US 5,626,879 A · Terfenadine oral granules

Abstract

The present invention contemplates a dry, granular terfenadine composition. That composition comprises (i) particulate terfenadine and (ii) a polyethylene oxide-polypropylene oxide-polyethylene oxide block copolymer having an HLB number of 24 that is a wetting agent for the terfenadine that are dry-blendedly dispersed onto (iii) spray-dried sorbitol particles that are loosely packed, randomly oriented filamentary crystals having pores that entrap the particulate terfenadine and wetting agent upon the dry-blended dispersal. The weight ratio of particulate terfenadine to the block copoymer is about 1:1 to about 1:5:1, and the weight ratio of terfenadine to the spray-dried sorbitol is about 1:4 to about 1:10. The composition is free-flowing and is substantially free from the taste of solubilized terfenadine when placed on the human tongue in dry form or when dispersed in water and tasted within about five minutes of said dispersal. A preferred composition further includes dry-blendedly admixed polyvinylpyrrolidone present in an amount of about 0.5 to about 5 weight percent of the total composition. Flavorants can also be present.

Claims20

Dependent claims

A dry, granular terfenadine composition that comprises

(a) a mixture of:
(i) about 0.20 to about 25 parts by weight particulate terfenadine and
(ii) about 0.1 to about 15 parts by weight a polyethylene oxide-polypropylene oxide-polyethylene oxide block copolymer having an HLB number of 24 that is a wetting agent for said terfenadine;
that are dry-blendedly dispersed into:
(b) about 10 to about 80 parts by weight spray-dried sorbitol particles that are loosely packed, randomly oriented filamentary crystals having pores that entrap said terfenadine particles and wetting agent upon said dry-blended dispersal, said components being further dry blended with
(c) about 0.5 to about 10 parts by weight dry polyvinylpyrrolidone;
(d) about zero to about 5 parts by weight dry microcrystalline cellulose mixture that contains about 7 to about 20 weight percent sodium carboxymethylcellulose;
and
(e) a dry flavorant that is absent or present in an amount sufficient to provide a desired taste to said powder;
said composition being free-flowing and is substantially free from the taste of solubilized terfenadine when placed on the human tongue in dry form or when dispersed in water and tasted within about five minutes of said dispersal.

7 more elements

Dependencies are inferred from the claim text.

Terfenadine oral granules

Life of this patent

Terfenadine oral granules

Life of this patent

Abstract

Claims20