Claims for Patent: 4,758,423

Summary for Patent: 4,758,423

Title:	Certain ergot peptide alkaloids administered to the nasal mucosa
Abstract:	The present invention provides a nasal 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 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, 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:	First Fidelity Bank, National Association, New Jersey (Newark, NJ)
Application Number:	06/871,985
Patent Claims:	1. A pharmaceutically acceptable nasal spray applicator consisting essentially of a nasal applicator containing therein an ergot peptide alkaloid composition for nasal administration comprising per unit dose a therapeutically effective amount of dihydroergocristine or an ergot peptide alkaloid of the formula ##STR3## wherein R.sub.1 is hydrogen or halogen, R.sub.2 is hydrogen, methyl or isopropyl, and 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 and 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 a pharmaceutically acceptable acid addition salt thereof, in association with a pharmaceutically acceptable carrier suitable for nasal spray administration, said nasal applicator being adapted to administer a unit dose of the ergot peptide alkaloid to the mucous membrane of the nose. 2. A pharmaceutically acceptable nasal spray applicator as claimed in claim 1 wherein the composition comprises per unit dose 0.1 to 5 mg of the ergot peptide alkaloid. 3. The nasal spray applicator as claimed in claim 1 wherein the compound of formula I is dihydroergotamine. 4. The nasal spray applicator as claimed in claim 1 wherein the compound of formula I is bromocriptine. 5. The nasal spray applicator as claimed in claim 1 wherein the compound of formula I is dihydroergotoxine. 6. The nasal spray applicator as claimed in claim 1 adapted to administer 0.1 to 5 mg of the ergot peptide alkaloid per administration. 7. A nasal spray applicator according to claim 1 in which the ergot peptide alkaloid composition is in liquid form. 8. The nasal spray applicator as claimed in claim 7 wherein the ergot alkaloid composition contains 0.1 to 5 mg of active agent per ml of solution. 9. A nasal spray applicator according to claim 7 in which the ergot peptide alkaloid composition contains a propellant acceptable in nasal administration. 10. A nasal spray applicator according to claim 9 in which the propellant is a halogenated hydrocarbon. 11. A nasal spray applicator according to claim 7 in which the ergot peptide alkaloid composition is in the form of an aqueous solution containing a viscosity increasing agent. 12. A nasal spray applicator according to claim 11 in which the viscosity increasing agent is methyl cellulose. 13. A nasal spray applicator according to claim 7 in which the carrier is a non-aqueous solvent.