Sustained release formulations of guaifenesin and additional drug ingredients
First Claim
1. A modified release drug product comprising two portions, a first portion comprising a first quantity of guaifenesin in an immediate release formulation wherein the guaifenesin becomes bioavailable in the subject'"'"'s stomach;
- and a second portion comprising a second quantity of guaifenesin, a first quantity of at least one additional drug ingredient, and a release-delaying matrix, wherein the release-delaying matrix comprises a hydrophilic polymer and a water-insoluble polymer in a weight ratio of hydrophilic polymer to water-insoluble polymer from about 1;
1 to about 9;
1, wherein the guaifenesin has a Cmax in a human subject equivalent to the Cmax obtained when the first of three doses of a standard immediate release formulation having one third the amount of guaifenesin is dosed every four hours over a 12 hour period, and releases therapeutically effective bioavailable guaifenesin dose for at least twelve hours after a single dose in a human subject according to serum analysis.
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Accused Products
Abstract
The invention relates to a novel pharmaceutical sustained release formulation of guaifenesin and at least one additional drug ingredient. The formulation may comprise a hydrophilic polymer, preferably a hydroxypropyl methylcellulose, and a water-insoluble polymer, preferably an acrylic resin, in a ratio range of about one-to-one (1:1) to about nine-to-one (9:1), more preferably a range of about three-to-two (3:2) to about six-to-one (6:1), and most preferably in a range of about two-to-one (2:1) to about four-to-one (4:1) by weight. This formulation capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject. The invention also relates to a modified release product which has two portions: a first portion having an immediate release formulation of guaifenesin and a second portion having a sustained release formulation of guaifenesin, wherein one or both portions has at least one additional drug ingredient. The modified release product has a maximum guaifenesin serum concentration equivalent to that of an immediate release guaifenesin tablet, and is capable of providing therapeutically effective bioavailability of guaifenesin for at least twelve hours after dosing in a human subject.
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Citations
87 Claims
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1. A modified release drug product comprising two portions, a first portion comprising a first quantity of guaifenesin in an immediate release formulation wherein the guaifenesin becomes bioavailable in the subject'"'"'s stomach;
- and a second portion comprising a second quantity of guaifenesin, a first quantity of at least one additional drug ingredient, and a release-delaying matrix,
wherein the release-delaying matrix comprises a hydrophilic polymer and a water-insoluble polymer in a weight ratio of hydrophilic polymer to water-insoluble polymer from about 1;
1 to about 9;
1,wherein the guaifenesin has a Cmax in a human subject equivalent to the Cmax obtained when the first of three doses of a standard immediate release formulation having one third the amount of guaifenesin is dosed every four hours over a 12 hour period, and releases therapeutically effective bioavailable guaifenesin dose for at least twelve hours after a single dose in a human subject according to serum analysis. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79)
- and a second portion comprising a second quantity of guaifenesin, a first quantity of at least one additional drug ingredient, and a release-delaying matrix,
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29. A modified release drug product comprising two portions, a first portion comprising a first quantity of guaifenesin in an immediate release formulation wherein the guaifenesin becomes bioavailable in the subject'"'"'s stomach;
- and a second portion comprising a second quantity of guaifenesin and at least one additional drug ingredient in a sustained release form
wherein the guaifenesin has a Cmax in a human subject equivalent to the Cmax obtained when the first of three doses of a standard immediate release formulation having one third the amount of guaifenesin is dosed every four hours over a 12 hour period and wherein the product provides a therapeutically effective bioavailable guaifenesin dose for at least twelve hours after a single dose in a human subject according to serum analysis and a therapeutically effective bioavailable dose of the additional drug ingredient. - View Dependent Claims (30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47)
- and a second portion comprising a second quantity of guaifenesin and at least one additional drug ingredient in a sustained release form
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48. A drug release product comprising two portions, a first portion comprising a first quantity of guaifenesin in an immediate release formulation wherein guaifenesin becomes bioavailable in the subject'"'"'s stomach;
- and a second portion comprising a second quantity of guaifenesin and a first quantity of at least one additional drug ingredient in a sustained release formulation
wherein the ratio of the first quantity to the second quantity of guaifenesin is about 1;
1 to about 1;
49, the product provides a guaifenesin Cmax in a human subject equivalent to the Cmax obtained when the first of three doses of a standard immediate release formulation having one third the amount of guaifenesin is dosed every four hours over a 12 hour period, and the product provides a therapeutically effective bioavailable guaifenesin for at least twelve hours after a single dose in a human subject according to serum analysis and a therapeutically effective amount of the additional drug ingredient. - View Dependent Claims (49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65)
- and a second portion comprising a second quantity of guaifenesin and a first quantity of at least one additional drug ingredient in a sustained release formulation
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80. A method of treating or preventing coughing and symptoms or diseases associated with coughing which comprises administering to a subject in need of such treatment or prevention a therapeutically or prophylactically effective amount of a modified release drug product comprising two portions, a first portion comprising a first quantity of guaifenesin in an immediate release formulation wherein the guaifenesin becomes bioavailable in the subject'"'"'s stomach;
- and a second portion comprising a second quantity of guaifenesin, a first quantity of at least one additional drug ingredient, and a release-delaying matrix,
wherein the release-delaying matrix comprises a hydrophilic polymer and a water-insoluble polymer in a weight ratio of hydrophilic polymer to water-insoluble polymer from about 1;
1 to about 9;
1,wherein the guaifenesin has a Cmax in a human subject equivalent to the Cmax obtained when the first of three doses of a standard immediate release formulation having one third the amount of guaifenesin is dosed every four hours over a 12 hour period, and releases therapeutically effective bioavailable guaifenesin dose for at least twelve hours after a single dose in a human subject according to serum analysis.
- and a second portion comprising a second quantity of guaifenesin, a first quantity of at least one additional drug ingredient, and a release-delaying matrix,
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81. A method of treating or preventing coughing and symptoms or diseases associated with coughing which comprises administering to a subject in need of such treatment or prevention a therapeutically or prophylactically effective amount of a drug release product having two portions, wherein a first portion comprises a first quantity of guaifenesin in an immediate release form which becomes fully bioavailable in the subject'"'"'s stomach and a second portion comprises a second quantity of guaifenesin and a release-delaying matrix comprising a hydrophilic polymer and a water-insoluble polymer wherein the weight ratio of said hydrophilic polymer to said water-insoluble polymer is in the range of from about 1:
- 1 to about 6.8;
1, wherein said tablet demonstrates a Cmax in a human subject equivalent to the Cmax obtained when the first of three doses of a standard immediate release formulation having one third the amount of guaifenesin is dosed every four hours over a 12 hour period, and wherein said tablet also provides therapeutically effective bioavailability for at least twelve hours after a single dose in a human subject according to serum analysis. - View Dependent Claims (82, 83, 84, 85, 86, 87)
- 1 to about 6.8;
Specification