Subsaturated transdermal therapeutic system having improved release characteristics
First Claim
1. A method of producing a therapeutic effect which comprises placing a source of benztropine comprising a benztropine base permeable material having benztropine dissolved therein in benztropine transmitting relationship to an area of intact human skin and administering benztropine to the human subject from said source through said area of intact skin for an extended period of time at a therapeutically effective rate of approximately 10-40 μ
- g/hr for a substantial portion of said extended period of time.
1 Assignment
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Accused Products
Abstract
Rate-controlled transdermal delivery devices are disclosed which utilize an in-line adhesive to maintain the device on the skin and deliver an agent which is a solvent for the in-line adhesive. The initial equilibrated concentration of the agent in the agent reservoir and the adhesive is below saturation and the reservoir comprises the agent dissolved in a solvent with respect to which the rate controlling element of the device is substantially impermeable. In preferred embodiments the initial loading of the agent in reservoir is sufficient to prevent the activity of the agent in the reservoir from decreasing by more than about 50% and preferrably no more than about 25% during the predetermined period of administration; and the thicknesses of the adhesive, rate controlling membrane and reservoir layers are selected so that at least 50% and, preferrably at least 75% initial equilibrated agent loading is in the reservoir layer. The devices are usable to delivery oily non-polar agents which are liquid at body temperatures such as benztropine and secoverine.
183 Citations
29 Claims
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1. A method of producing a therapeutic effect which comprises placing a source of benztropine comprising a benztropine base permeable material having benztropine dissolved therein in benztropine transmitting relationship to an area of intact human skin and administering benztropine to the human subject from said source through said area of intact skin for an extended period of time at a therapeutically effective rate of approximately 10-40 μ
- g/hr for a substantial portion of said extended period of time.
- View Dependent Claims (2)
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3. A method for producing a therapeutic effect which comprises placing a source of dexsecoverine comprising a dexsecoverine permeable material having dexsecoverine dissolved therein in dexsecoverine transmitting relationship to an area of intact human skin and administering dexsecoverine to the human subject from such source through said area of intact skin for an extended period of time at a therapeutically effective rate of approximately 10-40 μ
- g/hr for a substantial portion of said extended period of time.
- View Dependent Claims (4, 5, 6)
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7. A medical device for the transdermal administration of dexsecoverine utilizing an in-line adhesive that is soluble in dexsecoverine, said device being adapted to deliver dexsecoverine at an antispasmolydically effective rate during a substantial portion of a predetermined administration period comprising, in combination:
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a. a dexsecoverine reservoir comprising dexsecoverine dissolved in an ethylene/vinyl acetate copolymer at a concentration less than saturation and at an initial dexsecoverine loading sufficient to prevent the thermodynamic activity of dexsecoverine in said ethylene/vinylacetate copolymer from decreasing by more than 50% during said administration period; b. dexsecoverine release rate controlling means disposed in the path of dexsecoverine migration from said reservoir to the skin, said rate controlling means being permeable to dexsecoverine and substantially impermeable to said solvent and being selected from the group consisting of polyethylene and ethylene/vinylacetate copolymers; and c. adhesive means disposed in the path of dexsecoverine migration from said release rate controlling means to the skin, said adhesive being soluble in dexsecoverine. - View Dependent Claims (8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19)
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20. A medical device for the transdermal administration of benztropine utilizing an in-line adhesive that is soluble in benztropine, said device being adapted to deliver benztropine at an anticholinergically effective rate during a substantial portion of a predetermined administration period comprising, in combination:
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a. a benztropine reservoir comprising benztropine dissolved in an ethylene/vinyl acetate copolymer at a concentration less than saturation and at an initial equilibrated benztropine loading sufficient to prevent the thermodynamic activity of benztropine in said ethylene/vinylacetate copolymer from decreasing by more than 50% during said administration period; b. benztropine release rate controlling means disposed in the path of benztropine migration from said reservoir to the skin, said rate controlling means being permeable to benztropine and substantially impermeable to said solvent and being selected from the group consisting of polyethylene and ethylene/vinylacetate copolymers; and c. adhesive means disposed in the path of benztropine migration from said release rate controlling means to the skin, said adhesive being soluble in benztropine. - View Dependent Claims (21, 22, 23, 24, 25, 26, 27, 28, 29)
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Specification