US4139627A
Expired / Lapsed
US
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Anesthetic lozenges
Assignee: GlaxoSmithKline LLC
•
Filing: 1977-11-07
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Granted: 1979-02-13
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Expires: 1997-11-07
Abstract
Abstract Anesthetic lozenges are prepared by combining an acid addition salt of 3-piperidino-p-alkoxypropiophenoneswith a molten hard candy base with either the prior or simultaneous addition of a stabilizing amount of a pharmaceutically acceptable acid such as citric acid.
Inventors
- 👤 Philip A. Lane
- 👤 Bruce A. Brown
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 13:32
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/44; A61K31/445; A61K9/00; A61K9/0012; A61K9/0053; A61K9/0056
Claims Analysis
Total Claims: 22
Claim 1
Independent Claim
106 words
A process for the production of a topical anesthetic lozenge which comprises heating a candy base suitable for said lozenges to the melting point, adding an amount of a pharmaceutically acceptable acid selected from the group consisting of citric acid, fumaric acid, malic acid, tartaric acid, lactic acid, adipic acid and phosphoric acid prior to or simultaneously with the addition of an anesthetically effective amount of a pharmaceutically acceptable acid addition salt of the compound of the formula ##STR1## wherein R is alkyl of 2 to 8 carbon atoms, sufficient to stabilize said salt, said amount being from 0.2% to about 1.0% by weight of lozenge.
Claim 2
Dependent Claim
106 words
A process for the production of a topical anesthetic lozenge which comprises heating a candy base suitable for said lozenges to the melting point, adding an amount of a pharmaceutically acceptable acid selected from the group consisting of citric acid, fumaric acid, malic acid, tartaric acid, lactic acid, adipic acid and phosphoric acid prior to or simultaneously with the addition of an anesthetically effective amount of a pharmaceutically acceptable acid addition salt of the compound of the formula ##STR1## wherein R is alkyl of 2 to 8 carbon atoms, sufficient to stabilize said salt, said amount being from 0.2% to about 1.0% by weight of lozenge.
Claim 3
Dependent Claim
12 words
A process according to claim 1 wherein the acid is citric acid.
Claim 4
Dependent Claim
14 words
A process according to claim 1 wherein about 0.5% of citric acid is added.
Claim 5
Dependent Claim
14 words
A process according to claim 1 wherein about 0.75% of citric acid is added.
Claim 6
Dependent Claim
14 words
A process according to claim 1 wherein about 1.0% of citric acid is added.
Claim 7
Dependent Claim
13 words
A process according to claim 1 wherein said salt is the hydrochloride salt.
Claim 8
Dependent Claim
10 words
A process according to claim 1 wherein R is n-butyl.
Claim 9
Dependent Claim
10 words
A process according to claim 1 wherein R is n-propyl.
Claim 10
Dependent Claim
17 words
A process according to claim 1 wherein R is n-butyl and the salt is the hydrochloride salt.
Claim 11
Dependent Claim
22 words
A process according to claim 1 wherein R is n-butyl, the salt is the hydrochloride salt and the acid is citric acid.
Claim 12
Dependent Claim
85 words
A lozenge comprising an anesthetically effective amount of a pharmaceutically acceptable acid addition salt of the compound of the formula ##STR2## wherein R is alkyl of 2 to 8 carbon atoms, and an amount of a pharmaceutically acceptable acid selected from the group consisting of citric acid, fumaric acid, malic acid, tartaric acid, lactic acid, adipic acid and phosphoric acid sufficient to stabilize said salt intimately mixed in a hard candy base, said amount being from about 0.2% to about 1.0% by weight of lozenge.
Claim 13
Dependent Claim
85 words
A lozenge comprising an anesthetically effective amount of a pharmaceutically acceptable acid addition salt of the compound of the formula ##STR2## wherein R is alkyl of 2 to 8 carbon atoms, and an amount of a pharmaceutically acceptable acid selected from the group consisting of citric acid, fumaric acid, malic acid, tartaric acid, lactic acid, adipic acid and phosphoric acid sufficient to stabilize said salt intimately mixed in a hard candy base, said amount being from about 0.2% to about 1.0% by weight of lozenge.
Claim 14
Dependent Claim
12 words
A lozenge according to claim 11 wherein the acid is citric acid.
Claim 15
Dependent Claim
14 words
A lozenge according to claim 11 which contains 0.5% by weight of citric acid.
Claim 16
Dependent Claim
14 words
A lozenge according to claim 11 which contains 0.75% by weight of citric acid.
Claim 17
Dependent Claim
14 words
A lozenge according to claim 11 which contains 1.0% by weight of citric acid.
Claim 18
Dependent Claim
13 words
A lozenge according to claim 11 wherein the salt is the hydrochloride salt.
Claim 19
Dependent Claim
10 words
A lozenge according to claim 11 wherein R is n-butyl.
Claim 20
Dependent Claim
10 words
A lozenge according to claim 11 wherein R is n-propyl.
Claim 21
Dependent Claim
17 words
A lozenge according to claim 11 wherein R is n-butyl and the salt is the hydrochloride salt.
Claim 22
Dependent Claim
22 words
A lozenge according to claim 11 wherein R is n-butyl, the salt is the hydrochloride salt and the acid is citric acid.
References Cited (Backward Citations)
US2208120A
Cited
US2771391A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-02-12 | 1982-08-14 | 1983-02-13 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-02-12 | 1986-08-14 | 1987-02-13 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-02-12 | 1990-08-14 | 1991-02-13 | $7700.00 | Window Closed / Lapsed |