JPH0417163B2 - - Google Patents

Description

Claim 1: A container having a plurality of pellets therein having an average pellet diameter of about 1 mm or less, each pellet comprising a quinidine coating on confectionery seeds, such that the quinidine coated confectionery has a weight of about 1 wt. a sustained release quinidine oral dosage formulation coated with a mixture of from about 3 to about 9 parts by weight of ethyl cellulose to 1 part of hydroxypropyl cellulose, the total of such pellets in the container forming one dosage unit of quinidine.

2. The long-acting quinidine oral preparation according to item 1 above, wherein the quinidine is in the form of quinidine bisulfate.

3. The sustained-release quinidine oral dosage formulation of item 1 above, wherein the weight of quinidine is about twice that of the confectionery.

4. The sustained release quinidine oral administration formulation of item 1 above, wherein the container is a capsule.

SUMMARY OF THE INVENTION Quinidine is a well-known alkaloid used to treat certain cardiac arrhythmias. It is a general cardiac depressant, decreasing myocardial excitability, automaticity, and conductance.

In accordance with the present invention, there is provided a sustained release quinidine oral dosage form comprising a container having a plurality of pellets therein having an average diameter of about 1 mm or less. Each pellet has a coating of quinidine on the nonpareil seeds. The quinidine coated confectionery is then coated with a mixture of about 3 to about 9 parts by weight ethylcellulose to about 1 part by weight hydroxypropylcellulose.

The present invention provides sustained release quinidine dosage forms, typically containing about 2,000 to about 15,000 polymer coated pellets.
Provided are capsules containing the following. Each of the pellets is typically based on confectionery, which is about 20 to about 25 mesh sugar types.

The confectionery is coated with an equal or greater weight of a quinidine compound, preferably quinidine bisulfate. In a preferred embodiment, about 2 parts by weight of quinidine bisulfate is coated onto 1 part by weight of confectionery seeds. In one embodiment, 500 g of confectionery seeds are placed in a coated pan and moistened with a 30% sucrose solution with the aid of a sprayer. Approximately 30 mg of quinidine bisulfate is sprinkled onto the pellets thus treated, dispensing the material by hand if necessary. Wetting and sprinkling operations are repeated until 1000 mg of quinidine bisulfate is deposited per 500 g of the confection.

Once coated with at least an equal weight of quinidine, the quinidine-coated confectionery is then coated with a sustained release polymer coating mix consisting of about 3 to about 9 parts by weight ethylcellulose to about 1 part by weight hydroxypropylcellulose. do.

In one embodiment, 700 g of the quinidine bisulfate confection prepared above (2:1 weight ratio) was placed in an air suspension coating column (manufactured by Glatt Air Techniques).
After starting air suspension of these pellets, ethylcellulose (Ethoceltype 10, Dow Chemical) was added to the air suspension.
Co., Ltd.) and hydroxypropyl cellulose (Klucel LF, Hercules).
1,400 ml of chloroform). This mixture has a weight ratio of 7 parts ethylcellulose to 3 parts hydroxypropylcellulose.

In the apparatus described above, typical conditions useful for preparing the polymer coating of the pellets include an inlet temperature of 40 DEG C., an atomization air pressure of 2 bar and a liquid feed rate of 12 c.c./min.

The pellets obtained according to the above method give a sustained release over a long period of time. When tested according to the USP XX dissolution procedure (in simulated gastric fluid and then in simulated intestinal fluid for 1 hour), the following release characteristics are observed:

Time (hours) % Release 1 6.0 2 20.1 4 43.1 6 64.5 8 84.1 10 96.1 12 99.9 The formulations of the present invention are particularly advantageous for pediatric and geriatric patients who may be unable or reluctant to swallow larger sustained release tablets. It is. For pediatric administration, it is particularly contemplated that the individually coated polymer pellets be administered in the diet.