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Buccal, polar and non-polar spray or capsule containing drugs for treating disorders of the central nervous system

a central nervous system and polar and nonpolar technology, applied in the direction of aerosol delivery, immunological disorders, metabolism disorders, etc., can solve the problems of presenting their own problems, and achieve the effect of rapid absorption through the oral mucosa and fast onset of

Inactive Publication Date: 2009-07-23
DUGGER III HARRY A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

"The present invention provides a buccal aerosol spray and soft bite gelatin capsule for transmucosal administration of a pharmacologically active compound. The spray and gelatin capsules can be used to quickly absorb the active compound through the oral mucosal membranes, resulting in a fast onset of effect. The spray compositions contain a pharmaceutically acceptable non-polar or polar solvent, an active compound, and a flavoring agent. The gelatin capsules contain a pharmaceutically acceptable non-polar or polar solvent, an active compound, and a flavoring agent. The soft bite gelatin capsules can also contain a small amount of water. The invention provides a convenient and effective method for transmucosal administration of pharmacologically active compounds."

Problems solved by technology

However, formulations suitable for such administration by these latter routes present their own problems.

Method used

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  • Buccal, polar and non-polar spray or capsule containing drugs for treating disorders of the central nervous system
  • Buccal, polar and non-polar spray or capsule containing drugs for treating disorders of the central nervous system

Examples

Experimental program
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Effect test

example 1

Biologically Active Peptides Including Peptide Hormones

[0063]

Amountspreferred amountmost preferred amountA. Cyclosporine lingual spraycyclosporine5-5010-3515-25water5-207.5-50 9.5-12 ethanol5-607.5-50 10-20polyethylene glycol20-60 30-4535-40flavors0.1-5  1-42-3B. Cyclosporine Non-Polar lingual spraycyclosporine1-50 3-40 5-30Migylol202530-40Polyoxyethylated castor oil202530-40Butane25-80 30-7033-50flavors0.1-5  1-42-3C. Cyclosporine non-polar bite caosulecyclosporine1-35 5-2510-20olive oil25-60 35-5530-45polyoxyethylated25-60 35-5530-45oleic glyceridesflavors0.1-5  1-42-3D. Cyclosporine bite capsulecyclosporine5-5010-3515-25polyethylene glycol20-60 30-4535-40glycerin5-307.5-25 10-20propylene glycol5-307.5-25 10-20flavors0.1-10  1-83-6E. Sermorelin (as the acetate) lingual spraysermorelin (as the acetate).01-5  .1-3  .2-1.0mannitol1-25 5-2010-15monobasic sodium phosphate,0.1-5   1-31 .5-2.5dibasic sodium phosphate water0.01-5   .05-3  0.1-0.5ethanol5-307.5-25 9.5-15 polyethylene glyco...

example 2

[0064]CNS active amines and their salts: including but not limited to tricyclic amines, GABA analogues, thiazides, phenothiazine derivatives, serotonin antagonists and serotonin reuptake inhibitors

mostAmountspreferred amountpreferred amountA. Sumatriptan succinate lingual spraysumatriptan succinate0.5-30   1-2010-15ethanol5-607.5-50 10-20propylene glycol5-307.5-20 10-15polyethylene glycol0-6030-4535-40water5-307.5-20 10-15flavors0.1-5  1-42-3B. Sumatriptan succinate bite capsulesumatriptan succinate0.01-5   0.05-3.5 0.075-1.75 polyethylene glycol25-70 30-6035-50glycerin25-70 30-6035-50flavors0.1-10  1-83-6C. Clozepine lingual sprayclozepine0.5-30   1-2010-15ethanol5-607.5-50 10-20propylene glycol5-307.5-20 10-15polyethylene glycol0-6030-4535-40water5-307.5-20 10-15flavors0.1-5  1-42-3D. Clozepine non-polar lingual spray with propellantclozepine0.5-30   1-2010-15Migylol20-85 25-7030-40Butanol5-8030-7560-70flavors0.1-5  1-42-3E. Clozepine non-polar lingual spray without propellantcloz...

example 3

Sulfonylureas

[0065]

mostAmountspreferred amountpreferred amountA. Glyburide lingual sprayglyburide0.25-250.5-20 0.75-15  ethanol  5-60−7.5-50   10-20propylene glycol  5-307.5-20 10-15polyethylene glycol  0-6030-4535-40water 2.5-30 5-20 6-15flavors0.1-51-42-3B. Glyburide non-polar bite capsuleglyburide0.01-100.025-7.5 0.1-4  olive oil  30-6035-5530-50polyoxyethylated oleic  30-6035-5530-50glyceridesflavors0.1-51-42-3

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Abstract

Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II: aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.

Description

CROSS REFERENCE TO RELATED APPLICATIONS[0001]This application is a continuation-in-part of application Ser. No. 09 / 537,118, filed Mar. 29, 2000 which is a continuation-in-part of the U.S. national phase designation of PCT / US97 / 17399 filed Oct. 1, 1997, the disclosures of which are incorporated by reference herein in their entirety.BACKGROUND OF THE INVENTION[0002]It is known that certain biologically active compounds are better absorbed through the oral mucosa than through other routes of administration, such as through the stomach or intestine. However, formulations suitable for such administration by these latter routes present their own problems. For example, the biologically active compound must be compatible with the other components of the composition such as propellants solvents, etc. Many such formulations have been proposed. For example, U.S. Pat. No. 4,689,233, Dvorsky et al., describes a soft gelatin capsule for the administration of the anticoronary drug nifedipine disso...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K33/08A61K38/13A61K38/02A61K38/12A61K38/16A61K38/28A61K31/404A61K31/551A61K31/135A61K31/7072A61K31/7048A61K31/496A61K31/403A61K31/522A61K31/4164A61K31/426A61K31/19A61K36/84A61K36/28A61K31/495A61P25/00A61F13/02A61K9/00A61K9/12A61K9/48A61K31/00A61K31/085A61K31/137A61K31/138A61K31/195A61K31/197A61K31/27A61K31/337A61K31/4178A61K31/421A61K31/433A61K31/4745A61K31/515A61K31/525A61K31/557A61K31/7076A61K38/00A61K38/43A61K39/00A61L9/04A61P31/00A61P33/00A61P35/00
CPCA61K9/0056A61K38/13A61K9/12A61K31/00A61K31/085A61K31/137A61K31/138A61K31/197A61K31/27A61K31/4178A61K31/421A61K31/433A61K31/437A61K31/7076A61K9/006A61P1/12A61P11/06A61P11/08A61P25/00A61P25/08A61P25/16A61P25/18A61P25/20A61P25/22A61P25/28A61P3/02A61P31/00A61P31/04A61P31/10A61P31/12A61P33/00A61P35/00A61P37/08A61P43/00A61P5/00
Inventor DUGGER, III, HARRY A.
Owner DUGGER III HARRY A