US4834984A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Controlled release dihydrocodeine composition
Assignee: PUREUE PHARMA LP
•
Filing: 1987-05-19
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Granted: 1989-05-30
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Expires: 2007-05-19
Abstract
Abstract A solid controlled release, oral dosage form, the dosage form comprising an analgesically effective amount of dihydrocodeine or a salt thereof in a controlled release matrix wherein the dissolution rate in vitro of the dosage form, when measured by the USP Paddle Method at 100 rpm in 900 ml aqueous buffer (pH between 1.6 and 7.2) at 37° C. is between 25% and 60% (by weight) dihydrocodeine released after 1 hour, between 45% and 80% (by weight) dihydrocodeine released after 2 hours, between 60% and 90% (by weight) dihydrocodeine released after 3 hours and between 70% and 100% (by weight) dihydrocodeine released after 4 hours, the in vitro release rate being independent of pH between pH 1.6 and 7.2 and chosen such that the peak plasma level of dihydrocodeine obtained in vivo occurs between 2 and 4 hours after administration of the dosage form.
Inventors
- 👤 Robert S. Goldie
- 👤 Sandra T. A. Malkowska
- 👤 Stewart T. Leslie
- 👤 Ronald B. Miller
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-03 02:08
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/20; A61K9/2004; A61K9/2022; A61K9/205; A61K9/2054; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/47; A61K31/485; A61K9/2013
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
169 words
A solid, controlled release, oral dosage form, the dosage form comprising an analgesically effective amount of dihydrocodeine or a salt thereof in a controlled release matrix of at least 2-20% by weight of at least one soluble hydroxyalkylcellulose and 8-40% by weight of at least one aliphatic alcohol of 12-36 carbon atoms wherein the dissolution rate in vitro of the dosage form, when measured by the USP Paddle Method at 100 rpm in 900 ml aqueous buffer (pH between 1.6 and 7.2) at 37° C. is between 25% and 60% (by wt) dihydrocodeine released after 1 hour, between 45% and 80% (by wt) dihydrocodeine released after 2 hours, between 60% and 90% (by wt) dihydrocodeine released after 3 hours and between 70% and 100% (by wt) dihydrocodeine released after 4 hours, the in vitro release rate being independent of pH between 1.6 and 7.2 and chosen such that the peak plasma level of dihydrocodeine obtained in vivo occurs between 2 and 4 hours after administration of the dosage form.
Claim 2
Dependent Claim
169 words
A solid, controlled release, oral dosage form, the dosage form comprising an analgesically effective amount of dihydrocodeine or a salt thereof in a controlled release matrix of at least 2-20% by weight of at least one soluble hydroxyalkylcellulose and 8-40% by weight of at least one aliphatic alcohol of 12-36 carbon atoms wherein the dissolution rate in vitro of the dosage form, when measured by the USP Paddle Method at 100 rpm in 900 ml aqueous buffer (pH between 1.6 and 7.2) at 37° C. is between 25% and 60% (by wt) dihydrocodeine released after 1 hour, between 45% and 80% (by wt) dihydrocodeine released after 2 hours, between 60% and 90% (by wt) dihydrocodeine released after 3 hours and between 70% and 100% (by wt) dihydrocodeine released after 4 hours, the in vitro release rate being independent of pH between 1.6 and 7.2 and chosen such that the peak plasma level of dihydrocodeine obtained in vivo occurs between 2 and 4 hours after administration of the dosage form.
Claim 3
Dependent Claim
59 words
The dosage form according to claim 1 wherein the in vitro dissolution rate is between 25% and 50% (by weight) dihydrocodeine released after 1 hour, between 45% and 70% (by weight) dihydrocodeine released after 2 hours, between 60% and 80% (by weight) dihydrocodeine released after 3 hours and between 70% and 90% (by weight) dihydrocodeine released after 4 hours.
Claim 4
Dependent Claim
59 words
The dosage form according to claim 2 wherein the in vitro dissolution rate is between 30% and 50% (by weight) dihydrocodeine released after 1 hour, between 45% and 65% (by weight) dihydrocodeine released after 2 hours, between 60% and 75% (by weight) dihydrocodeine released after 3 hours and between 70% and 85% (by weight) dihydrocodeine released after 4 hours.
Claim 5
Dependent Claim
24 words
The dosage form according to claim 1 wherein the dosage form contains between 3% and 12% (by weight) of the at least one hydroxyalkylcellulose.
Claim 6
Dependent Claim
25 words
The dosage form according to claim 1 wherein an analgesically effective amount of a dihydrocodeine salt is between 30 and 180 mg of dihydrocodeine tartrate.
Claim 7
Dependent Claim
25 words
The dosage form according to claim 5 wherein an analgesically effective amount of a dihydrocodeine salt is between 60 and 120 mg of dihydrocodeine tartrate.
Claim 8
Dependent Claim
18 words
The dosage according to claim 1 wherein the controlled release matrix also includes at least one polyalkylene glycol.
Claim 9
Dependent Claim
24 words
The dosage form according to claim 7 wherein the at least one water soluble hydroxyalkylcellulose is a hydroxy C 1 -C 6 alkyl cellulose.
Claim 10
Dependent Claim
20 words
The dosage form according to claim 1 wherein the at least one hydroxyalkyl cellulose is hydroxypropyl cellulose, hydroxypropylmethylcellulose or hydroxyethylcellulose.
Claim 11
Dependent Claim
15 words
The dosage form according to claim 9 wherein the at least one hydroxyalkylcellulose is hydroxyethylcellulose.
Claim 12
Dependent Claim
29 words
The dosage form according to claim 7 wherein the ratio of the at least one hydroxyalkylcellulose to the at least one aliphatic alcohol/polyalkylene glycol is between 1:2 and 1:4.
Claim 13
Dependent Claim
20 words
The dosage form according to claim 7 wherein the aliphatic alcohol is a C 14 to C 22 aliphatic alcohol.
Claim 14
Dependent Claim
23 words
The dosage form according to claim 12 wherein the aliphatic alcohol is lauryl alcohol, myristyl alcohol, stearyl alcohol, cetyl alcohol or cetostearyl alcohol.
Claim 15
Dependent Claim
17 words
The dosage form according to claim 13 wherein the aliphatic alcohol is cetyl alcohol or cetostearyl alcohol.
Claim 16
Dependent Claim
40 words
The dosage form according to claim 7 wherein the dosage form contains between 12% and 36% (by weight) of the at least one fatty alcohol or of the at least one fatty alcohol and the at least one polyalkylene glycol.
Claim 17
Dependent Claim
15 words
The dosage form according to claim 11 wherein the ratio is between 1:3 and 1:4.
Claim 18
Dependent Claim
173 words
A process for the preparation of a solid, controlled release, oral dosage form comprising incorporating an analgesically effective amount of dihydrocodeine or a salt thereof in as controlled release matrix of at least 2-20% by weight of at least one soluble hydroxyalkylcellulose and 8-40% by weight of at least one aliphatic alcohol of 12-36 carbon atoms wherein the dissolution rate in vitro of the dosage form, when measured by the USP Paddle Method of 100 rpm in 900 ml aqueous buffer (pH between 1.6 and 7.2) at 37° C. is between 25% and 60% (by weight) dihydrocodeine released after 1 hour, between 45% and 80% (by weight) dihydrocodeine released after 2 hours, between 60% and 90% (by weight) dihydrocodeine released after 3 hours and between 70% and 100% (by weight) dihydrocodeine released after 4 hours, the in vitro release rate being independent of pH between 1.6 and 7.2 and chosen such that the peak plasma level of dihydrocodeine obtained in vivo occurs between 2 and 4 hours after administration of the dosage form.
Claim 19
Dependent Claim
173 words
A process for the preparation of a solid, controlled release, oral dosage form comprising incorporating an analgesically effective amount of dihydrocodeine or a salt thereof in as controlled release matrix of at least 2-20% by weight of at least one soluble hydroxyalkylcellulose and 8-40% by weight of at least one aliphatic alcohol of 12-36 carbon atoms wherein the dissolution rate in vitro of the dosage form, when measured by the USP Paddle Method of 100 rpm in 900 ml aqueous buffer (pH between 1.6 and 7.2) at 37° C. is between 25% and 60% (by weight) dihydrocodeine released after 1 hour, between 45% and 80% (by weight) dihydrocodeine released after 2 hours, between 60% and 90% (by weight) dihydrocodeine released after 3 hours and between 70% and 100% (by weight) dihydrocodeine released after 4 hours, the in vitro release rate being independent of pH between 1.6 and 7.2 and chosen such that the peak plasma level of dihydrocodeine obtained in vivo occurs between 2 and 4 hours after administration of the dosage form.
Claim 20
Dependent Claim
48 words
The process according to claim 17 comprising (a) wet granulating at least one water soluble hydroxyalkylcellulose with dihydrocodeine or a dihydrocodeine salt to form granules, (b) mixing the hydroxyalkylcellulose containing granules with at least one C 12 -C 36 aliphatic alcohol, and (c) compressing and shaping the granules.
Claim 21
Dependent Claim
53 words
The process according to claim 18 wherein the at least one water soluble hydroxyalkylcellulose and the dihydrocodeine or the dihydrocodeine salt are wet granulated with water, the weight ratio of the water to the dry weight of the at least one water soluble hydroxyalkylcellulose being between 1.5 to 1 and 5 to 1.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-05-29 | 1992-11-28 | 1993-05-30 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-05-29 | 1996-11-28 | 1997-05-30 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-05-29 | 2000-11-28 | 2001-05-30 | $7700.00 | Window Closed / Lapsed |