US4599342A
Expired / Lapsed
US
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Pharmaceutical products providing enhanced analgesia
Assignee: Procter and Gamble Co
•
Filing: 1984-01-16
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Granted: 1986-07-08
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Expires: 2004-01-16
Abstract
Abstract An analgesic composition comprising capsaicin or a capsaicin analog and an analgesic selected from the class of opioids is disclosed. This combination has been found to exhibit unexpectedly enhanced analgesic activity in humans and lower animals without a corresponding increase in undesirable side effects.
Inventors
- 👤 Thomas R. LaHann
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 23:32
CPC Classifications
A; A61; A61K; A61K45/00; A61K45/06; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/47; A61K31/485; A61P; A61P25/00; A61P25/04
Claims Analysis
Total Claims: 27
Claim 1
Independent Claim
127 words
An analgesic composition comprising a safe and effective amount of: (a) an analgesic compound of the formula ##STR11## wherein R 1 is selected from the group consisting of OH and OCH 3 , R 2 is OH, X is selected from the group consisting of ##STR12## and R is selected from the group consisting of a C 5 -C 11 alkyl, C 5 -C 11 alkenyl, C 11 -C 23 cis alkenyl, C 11 -C 23 alkynyl, C 11 -C 23 alkadienyl and C 11 -C 23 methylene substituted alkane; (b) an analgesic opioid selected from the group consisting of morphine, oxycodone, derivatives thereof, salts thereof and mixtures thereof; and (c) a pharmaceutically-acceptable carrier; wherein the weight ratio of (a):(b) is from about 20,000:1 to about 1:20.
Claim 2
Dependent Claim
127 words
An analgesic composition comprising a safe and effective amount of: (a) an analgesic compound of the formula ##STR11## wherein R 1 is selected from the group consisting of OH and OCH 3 , R 2 is OH, X is selected from the group consisting of ##STR12## and R is selected from the group consisting of a C 5 -C 11 alkyl, C 5 -C 11 alkenyl, C 11 -C 23 cis alkenyl, C 11 -C 23 alkynyl, C 11 -C 23 alkadienyl and C 11 -C 23 methylene substituted alkane; (b) an analgesic opioid selected from the group consisting of morphine, oxycodone, derivatives thereof, salts thereof and mixtures thereof; and (c) a pharmaceutically-acceptable carrier; wherein the weight ratio of (a):(b) is from about 20,000:1 to about 1:20.
Claim 3
Dependent Claim
19 words
A composition according to claim 1, wherein the weight ratio of (a):(b) is from about 10,000:1 to about 1:10.
Claim 4
Dependent Claim
11 words
A composition according to claim 2, wherein R 1 is OH.
Claim 5
Dependent Claim
20 words
A composition according to claim 3, wherein X is ##STR13## and R is a C 7 -C 10 alkyl group.
Claim 6
Dependent Claim
14 words
A composition according to claim 4, wherein R is C 8 H 17 .
Claim 7
Dependent Claim
15 words
A composition according to claim 2, wherein R 1 R 1 is OCH 3 .
Claim 8
Dependent Claim
10 words
A composition according to claim 6, wherein X is ##STR14##
Claim 9
Dependent Claim
18 words
A composition according to claim 7, wherein R is a C 7 -C 10 alkyl or trans alkenyl.
Claim 10
Dependent Claim
14 words
A composition according to claim 8, wherein R is C 9 H 17 .
Claim 11
Dependent Claim
18 words
A composition according to claim 7, wherein R is a C 16 -C 21 cis alkenyl or alkadienyl.
Claim 12
Dependent Claim
14 words
A composition according to claim 10, wherein R is C 17 H 33 .
Claim 13
Dependent Claim
25 words
A composition according to claim 2, wherein the opioid is selected from the group consisting of morphine and analgesic morphine derivatives and their pharmaceutically-acceptable salts.
Claim 14
Dependent Claim
12 words
A composition according to claim 12, wherein the opiod analgesic is morphine.
Claim 15
Dependent Claim
21 words
A composition according to claim 13, wherein the weight ratio of capsaicinoid to morphine is from about 1200:1 to about 1:3.
Claim 16
Dependent Claim
11 words
A composition according to claim 14, wherein the capsaicinoid is N-vanillyl-9E-octadecenamide.
Claim 17
Dependent Claim
21 words
A composition according to claim 15, wherein the weight ratio of N-vanillyl-9E-octadecenamide to morphine is from about 50:1 to about 1:1.
Claim 18
Dependent Claim
11 words
A composition according to claim 2, wherein the opiod is oxycodone.
Claim 19
Independent Claim
144 words
A method for providing analgesia in humans and lower animals which comprises administering concurrently to a human or lower animal in need of such treatment a safe and effective amount of: (a) an analgesic compound of the formula ##STR15## wherein R 1 is selected from the group consisting of OH and OCH 3 , R 2 is OH, X is selected from the group consisting of ##STR16## and R is selected from the group consisting of a C 5 -C 11 alkyl, C 5 -C 11 alkenyl, C 11 -C 23 cis alkenyl, C 11 -C 23 alkynyl, C 11 -C 23 alkadienyl and C 11 -C 23 methylene substituted alkane; and (b) an analgesic opioid selected from the group consisting of morphine, oxycodone, derivatives thereof, salts thereof and mixture thereof; wherein the weights ratio of (a):(b) is from about 20,000:1 to about 1:20.
Claim 20
Independent Claim
144 words
A method for providing analgesia in humans and lower animals which comprises administering concurrently to a human or lower animal in need of such treatment a safe and effective amount of: (a) an analgesic compound of the formula ##STR15## wherein R 1 is selected from the group consisting of OH and OCH 3 , R 2 is OH, X is selected from the group consisting of ##STR16## and R is selected from the group consisting of a C 5 -C 11 alkyl, C 5 -C 11 alkenyl, C 11 -C 23 cis alkenyl, C 11 -C 23 alkynyl, C 11 -C 23 alkadienyl and C 11 -C 23 methylene substituted alkane; and (b) an analgesic opioid selected from the group consisting of morphine, oxycodone, derivatives thereof, salts thereof and mixture thereof; wherein the weights ratio of (a):(b) is from about 20,000:1 to about 1:20.
Claim 21
Dependent Claim
38 words
A method according to claim 18, wherein R is selected from the group consisting of C 7 -C 10 alkyl, C 7 -C 10 trans alkenyl, C 17 -C 21 cis alkenyl, and C 16 -C 21 alkadienyl.
Claim 22
Dependent Claim
30 words
A method according to claim 18, wherein the capsaicinoid is N-vanillyl-9E-octadecenamide, the opioid is morphine, and the weight ratio of N-vanillyl-9E-octadecenamide to morphine is from about 50:1 to about 1:1.
Claim 23
Dependent Claim
12 words
A method according to claim 18, wherein the components are administered subcutaneously.
Claim 24
Dependent Claim
12 words
A method according to claim 18, wherein the components are administered intravenously.
Claim 25
Dependent Claim
12 words
A method according to claim 18, wherein the components are administered intramuscularly.
Claim 26
Dependent Claim
12 words
A method according to claim 18, wherein the components are administered orally.
Claim 27
Dependent Claim
12 words
A method according to claim 18, wherein the components are administered topically.
References Cited (Backward Citations)
US3060091A
Cited
US3110650A
Cited
US3106513A
Cited
US4083981A
Cited
US4238508A
Cited
US4315936A
Cited
US4379789A
Cited
US4313958A
Cited
US4401663A
Cited
US4424205A
Cited
US4404210A
Cited
US4407805A
Cited
US4407804A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1989-07-07 | 1990-01-06 | 1990-07-08 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1993-07-07 | 1994-01-06 | 1994-07-08 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1997-07-07 | 1998-01-06 | 1998-07-08 | $7700.00 | Window Closed / Lapsed |