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Prilocaine and hydrofluourocarbon aerosol preparations

Patent 5589156 Issued on December 31, 1996. Estimated Expiration Date: Icon_subject May 5, 2015. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.

Patent References

5118494

Formulation for delivery of drugs by metered dose inhalers with reduced or no chlorofluorocarbon content
Patent #: 5190029
Issued on: 03/02/1993
Inventor: Byron, et al.

Medicinal aerosol formulations
Patent #: 5225183
Issued on: 07/06/1993
Inventor: Purewal, et al.

Vision aid and anesthetic composition
Patent #: 5276032
Issued on: 01/04/1994
Inventor: King, et al.

Topical composition enhancing healing of viral lesions Patent #: 5380754
Issued on: 01/10/1995
Inventor: Miller, et al.

Inventor

Application

No. 435812 filed on 05/05/1995

US Classes:

424/45, Organic pressurized fluid424/46, Powder or dust containing424/47, Topical live body grooming or adorning aid (e.g., hair spray, antiperspirant, etc.)514/818, ANESTHETIC, LOCAL514/974CONTAINING DESIGNATED INGREDIENT TO REDUCE NOXIOUS EFFECTS OF ACTIVE INGREDIENT (E.G., TASTE MASKING, ODOR REDUCING, ETC.)

Examiners

Primary: Bawa, Raj

Attorney, Agent or Firm

Foreign Patent References

  • 07333 WO 07/13/1990
  • 14466 WO 09/13/1992

International Class

A61K 009/12

Abstract

Aerosol compositions used for anesthetizing mammals in both human and veterinary applications include prilocaine base solubilized in the hydrofluorocarbon (HFC) propellants 1,1,1,2-tetrafluoroethane and 1,1,1,2,3,3,3-heptafluoropropane. Prilocaine base has been found to be readily soluble in HFC propellants when combined in liquid or micro rod form, and a solution stable to temperatures as low as -82° C. is formed upon combination of the two components. In the aerosol compositions, the HFCs are the only propellants used. Additional pharmaceutical constituents can also be combined the the prilocaine base/HFC composition to provide a multi-component anesthetic, and it has been found that the presence of prilocaine in the combination can assist in solubilizing and/or suspending these pharmaceutical consituents. Some example pharmaceutical compositions within the practice of this invention include HFC, prilocaine base, and a pharmaceutical other prilocaine selected from the group consisting of bronchodilators, antiinflammatories, antitusives, vasoactive drugs, vasoconstrictors, antibiotics, peptides, steroids, enzymes, antihistamines, hormones, enzyme and receptor inhibitors and agonists, 5-aminolevulinic acid, antiseptics, disinfectants, procaine, cocaine, chloroprocaine, tetractaine, mepivacaine, lidocaine, bupivacaine, etidocaine, ropivacaine, benzocaine, and phenylephrine.

Other References

  • Mor en, F. et al. (1993). Aerosols in Medicine. Principles, Diagnosis and Therapy. Elsevier Sci. Publishers, pp. 303-319
  • Madar, M. J. (1993). J. Appl. Physiology 74(3): 1419-1424
  • "Neural blockade in Clinical Anesthesia and Management of Pain" 2nd Edition. Chapters 1 and 2. Edited by Michael J. Cousins and Phillip O. Bridenbaugh. Published by Lippencott. (1989
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