US4626539A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Trandermal delivery of opioids
Assignee: Bristol Myers Squibb Pharma Co
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Filing: 1985-06-10
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Granted: 1986-12-02
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Expires: 2005-06-10
Abstract
Abstract Opioid-containing pharmaceutical compositions are provided which are useful in effecting transdermal delivery of a therapeutic dose of the opioid to the systemic circulation of a mammal. These pharmaceutical compositions consist essentially of the opioid, a penetration enhancer which is at least one of a saturated fatty alcohol or fatty acid of 8-15 carbon atoms or of an unsaturated fatty alcohol or fatty acid of 8-18 carbon atoms, and a suitable pharmaceutical carrier, preferably propylene glycol.
Inventors
- 👤 Bruce Aungst
- 👤 Robert C. DiLuccio
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 19:42
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/47; A61K31/485; A61K47/00; A61K47/06; A61K47/08; A61K47/10; A61K47/12; A61K47/30; A61K47/36; A61K47/38; A61K9/00; A61K9/0012; A61K9/0014; A61K9/70; A61K9/7023
Claims Analysis
Total Claims: 29
Claim 1
Independent Claim
83 words
A method of administering a therapeutic dose of an opioid to the systemic circulation of a mammal which comprises topically administering to the mammal an opioid-containing pharmaceutical composition, wherein the composition consists essentially of a therapeutically effective amount of an opioid or a pharmaceutically acceptable salt thereof; an effective penetration enhancing amount of at least one of a saturated fatty acid of 8-15 carbon atoms or of an unsaturated fatty acid of 8-18 carbon atoms; and propylene glycol as a suitable pharmaceutical carrier.
Claim 2
Independent Claim
83 words
A method of administering a therapeutic dose of an opioid to the systemic circulation of a mammal which comprises topically administering to the mammal an opioid-containing pharmaceutical composition, wherein the composition consists essentially of a therapeutically effective amount of an opioid or a pharmaceutically acceptable salt thereof; an effective penetration enhancing amount of at least one of a saturated fatty acid of 8-15 carbon atoms or of an unsaturated fatty acid of 8-18 carbon atoms; and propylene glycol as a suitable pharmaceutical carrier.
Claim 3
Dependent Claim
57 words
A method according to claim 1 wherein the opioid is a natural or synthetic opioid analgesic such as morphine, oxymorphone, fentanyl, meperidine, propoxyphene, or oxycodone; a natural or synthetic narcotic antagonist such as nalmefene, naloxone, or naltrexone; a natural or synthetic mixed opioid agonist/antagonist such as nalbuphine, butorphanol, buprenorphine or pentazocine; or a pharmaceutically acceptable salt thereof.
Claim 4
Dependent Claim
29 words
A method according to claim 2 wherein the saturated fatty acid has from 10 to 15 carbon atoms and the unsaturated fatty acid has 10 to 15 carbon atoms.
Claim 5
Dependent Claim
14 words
A method according to claim 3 wherein the fatty acid has 14 carbon atoms.
Claim 6
Dependent Claim
13 words
A method according to claim 4 wherein the fatty acid is myristic acid.
Claim 7
Dependent Claim
12 words
A method according to claim 5 wherein the vehicle is propylene glycol.
Claim 8
Dependent Claim
15 words
A method according to claim 3 wherein the composition is in lotion or cream form.
Claim 9
Dependent Claim
24 words
A method according to claim 7 wherein the composition comprises 1 to 15% opioid, 30 to 80% vehicle, and 1 to 45% fatty acid.
Claim 10
Dependent Claim
24 words
A method according to claim 7 wherein the composition comprises 5 to 15% opioid, 30 to 80% propylene glycol, 2 to 25% fatty acid.
Claim 11
Dependent Claim
23 words
A method according to claim 8 wherein the composition further comprises water as an emulsifying agent to provide a composition in emulsion form.
Claim 12
Dependent Claim
16 words
A method according to claim 10 wherein the composition contains from about 30 to 50% water.
Claim 13
Dependent Claim
32 words
A method according to claim 8 wherein the composition further comprises a polymeric substance to provide a composition in gel form, said polymeric substance selected from ethylcellulose, hydroxypropylcellulose or a mixture thereof.
Claim 14
Dependent Claim
17 words
A method according to claim 12 wherein the composition contains from about 20 to 30% polymeric substance.
Claim 15
Dependent Claim
77 words
A pharmaceutical composition effective in producing transdermal delivery of a therapeutically effective amount of an opioid to the systemic circulation of a mammal, the composition consisting essentially of a therapeutically effective amount of an opioid or a pharmaceutically acceptable salt thereof; an effective penetration enhancing amount of at least one of a saturated fatty acid of 8-15 carbon atoms or of an unsaturated fatty acid of 8-18 carbon atoms; and propylene glycol as a suitable pharmaceutical carrier.
Claim 16
Dependent Claim
77 words
A pharmaceutical composition effective in producing transdermal delivery of a therapeutically effective amount of an opioid to the systemic circulation of a mammal, the composition consisting essentially of a therapeutically effective amount of an opioid or a pharmaceutically acceptable salt thereof; an effective penetration enhancing amount of at least one of a saturated fatty acid of 8-15 carbon atoms or of an unsaturated fatty acid of 8-18 carbon atoms; and propylene glycol as a suitable pharmaceutical carrier.
Claim 17
Dependent Claim
57 words
A composition according to claim 14 wherein the opioid is a natural or synthetic opioid analgesic such as morphine, oxymorphone, fentanyl, meperidine, propoxyphene, or oxycodone; a natural or synthetic narcotic antagonist such as nalmefene, naloxone, or naltrexone; a natural or synthetic mixed opioid agonist/antagonist such as nalbuphine, butorphanol, buprenorphine or pentazocine; or a pharmaceutically acceptable salt thereof.
Claim 18
Dependent Claim
29 words
A composition according to claim 15 wherein the saturated fatty acid has from 10 to 15 carbon atoms and the unsaturated fatty acid has 10 to 15 carbon atoms.
Claim 19
Dependent Claim
14 words
A composition according to claim 16 wherein the fatty acid has 14 carbon atoms.
Claim 20
Dependent Claim
13 words
A composition according to claim 11 wherein the fatty acid is myristic acid.
Claim 21
Dependent Claim
12 words
A composition according to claim 10 wherein the vehicle is propylene glycol.
Claim 22
Dependent Claim
15 words
A composition according to claim 16 wherein the composition is in lotion or cream form.
Claim 23
Dependent Claim
28 words
A composition according to claim 11 which comprises 1 to 15% opioid, 30 to 80% vehicle, and 1 to 45% fatty acid, and the balance being an excipient.
Claim 24
Dependent Claim
28 words
A composition according to claim 21 which comprises 5 to 15% opioid, 30 to 80% propylene glycol, 2 to 25% fatty acid, and the balance being an excipient.
Claim 25
Dependent Claim
21 words
A composition according to claim 21 which further comprises water and an emulsifying agent to provide a composition in emulsion form.
Claim 26
Dependent Claim
14 words
A composition according to claim 23 which contains from about 30 to 50% water.
Claim 27
Dependent Claim
30 words
A composition according to claim 21 which further comprises a polymeric substance to provide a composition in gel form, said polymeric substance selected from ethylcellulose, hydroxypropylcellulose or a mixture thereof.
Claim 28
Dependent Claim
15 words
A composition according to claim 25 which contains from about 20 to 30% polymeric substance.
Claim 29
Dependent Claim
29 words
The composition of claim 22 which comprises about 10% oxymorphone, about 10% myristic acid, about 55% propylene glycol, and about 25% of ethylcellulose, hydroxypropylcellulose, or a combination of both.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1989-12-01 | 1990-06-02 | 1990-12-02 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1993-12-01 | 1994-06-02 | 1994-12-02 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1997-12-01 | 1998-06-02 | 1998-12-02 | $7700.00 | Window Closed / Lapsed |