Prilocaine and hydrofluourocarbon aerosol preparations

Drug – bio-affecting and body treating compositions – Effervescent or pressurized fluid containing – Organic pressurized fluid

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Details

424 46, 424 47, 514818, 514974, A61K 912

Patent

active

055891560

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.degree. 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.

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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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