Title:  Pharmaceutical composition for piperidinoalkanol compounds

United States Patent:  5,932,247

Inventors:  Ortyl; Thomas T. (Overland Park, KS); Skultety; Paul F. (Leawood, KS); Mitchell; Kristen C. (Lee's Summit, MO); Phadke; Deepak S. (Olathe, KS); Attarchi; Faraneh (Kansas City, MO); Pierce; Marguerite L. (Fairway, KS); Schoeneman; Aaron W. (Lee's Summit, MO); Schnitz; Joseph M. (Kansas City, MO)

Appl. No.:  948005

The invention provides a pharmaceutical composition in solid unit dosage form, comprising, a) a therapeutically effective amount of a piperidinoalkanol compound or a pharmaceutically acceptable salt thereof; and, b) at least one inert ingredient.

Summary of the Invention

The present invention provides a pharmaceutical composition in solid unit dosage form, comprising,

a) a therapeutically effective amount of a piperidinoalkanol compound or a pharmaceutically acceptable salt thereof; and

b) at least one inert ingredient.

The present invention further provides a pharmaceutical composition prepared by a wet granulation process comprising, preparing the wet granulation wherein a compound of the formula; (see above for the chemical structure) wherein X is a number ranging from about zero to 5, and the individual optical isomers thereof, a diluent and a disintegrant are mixed with a solution of a binding agent; the wet granulation is screened; and the wet granulation is dried. In addition, the present invention provides combining the above dry granulation with a lubricant. The present invention further provides pressing the above final mixture into a tablet.

Example 1 of the Patent

20 mg Gelatin Capsules for Oral Administration

Combine 32.4 kg of 4-›4-›4-(Hydroxydiphenylmethyl)-1-piperidinyl-
1-hydroxybutyl-.alpha.,.al pha.-dimethylbenzeneacetic acid hydrochloride with a particle surface area of about 2-4 m.sup.2 /g, 76.1 kg microcrystalline cellulose, 76.1 kg lactose, and 21.6 kg pregelatinized starch and blend in a mixer for 5 minutes. To this mixture, add a solution of 7.9 kg of gelatin in 55.0 kg purified water (prepared by adding the gelatin to the water and heating the dispersion with mixing until solution of the gelatin is attained) and continue mixing until a good granulation is formed. Pass the granulation through a 0.375 inch screen and dry at 60^oC. until a moisture content of less than 3.0% is achieved as determined by a Computrac moisture balance at 125^oC. Mill the dried granulation through a 0.065 inch screen. To the granulation add 10.8 kg of croscarmellose sodium and mix for about 10 minutes. Fill the granulation into size 3 hard gelatin capsules to a fill weight of 138.9 mg granulation per capsule. This procedure results in about 1,620,000 capsules of the composition shown in table 6 below.

Claim 1 of 4 Claims

1. A pharmaceutical composition in solid unit dosage form prepared by a process comprising blending together a compound of the formula: 

wherein X is a number ranging from about zero to 5, and the individual optical isomers thereof, with microcrystalline cellulose, lactose and pregelatinized starch; adding a solution of gelatin in water mixing; drying and milling the mixture; and adding croscarmellose sodium with mixing, wherein the resulting mixture is filled into capsules.

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