Patent US4179680A successfully refreshed from Google Patents.
Patent US4411882A successfully refreshed from Google Patents.
US4411882A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Galenical compositions
Assignee: FIRST NATIONAL STATE BANK NEWARK NEW JERSEY
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Filing: 1981-06-17
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Granted: 1983-10-25
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Expires: 2001-06-17
Abstract
Abstract The invention provides solid enteric-coated compositions in unit dose form for oral application, the core of the composition containing an ergot alkaloid and a polyalkoxyalkylene sterol ether. The compositions are characterized by a prolonged effect and a good bioavailability of the active agent. The core may be in solid solution form. The enteric-coating may also be surrounded by an outer medicament layer.
Inventors
- 👤 Joachim Franz
- 👤 Ludwig Patt
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 08:46
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/14; A61K9/16; A61K9/1605; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/47; A61K31/48; A61K31/56; A61K31/575; A61K9/141; A61K9/145; A61K9/146; A61K9/20; A61K9/2004; A61K9/2013; A61K9/2072; A61K9/2086; A61K9/209; A61K9/28; A61K9/2806; A61K9/2833; A61K9/286; A61K9/2866; A61K9/48; A61K9/4891; A61K9/50; A61K9/5005; A61K9/5015; A61K9/5021; A61K9/5036; A61K9/5042; A61K9/5047
Claims Analysis
Total Claims: 31
Claim 1
Independent Claim
144 words
A solid eneric-coated composition in unit dosage form for oral application, the core of the composition containing a therapeutically effective amount of an ergot alkaloid compound of formula I, ##STR2## wherein R 1 is hydrogen or halogen, R 2 is hydrogen or C 1-4 alkyl, R 3 is isopropyl, sec.-butyl, isobutyl or benzyl, R 4 is methyl, ethyl or isopropyl, and either R 5 is hydrogen and R 6 is hydrogen or methoxy or R 5 and R 6 together are an additional bond or mixtures thereof. and a polyalkoxyalkylene sterol ether wherein the sterol part of the polyalkoxyalkylene sterol ether is chosen from the group consisting of lanosterol, dihydrochlolesterine, cholesterine and sitosterol, campesterol and stigmasterol, and wherein the enteric coating is selected from a cellulose ester derivative, a cellulose ether, an acrylic resin or a copolymer of maleic acid and phthalic acid derivatives.
Claim 2
Dependent Claim
144 words
A solid eneric-coated composition in unit dosage form for oral application, the core of the composition containing a therapeutically effective amount of an ergot alkaloid compound of formula I, ##STR2## wherein R 1 is hydrogen or halogen, R 2 is hydrogen or C 1-4 alkyl, R 3 is isopropyl, sec.-butyl, isobutyl or benzyl, R 4 is methyl, ethyl or isopropyl, and either R 5 is hydrogen and R 6 is hydrogen or methoxy or R 5 and R 6 together are an additional bond or mixtures thereof. and a polyalkoxyalkylene sterol ether wherein the sterol part of the polyalkoxyalkylene sterol ether is chosen from the group consisting of lanosterol, dihydrochlolesterine, cholesterine and sitosterol, campesterol and stigmasterol, and wherein the enteric coating is selected from a cellulose ester derivative, a cellulose ether, an acrylic resin or a copolymer of maleic acid and phthalic acid derivatives.
Claim 3
Dependent Claim
16 words
A composition according to claim 1 wherein the sterol is chosen from lanosterol, dihydrochlolesterine and cholesterine.
Claim 4
Dependent Claim
12 words
A composition according to claim 2 wherein the ergot alkaloid is dihydroergotamine.
Claim 5
Dependent Claim
12 words
A composition according to claim 2 wherein the ergot alkaloid is dihydroergotoxine.
Claim 6
Dependent Claim
12 words
A composition according to claim 2 wherein the ergot alkaloid is bromoergocryptine.
Claim 7
Dependent Claim
20 words
A composition according to claim 2 wherein the polyalkoxyalkylene sterol ether has a hydrophilic-lipophilic balance of from 10 to 20.
Claim 8
Dependent Claim
20 words
A composition according to claim 6 wherein the polyalkoxyalkylene sterol ether has a hydrophilic-lipophilic balance of from 12 to 16.
Claim 9
Dependent Claim
24 words
A composition according to claim 2 wherein the polyalkoxyalkylene sterol ether is a sterol etherified with about 8 to about 75 alkylene oxide units.
Claim 10
Dependent Claim
20 words
A composition according to claim 8, wherein the sterol is etherified with from about 9 to about 30 alkylene units.
Claim 11
Dependent Claim
21 words
A composition according to claim 2 wherein the polyalkoxyalkylene sterol ether is a sterol etherified with ethylene oxide or propylene oxide.
Claim 12
Dependent Claim
14 words
A composition according to claim 2 wherein the enteric-coating is a cellulose acetate phthalate.
Claim 13
Dependent Claim
13 words
A composition according to claim 2 wherein the enteric-coating is hydroxypropyl methyl-cellulose phthalate.
Claim 14
Dependent Claim
22 words
A composition according to claim 2 wherein the enteric-coating is of methylacrylic acid and esters thereof, containing at least 40% methyl-acrylic acid.
Claim 15
Dependent Claim
12 words
A composition according to claim 2 wherein the enteric-coating contains a softener.
Claim 16
Dependent Claim
11 words
A composition according to claim 2 wherein the softener is di-n-butylphthalate.
Claim 17
Dependent Claim
12 words
A composition according to claim 2 in the form of a tablet.
Claim 18
Dependent Claim
16 words
A composition according to claim 2 in the form of enteric coated pellets in a capsule.
Claim 19
Dependent Claim
20 words
A composition according to claim 2 wherein the weight ratio ergot alkaloid: polyalkoxyalkylene sterol ether is from 1:2 to 1:8.
Claim 20
Dependent Claim
15 words
A composition according to claim 2 wherein the ergot alkaloid is in solid solution form.
Claim 21
Dependent Claim
14 words
A composition according to claim 19 wherein the core contains polyvinylpyrrolidone as solid solvent.
Claim 22
Dependent Claim
24 words
A composition according to claim 20 wherein the weight ratio within the core of ergot alkaloid: polyalkoxyalkylene sterol ether: solid solvent is 1:1-10: 0.1:10.
Claim 23
Dependent Claim
13 words
A composition according to claim 21 wherein the weight ratio is 1:2-8: 0.1-10.
Claim 24
Dependent Claim
13 words
A composition according to claim 22 wherein the weight ratio is 1:2-5: 0.1-5.
Claim 25
Dependent Claim
12 words
A composition according to claim 2 wherein the core contains a stabilizer.
Claim 26
Dependent Claim
19 words
A composition according to claim 24 wherein the core is stabilized at pH 4 to 6 by an acid.
Claim 27
Dependent Claim
20 words
A method for providing the sustained absorption of an ergot alkaloid comprising administering the ergot as defined in claim 1.
Claim 28
Dependent Claim
81 words
A solid enteric coated composition for oral administration in unit dosage form comprising a core containing a therapeutically effective amount of an ergot alkaloid compound selected from dihydroergotoxine, dihydroergotamine and bromocryptine and a sterol selected from lanosterol, dihydrochlolesterine or cholesterine which sterol is ethoxylated with from 9 to 35 ethylene oxide units the weight ratio of ergot alkaloid to ethoxylated sterol being from 1:2 to 1:8 and the enteric coating being selected from hydroxypropyl methyl cellulose phthalate and cellulose acetate phthalate.
Claim 29
Dependent Claim
81 words
A solid enteric coated composition for oral administration in unit dosage form comprising a core containing a therapeutically effective amount of an ergot alkaloid compound selected from dihydroergotoxine, dihydroergotamine and bromocryptine and a sterol selected from lanosterol, dihydrochlolesterine or cholesterine which sterol is ethoxylated with from 9 to 35 ethylene oxide units the weight ratio of ergot alkaloid to ethoxylated sterol being from 1:2 to 1:8 and the enteric coating being selected from hydroxypropyl methyl cellulose phthalate and cellulose acetate phthalate.
Claim 30
Dependent Claim
17 words
A composition according to claim 27 wherein the ergot alkaloid is in a solid solution in polyvinylpyrrolidone.
Claim 31
Dependent Claim
17 words
A composition according to claim 27 or 28 in the form of a tablet or a capsule.
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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) | 1986-10-24 | 1987-04-25 | 1987-10-25 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1990-10-24 | 1991-04-25 | 1991-10-25 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1994-10-24 | 1995-04-25 | 1995-10-25 | $7700.00 | Window Closed / Lapsed |