US4091090A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Potentiated anesthetics
Assignee: Johnson and Johnson
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Filing: 1976-12-10
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Granted: 1978-05-23
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Expires: 1996-12-10
Abstract
Abstract Topical anesthetic compositions are provided wherein there is obtained an enhancement of the activity of the topical anesthetic agent by combining the anesthetic agent with an effective amount of a penetrant accelerator selected from the group consisting of the cyclohexyl substituted alkanols of the structure <IMAGE> wherein R1 is C1 to C4 alkyl, halogen or hydrogen; R2 and R3 are independently selected from hydrogen, C1 to C3 alkyl, and cyclopropyl; and n is 1 to 4, provided that only one of R2 and R3 may be propyl or cyclopropyl.
Inventors
- 👤 Tibor Sipos
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 23:23
CPC Classifications
A; A61; A61K; A61K8/00; A61K8/18; A61K8/30; A61K8/33; A61K8/34; A01; A01N; A01N31/00; A01N31/02; A01N31/04; A01N31/08; A01N31/14; A01N31/16; A01N33/00; A01N33/02; A01N33/08; A01N33/10; A61K31/00; A61K31/045; A61K31/16; A61K31/165; A61K31/21; A61K31/215; A61K31/235; A61K31/24; A61K31/245; A61K31/33; A61K31/395; A61K31/435; A61K31/44; A61K31/445; A61K45/00; A61K45/06; A61K47/00; A61K47/06; A61K47/08; A61K47/10; A61K8/40; A61K8/41; A61K8/416; A61K9/00; A61K9/0012; A61K9/0014; A61L; A61L15/00; A61L15/16; A61L15/42; A61L15/44; A61Q; A61Q11/00; A61Q17/00; A61Q17/005; A61L2300/00; A61L2300/40; A61L2300/404
Claims Analysis
Total Claims: 27
Claim 1
Independent Claim
101 words
A topical anesthetic composition comprising an effective amount of a topical anesthetic agent and an amount of a penetrant accelerator effective to enhance the skin penetration of said anesthetic agent, said penetrant accelerator being selected from the group consisting of the cyclohexyl substituted alkanols of the structure ##STR11## wherein R 1 is C 1 to C 4 alkyl, halogen or hydrogen; R 2 and R 3 are independently selected from hydrogen, C 1 to C 3 alkyl, and cyclopropyl; and n is 1 to 4, provided that only one of said R 2 and R 3 may be propyl or cyclopropyl.
Claim 2
Dependent Claim
101 words
A topical anesthetic composition comprising an effective amount of a topical anesthetic agent and an amount of a penetrant accelerator effective to enhance the skin penetration of said anesthetic agent, said penetrant accelerator being selected from the group consisting of the cyclohexyl substituted alkanols of the structure ##STR11## wherein R 1 is C 1 to C 4 alkyl, halogen or hydrogen; R 2 and R 3 are independently selected from hydrogen, C 1 to C 3 alkyl, and cyclopropyl; and n is 1 to 4, provided that only one of said R 2 and R 3 may be propyl or cyclopropyl.
Claim 3
Dependent Claim
52 words
The topical anesthetic composition of claim 1 wherein said penetrant accelerator is at least one primary, secondary or tertiary cyclohexylalkanol or alkylcyclohexyl alkanol selected from the group consisting of cyclohexylmethanol, 1-cyclohexylethanol, 2-cyclohexylethanol, 1-cyclohexyl-1-propanol, (cyclohexyl)-dimethyl-carbinol, (4-isopropylcyclohexyl)-dimethylcarbinol, 3-cyclohexyl-1-propanol, 2-cyclohexyl-1-propanol, 1-cyclohexyl-2-propanol, 2-cyclohexyl-1,1-dimethylethanol, 2-cyclohexyl-2-methylpropanol, 2-cyclohexyl-1-methylpropanol, 2-cyclohexyl-1, 2-dimethylpropanol, 2-cyclohexyl-1, 1-dimethylpropanol, 3-cyclohexyl-2-methylpropanol, 3-cyclohexyl-1-methylpropanol, 3-cyclohexylbutanol, 3-cyclohexyl-2-methylbutanol and 3-cyclohexyl-1, 2-dimethylbutanol.
Claim 4
Dependent Claim
69 words
The topical anesthetic composition of claim 1 wherein said anesthetic agent is selected from the group consisting of lidocaine, benzocaine, tetracaine, carbocaine and rodocaine, and said penetrant accelerator is at least one primary, secondary or tertiary cyclohexylalkanol or alkylcyclohexyl alkanol selected from the group consisting of cyclohexylmethanol, 1-cyclohexylethanol, 2-cyclohexylethanol, 1-cyclohexyl-1-propanol, (cyclohexyl)-dimethyl-carbinol, (4-isopropylcyclohexyl)-dimethylcaarbinol, 3-cyclohexyl-1-propanol, 2-cyclohexyl-1-propanol, 1-cyclohexyl-2-propanol, 2-cyclohexyl-1,1-dimethylethanol, 2-cyclohexyl-2-methylpropanol, 2-cyclohexyl-1-methyl-propanol, 2-cyclohexyl-1, 2-dimethylpropanol, 2-cyclohexyl-1, 1-dimethylpropanol, 3-cyclohexyl-2-methylpropanol, 3-cyclohexyl-1-methylpropanol, 3-cyclohexylbutanol, 3-cyclohexyl-2-methylbutanol and 3-cyclohexyl-1, 2-dimethylbutanol.
Claim 5
Dependent Claim
21 words
The topical anesthetic composition of claim 1 wherein the anesthetic agent comprises Lidocaine HCl and the penetrant accelerator comprises 2-cyclohexyl-1, 1-dimethylethanol.
Claim 6
Dependent Claim
18 words
The anesthetic composition of claim 1 wherein the anesthetic agent comprises Lidocaine and the penetrant accelerator comprises 2-cyclohexylethanol.
Claim 7
Dependent Claim
18 words
The composition of claim 4 which further comprises about 50% ethanol, about 10% propylene glycol, and distilled water.
Claim 8
Dependent Claim
11 words
The composition of claim 5 which further comprises about 45% ethanol.
Claim 9
Dependent Claim
13 words
The anesthetic composition of claim 1 which further comprises a pharmaceutically acceptable carrier.
Claim 10
Dependent Claim
42 words
The anesthetic composition of claim 1 which contains up to about 12% of the anesthetic agent, up to about 15% of the penetrant accelerator, and a pharmaceutically acceptable carrier selected from the group consisting of water, the lower alkanols and propylene glycol.
Claim 11
Dependent Claim
24 words
The composition of claim 9 which contains from about 1% to about 10% anesthetic agent and from about 1% to about 12% penetrant accelerator.
Claim 12
Dependent Claim
13 words
The anesthetic composition of claim 9 in which said carrier is aqueous ethanol.
Claim 13
Dependent Claim
16 words
The anesthetic composition of claim 9 in which said carrier is aqueous ethanol plus propylene glycol.
Claim 14
Dependent Claim
23 words
The topical composition of claim 1 wherein the anesthetic agent is selected from the group consisting of lidocaine, benzocaine, tetracaine, carbocaine and rodocaine.
Claim 15
Dependent Claim
41 words
The topical composition of claim 1 in which the penetrant accelerator is selected from the group consisting of cyclohexylmethanol, 1-cyclohexylethanol, 2-cyclohexylethanol, 1-cyclohexyl-1-propanol, (cyclohexyl)-dimethyl carbinol, (4-isopropylcyclohexyl)-dimethylcarbinol, 3-cyclohexyl-1-propanol, 2-cyclohexyl-1-propanol, 1-cyclohexyl-2-propanol, 2-cyclohexyl-1, 1-dimethylethanol, 2-cyclohexyl-2-methylpropanol, 2-cyclohexyl-1-methylpropanol, 2-cyclohexyl-1,2-dimethylpropanol, 2-cyclohexyl-1, 1-dimethylpropanol, 3-cyclohexyl-2-methylpropanol, 3-cyclohexyl-1-methylpropanol, 3-cyclohexylbutanol, 3-cyclohexyl-2-methylbutanol and 3-cyclohexyl-1,2-dimethylbutanol.
Claim 16
Dependent Claim
25 words
The topical composition of claim 1 in which the amount of penetrant accelerator is from about 1 to about 12% by weight of the composition.
Claim 17
Dependent Claim
20 words
The topical composition of claim 1 which includes from about 0.5 to about 12% by weight of said anesthetic agent.
Claim 18
Dependent Claim
21 words
The topical composition of claim 16 wherein the amount of anesthetic agent is from about 1% to about 10% by weight.
Claim 19
Dependent Claim
13 words
The topical composition of claim 3 which further includes a pharmaceutically acceptable carrier.
Claim 20
Dependent Claim
24 words
The topical composition of claim 18 in which the carrier is selected from the group consisting of water, the lower alkanols and propylene glycol.
Claim 21
Dependent Claim
12 words
The topical composition of claim 19 in which said carrier comprises water.
Claim 22
Dependent Claim
19 words
The topical composition of claim 1 in the form of an ointment, cream, lotion, aerosol preparation, suspension or solution.
Claim 23
Dependent Claim
20 words
A method of inducing anesthesia topically comprising applying to the skin of an animal a topical composition of claim 1.
Claim 24
Dependent Claim
80 words
In the topical inducement of anesthesia by applying to the skin of an animal a topical anesthetic agent, the improvement comprising potentiating the activity or penetration of the anesthetic agent by applying the same in conjunction with a potentiator which is a primary, secondary or tertiary cyclohexylalkanol or alkylcyclohexyl alkanol selected from the group consisting of cyclohexylmethanol, 1-cyclohexylethanol, 2-cyclohexylethanol, 1-cyclohexyl-1-propanol, (cyclohexyl)-dimethylcarbinol, (4,isoproyl-cyclohexyl)-dimethylcarbinol, 3-cyclohexyl-1-propanol, 2-cyclohexyl-1-propanol, 1-cyclohexyl-2-propanol, 2-cyclohexyl-1, 1-dimethylethanol, 2-cyclohexyl-2-methylpropanol, 2-cyclohexyl-1-methylpropanol, 2-cyclohexyl-1, 2-dimethylpropanol, 2-cyclohexyl-1, 1-dimethylpropanol, 3-cyclohexyl-2-methylpropanol, 3-cyclohexyl-1-methylpropanol, 3-cyclohexylbutanol, 3-cyclohexyl-2-methylbutanol and 3-cyclohexyl-1, 2-dimethylbutanol.
Claim 25
Dependent Claim
80 words
In the topical inducement of anesthesia by applying to the skin of an animal a topical anesthetic agent, the improvement comprising potentiating the activity or penetration of the anesthetic agent by applying the same in conjunction with a potentiator which is a primary, secondary or tertiary cyclohexylalkanol or alkylcyclohexyl alkanol selected from the group consisting of cyclohexylmethanol, 1-cyclohexylethanol, 2-cyclohexylethanol, 1-cyclohexyl-1-propanol, (cyclohexyl)-dimethylcarbinol, (4,isoproyl-cyclohexyl)-dimethylcarbinol, 3-cyclohexyl-1-propanol, 2-cyclohexyl-1-propanol, 1-cyclohexyl-2-propanol, 2-cyclohexyl-1, 1-dimethylethanol, 2-cyclohexyl-2-methylpropanol, 2-cyclohexyl-1-methylpropanol, 2-cyclohexyl-1, 2-dimethylpropanol, 2-cyclohexyl-1, 1-dimethylpropanol, 3-cyclohexyl-2-methylpropanol, 3-cyclohexyl-1-methylpropanol, 3-cyclohexylbutanol, 3-cyclohexyl-2-methylbutanol and 3-cyclohexyl-1, 2-dimethylbutanol.
Claim 26
Dependent Claim
19 words
The method of claim 23 wherein the anesthetic agent comprises Lidocaine HCl and the penetrant accelerator comprises 2-cyclohexyl-1, 1-dimethylethanol.
Claim 27
Dependent Claim
17 words
The method of claim 23 wherein the anesthetic agent comprises Lidocaine and the penetrant accelerator comprises 2-cyclohexylethanol.
References Cited (Backward Citations)
US3891757A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1981-05-22 | 1981-11-21 | 1982-05-23 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-05-22 | 1985-11-21 | 1986-05-23 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-05-22 | 1989-11-21 | 1990-05-23 | $7700.00 | Window Closed / Lapsed |