Captopril formulation providing increased duration of activity
AssigneeE. R. Squibb & Sons, Inc.
InventorsRobert Abramowitz, Yatinda M. Joshi, Nemichand B. Jain
Life of this patent
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Abstract
A formulation comprising captopril within an enteric or delayed release coated pH stable core combined with additional captopril that is available for immediate release following administration.
Claims7
A composition for oral administration of captopril consisting essentially of enteric or delayed release coated captopril containing pH stable beads combined with additional captopril for immediate release following administration, the pH stable core of each of said enteric or delayed release coated pH stable beads consisting essentially of on a weight percent basis from about 5% to about 50% captopril, from about 1% to about 20% of disodium edetate, from about 10% to about 70% of the combination of ascorbic acid and sodium ascorbate, and from about 10% to about 30% of the combination of microcrystalline cellulose and sodium carboxymethylcellulose, and the enteric or delayed release coating consisting essentially of a polymeric material selected from the group consisting of methacrylic acid copolymers, ethylcellulose, hydroxypropyl methylcellulose phthalate, cellulose acetate trimellitate, cellulose acetate phthalate, and blends of cellulose acetate trimellitate and cellulose acetate phthalate, a plasticizer selected from the group consisting of acetyltri-n-butyl citrate, triethyl citrate, acetyltriethyl citrate, tri-n-butyl citrate, castor oil, polyethylene glycol, and dibutyl phthalate, and a glidant selected from the group consisting of talc, microfine silicas, and metallic stearates.
A tablet for oral administration of captopril consisting essentially of a pH stable core, an enteric or delayed release first coating, and a captopril containing second coating, said pH stable core consisting essentially of on a weight percentage basis from about 5% to about 50% captopril, from about 1% to about 20% of disodium edetate, from about 10% to about 70% of the combination of ascorbic acid and sodium ascorbate, and from about 10% to about 30% of the combination of microcrystalline cellulose, stearic acid, and cornstarch, said enteric or delayed release first coating consisting essentially of a polymeric material selected from the group consisting of methacrylic acid copolymers, ethylcellulose, hydroxypropyl methylcellulose phthalate, cellulose acetate trimellitate, cellulose acetate phthalate, and blends of cellulose acetate trimellitate and cellulose acetate phthalate, a plasticizer selected from the group consisting of acetyltri-n-butyl citrate, triethyl citrate, acetyltriethyl citrate, tri-n-butyl citrate, castor oil, polyethylene glycol, and dibutyl phthalate, and a glidant selected from the group consisting of talc, microfine silicas and metallic stearates, and said second coating consisting essentially of captopril and a water soluble polymer selected from the group consisting of hydroxypropylmethyl cellulose, hydroxypropylcellulose, and blends of hydroxypropylmethyl cellulose and hydroxypropylcellulose
Dependencies are inferred from the claim text.