US5589156A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Prilocaine and hydrofluourocarbon aerosol preparations
Assignee: LYNCHRIS PHARMACEUTICALS Ltd
•
Filing: 1995-05-05
•
Granted: 1996-12-31
•
Expires: 2015-05-05
Abstract
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.
Inventors
- 👤 Richard A. Henry
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 05:46
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/21; A61K31/215; A61K31/235; A61K31/24; A61K31/245; A61K31/16; A61K31/165; A61K31/167; A61K31/33; A61K31/395; A61K31/41; A61K31/415; A61K31/435; A61K31/44; A61K31/445; A61K9/00; A61K9/0012; A61K9/007; A61K9/0073; A61K9/008; A61K9/10; A61K9/12; A61K9/124; A61P; A61P23/00; A61P23/02; A61P25/00; A61P25/02; A61P43/00
Claims Analysis
Total Claims: 32
Claim 1
Independent Claim
126 words
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.
Claim 2
Dependent Claim
126 words
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.
Claim 3
Dependent Claim
70 words
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.
Claim 4
Dependent Claim
70 words
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.
Claim 5
Independent Claim
149 words
A method of solubilizing or suspending medicaments in hydrofluorocarbon propellants to form an aerosol composition for delivery to a mammal, comprising the steps of: 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; and incorporating 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.
Claim 6
Independent Claim
149 words
A method of solubilizing or suspending medicaments in hydrofluorocarbon propellants to form an aerosol composition for delivery to a mammal, comprising the steps of: 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; and incorporating 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.
Claim 7
Dependent Claim
14 words
The method of claim 3 wherein said dissolving and incorporating steps are performed simultaneously.
Claim 8
Dependent Claim
12 words
The aerosol composition of claim 1 wherein said pharmaceutical is a bronchodilator.
Claim 9
Dependent Claim
12 words
The aerosol composition of claim 1 wherein said pharmaceutical is an antiinflammatory.
Claim 10
Dependent Claim
12 words
The aerosol composition of claim 1 wherein said pharmaceutical is an antitusive.
Claim 11
Dependent Claim
20 words
The aerosol composition of claim 1 wherein said pharmaceutical is selected from the group consisting of vasoactive drugs and vasoconstrictors.
Claim 12
Dependent Claim
12 words
The aerosol composition of claim 1 wherein said pharmaceutical is an antibiotic.
Claim 13
Dependent Claim
12 words
The aerosol composition of claim 1 wherein said pharmaceutical is a peptide.
Claim 14
Dependent Claim
12 words
The aerosol composition of claim 1 wherein said pharmaceutical is a steroid.
Claim 15
Dependent Claim
12 words
The aerosol composition of claim 1 wherein said pharmaceutical is an enzyme.
Claim 16
Dependent Claim
12 words
The aerosol composition of claim 1 wherein said pharmaceutical is an antihistamine.
Claim 17
Dependent Claim
12 words
The aerosol composition of claim 1 wherein said pharmaceutical is a hormone.
Claim 18
Dependent Claim
22 words
The aerosol composition of claim 1 wherein said pharmaceutical is selected from the group consisting of enzyme and receptor inhibitors and agonists.
Claim 19
Dependent Claim
12 words
The aerosol composition of claim 1 wherein said pharmaceutical is 5-aminolevulinic acid.
Claim 20
Dependent Claim
12 words
The aerosol composition of claim 1 wherein said pharmaceutical is an antiseptic.
Claim 21
Dependent Claim
12 words
The aerosol composition of claim 1 wherein said pharmaceutical is a disinfectant.
Claim 22
Dependent Claim
11 words
The aerosol composition of claim 1 wherein said pharmaceutical is procaine.
Claim 23
Dependent Claim
11 words
The aerosol composition of claim 1 wherein said pharmaceutical is cocaine.
Claim 24
Dependent Claim
11 words
The aerosol composition of claim 1 wherein said pharmaceutical is chloroprocaine.
Claim 25
Dependent Claim
11 words
The aerosol composition of claim 1 wherein said pharmaceutical is tetracaine.
Claim 26
Dependent Claim
11 words
The aerosol composition of claim 1 wherein said pharmaceutical is mepivacaine.
Claim 27
Dependent Claim
11 words
The aerosol composition of claim 1 wherein said pharmaceutical is lidocaine.
Claim 28
Dependent Claim
11 words
The aerosol composition of claim 1 wherein said pharmaceutical is bupivacaine.
Claim 29
Dependent Claim
11 words
The aerosol composition of claim 1 wherein said pharmaceutical is etidocaine.
Claim 30
Dependent Claim
11 words
The aerosol composition of claim 1 wherein said pharmaceutical is ropivacaine.
Claim 31
Dependent Claim
11 words
The aerosol composition of claim 1 wherein said pharmaceutical is benzocaine.
Claim 32
Dependent Claim
11 words
The aerosol composition of claim 1 wherein said pharmaceutical is phenylephrine.
References Cited (Backward Citations)
US5380754A
Cited
US5225183A
Cited
WO1990007333A1
Cited
US5276032A
Cited
US5118494A
Cited
US5190029A
Cited
WO1992014466A1
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1999-12-31 | 2000-07-01 | 2000-12-31 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2003-12-31 | 2004-07-01 | 2004-12-31 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2007-12-31 | 2008-07-01 | 2008-12-31 | $7700.00 | Window Closed / Lapsed |