US4235870A
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US
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Slow release pharmaceutical compositions
Assignee: Syngergistics
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Filing: 1975-12-15
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Granted: 1980-11-25
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Expires: 1995-12-15
Abstract
Abstract Slow release pharmaceutical compositions comprising a combination of a higher aliphatic alcohol and a hydrated hydroxy-alkyl cellulose in ratio of from 2:1 to 4:1 parts by weight and comprising from 20 to 40 percent by weight of the composition; the method for making the same, and their inclusion in pharmaceutical dosage forms intended for oral administration, to provide a slow release of a therapeutically active compound during a predetermined period of time of from five to ten hours, after oral ingestion by humans and animals.
Inventors
- 👤 Stewart T. Leslie
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 11:49
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/14; A61K9/16; A61K9/1605; A61K9/1629; A61K9/1652; A61K9/1617; A61K9/20; A61K9/2004; A61K9/2013; A61K9/2022; A61K9/205; A61K9/2054
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
129 words
A composition for use in admixture with pharmacologically active compounds to sustain release thereof over a prolonged period after oral ingestion, the composition comprising a higher aliphatic alcohol selected from the group consisting of aliphatic alcohols with the formula ROH, wherein R is an alkyl group having from 8 to 18 carbon atoms in chain length, ceto-stearyl alcohol and mixtures thereof, admixed with a hydrated hydroxy alkyl cellulose compound selected from the group consisting of hydroxymethyl cellulose, hydroxyethyl cellulose, hydropropyl cellulose and mixtures thereof, the cellulose compound having been hydrated with from 2 to 4 parts by weight water per part of dry hydroxyalkyl cellulose compound prior to admixture, the weight ratio of said aliphatic alcohol to said cellulose compound being within the range of from 2:1 to 4:1.
Claim 2
Dependent Claim
129 words
A composition for use in admixture with pharmacologically active compounds to sustain release thereof over a prolonged period after oral ingestion, the composition comprising a higher aliphatic alcohol selected from the group consisting of aliphatic alcohols with the formula ROH, wherein R is an alkyl group having from 8 to 18 carbon atoms in chain length, ceto-stearyl alcohol and mixtures thereof, admixed with a hydrated hydroxy alkyl cellulose compound selected from the group consisting of hydroxymethyl cellulose, hydroxyethyl cellulose, hydropropyl cellulose and mixtures thereof, the cellulose compound having been hydrated with from 2 to 4 parts by weight water per part of dry hydroxyalkyl cellulose compound prior to admixture, the weight ratio of said aliphatic alcohol to said cellulose compound being within the range of from 2:1 to 4:1.
Claim 3
Dependent Claim
29 words
The slow release pharmaceutical composition of claim 1 said alcohol component being selected from the group consisting of lauryl alcohol, myristyl alcohol, stearyl alcohol and mixtures of the same.
Claim 4
Dependent Claim
38 words
The slow release pharmaceutical composition of claim 1, said alcohol being cetyl alcohol and said cellulose compound being hydrated hydroxy ethyl cellulose, said proportion of cetyl alcohol to hydrated hydroxy ethyl cellulose compound being 3:1 parts by weight.
Claim 5
Independent Claim
144 words
A method for the preparation of a slow-release pharmaceutical preparation, the composition comprising a higher aliphatic alcohol and a hydrated hydroxyalkyl cellulose compound, the process comprising: (a) melting and granulating a higher aliphatic alcohol having the formula ROH, wherein R is selected from the group consisting of alkyl groups having from 8 to 18 carbon atoms in chain length and ceto-stearyl alcohol and mixtures thereof, (b) hydrating a hydroxyalkyl cellulose selected from the group consisting of hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose and mixtures thereof, the cellulose compound being hydrated with 2 to 4 parts of water for each part by weight of dry cellulose compound and granulating said hydrated cellulose compound, (c) blending the granulated cellulose compound with the granulated alcohol, and (d) drying the blend to obtain a composition capable of providing a sustained, or slow, release of a pharmacologically active material.
Claim 6
Independent Claim
144 words
A method for the preparation of a slow-release pharmaceutical preparation, the composition comprising a higher aliphatic alcohol and a hydrated hydroxyalkyl cellulose compound, the process comprising: (a) melting and granulating a higher aliphatic alcohol having the formula ROH, wherein R is selected from the group consisting of alkyl groups having from 8 to 18 carbon atoms in chain length and ceto-stearyl alcohol and mixtures thereof, (b) hydrating a hydroxyalkyl cellulose selected from the group consisting of hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose and mixtures thereof, the cellulose compound being hydrated with 2 to 4 parts of water for each part by weight of dry cellulose compound and granulating said hydrated cellulose compound, (c) blending the granulated cellulose compound with the granulated alcohol, and (d) drying the blend to obtain a composition capable of providing a sustained, or slow, release of a pharmacologically active material.
Claim 7
Dependent Claim
164 words
A pharmaceutical capsule for providing the slow release of a therapeutic agent, the capsule comprising a therapeutically sufficient quantity of a pharmacologically active compound in admixture with a slow-release composition comprising a higher aliphatic alcohol selected from the group consisting of aliphatic alcohols with the formula ROH, wherein R is an alkyl group having from 8 to 18 carbon atoms in chain length, ceto-stearyl alcohol and mixtures thereof, admixed with a hydrated hydroxyalkyl cellulose compound selected from the group consisting of hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose and mixtures thereof, the cellulose compound having been hydrated with from 2 to 4 parts by weight water per part of dry hydroxyalkyl cellulose compound prior to admixture, the weight ratio of said aliphatic alcohol to said hydrated cellulose compound being within the range of from 2:1::4:1, and a diluent, the proportion of said slow-release composition in the capsule being in the range of from 20% to 30% by weight of the total weight of the capsule.
Claim 8
Dependent Claim
164 words
A pharmaceutical capsule for providing the slow release of a therapeutic agent, the capsule comprising a therapeutically sufficient quantity of a pharmacologically active compound in admixture with a slow-release composition comprising a higher aliphatic alcohol selected from the group consisting of aliphatic alcohols with the formula ROH, wherein R is an alkyl group having from 8 to 18 carbon atoms in chain length, ceto-stearyl alcohol and mixtures thereof, admixed with a hydrated hydroxyalkyl cellulose compound selected from the group consisting of hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose and mixtures thereof, the cellulose compound having been hydrated with from 2 to 4 parts by weight water per part of dry hydroxyalkyl cellulose compound prior to admixture, the weight ratio of said aliphatic alcohol to said hydrated cellulose compound being within the range of from 2:1::4:1, and a diluent, the proportion of said slow-release composition in the capsule being in the range of from 20% to 30% by weight of the total weight of the capsule.
Claim 9
Dependent Claim
11 words
The capsule of claim 5, said pharmacologically active compound being nitroglycerin.
Claim 10
Dependent Claim
12 words
The capsule of claim 5, said pharmacologically active compound being potassium hydrochloride.
Claim 11
Dependent Claim
12 words
The capsule of claim 5, said pharmacologically active compound being papaverine hydrochloride.
Claim 12
Dependent Claim
11 words
The capsule of claim 5, said pharmacologically active compound being aminophylline.
Claim 13
Independent Claim
147 words
A method for achieving a delayed release and sustained availability of a pharmacologically active substance over a period of from 5 to 10 hours after ingestion, the process comprising the steps of orally administering to a human or animal a slow-release pharmaceutical composition comprising a higher aliphatic alcohol selected from the group consisting of aliphatic alcohols with the formula ROH, wherein R is an alkyl group having from 8 to 18 carbon atoms in chain length, ceto-stearyl alcohol and mixtures thereof, admixed with a hydrated hydroxyalkyl cellulose compound selected from the group consisting of hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose and mixtures thereof, the cellulose compound having been hydrated with from 2 to 4 parts by weight water per part of dry hydroxyalkyl cellulose compound, prior to admixture the weight ratio of said aliphatic alcohol to said hydrated cellulose compound being within the range of from 2:1::4:1.
Claim 14
Independent Claim
147 words
A method for achieving a delayed release and sustained availability of a pharmacologically active substance over a period of from 5 to 10 hours after ingestion, the process comprising the steps of orally administering to a human or animal a slow-release pharmaceutical composition comprising a higher aliphatic alcohol selected from the group consisting of aliphatic alcohols with the formula ROH, wherein R is an alkyl group having from 8 to 18 carbon atoms in chain length, ceto-stearyl alcohol and mixtures thereof, admixed with a hydrated hydroxyalkyl cellulose compound selected from the group consisting of hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose and mixtures thereof, the cellulose compound having been hydrated with from 2 to 4 parts by weight water per part of dry hydroxyalkyl cellulose compound, prior to admixture the weight ratio of said aliphatic alcohol to said hydrated cellulose compound being within the range of from 2:1::4:1.
Claim 15
Dependent Claim
16 words
The method of claim 10, wherein the pharmaceutical composition is in the form of a tablet.
Claim 16
Dependent Claim
15 words
The method of claim 10, wherein the pharmaceutical composition is administered within a gelatin capsule.
Claim 17
Dependent Claim
89 words
In a process for providing a sustained release pharmaceutical composition comprising admixing an aliphatic alcohol having the formula ROH wherein R comprises an alkyl group having from 8 to 18 carbon atoms in chain length, ceto-stearyl alcohol and mixtures thereof, with a pharmacologically-active compound, the improvement which comprises preliminarily admixing the aliphatic alcohol with a hydrated hydroxyalkyl cellulose compound, the cellulose compound having been hydrated with from two to four parts by weight of water per part of dry cellulose compound so as to form a uniform blend therewith.
Claim 18
Dependent Claim
89 words
In a process for providing a sustained release pharmaceutical composition comprising admixing an aliphatic alcohol having the formula ROH wherein R comprises an alkyl group having from 8 to 18 carbon atoms in chain length, ceto-stearyl alcohol and mixtures thereof, with a pharmacologically-active compound, the improvement which comprises preliminarily admixing the aliphatic alcohol with a hydrated hydroxyalkyl cellulose compound, the cellulose compound having been hydrated with from two to four parts by weight of water per part of dry cellulose compound so as to form a uniform blend therewith.
Claim 19
Dependent Claim
12 words
The process of claim 13, comprising in addition admixing a diluent therewith.
Claim 20
Dependent Claim
12 words
The process of claim 14, comprising in addition drying the uniform blend.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1983-11-25 | 1984-05-26 | 1984-11-25 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-11-25 | 1988-05-26 | 1988-11-25 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-11-25 | 1992-05-26 | 1992-11-25 | $7700.00 | Window Closed / Lapsed |