US4366145A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Soft gelatin capsule with a liquid ergot alkaloid center fill solution and method of preparation
Assignee: Novartis Pharmaceuticals Corp
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Filing: 1981-06-24
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Granted: 1982-12-28
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Expires: 2001-06-24
Abstract
Abstract A stable ergot alkaloid soft gelatin capsule consisting essentially of a soft gelatin capsule shell and encapsulated therein a liquid center fill solution consisting essentially of a therapeutically effective amount of an ergot alkaloid of the formula <IMAGE> I wherein R1 is hydrogen or halogen, R2 is hydrogen or C1-4alkyl, R3 is isopropyl, sec.-butyl, isobutyl or benzyl, R4 is methyl, ethyl or isopropyl, and either R5 is hydrogen and R6 is hydrogen or methoxy or R5 and R6 together is an additional bond, or mixtures thereof, dissolved in a pharmaceutically acceptable polar, hydrophilic soft gelatin capsule center fill solvent.
Inventors
- 👤 Samuel B. Stoopak
- 👤 Saul S. Kornblum
- 👤 Allen L. Jacobs
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 18:35
CPC Classifications
C; C21; C21C; C21C7/00; C21C7/0006; A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/47; A61K31/48; A61K9/00; A61K9/48; A61K9/4841; A61K9/4858; C22; C22B; C22B1/00; C22B1/14; C22B1/24; C22B1/248
Claims Analysis
Total Claims: 26
Claim 1
Independent Claim
137 words
A method of preparing a stable ergot alkaloid soft gelatin capsule which comprises the steps of dissolving a therapeutically effective amount of a ergot alkaloid of the formula ##STR3## 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 isorpropyl, and either R 5 is hydrogen and R 6 is hydrogen or methoxy or R 5 and R 6 together is an additional bond, or mixtures thereof, in a pharmaceutically acceptable polar, hydrophilic soft gelatin capsule center fill solvent to prepare a liquid soft gelatin capsule center fill solution; and thereafter encapsulating the center fill solution obtained in a soft gelatin capsule shell before the percent of ergot alkaloid drops below 90% of the original therapeutically effective amount.
Claim 2
Independent Claim
137 words
A method of preparing a stable ergot alkaloid soft gelatin capsule which comprises the steps of dissolving a therapeutically effective amount of a ergot alkaloid of the formula ##STR3## 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 isorpropyl, and either R 5 is hydrogen and R 6 is hydrogen or methoxy or R 5 and R 6 together is an additional bond, or mixtures thereof, in a pharmaceutically acceptable polar, hydrophilic soft gelatin capsule center fill solvent to prepare a liquid soft gelatin capsule center fill solution; and thereafter encapsulating the center fill solution obtained in a soft gelatin capsule shell before the percent of ergot alkaloid drops below 90% of the original therapeutically effective amount.
Claim 3
Dependent Claim
19 words
A method according to claim 1 in which the center fill solution is encapsulated within 72 hours after preparation.
Claim 4
Dependent Claim
19 words
A method according to claim 1 in which the center fill solution is encapsulated within 24 hours after preparation.
Claim 5
Dependent Claim
19 words
A method according to claim 1 in which the ergot alkaloid is 0.5 to 6 milligrams of ergoloid mesylates.
Claim 6
Dependent Claim
19 words
A method according to claim 1 in which the ergot alkaloid is 0.5 to 3 milligrams of dihydroergotamine mesylate.
Claim 7
Dependent Claim
19 words
A method according to claim 1 in which the ergot alkaloid is 1 to 3 milligrams of bromocryptine mesylate.
Claim 8
Dependent Claim
22 words
A method according to claim 1 in which the center fill solution contains about 0.5 to 1.5% weight to volume ascorbic acid.
Claim 9
Dependent Claim
20 words
A method according to claim 1 in which the center fill solution contains about 1.5% weight to volume ascorbic acid.
Claim 10
Dependent Claim
25 words
A method according to claim 1 in which the center fill solvent is polyethylene glycol with a molecular weight of from about 200 to 600.
Claim 11
Dependent Claim
22 words
A method according to claim 9 in which the center fill solvent is polyethylene glycol with a molecular weight of about 400.
Claim 12
Dependent Claim
19 words
A method according to claim 10 in which the center fill solvent contains about 10% by volume propylene glycol.
Claim 13
Dependent Claim
51 words
A stable ergot alkaloid soft gelatin capsule consisting essentially of a soft gelatin capsule shell and encapsulated therein a liquid center fill solution consisting essentially of a therapeutically effective amount of an ergot alkaloid according to claim 1 dissolved in a pharmaceutically acceptable polar, hydrophilic, soft gelatin capsule center fill solvent.
Claim 14
Dependent Claim
19 words
A capsule according to claim 12 in which the ergot alkaloid is 0.5 to 6 milligrams of ergoloid mesylates.
Claim 15
Dependent Claim
19 words
A capsule according to claim 12 in which the ergot alkaloid is 0.5 to 3 milligrams of dihydroergotamine mesylate.
Claim 16
Dependent Claim
19 words
A capsule according to claim 12 in which the ergot alkaloid is 1 to 3 milligrams of bromocryptine mesylate.
Claim 17
Dependent Claim
21 words
A capsule according to claim 12 in which center fill solution contains about 0.5 to 1.5% weight to volume ascorbic acid.
Claim 18
Dependent Claim
20 words
A capsule according to claim 12 in which the center fill solution contains about 1.5% weight to volume ascorbic acid.
Claim 19
Dependent Claim
25 words
A capsule according to claim 12 in which the center fill solvent is polyethylene glycol with a molecular weight of from about 200 to 600.
Claim 20
Dependent Claim
22 words
A capsule according to claim 18 in which the center fill solvent is polyethylene glycol with a molecular weight of about 400.
Claim 21
Dependent Claim
19 words
A capsule according to claim 19 in which the center fill solvent contain about 10% by volume propylene glycol.
Claim 22
Dependent Claim
64 words
A capsule according to claim 12 in which the liquid center fill solution consists essentially of 1 milligram of ergoloid mesylates or dihydroergotamine mesylate or 2.5 milligrams of bromocryptine mesylate, 7 milligrams of ascorbic acid, 0.05 milliliters of propylene glycol and an amount of polyethylene glycol with a molecular weight of about 400 to bring the center fill solution volume to about 0.500 milliliters.
Claim 23
Dependent Claim
21 words
A capsule according to claim 20 in which the soft gelatin capsule shell is #9.5 oblong "A" off-white opaque capsule shell.
Claim 24
Dependent Claim
49 words
A capsule according to claim 12 in which the liquid center fill solution consists essentially of 1 milligram of ergoloid mesylates, 3 milligrams of ascorbic acid, 0.02 milliliters of propylene glycol and an amount of polyethylene glycol 400 to bring the center fill solution volume to about 0.200 milliliters.
Claim 25
Dependent Claim
22 words
A capsule according to claim 23 in which the soft gelatin capsule shell is a #4 oval "B" opaque blue capsule shell.
Claim 26
Dependent Claim
55 words
A capsule according to claim 21 in which the liquid center fill solution consists essentially of 1 milligram of ergoloid mesylates, 7 milligrams of ascorbic acid, 0.05 milliliters of propylene glycol and an amount of polyethylene glycol with a molecular weight of about 400 to bring the center fill solution volume to about 0.500 milliliters.
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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) | 1985-12-27 | 1986-06-28 | 1986-12-28 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1989-12-27 | 1990-06-28 | 1990-12-28 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1993-12-27 | 1994-06-28 | 1994-12-28 | $7700.00 | Window Closed / Lapsed |