US4806341A
Expired / Lapsed
US
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Transdermal absorption dosage unit for narcotic analgesics and antagonists and process for administration
Assignee: Rutgers, The State University of New Jersey
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Filing: 1986-09-03
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Granted: 1989-02-21
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Expires: 2006-09-03
Abstract
Abstract Transdermal absorption morphinan narcotic analgesic or antagonist pharmaceutical polymer matrix dosage units have been developed which comprise a backing layer and an adjoining layer of a solid polymer matrix in which minimum effective doses of morphinan narcotic analgesic or antagonist pharmaceuticals are microdispersed and transdermally supplied. A presently preferred analgesic is hydromoprhone. The dosage units use a biologically acceptable adhesive polymer means to adhere the dosage units to the subject to be treated. The polymer matrix has dispersed one or more skin permeation enhancers. The invention also provides a process for transdermal absorption of said pharmaceuticals in at least minimum dosage amounts.
Inventors
- 👤 Yie W. Chien
- 👤 Chin-Chih Chiang
- 👤 Kabuji Tojo
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 14:49
CPC Classifications
A; A61; A61F; A61F13/00; A61K; A61K9/00; A61K9/70; A61K9/7023; A61K9/703; A61K9/7038; A61K9/7046; A61K9/7069; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/47; A61K31/485; A61K9/7084; A61P; A61P25/00; A61P25/04
Claims Analysis
Total Claims: 26
Claim 1
Independent Claim
105 words
A transdermal morphinan narcotic analgesic or antagonist pharmaceutical polymer matrix dosage unit comprising: (a) a backing layer which is substantially impervious to said pharmaceutical to be delivered transdermally; and (b) a polymer matrix disc layer which is adhered to said backing layer and which has microdispersed therein effective dosage amounts of one or more pharmaceuticals selected from the group consisting of morphinan narcotic analgestic and antagonist pharmaceuticals, said polymer being bioacceptable and permitting said pharmaceuticals to be transmitted for transdermal absorption, said pharmaceuticals being stable in said polymer matrix and being transdermally absorbed simultaneously to provide at least minimum effective daily doses of said pharmaceuticals.
Claim 2
Dependent Claim
105 words
A transdermal morphinan narcotic analgesic or antagonist pharmaceutical polymer matrix dosage unit comprising: (a) a backing layer which is substantially impervious to said pharmaceutical to be delivered transdermally; and (b) a polymer matrix disc layer which is adhered to said backing layer and which has microdispersed therein effective dosage amounts of one or more pharmaceuticals selected from the group consisting of morphinan narcotic analgestic and antagonist pharmaceuticals, said polymer being bioacceptable and permitting said pharmaceuticals to be transmitted for transdermal absorption, said pharmaceuticals being stable in said polymer matrix and being transdermally absorbed simultaneously to provide at least minimum effective daily doses of said pharmaceuticals.
Claim 3
Dependent Claim
28 words
A transdermal polymer matrix dosage unit of claim 1 wherein said polymer matrix layer has dispersed therein an effective amount of one or more skin permeation enhancing agents.
Claim 4
Dependent Claim
17 words
A transdermal dosage unit of claim 1 wherein the polymer matrix is a silicon polymer or copolymer.
Claim 5
Dependent Claim
28 words
A transdermal polymer matrix dosage unit of claim 3 wherein the silicon polymer or copolymer is a methyl silicone polymer or copolymer or methylvinyl silicone polymer or copolymer.
Claim 6
Dependent Claim
49 words
A transdermal polymer matrix dosage unit of claim 1 wherein the polymer matrix disc layer is a crosslinked polysiloxane polymer of the following formula: ##STR6## wherein R is alkyl or alkoxy having 1-7 carbon atoms, vinyl, phenyl or combination thereof; and wherein n is about 100 to about 5,000.
Claim 7
Dependent Claim
30 words
A transdermal polymer matrix dosage unit of claim 3 wherein the matrix is made up of microdispersed compartments having a cross-sectional dimension of from about 10 to about 200 microns.
Claim 8
Dependent Claim
14 words
A transdermal polymer matrix dosage unit of claim 1 wherein the pharmaceutical is hydromorphone.
Claim 9
Dependent Claim
37 words
A transdermal polymer matrix dosage unit of claim 7 wherein the hydromorphone is present in the polymer matrix layer in a loading amount of at least about 10 percent by weight based on the matrix polymer weight.
Claim 10
Dependent Claim
35 words
A transdermal polymer matrix dosage unit of claim 7 wherein the hydromorphone is present in the polymer matrix layer in a loading amount of about 10 percent by weight based on the matrix polymer weight.
Claim 11
Dependent Claim
29 words
A transdermal polymer matrix dosage unit of claim 1 wherein an effective dosage of at least about 1.2 mg of said pharmaceutical is transdermally delivered in a 24-hour period.
Claim 12
Dependent Claim
14 words
A transdermal polymer matrix dosage unit of claim 10 wherein the pharmaceutical is hydromorphone.
Claim 13
Dependent Claim
27 words
A transdermal polymer matrix dosage unit of claim 11 wherein the hydromorphone is transdermally delivered in an amount of at least 2.4 mg in a 24-hour period.
Claim 14
Dependent Claim
37 words
A transdermal polymer matrix dosage unit of claim 3 wherein the silicone polymer is a cross-linked siloxane polymer and the pharmaceutical hydromorphone is transdermally delivered in an amount of at least 1.2 mg in a 24-hour period.
Claim 15
Dependent Claim
23 words
A transdermal polymer matrix dosage unit of claim 13 wherein the amount transdermally delivered is at least 2.4 mg in a 24-hour period.
Claim 16
Dependent Claim
16 words
A transdermal polymer matrix dosage unit of claim 13 wherein the cross-linked silicone polymer is polydimethylsiloxane.
Claim 17
Dependent Claim
20 words
A transdermal polymer matrix dosage unit of claim 13 wherein the cross-linked silicone polymer is a crosslinked methylvinyl silicone polymer.
Claim 18
Dependent Claim
96 words
A transdermal polymer matrix dosage unit of claim 13 wherein the skin permeation enhancing agent present in the matrix layer or adhesive layer or both layers and is selected from the group consisting of isopropyl myristate, saturated fatty acids having the structure CH 3 (CH 2 ) n COOH wherein n is an integer of 4 to 16, saturated alcohols having the structure CH 3 (CH 2 ) n CH 2 OH wherein n is an integer of 4 to 16, azone, ethyl caprylate, hexamethylene lauramide, hexamethylene palmitamide, and combinations of ethyl caprylate and capryl alcohol.
Claim 19
Dependent Claim
15 words
A transdermal dosage unit of claim 17 wherein the skin permeation enhancing agent is azone.
Claim 20
Dependent Claim
15 words
A transdermal dosage unit of claim 17 wherein the skin permeation agent is isopropyl myristate.
Claim 21
Dependent Claim
15 words
A transdermal dosage unit of claim 17 wherein the skin permeation agent is ethyl caprylate.
Claim 22
Dependent Claim
21 words
A transdermal dosage unit of claim 17 wherein the skin permeation agent is a combination of ethyl caprylate and capryl alcohol.
Claim 23
Dependent Claim
26 words
A process of administering an effective dose amount of a morphinan narcotic analgesic or antagonist pharmaceutical by applying a dosage unit as described in claim 1.
Claim 24
Dependent Claim
10 words
A process of claim 22 wherein the pharmaceutical is hydromorphone.
Claim 25
Dependent Claim
48 words
A dosage unit of claim 1 wherein the morphinan pharmaceutical is selected from the group consisting of hydromorphone, oxymorphone, buprenorphine, diprenorphine, butorphanol, levallorphan, nalorphine, naloxone, nalbuphine, oxilorphan, nalmexone, naltrexone, ketobemidone, apocodeine, profadol, cyclorphan, cyprenorphine, desomorphine, dihydromorphine, 3-hydroxy-N-methylmorphinan, levophenacylmorphinan, norlevorphanol, oxymorphone, phenomorphan, pholcodine, hydroxypethidine, apomorphine, codeine, morphine and hydrocodone.
Claim 26
Dependent Claim
25 words
A dosage unit of claim 22 wherein said polymer matrix layer has dispersed therein an effective amount of one or more skin permeation enhancing agents.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-02-21 | 1992-08-22 | 1993-02-21 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-02-21 | 1996-08-22 | 1997-02-21 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-02-21 | 2000-08-22 | 2001-02-21 | $7700.00 | Window Closed / Lapsed |