US5026560A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Spherical granules having core and their production
Assignee: Takeda Pharmaceutical Co Ltd
•
Filing: 1988-01-14
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Granted: 1991-06-25
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Expires: 2008-01-14
Abstract
Abstract The spherical granules having a core coated with spraying powder containing a drug and low substituted hydroxypropylcellulose, because of their excellent hardness, can be coated further evenly, (e.g. sustained release coating, gastric coating, enteric coating), and at the time the granules are excellent in disintegration.
Inventors
- 👤 Tadashi Makino
- 👤 Tetsuro Tabata
- 👤 Shin-Ichiro Hirai
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 14:46
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/14; A61K9/16; A61K9/48; A61K9/50; A61K9/5073; A61K9/5078; A61K9/167; A61K9/1676
Claims Analysis
Total Claims: 32
Claim 1
Independent Claim
42 words
Spherical granules having a core coated with a binder and spraying powder containing a drug and low substituted hydroxypropylcellulose having a mean particle diameter not more than 200 μm, wherein the low substituted hydroxypropylcellulose contains 4 to 20% of a hydroxypropoxyl group.
Claim 2
Dependent Claim
42 words
Spherical granules having a core coated with a binder and spraying powder containing a drug and low substituted hydroxypropylcellulose having a mean particle diameter not more than 200 μm, wherein the low substituted hydroxypropylcellulose contains 4 to 20% of a hydroxypropoxyl group.
Claim 3
Dependent Claim
20 words
The spehrical granules having a core according to claim 1, wherein the drug is a drug for the digestive system.
Claim 4
Dependent Claim
30 words
The spherical granules having a core according to claim 2, wherein the drug for the digestive system is a benzimidazole compound having antiulcer activity, cimetidine, ranitidine, pancreatin or 5-aminosalicylic acid.
Claim 5
Dependent Claim
100 words
The spherical granules having a core according to claim 3, wherein the benzimdazole compound is represented by the formula ##STR2## wherein R 1 is hydrogen, alkyl, halogen, cyano, carboxy, carboalkoxy, carboalkoxyalkyl, carbamoyl, carbamoylalkyl, hydroxy, alkoxy, hydroxyalkyl, trifuluoromethyl, acyl, carbamoyloxy, nitro, acyloxy, aryl, aryloxy, alkylthio or alkylsulfinyl, R 2 is hydrogen, alkyl, acyl, carboalkoxy, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarbonylmethyl, alkoxycarbonylmethyl or alkylsulfon R 3 and R 5 are the same or different and each is hydrogen, alkyl, alkoxy or alkoxyalkoxy, R 4 is hydrogen, alkyl, alkoxy which may optionally be fluorinated, or alkoxyalkoxy, and m is an integer of 0 through 4.
Claim 6
Dependent Claim
19 words
The spherical granules having a core according to claim 3, wherein the benzimidazole compound is 2-[[3- methyl-4-(2,2,2-trifluoroethoxy)-2pyridyl]methylsulfinyl]benzimidazole or 5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridyl)-methylsulfinyl]benzimidazole.
Claim 7
Dependent Claim
17 words
The spherical granules having a core according to claim 1, wherein the content is 5.0 to 16.0%.
Claim 8
Dependent Claim
17 words
The spherical granules having a core according to claim 1, wherein the content is 10.0 to 13.0%.
Claim 9
Dependent Claim
21 words
The spherical granules having a core according to claim 1, wherein the mean particle diameter is not more then 100 μm.
Claim 10
Dependent Claim
21 words
The spherical granules having a core according to claim 1, wherein the mean particle diameter is not more than 30 μm.
Claim 11
Dependent Claim
26 words
The spherical granules having a core according to claim 1, wherein the granules pass through 12 mesh sieve but do not pass through 32 mesh sieve.
Claim 12
Dependent Claim
15 words
The spherical granules having a core according to claim 1, wherein the granules are enteric-coated.
Claim 13
Independent Claim
55 words
A method for producing spherical granules having acore characterized in that seed cores are coated, while being sprayed with an aqueous binder, with spraying powder containing a drug and low substituted hydroxypropylcellulose having a means particle diameter not more than 200 μm, wherein the low substituted hydroxypropylcellulose contains 4 to 20% of a hydroxypropoxyl group.
Claim 14
Independent Claim
55 words
A method for producing spherical granules having acore characterized in that seed cores are coated, while being sprayed with an aqueous binder, with spraying powder containing a drug and low substituted hydroxypropylcellulose having a means particle diameter not more than 200 μm, wherein the low substituted hydroxypropylcellulose contains 4 to 20% of a hydroxypropoxyl group.
Claim 15
Dependent Claim
27 words
The method according to claim 12, wherein the seed cores are nonpareils produced by coating 75 weight parts of sucrose with 25 weight parts of corn starch
Claim 16
Dependent Claim
15 words
The method according to claim 12, wherein the seed cores are made with crystalline cellulose.
Claim 17
Dependent Claim
14 words
The method according to claim 12, wherein the aqueous binder is water or ethanol.
Claim 18
Dependent Claim
19 words
The method according to claim 12, wherein the aqueous binder is solution of binder in water or in ethanol.
Claim 19
Dependent Claim
16 words
The method according to claim 16, wherein the solution has 0.1 to 80.% (w/v) of concentration.
Claim 20
Dependent Claim
28 words
The method according to claim 16, wherein the binder is one or more selected from the group consisting of sucrose, hydroxypropylcellulose, hydroxypropylmethylcellulose, methylcellulose, polyvinylpyrrolidone, pullulan and gum arabic.
Claim 21
Dependent Claim
19 words
The method according to claim 12, wherein the spraying powder is not more than 100 μm in particle size.
Claim 22
Dependent Claim
19 words
The method according to claim 12, wherein the spraying powder contains 5 to 90% (w/w) of low substituted hydroxypropylcellulose.
Claim 23
Dependent Claim
18 words
The method according to claim 12, wherein the spraying powder contains 2 to 70% (w/w) of the drug.
Claim 24
Dependent Claim
21 words
The method according to claim 12, wherein the ratio of the aqueous binder to the spraying powder is 1:1 to 1:2.
Claim 25
Dependent Claim
20 words
The spherical granules having a core according to claim 1, wherein the spraying powder contains magnesium carbonate and/or calcium carbonate.
Claim 26
Dependent Claim
25 words
The spherical granules having a core according to claim 1, wherein the coated spherical granules are further coated with spraying powder containing low substituted hydroxypropylcellulose.
Claim 27
Dependent Claim
22 words
The spherical granules having a core according to claim 24, wherein the spherical granules are further coated with an enteric coating agent.
Claim 28
Dependent Claim
25 words
The spherical granules having a core 3 according to claim 25, wherein the enteric coating agent is acrylate copolymers anionic in charcter or hydroxypropylmethylcellulose phthalate.
Claim 29
Dependent Claim
16 words
The method according to claim 12, wherein the spraying powder contains magnesium carbonate and/or calcium carbonate.
Claim 30
Dependent Claim
20 words
The methdo according to claim 12, wherein the spherical granules are further coated with spraying powder containing low substituted hydroxypropylcellulose.
Claim 31
Dependent Claim
18 words
The method according to claim 28, wherein the spherical granules are further coated with an enteric coating agent.
Claim 32
Dependent Claim
20 words
The methdo according to claim 29, wherein the enteric coating agent is acrylate copolymers anionic in character or hydroxyporpylmethylcellulose phthalate.
References Cited (Backward Citations)
US3477864A
Cited
US4226849A
Cited
US4758437A
Cited
GB2134523A
Cited
EP0159891A1
Cited
EP0200902A2
Cited
US4695591A
Cited
EP0244380A2
Cited
US4786505A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1994-06-24 | 1994-12-24 | 1995-06-25 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1998-06-24 | 1998-12-24 | 1999-06-25 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2002-06-24 | 2002-12-24 | 2003-06-25 | $7700.00 | Window Closed / Lapsed |