.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Claims for Patent: 4,366,145

« Back to Dashboard

Claims for Patent: 4,366,145

Title: Soft gelatin capsule with a liquid ergot alkaloid center fill solution and method of preparation
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 ##STR1## wherein R.sub.1 is hydrogen or halogen, R.sub.2 is hydrogen or C.sub.1-4 alkyl, R.sub.3 is isopropyl, sec.-butyl, isobutyl or benzyl, R.sub.4 is methyl, ethyl or isopropyl, and either R.sub.5 is hydrogen and R.sub.6 is hydrogen or methoxy or R.sub.5 and R.sub.6 together is an additional bond, or mixtures thereof, dissolved in a pharmaceutically acceptable polar, hydrophilic soft gelatin capsule center fill solvent.
Inventor(s): Stoopak; Samuel B. (West Caldwell, NJ), Kornblum; Saul S. (Springfield, NJ), Jacobs; Allen L. (Randolph, NJ)
Assignee: Sandoz, Inc. (East Hanover, NJ)
Application Number:06/277,980
Patent Claims: 1. 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.sub.1 is hydrogen or halogen,

R.sub.2 is hydrogen or C.sub.1-4 alkyl,

R.sub.3 is isopropyl, sec.-butyl, isobutyl or benzyl,

R.sub.4 is methyl, ethyl or isorpropyl, and either

R.sub.5 is hydrogen and

R.sub.6 is hydrogen or methoxy or

R.sub.5 and R.sub.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.

2. A method according to claim 1 in which the center fill solution is encapsulated within 72 hours after preparation.

3. A method according to claim 1 in which the center fill solution is encapsulated within 24 hours after preparation.

4. A method according to claim 1 in which the ergot alkaloid is 0.5 to 6 milligrams of ergoloid mesylates.

5. A method according to claim 1 in which the ergot alkaloid is 0.5 to 3 milligrams of dihydroergotamine mesylate.

6. A method according to claim 1 in which the ergot alkaloid is 1 to 3 milligrams of bromocryptine mesylate.

7. A method according to claim 1 in which the center fill solution contains about 0.5 to 1.5% weight to volume ascorbic acid.

8. A method according to claim 1 in which the center fill solution contains about 1.5% weight to volume ascorbic acid.

9. 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.

10. A method according to claim 9 in which the center fill solvent is polyethylene glycol with a molecular weight of about 400.

11. A method according to claim 10 in which the center fill solvent contains about 10% by volume propylene glycol.

12. 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.

13. A capsule according to claim 12 in which the ergot alkaloid is 0.5 to 6 milligrams of ergoloid mesylates.

14. A capsule according to claim 12 in which the ergot alkaloid is 0.5 to 3 milligrams of dihydroergotamine mesylate.

15. A capsule according to claim 12 in which the ergot alkaloid is 1 to 3 milligrams of bromocryptine mesylate.

16. A capsule according to claim 12 in which center fill solution contains about 0.5 to 1.5% weight to volume ascorbic acid.

17. A capsule according to claim 12 in which the center fill solution contains about 1.5% weight to volume ascorbic acid.

18. 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.

19. A capsule according to claim 18 in which the center fill solvent is polyethylene glycol with a molecular weight of about 400.

20. A capsule according to claim 19 in which the center fill solvent contain about 10% by volume propylene glycol.

21. 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.

22. A capsule according to claim 20 in which the soft gelatin capsule shell is #9.5 oblong "A" off-white opaque capsule shell.

23. 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.

24. A capsule according to claim 23 in which the soft gelatin capsule shell is a #4 oval "B" opaque blue capsule shell.

25. 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.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc