Claims
- 1. A predominantly nonaqueous formulation for intra-oral delivery of at least one pharmaceutical agent to a patient comprising a dispersion of an effective amount of the pharmaceutical agent and an orally-acceptable oral-absorption enhancer operable to modify the absorptive surface of the targeted intra-oral membrane and enhance bioavailability of the pharmaceutical agent across the membrane, in an orally-acceptable nonaqueous carrier-solvent containing a quantity of a formulation surfactant at least sufficient to increase the miscibility of the pharmaceutical agent in the nonaqueous carrier-solvent.
- 2. The formulation according to claim 1 in which the pharmaceutical agent is a glucocorticoid steroid, testosterone, dexamethasone, prednisolone, prednisone, stanozolol, barbituates, seconal, benzodizepines, a sedative-hypnotic, nitroglycerine, an analgesic or a peptide or protein having a molecular weight up to about 50,000 Daltons, or an orally administerable non-toxic salt of said pharmaceutical agent.
- 24. The formulation according to claim 2 in which the peptide or protein is calcitonin, insulin, GLP, HGH, or leuprolide.
- 25. The formulation according to claim 2 in which the analgesic is ketorolac, oxandrolone, morphine, fentanyl, codeine, or a salt thereof.
- 3. The formulation according to claim 2 in which the pharmaceutical agent is present in an amount of about 0.01 to 25% by weight of the composition.
- 4. The formulation according to claim 1 in which the oral-absorption enhancer is selected from the group consisting of hydroxypropyl-beta-cyclodextrin, benzalkonium chloride, benzethonium chloride, polysorbate 80, sodium lauryl sulfate, polyoxyethylene ethers of aliphatic alcohols, polyoxyethylene derivatives of fatty acid partial esters of sorbitol anhydride, and polyoxyalkylene block copolymers.
- 5. The formulation according to claim 1 in which the oral-absorption enhancer is present in an amount of about 0.1 to 20% by weight.
- 6. The formulation according to claim 1 in which the carrier solvent is selected from the group consisting of ethanol, glycerol, glycol, propylene glycol, polyethylene glycol, sorbitol, vitamin E, derivatives of vitamin E, and polyvinylpyrrolidone.
- 7. The formulation according to claim 1 in which the carrier solvent is present in an amount of about 0.5 to 50% by weight of the composition.
- 8. The formulation according to claim 1 in which the formulation surfactant reduces the pharmaceutical agent to an average droplet size of from about 10 to about 200 microns.
- 9. The formulation according to claim 1 further comprising a propellant.
- 10. The formulation according to claim 9 in which the propellant is selected from the group consisting of hydrofluoroalkane, propane, HFA-134A, HFA-152A, HFA-227, freone 12, freone 13, butane, and carbon dioxide.
- 11. The formulation according to claim 10 in which the propellant is present in an amount of from 20 to 95 % by weight.
- 12. The formulation according to claim 1 in which the pharmaceutical agent comprises insulin.
- 13. The formulation according to claim 1 in which the pharmaceutical agent comprises fentanyl citrate.
- 14. (Canceled.)
- 15. A predominantly nonaqueous formulation effective for intra-oral delivery of at least one pharmaceutical agent to a patient, the formulation comprising a dispersion of an effective amount of the pharmaceutical agent mixed with an oral-absorption enhancer operable to modify the absorptive surface of the targeted intra-oral membrane and enhance bioavailability improve absorption of the pharmaceutical agent across the membrane, a formulation surfactant operable to reduce the pharmaceutical agent to an average droplet size of less than 200 microns, ethanol, and a nonaqueous propellant operable to deliver pharmaceutical agent to the mucosa of the patient's intra-oral cavity.
- 16. A predominantly nonaqueous formulation consisting essentially of about 0.1 to 10% by weight insulin, about 0.1 to 10% by weight oral-absorption enhancer selected from the group consisting of hydroxypropyl-beta-cyclodextrin, benzalkonium chloride, benzethonium chloride, polysorbate 80, sodium lauryl sulfate, polyoxyethylene ethers of aliphatic alcohols, polyoxyethylene derivatives of fatty acid partial esters of sorbitol anhydride, and polyoxyalkylene block copolymers; about 0.1 to 10% of a formulation surfactant; about 5 to 50% of a carrier solvent; and a nonaqueous propellant.
- 17. (Canceled.)
- 18. A predominantly nonaqueous system for intra-oral delivery to a patient of a pharmaceutical agent comprising:
a formulation comprising an effective amount of a pharmaceutical agent mixed with a formulation surfactant and an oral absorption enhancer in a carrier-solvent, and a mechanical assembly operable for dispensing the formulation to the mucosa of the intra-oral cavity of the patient, wherein the mechanical assembly includes an aerosolizing device and the formulation is disposed within the mechanical assembly and emitted therefrom in a spray caused by the aerosolizing device.
- 19. The system of claim 18 in which the mechanical assembly comprises a pump device.
- 20. The system of claim 18 in which the mechanical assembly comprises a propellant device.
- 21. A system for treating a patient with a pharmaceutical agent comprising
(i) a predominantly nonaqueous formulation comprising a pharmaceutical agent stabilized until ready for administration to the patient, and an orally-acceptable oral-absorption enhancer operable to modify the absorptive surface of the targeted intra-oral membrane and enhance bioavailability improve absorption of the pharmaceutical agent across the membrane, and a formulation surfactant and (ii) a mechanical assembly for dispensing the formulation to the mucosa of the intra-oral cavity, the mechanical assembly having an aerosolizing device for reducing the formulation to a spray.
- 22. A method for administering a pharmaceutical agent to a patient comprising providing the system of claim 21 and spraying the formulation into the patient's intra-oral cavity.
- 23. (Canceled.)
RELATED APPLICATIONS
[0001] This application is related to, and claims the benefit of priority under, U.S. provisional patent application Ser. No. 60/119,923, filed Feb. 12, 1999.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60119923 |
Feb 1999 |
US |
Continuations (1)
|
Number |
Date |
Country |
Parent |
09502871 |
Feb 2000 |
US |
Child |
09944492 |
Aug 2001 |
US |