Title: Dosage forms of risedronate
United States Patent: 5,935,602
Inventors: Dansereau; Richard John (Sherburne, NY); Mosher; Russell Youker (Norwich, NY); Axelrod; Douglas Wayne (Norwich, NY); Sietsema; William Kendall (Norwich, NY)
Assignee: The Procter & Gamble Company (Cincinnati, OH)Appl. No.: 820430
Filed: March 12, 1997
The present invention is directed to a novel enteric-coated oral dosage form of a risedronate active ingredient comprised of a safe and effective amount of a pharmaceutical compostion which is comprised of a risedronate active ingredient and pharmaceutically-acceptable excipients. Said dosage forms prohibit the exposure of the risedronate active ingredient to the epichelial and mucosal tissues of the buccal cavity, pharynx, esophagus, and stomach and thereby protects said tissues from erosion, ulceration or other like irritation. Accordingly, the said dosage forms effect the delivery to the lower intestinal tract of said human or other mammal of a safe and effective amount of the risedronate active ingredient, and substantially alleviate the esophagitis or esophageal irritation which sometimes accompanies the oral administration of risedronate active ingredients.
Example 1 of Patent
EXAMPLE IENTERIC-COATED RISEDRONATE TABLETS
Enteric-coated Risedronate tablets are made by preparing a coating composition and compressed tablets containing the risedronate active ingredient, and then applying said coating composition to said tablets.
An enteric coating composition is prepared in the form of a lacquer containing the following excipients, per tablet:
A. Enteric Coating Suspension
______________________________________
Excipients
______________________________________
Eudragit L-30-D .RTM. 33.400 mg
(manufactured by Rohm Pharma
GmbH, Weiterstadt, West Germany)
Polyethlene glycol 1.000 mg
Talc 2.500 mg
Yellow Iron Oxide 0.034 mg
Simethicone emulsion 0.800 mg
Purified Water 75.000 mg
______________________________________
The enteric coating is
prepared utilizing the following method:The talc and yellow iron oxide is added to a portion of purified water and mixed until uniform. The polyethylene glycol 8000 and the simethicone emulsion are added with continuous mixing. The resulting pigment suspension is next passed through a screen or a suitable mill to break up agglomerates. The Eudragit L-30-D.RTM. is screened and then added to a suitable vessel and diluted with a portion of the purified water. The pigment suspension is then added to the diluted Eudragit suspension and mixed until uniform.
In a suitable coating pan, the risedronate sodium tablets prepared as described below are warmed to about 35o-40oC. The enteric coating suspension is sprayed onto the tablets at approximately 50 grams per minute. When the spray cycle is completed, the temperature is reduced and the tablets are removed and dried at 30o - 40oC. for approximately 1 hour.
A coating of 4 mg/cm.sup.2 dried lacquer substance (i.e., about 45 microns thick) is applied by spraying the above composition onto risedronate active ingredient tablets, prepared in part B. below.
B. Risedronate Sodium Compressed Tablets onto 30 mg risedronate round-shaped tablets, each weighing 250 mg and each containing:
______________________________________
Active ingredient
Risedronate 30.00 mg*
Excipients
Lactose 156.00 mg
Microcrystalline Cellulose
60.50 mg
Crosporidone 7.40 mg
Magnesium Stearate 1.10 mg
______________________________________
*This quantity of risedronate soidum is determined
by assay and then adjusted to provide the designed
dosage level of risedronate sodium on an
anhydrous basis.
Tablets having the composition
set forth above are prepared as follows:The tablets are prepared by mixing the risedronate active ingredient with the microcrystalline cellulose in a twin shell blender. The blend is passed through an oscillator equipped with a 60 mesh screen. The milled blend is then returned to the turn shell blender along with the lactose and crospovidone and mixed until uniform. The magnesium stearate is added and mixed until adequate lubrication is achieved. Tablets are then compressed on a rotary tablet press.
Claim 1 of 14 Claims
1. A process
for making a tablet containing risedronate; or a pharmaceutically
acceptable salt thereof, comprising the step of:
a) mixing the risedronate with:
a filler; a viscosity agent; and optionally one or more additional
ingredients selected from the group consisting of: buffer systems,
flavoring agents, plasticizers, resins, solvents, co-solvents,
surfactants, sweeteners and preservatives;
b) adding a lubricant; and
c) compressing the resulting mixture into tablet form.
____________________________________________
If you want to learn more
about this patent, please go directly to the US
Patent and Trademark Office web site to access the full
patent.
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