Prilocaine and hydrofluourocarbon aerosol preparations
First Claim
1. An aerosol composition for delivering topical local anesthetic to a mammal, comprising:
- 1-99% wt of hydrofluorocarbon propellant selected from the group consisting of 1,1,1,2-tetrafluoroethane and 1,1,1,2,3,3,3-heptafluoropropane and combinations thereof, said hydrofluorocarbon propellant being the sole propellant in said aerosol composition;
1-99% wt prilocaine base solubilized within said hydrofluorocarbon propellant, said prilocaine base and said hydrofluorocarbon propellant forming a solution that is stable at reduced temperature of at least -82°
C.; and
0.01-99% wt of a pharmaceutical other than prilocaine solubilized in said hydrofluorocarbon propellant selected from the group consisting of bronchodilators, antiinflammatories, antitusives, vasoactive drugs, vasoconstrictors, antibiotics which are not antiseptics, peptides which are not enzymes, steroids, enzymes, antihistamines, hormones, 5-aminolevulinic acid, antiseptics, disinfectants, procaine, cocaine, chloroprocaine, tetracaine, mepivacaine, lidocaine, bupivacaine, etidocaine, ropivacaine, benzocaine, and phenylephrine.
2 Assignments
0 Petitions
Accused Products
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.
58 Citations
29 Claims
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1. An aerosol composition for delivering topical local anesthetic to a mammal, comprising:
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1-99% wt of hydrofluorocarbon propellant selected from the group consisting of 1,1,1,2-tetrafluoroethane and 1,1,1,2,3,3,3-heptafluoropropane and combinations thereof, said hydrofluorocarbon propellant being the sole propellant in said aerosol composition; 1-99% wt prilocaine base solubilized within said hydrofluorocarbon propellant, said prilocaine base and said hydrofluorocarbon propellant forming a solution that is stable at reduced temperature of at least -82°
C.; and0.01-99% wt of a pharmaceutical other than prilocaine solubilized in said hydrofluorocarbon propellant selected from the group consisting of bronchodilators, antiinflammatories, antitusives, vasoactive drugs, vasoconstrictors, antibiotics which are not antiseptics, peptides which are not enzymes, steroids, enzymes, antihistamines, hormones, 5-aminolevulinic acid, antiseptics, disinfectants, procaine, cocaine, chloroprocaine, tetracaine, mepivacaine, lidocaine, bupivacaine, etidocaine, ropivacaine, benzocaine, and phenylephrine. - View Dependent Claims (5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29)
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2. An aerosol composition for delivering topical local anesthetic to a mammal, comprising:
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1-99% wt of hydrofluorocarbon propellant selected from the group consisting of 1,1,1,2-tetrafluoroethane and 1,1,1,2,3,3,3-heptafluoropropane and combinations thereof, said hydrofluorocarbon propellant being the sole propellant in said aerosol composition; 1-99% wt prilocaine base solubilized within said hydrofluorocarbon propellant, said prilocaine base and said hydrofluorocarbon propellant forming a solution that is stable at reduced temperature of at least -82°
C.
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3. A method of solubilizing or suspending medicaments in hydrofluorocarbon propellants to form an aerosol composition for delivery to a mammal, comprising the steps of:
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dissolving 1-99 wt % prilocaine base in 1-99% wt of a hydrofluorocarbon propellant selected from the group consisting of 1,1,1,2-tetrafluoroethane and 1,1,1,2,3,3,3-heptafluoropropane, and combinations thereof, to produce a solution of prilocaine base and hydrofluorocarbon propellant that is stable at a reduced temperature of at least -82°
C., said hydrofluorocarbon propellant being the sole propellant in said aerosol composition; andincorporating 0.01-99wt % of a medicament other than prilocaine selected from the group consisting of bronchodilators, antiinflammatories, antitusives, vasoactive drugs, vasoconstrictors, antibiotics which are not antiseptics, peptides which are not enzymes, steroids, enzymes, antihistamines, hormones, 5-aminolevulinic acid, antiseptics, disinfectants, procaine, cocaine, chloroprocaine, tetracaine, mepivacaine, lidocaine, bupivacaine, etidocaine, ropivacaine, benzocaine, and phenylephrine into said solution by a method selected from the group consisting of solubilizing and suspending. - View Dependent Claims (4)
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Specification
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- Resources
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Current AssigneeLynchris Pharmaceuticals, Ltd.
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Original AssigneeRichard A. Henry
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InventorsHenry, Richard A.
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Primary Examiner(s)Bawa, Raj
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Application NumberUS08/435,812Time in Patent Office606 DaysField of Search424/45, 424/47, 424/46, 514/818, 514/974US Class Current424/45CPC Class CodesA61K 2300/00 Mixtures or combinations of...A61K 31/165 having aromatic rings, e.g....A61K 31/167 having the nitrogen of a ca...A61K 31/245 Amino benzoic acid types, e...A61K 31/415 1,2-DiazolesA61K 31/435 having six-membered rings w...A61K 31/445 Non condensed piperidines, ...A61K 9/008 comprising drug dissolved o...A61K 9/12 Aerosols; Foams A61K9/0043,...A61K 9/124 characterised by the propel...A61P 23/02 Local anaestheticsA61P 25/02 for peripheral neuropathiesA61P 43/00 Drugs for specific purposes...
