Title:  Organoleptically pleasant in-mouth rapidly disintegrable potassium chloride tablet

United States Patent:  6,365,182

Assignee:  Cima Labs Inc. (Eden Prairie, MN)

Filed:  August 12, 1998

The present invention relates to a potassium containing dosage form which is capable of rapidly disintegrating in a patient's mouth to form an easy to swallow slurry.

SUMMARY OF THE INVENTION

The present invention solves this need by providing an orally disintegrable tablet suitable for use in the delivery of potassium. The tablet contains between about 50 and about 80% coated potassium chloride crystals by weight of the tablet. These coated potassium chloride crystals have a particle size ranging from between about 100 to about 2,000 microns and include between about 10 and about 20% of a coating based on the weight of the coated potassium chloride crystals. The coating is generally an extended release coating. The tablet also includes between about 5 and about 35% of a rapidly dissolvable sugar or sugar alcohol filler. The rapidly dissolvable sugar or sugar alcohol filler has a particle size selected to be complementary to the particle size of the coated potassium chloride crystals and generally ranges between about 300 and about 1,500 microns. The tablet also includes between about 0 and about 15% of a binder, including insoluble filler-binders, between about 1 and about 10% of a disintegrant; and between about 0 and about 15% of an effervescent couple. The sugar or sugar alcohol, binder disintegrant and effervescent couple are all provided in amounts based on the weight of the finished tablet.

In a particularly preferred embodiment, the tablet of the present invention weighs between about 1200 and about 3000 mg and contains between about 5 and about 25 milliequivalents (mEq) of potassium. More preferable, the tablet will weigh between about 1300 and about 2800 mg and contain between about 10 and about 20 mEq of potassium.

The present invention solves the aforementioned problems by using some rather counterintuitive insights. First, the instructions approved by the Food and Drug Administration for use of potassium chloride tablets specifically direct one not to crush, chew or suck on such supplements. However, by employing just such a suckable formulation, it has been unexpectedly found that one is able to obtain an organoleptically pleasing dosage form--one that can enhance compliance. Second, one of the more daunting aspects of current potassium supplements is their relative size, chalkiness and desiccating nature. Particularly for older patients, such tablets present a significant problem. To overcome the problem of a large chalky tablet, one would seek to use either an entirely different dosage form (liquid, etc.), or find a way of reducing the tablet's size and volume. However, it has now been found that by actually increasing the amount of material administered, and to some lesser extent, the size of the resulting tablet, one is nonetheless able to obtain a dosage form which overcomes the difficulties and inabilities of the patients most likely to use same. It is indeed ironic that while one would think of making the potassium containing tablet lighter and/or smaller to overcome compliance issues, the answer was actually found by going in the completely opposite direction.

Third and even more surprisingly, if one were to ignore the instructions of the manufacturer, take a commercially available potassium chloride supplement tablet, and allow it to dissolve in their mouth, two things would happen. First, the tablet which contains upwards of 90% or more coated potassium chloride would take between about 40 seconds and a minute to actually disintegrate. Second, because the tablet contains such a significant quantity of insoluble coated active material, the results of disintegration would the formation of a "sandbox" in the patient's mouth; a most unpleasant sensation to say the least. This would be both unpleasant in the mouth and difficult to swallow.

It has now been found that by decreasing the relative proportion of active ingredients and supplementing with a rapidly water dissolvable filler, by selecting fillers and materials having relatively similar particle size to the coated active, one is actually able to obtain a tablet which is rapidly disintegrable in the mouth without the objectionable organoleptic properties of present formulations. Moreover, despite the fact that the size and volume of the tablet have actually been increased, the disintegration time is maintained and preferably decreased. A commercially available 10 milliequivalent potassium chloride tablet can dissolve in the mouth between 30 seconds and a minute as previously stated. In truth, disintegration times of about 45 seconds or more are to be expected. An otherwise equivalent formulation of the present invention, despite being 50% greater in overall weight nonetheless can substantially disintegrate in under 30 seconds.

The use of organoleptically pleasing ingredients such as a mild level of effervescence to stimulate the production of saliva and accentuate disintegration, and rapidly dissolving filler such as mannitol (mannitol has a negative heat of solution which further adds to the organoleptically pleasing nature of the formation), one obtains a dosage form which rapidly disintegrates and forms a watery slurry which is much more organoleptically pleasing and very easy to swallow.

Claim 1 of 24 Claims

We claim:

1. An orally disintegrable tablet suitable for use in the delivery of potassium comprising: between about 50 and about 80% coated potassium chloride crystals by weight of the tablet, said coated potassium crystals having a particle size ranging from between about 100 to about 2,000 microns and including between about 10 and about 20% of an extended release coating based on the weight of the coated potassium chloride crystals; between about 10 and about 35% of a rapidly dissolvable sugar or sugar alcohol filler by weight of the tablet, said rapidly dissolvable sugar or sugar alcohol filler having a particle size selected to be complementary to the particle size of said coated potassium chloride crystals and being between about 150 and about 1,500 microns; between about 0 and about 15% of a binder by weight of the tablet; between about 3 and about 10% of a disintegrant by weight based on the weight of the tablet; and optionally between about 0 and about 15% of an effervescent couple based on the weight of the tablet wherein the tablet contains between about 5 and about 25 millieguivalents of potassium.

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