US5128143A — Sustained release excipient and tablet formulation

Claim 1

Independent Claim 109 words

A controlled release pharmaceutical excipient for use in oral solid dosage forms, comprising from about 20 to about 60 percent by weight of a hydrophilic material comprising xanthan gum and a galactomannan gum capable of cross-linking said xanthan gum in the presence of aqueous solutions, the ratio of said xanthan gum to said galactomannan gum being from about 3:1 to about 1:3, and from about 40 to about 80 percent by weight of an inert diluent selected from the group consisting of a monosaccharide, a disaccharide, a polyhydric alcohol, and mixtures thereof, the ratio of said inert diluent to said hydrophilic material being from about 4:1 to about 0.67:1.

Claim 2

Dependent Claim 109 words

A controlled release pharmaceutical excipient for use in oral solid dosage forms, comprising from about 20 to about 60 percent by weight of a hydrophilic material comprising xanthan gum and a galactomannan gum capable of cross-linking said xanthan gum in the presence of aqueous solutions, the ratio of said xanthan gum to said galactomannan gum being from about 3:1 to about 1:3, and from about 40 to about 80 percent by weight of an inert diluent selected from the group consisting of a monosaccharide, a disaccharide, a polyhydric alcohol, and mixtures thereof, the ratio of said inert diluent to said hydrophilic material being from about 4:1 to about 0.67:1.

Claim 3

Dependent Claim 109 words

A controlled-release tablet for absorption of an active medicament in the gastrointestinal tract, comprising a controlled-released excipient comprising a hydrophilic gum matrix comprising a xanthan gum and a galactomannan gum capable of cross-linking said xanthan gum when exposed to gastric fluid, the ratio of said xanthan gum to said galactomannan gum being from about 3:1 to doubt 1:3, and an inert diluent, the ratio of said inert diluent to said hydrophilic gum matrix being from about 4:1 to about 0.67:1, and an effective amount of a medicament to render a therapeutic effect, the ratio of said medicament to said hydrophilic gum matrix being from about 1:3 to about 1:10.

Claim 4

Dependent Claim 109 words

A controlled-release tablet for absorption of an active medicament in the gastrointestinal tract, comprising a controlled-released excipient comprising a hydrophilic gum matrix comprising a xanthan gum and a galactomannan gum capable of cross-linking said xanthan gum when exposed to gastric fluid, the ratio of said xanthan gum to said galactomannan gum being from about 3:1 to doubt 1:3, and an inert diluent, the ratio of said inert diluent to said hydrophilic gum matrix being from about 4:1 to about 0.67:1, and an effective amount of a medicament to render a therapeutic effect, the ratio of said medicament to said hydrophilic gum matrix being from about 1:3 to about 1:10.

Claim 5

Dependent Claim 12 words

The excipient of claim 1, wherein said galactomannan comprises locust bean gum.

Claim 6

Dependent Claim 22 words

The excipient of claim 1, wherein said inert pharmaceutical filler comprises lactose, dextrose, sucrose, fructose, microcrystalline cellulose, xylitol, sorbitol or mixtures thereof.

Claim 7

Dependent Claim 17 words

The excipient of claim 1 to which an effective amount of a therapeutically active medicament is added.

Claim 8

Dependent Claim 39 words

The excipient of claim 1, wherein an effective amount of a therapeutically active medicament is added via dry granulation, yet granulation or a combination of dry and wet granulation and the resultant granulation is compressed to form solid tablets.

Claim 9

Dependent Claim 41 words

The excipient of claim 3, wherein said hydrophilic material further comprises one or more of tragacanth, acacia, karaya, alginates, agar, pectin, guar, hydroxypropyl guar, carrageenan, hydroxypropylmethyl cellulose, hydroxypropyl cellulose, methylcellulose, carboxymethyl cellulose, polyvinyl pyrollidone, and mixtures of any of the foregoing.

Claim 10

Dependent Claim 14 words

The excipient of claim 3, wherein said hydrophilic material further comprises propylene glycol alginate.

Claim 11

Dependent Claim 26 words

The excipient of claim 3, wherein said hydrophilic material further comprises a hydrocolloid, said hydrocolloid comprising up to about 50% by weight of said hydrophilic material.

Claim 12

Dependent Claim 22 words

The excipient of claim 1, wherein an effective amount of a therapeutically active medicament is added and the resulting mixture is encapsulated.

Claim 13

Dependent Claim 34 words

The excipient of to claim 1, wherein an effective amount of a therapeutically active ingredient is added and the resulting mixture provides a zero order controlled release when provided as a solid dosage form.

Claim 14

Dependent Claim 18 words

The excipient of claim 3, wherein said ratio of xanthan gum to locust bean gum is about 1:1.

Claim 15

Dependent Claim 55 words

A slow release pharmaceutical excipient, for use in solid oral dosage forms comprising a hydrophilic gum matrix comprising xanthan gum and locust bean gum in a ratio of about 3:1 to about 1:3; and an inert diluent, the ratio of said inert diluent to said hydrophilic gum matrix being from about 2.3:1 to about 1:1.

Claim 16

Dependent Claim 55 words

A slow release pharmaceutical excipient, for use in solid oral dosage forms comprising a hydrophilic gum matrix comprising xanthan gum and locust bean gum in a ratio of about 3:1 to about 1:3; and an inert diluent, the ratio of said inert diluent to said hydrophilic gum matrix being from about 2.3:1 to about 1:1.

Claim 17

Dependent Claim 13 words

The tablet of claim 2, wherein said galactomannan gum is locust bean gum.

Claim 18

Dependent Claim 26 words

The tablet of claim 2, wherein said medicament is added to said excipient via dry granulation, wet granulation or a combination of dry and wet granulation.

Claim 19

Dependent Claim 111 words

A controlled release tablet for oral administration comprising (I) from about 20 to about 60 percent by weight of a hydrophilic material comprising from about 10 to about 90 percent of a heteropolysaccharide and from about 90 to about 10 percent of a cross-linking agent capable of cross-linking said heteropolysaccharide; and (II) up to about 80 percent of an inert pharmaceutical filler selected from the group consisting of a monosaccharide, a disaccharide, a polyhydric alcohol, and mixtures thereof, the ratio of said inert pharmaceutical filler to said hydrophilic material being from about 4:1 to about 0.67:1; and (III) an effective amount of a therapeutically active medicament to render a therapeutic effect.

Claim 20

Dependent Claim 111 words

A controlled release tablet for oral administration comprising (I) from about 20 to about 60 percent by weight of a hydrophilic material comprising from about 10 to about 90 percent of a heteropolysaccharide and from about 90 to about 10 percent of a cross-linking agent capable of cross-linking said heteropolysaccharide; and (II) up to about 80 percent of an inert pharmaceutical filler selected from the group consisting of a monosaccharide, a disaccharide, a polyhydric alcohol, and mixtures thereof, the ratio of said inert pharmaceutical filler to said hydrophilic material being from about 4:1 to about 0.67:1; and (III) an effective amount of a therapeutically active medicament to render a therapeutic effect.

Claim 21

Dependent Claim 18 words

The tablet of claim 16, wherein said heteropolysaccharide comprises xanthan gum and said cross-linking agent comprises a galactomannan.

Claim 22

Dependent Claim 31 words

The tablet of claim 17, wherein at least 3.5 hours ar required for 50 percent of said therapeutically active medicament to be released when said tablet is exposed to gastric fluid.

Claim 23

Dependent Claim 27 words

The tablet of claim 17, wherein said tablet provides a zero order controlled release of said therapeutically active medicament when said tablet is exposed to gastric fluid.

Claim 24

Dependent Claim 25 words

The tablet of claim 17, wherein said galactomannan comprises locust bean gum, and the ratio of xanthan gum to locust bean gum is about 1:1.

Claim 25

Dependent Claim 20 words

The tablet of claim 17, wherein said inert pharmaceutical filler comprises lactose, dextrose, sucrose, fructose, xylitol, sorbitol or mixtures thereof.

Claim 26

Dependent Claim 43 words

The tablet of claim 17, wherein said hydrophilic material further comprises a polysaccharide gum selected from the group consisting of tragacanth, acacia, karaya, alginates, agar, pectin, carrageenan, hydroxypropylmethyl cellulose, hydroxypropyl cellulose, methylcellulose, carboxymethyl cellulose, polyvinyl pyrollidone, and mixtures of any of the foregoing.

Claim 27

Dependent Claim 14 words

The tablet of claim 22, wherein said hydrophillic material further comprises propylene glycol alginate.

Claim 28

Dependent Claim 13 words

The tablet of claim 22, wherein said hydrophilic material further comprises a hydrocolloid.

Annuity Stage	Window Opens	Payment Deadline	Surcharge Period Until	Estimated Fee	Status
3.5 Years (Year 4)	1995-07-07	1996-01-06	1996-07-07	$2000.00	Window Closed / Lapsed
7.5 Years (Year 8)	1999-07-07	2000-01-06	2000-07-07	$3760.00	Window Closed / Lapsed
11.5 Years (Year 12)	2003-07-07	2004-01-06	2004-07-07	$7700.00	Window Closed / Lapsed

Sustained release excipient and tablet formulation

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