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EP0272987A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Resilient transdermal drug-delivery device and compositions and devices employing fatty acid esters/ethers or alkanediols as percutaneous absorption enhancers

Assignee: Janssen Pharmaceuticals Inc
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Filing: 1987-12-21
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Granted: —
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Expires: 2007-12-21
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Abstract

Abstract A solid state, resilient laminated composite for administering estradiol transdermally consisting of a multiplicity of spaced structural laminas (12, 14, 16) of a resilient elastomer, one of which (12) forms the top of the composite, a viscoelastic hydrophobic poly­mer lamina (13, 15) containing propylene glycol monolau­rate interposed between each structural lamina (12, 14, 16) and a pressure-sensitive adhesive lamina (17) that provides the basal surface of the composite and consists of a blend of a pressure-sensitive adhesive, estradiol, and propylene glycol monolaurate.

Inventors

  • 👤 Gary W. Cleary

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-05 06:21
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/70; A61K9/7023; A61K9/703; A61K31/00; A61K31/33; A61K31/395; A61K31/435; A61K31/44; A61K31/445; A61K47/00; A61K47/06; A61K47/08; A61K47/14; A61K9/0012; A61K9/0014; A61K9/7038; A61K9/7046; A61K9/7053; A61K9/7061; A61K9/7069

Claims Analysis

Total Claims: 30
Claim 1
Independent Claim 294 words
A transdermal drug-delivery device in the form of a solid state laminated composite adapted to be adhered to a predetermined area of unbroken skin and having mechanical properties that enable it to expand and contract in concert with the normal expansion and contraction of said area of skin comprising : (a) at least two spaced structural laminas (12, 14, 16) of a resilient polymer, one of which (12) forms the upper face surface of the composite, said laminas providing the composite with said mechanical properties; (b) at least one lamina (13, 15) of a viscoelastic hydrophobic polymer optionally in which (i) a drug and/­or (ii) an agent that enhances the solubility of the drug in the viscoelastic hydrophobic polymer and/or is a percutaneous absorption enhancer that increases the permeability of the skin to the drug is dispersed and at least partly dissolved, the viscoelastic hydrophobic polymer lamina (13, 15) being positioned between the structural laminas (12, 14, 16) with the structural lami­na(s) (14, 16) underlying the viscoelastic hydrophobic polymer lamina(s) (13, 15) providing no rate-controlling barrier to diffusion of drug and/or agent from the visco­elastic hydrophobic polymer lamina(s) to the skin; and (c) a lamina (17) of a pharmaceutically acceptable pressure-sensitive adhesive optionally in which (i) said drug and/or (ii) said agent is dispersed and at least partly dissolved, one face of the pressure-sensitive ad­hesive lamina (17) defining the basal surface of the composite and contacting and adhering to the area of un­broken skin when the device is in use, said pressure-­sensitive adhesive lamina (17) providing no rate-control­ling barrier to duffision of the drug and/or agent from device to the skin, with the proviso that at least one of said viscoelastic hydrophobic polymer lamina(s) (13,15) and said pressure-sensitive adhesive lamina (17) contains the drug.
Claim 2
Dependent Claim 294 words
A transdermal drug-delivery device in the form of a solid state laminated composite adapted to be adhered to a predetermined area of unbroken skin and having mechanical properties that enable it to expand and contract in concert with the normal expansion and contraction of said area of skin comprising : (a) at least two spaced structural laminas (12, 14, 16) of a resilient polymer, one of which (12) forms the upper face surface of the composite, said laminas providing the composite with said mechanical properties; (b) at least one lamina (13, 15) of a viscoelastic hydrophobic polymer optionally in which (i) a drug and/­or (ii) an agent that enhances the solubility of the drug in the viscoelastic hydrophobic polymer and/or is a percutaneous absorption enhancer that increases the permeability of the skin to the drug is dispersed and at least partly dissolved, the viscoelastic hydrophobic polymer lamina (13, 15) being positioned between the structural laminas (12, 14, 16) with the structural lami­na(s) (14, 16) underlying the viscoelastic hydrophobic polymer lamina(s) (13, 15) providing no rate-controlling barrier to diffusion of drug and/or agent from the visco­elastic hydrophobic polymer lamina(s) to the skin; and (c) a lamina (17) of a pharmaceutically acceptable pressure-sensitive adhesive optionally in which (i) said drug and/or (ii) said agent is dispersed and at least partly dissolved, one face of the pressure-sensitive ad­hesive lamina (17) defining the basal surface of the composite and contacting and adhering to the area of un­broken skin when the device is in use, said pressure-­sensitive adhesive lamina (17) providing no rate-control­ling barrier to duffision of the drug and/or agent from device to the skin, with the proviso that at least one of said viscoelastic hydrophobic polymer lamina(s) (13,15) and said pressure-sensitive adhesive lamina (17) contains the drug.
Claim 3
Dependent Claim 28 words
The device of claim 1 wherein at least one of said lamina(s) (13,15) of viscoelastic hydrophobic po­lymer and said lamina of pharmaceutically acceptable pres­sure-sensitive adhesive contains said agent.
Claim 4
Dependent Claim 34 words
The transdermal drug delivery device of claim 1 or 2 wherein the device is a sufficient barrier to wa­ter vapor transmission that said area of skin becomes hy­drated when the device is placed thereon.
Claim 5
Dependent Claim 18 words
The device of claim 3 wherein said viscoelas­tic hydrophobic polymer lamina(s) provide(s) said barrier to water vapor transmission.
Claim 6
Dependent Claim 13 words
The device of claim 3 or 4 wherein the drug is a steroid.
Claim 7
Dependent Claim 10 words
The device of claim 5 wherein the drug is estradiol.
Claim 8
Dependent Claim 16 words
The device of claim 3 or 4 wherein the drug is fentanyl or a fentanyl analog.
Claim 9
Dependent Claim 16 words
The transdermal drug delivery device of claim 1 or 2 wherein the device is not occlusive.
Claim 10
Dependent Claim 20 words
The transdermal drug delivery device of claim 8, wherein the water vapor transmission rate of the device is 11-18 g/m²-hr.
Claim 11
Independent Claim 57 words
The device of any of claims 1, 2, 3, 4, 5, 6, 7, 8 or 9 wherein the drug is contained in the lamina (17) of pharmaceutically acceptable pressure-­sensitive adhesive and said agent is contained in the lamina (17) of pharmaceutically acceptable pressure-­sensitive adhesive and at least one of the lamina(s) (13, 15) of viscoelastic hydrophobic polymer.
Claim 12
Dependent Claim 58 words
The transdermal drug-delivery device of any of claims 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 inclusive, wherein the agent is a fatty acid ester or fatty alcohol ether of a C₂ to C₄ alkanedoil where each fatty acid or fatty alcohor portion of the ester or ether is of 8 to 22 carbon atoms.
Claim 13
Dependent Claim 66 words
The transdermal drug-delivery device of claims wherein the drug is estradiol, fentanyl or a fentanyl analog and the agent is a fatty acid monoester of propyle­ne glucol in which the fatty acid portion is of 8 to 22 carbon atoms or a mixture of said monoester and a fatty acid diester of propylene glycol wherein each fatty acid portion is of 8 to 22 carbon atoms.
Claim 14
Dependent Claim 31 words
The transdermal drug-delivery device of claim 12 wherein the fatty acid monoester of propylene glycol is propylene glycol monolaurate and the fatty acid diester of propylene glycol is propylene glycol dilaurate.
Claim 15
Dependent Claim 58 words
A transdermal drug delivery device comprising a body that contains a drug and a percutaneous absorption enhancer, characterized in that percutaneous absorption enhancer is a fatty acid ester or fatty alcohol ether of a C₂ to C₄ alkanediol where each fatty acid or fatty alcohol portion of the ester or ether is of 8 to 22 carbon atoms.
Claim 16
Dependent Claim 58 words
A transdermal drug delivery device comprising a body that contains a drug and a percutaneous absorption enhancer, characterized in that percutaneous absorption enhancer is a fatty acid ester or fatty alcohol ether of a C₂ to C₄ alkanediol where each fatty acid or fatty alcohol portion of the ester or ether is of 8 to 22 carbon atoms.
Claim 17
Dependent Claim 14 words
The transdermal drug delivery device of claim 14 wherein the drug is a steroid.
Claim 18
Dependent Claim 13 words
The transdermal drug delivery device of claim 15 wherein the drug is estradiol.
Claim 19
Dependent Claim 17 words
The transdermal drug delivery device of claim 14 wherein the drug is fentanyl or a fentanyl analog.
Claim 20
Dependent Claim 18 words
The transdermal drug delivery device of claims 14, 15, 16 or 17 wherein the alkanediol is propylene glycol.
Claim 21
Dependent Claim 23 words
The transdermal drug delivery device of claim 18 wherein the fatty acid ester of propylene glycol is a monoester, diester or mixtures thereof.
Claim 22
Dependent Claim 19 words
The transdermal drug delivery device of claims 18 or 19 wherein each fatty acid portion contains 12 carbon atoms.
Claim 23
Dependent Claim 61 words
A pharmaceutical composition for administering a drug transdermally comprising a mixture of the drug and a percutaneous absorption enhancer characterized in that the percutaneous absorption enhancer is a fatty acid ester or fatty alcohol ether of a C₂ to C₄ alkanediol where each fatty acid or fatty alcohol portion of the ester or ether is of 8 to 22 carbon atoms.
Claim 24
Dependent Claim 61 words
A pharmaceutical composition for administering a drug transdermally comprising a mixture of the drug and a percutaneous absorption enhancer characterized in that the percutaneous absorption enhancer is a fatty acid ester or fatty alcohol ether of a C₂ to C₄ alkanediol where each fatty acid or fatty alcohol portion of the ester or ether is of 8 to 22 carbon atoms.
Claim 25
Dependent Claim 12 words
The pharmaceutical composition of claim 21 wherein the drug is a steroid.
Claim 26
Dependent Claim 11 words
The pharmaceutical composition of claim 18 wherein the drug is estradiol.
Claim 27
Dependent Claim 15 words
The pharmaceutical composition of claim 21 wherein the drug is fentanyl or a fentanyl analog.
Claim 28
Dependent Claim 16 words
The pharmaceutical composition of claims 21, 22, 23, or 24 wherein the alkanediol is propylene glycol.
Claim 29
Dependent Claim 21 words
The pharmaceutical composition of claim 25 wherein the fatty acid ester of propylene glycol is a monoester, diester or mixtures thereof.
Claim 30
Dependent Claim 17 words
The pharmaceutical composition of claims 25 or 26 wherein each fatty acid portion contains 12 carbon atoms.

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