely of a cation exchange resin. The present invention was achieved on the basis of these findings.
The present invention thus relates to a cation exchange resin preparation which comprises a cation exchange resin and a gelling agent, preferably, it relates to the cation exchange resin preparation which further comprises a binder, a disintegrator and the like. According to a preferred embodiment, there is provided the cation exchange resin preparation comprising a cation exchange resin, a gelling agent, and a binder, whose dosage form is granules, powders, or dry syrups, and more preferably in the form of dry syrups.
According to further preferred embodiments, the cation exchange resin may be a polystyrene sulfonic acid metal salt such as, for example, a polystyrene calcium sulfonate or a polystyrene sodium sulfonate. The gelling agent may be one or more substances selected from the group consisting of carboxymethylcellulose sodium (CMC-Na), hydroxypropyl methylcellulose (HPMC) and methylcellulose (MC), and the binder may be one or more substances selected from the group consisting of dextrin, crystalline cellulose, hydroxypropyl cellulose (HPC), and ethyl cellulose (EC).
According to particularly preferred embodiments, the gelling agent is carboxymethylcellulose sodium (CMC-Na), and the binder is hydroxypropyl cellulose (HPC). Most preferably, the cation exchange resin is a polystyrene calcium sulfonate, the gelling agent is carboxymethylcellulose sodium (CMC-Na), and the binder is hydroxypropyl cellulose (HPC).
BEST MODE FOR CARRYING OUT THE INVENTION
The present invention will be explained in detail.
The cation exchange resin preparation of the present invention may preferably be in the dosage form of granules, powders, or dry syrups, and dry syrups are particularly preferred.
As the cation exchange resin, polystyrene sulfonic acid metal salts, particularly a polystyrene calcium sulfonate or a polystyrene sodium sulfonate, are preferred. Particle size of the cation exchange resin may be from 5 to 500 &mgr;m, and in particular, 50 to 100 &mgr;m is preferred.
As the gelling agent used in the present invention, examples include carboxymethylcellulose sodium (CMC-Na, carmellose sodium), hydroxypropyl methylcellulose (HPMC), methylcellulose (MC), croscarmellose sodium (CCMC-Na) and the like. Preferable examples include CMC-Na, HPMC and MC, and CMC-Na is particularly preferred. The gelling agent is used in an amount of from 0.5 to 20% based on the total weight of the preparation of the present invention, preferably from 1 to 10%, and more preferably from 1 to 5%.
As the binder, examples include dextrin, crystalline cellulose, hydroxypropyl cellulose (HPC), ethylcellulose (EC) and the like, and particularly HPC. The binder is used in an amount of from 0.1 to 20% based on the total weight of the preparation of the present invention, preferably from 1 to 10%.
The preparations of the present invention can be added with, if desired, a disintegrator such as carboxymethylcellulose (CMC) and carboxymethylcelulose calcium (CMC-Ca) in addition to the gelling agent and the binder.
If desired, a small amount of a corrigent of taste may be used in the preparations of the present invention to higher sweetness and/or improve taste. Examples include, for example, fructose, xylitol, purified sucrose, glucose, maltose, D-mannitol, stevioside, glycyrrhizic acid, a salt of glycyrrhizic acid, and thaumatin, or artificial sweeteners such as, for example, aspartame, saccharin, and sodium saccharin. These natural and artificial corrigent of taste are well-known, and any of them may suitably used for the present invention. Among them, aspartame is particularly preferred when the preparation is administered to patients with renal failure and/or diabetes. The corrigent of taste may be used alone or in combination of two or more.
Also if desired, a small amount of corrigent of smell may be used in the preparations of the present invention to increase flavor and/or mask smells. Examples include, for example, flavors of mixed fruit, pineapple, strawberry, orange, grape, raspberry, apricot, lemon, lime, cherry, glycyrrhiza, spearmint, peppermint, chocolate, coffee, banana, vanilla and the like. The corrigent of smell may be used alone or in combination of two of more.
The cation exchange resin preparation of the present invention can be manufactured by kneading a small amount of the gelling agent, and optionally further additives such as a binder and a disintegrator, into the cation exchange resin; extruding the mixture for granulation; and then drying to obtain granules; and if desired, adding a small amount of the corrigent of taste and/or smell. In addition, the cation exchange resin preparation of the present invention can be prepared by the processes of knead
Imai Hiromi
Kamakura Minoru
Birch & Stewart Kolasch & Birch, LLP
Fubara Blessing
Nikken Chemicals Co., Ltd.
Page Thurman K.
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