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Last Updated: May 4, 2024

Claims for Patent: 4,462,983


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Summary for Patent: 4,462,983
Title: Certain ergot peptide alkaloids administered to the nasal mucosa
Abstract:The present invention provides a nasal or pulmonary pharmaceutical composition comprising as active agent a compound of formula I, ##STR1## wherein R.sub.1 is hydrogen or halogen, R.sub.2 is hydrogen or alkyl of 1 to 4 carbon atoms, either (i) R.sub.3 is isopropyl, sec-butyl, or isobutyl, R.sub.4 methyl, ethyl or isopropyl and R.sub.5 is hydrogen and R.sub.6 is hydrogen or methoxy or R.sub.5 and R.sub.6 are together a single bond, or (ii) R.sub.3 is benzyl, R.sub.4 is methyl, R.sub.5 is hydrogen and R.sub.6 is hydrogen or methoxy, or (III) dihydroergocristine, in association with a pharmaceutically acceptable carrier or diluent, adapted for nasal or pulmonary administration.
Inventor(s): Azria; Moise (Paris, FR), Cavanak; Thomas (Oberwil, CH)
Assignee: Sandoz Ltd. (Basel, CH)
Application Number:06/328,680
Patent Claims: 1. An improved method of systemically administering a pharmaceutically effective amount of an ergot peptide alkaloid active agent of formula I, ##STR3## wherein R.sub.1 is hydrogen or halogen,

R.sub.2 is hydrogen, methyl or isopropyl,

either (i)

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

R.sub.4 is methyl, ethyl or isopropyl, and

R.sub.5 is hydrogen and R.sub.6 is hydrogen or methoxy

or R.sub.5 and R.sub.6 are together a single bond,

or (ii)

R.sub.3 is benzyl, R.sub.4 is methyl, R.sub.5 is hydrogen and R.sub.6 is hydrogen or methoxy, or (III) dihydroergocristine,

or a pharmaceutically acceptable acid addition salt thereof, the improvement which comprises locally administering to the nasal mucous membranes a therapeutically effective amount of the ergot peptide alkaloid active agent.

2. A method as claimed in claim 1 wherein the compound of formula I is dihydroergotamine.

3. A method as claimed in claim 1 wherein the compound of formula I is bromocriptine.

4. A method as claimed in claim 1 wherein the compound of formula I is dihydroergotoxine.

5. A method as claimed in claim 1 wherein the ergot alkaloid active agent is administered in the form of a spray.

6. A method as claimed in claim 5 wherein an atomiser containing a propellant produces the spray.

7. A method as claimed in claim 6 wherein the propellant is a halogenated hydrocarbon.

8. A method as claimed in claim 5 wherein 0.1 to 5 mg of the ergot peptide alkaloid active agent is administered per administration.

9. A method as claimed in claim 5 wherein the spray is a powder spray.

10. A method as claimed in claim 5 wherein the spray is a liquid spray.

11. A method as claimed in claim 5 wherein the spray is produced from a solution of the ergot peptide alkaloid active agent containing 0.1 to 5 mg of active agent per ml of solution.

12. A method as claimed in claim 1 wherein the active agent is in the form of a pharmaceutically acceptable acid addition salt.

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