US5162057A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Coatings for stable sustained release preparations
Assignee: Takeda Pharmaceutical Co Ltd
•
Filing: 1991-02-22
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Granted: 1992-11-10
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Expires: 2011-02-22
Abstract
Abstract Fatty acid esters of polyglycerols, such as stearic acid penta(tetra)glyceryl ester, behenic acid hexa(tetra)glyceryl ester, lauric acid mono(deca)glyceryl ester, oleic acid di(tri)glyceryl ester, linolic acid di(hepta)glyceryl ester, palmitic acid deca(deca)glyceryl ester, etc. are employed as coating agents for coating solid preparations such as tablets, pills, granules, fine granules, etc. By coating with the coating agents, stable sustained release of active ingredients contained in the preparations is obtained, even after a long period of storage.
Inventors
- 👤 Yohko Akiyama
- 👤 Naoki Nagahara
- 👤 Minoru Yoshioka
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 01:47
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/20; A61K9/48; A61K9/50; A61K9/5005; A61K9/5015; A61K9/5073; A61K9/5078
Claims Analysis
Total Claims: 35
Claim 1
Independent Claim
27 words
In a sustained release composition comprising a solid preparation coated with a coating agent, the improvement wherein said coating agent comprises a fatty acid ester of polyglycerol.
Claim 2
Dependent Claim
27 words
In a sustained release composition comprising a solid preparation coated with a coating agent, the improvement wherein said coating agent comprises a fatty acid ester of polyglycerol.
Claim 3
Dependent Claim
19 words
The sustained release composition according to claim 11, wherein the coating agent further comprises a lipid or a wax.
Claim 4
Dependent Claim
31 words
The sustained release composition according to claim 2, wherein said lipid or wax is selected from the group consisting of paraffin, microcystalline wax, a higher fatty acid and a higher alcohol.
Claim 5
Dependent Claim
25 words
The sustained release composition according to claim 2, wherein said lipid or wax is selected from the group consisting of stearic acid and palmitic acid.
Claim 6
Dependent Claim
16 words
The sustained release composition according to claim 2, wherein said lipid or wax is stearyl alcohol.
Claim 7
Dependent Claim
24 words
The sustained release composition according to claim 2, wherein said lipid or wax is selected from the group consisting of paraffin and microcrystalline wax.
Claim 8
Dependent Claim
22 words
The sustained release composition according to claim 11, wherein the coating agent has a melting point of from 40° to 120° C.
Claim 9
Dependent Claim
20 words
The sustained release composition according to claim 1, wherein the fatty acid ester of polyglycerol is solid at room temperature.
Claim 10
Dependent Claim
28 words
The sustained release composition according to claim 1, wherein the melting point of the fatty acid ester of polyglycerol is in the range of 15° to 70° C.
Claim 11
Dependent Claim
25 words
The sustained release composition according to claim 1, wherein the melting point of the fatty acid ester of polyglycerol ranges from 45° to 70° C.
Claim 12
Dependent Claim
23 words
The sustained release composition according to claim 1, wherein the fatty acid ester of polyglycerol has an HLB value from 1 to 15.
Claim 13
Dependent Claim
23 words
The sustained release composition according to claim 1, wherein the fatty acid ester of polyglycerol has an HLB value from 2 to 9.
Claim 14
Dependent Claim
28 words
The sustained release composition according to claim 1, wherein a degree of polymerization of the polyglycerol of said fatty acid ester of polyglycerol ranges from 2 to 40.
Claim 15
Dependent Claim
28 words
The sustained release composition according to claim 1, wherein a degree of polymerization of the polyglycerol of said fatty acid ester of polyglycerol ranges from 2 to 10.
Claim 16
Dependent Claim
31 words
The sustained release composition according to claim 1, wherein the polyglycerol of said fatty acid ester of polyglycerol is selected from the group consisting of diglycerol, tetraglycerol, hexaglycerol, heptaglycerol and decaglycerol.
Claim 17
Dependent Claim
29 words
The sustained release composition according to claim 1, wherein the polyglycerol of said fatty acid ester of polyglycerol is selected from the group consisting of diglycerol, tetraglycerol and hexaglycerol.
Claim 18
Dependent Claim
20 words
The sustained release composition according to claim 11, wherein the polyglycerol of said fatty acid ester of polyglycerol is tetraglycerol.
Claim 19
Dependent Claim
47 words
The sustained release composition according to claim 11, wherein the fatty acid of said fatty acid ester of polyglycerol is selected from the group consisting of caprylic acid, lauric acid, myristic acid, palmitic acid, stearic acid, oleic acid, linolic acid, ricinolic acid, ricinoleic acid and behenic acid.
Claim 20
Dependent Claim
24 words
The sustained release composition according to claim 1, wherein the fatty acid of said fatty acid ester of polyglycerol is a saturated fatty acid.
Claim 21
Dependent Claim
31 words
The sustained release composition according to claim 19, wherein the saturated fatty acid is selected from the group consisting of caprylic acid, lauric acid, stearic acid, palmitic acid and behenic acid.
Claim 22
Dependent Claim
21 words
The sustained release composition according to claim 1, wherein the saturated fatty acid of said fatty acid ester is stearic acid.
Claim 23
Dependent Claim
45 words
The sustained release composition according to claim 1, wherein said fatty acid ester of polyglycerol is selected from the group consisting of stearic acid penta(tetra)glyceryl ester, stearic acid mono(tetra)glyceryl ester, stearic acid penta(hexa)glyceryl ester, stearic acid sesqui(hexa)glyceryl ester, stearic acid mono-deca)glyceryl ester and mixtures thereof.
Claim 24
Dependent Claim
27 words
The sustained release composition according to claim 1, wherein said fatty acid ester of polyglycerol is present in the coating agent at 20 to 100% by weight.
Claim 25
Dependent Claim
27 words
The sustained release composition according to claim 1, wherein said fatty acid ester of polyglycerol is present in the coating agent at 20 to 60% by weight.
Claim 26
Dependent Claim
19 words
The sustained release composition according to claim 1, wherein said coating agent further comprises water and a solid additive.
Claim 27
Dependent Claim
41 words
The sustained release composition according to claim 25 wherein the coating agent comprises 20 to 60 weight % of the fatty acid ester of polyglycerol, 40 to 90 weight % of water and 20 to 60 weight % of solid additive.
Claim 28
Dependent Claim
28 words
The sustained release composition according to claim 25, wherein said solid additive is selected from the group consisting of talc, corn starch, lactose, mannitol, sucrose and mixtures thereof.
Claim 29
Dependent Claim
17 words
The sustained release composition according to claim 11, comprising a pharmaceutical preparation coated with said coating agent.
Claim 30
Independent Claim
26 words
A method of forming a solid sustained release composition comprising coating a solid preparation with a coating agent which comprises a fatty acid ester of polyglycerol.
Claim 31
Independent Claim
26 words
A method of forming a solid sustained release composition comprising coating a solid preparation with a coating agent which comprises a fatty acid ester of polyglycerol.
Claim 32
Independent Claim
34 words
A method for sustaining the release of a pharmaceutical ingredient comprising administering orally an effective amount of a pharmaceutical preparation which is coated with a coating agent comprising a fatty acid ester of polyglycerol.
Claim 33
Independent Claim
34 words
A method for sustaining the release of a pharmaceutical ingredient comprising administering orally an effective amount of a pharmaceutical preparation which is coated with a coating agent comprising a fatty acid ester of polyglycerol.
Claim 34
Independent Claim
36 words
A method for maintaining the release-sustaining ability of a sustained release pharmaceutical preparation over an extended period of time comprising coating a pharmaceutical ingredient with a coating agent which comprises a fatty acid ester of polyglycerol.
Claim 35
Independent Claim
36 words
A method for maintaining the release-sustaining ability of a sustained release pharmaceutical preparation over an extended period of time comprising coating a pharmaceutical ingredient with a coating agent which comprises a fatty acid ester of polyglycerol.
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) | 1995-11-10 | 1996-05-11 | 1996-11-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1999-11-10 | 2000-05-11 | 2000-11-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2003-11-10 | 2004-05-11 | 2004-11-10 | $7700.00 | Window Closed / Lapsed |