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Claims for Patent: 4,201,211

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Claims for Patent: 4,201,211

Title: Therapeutic system for administering clonidine transdermally
Abstract:Therapeutic system in the form of a skin patch that administers clonidine transdermally in an initial priming dose of 10 to 300 mcg/cm.sup.2 of skin that brings the concentration of clonidine in the blood to a level sufficient to elicit alpha-adrenergic stimulation without intolerable side effects, followed by a substantially constant continuous dosage in the range of 0.1 to 100 mcg/hr that maintains said level. The system is a four-layer laminate of, from the top: a protective backing; a gelled, mineral oil-polyisobutene-clonidine reservoir lamina that is the source of the clonidine for the continuous constant dosage; a microporous membrane that controls the constant dosage rate; and a gelled, mineral oil-polyisobutene-clonidine contact adhesive layer that is the source of the clonidine for the priming dose and the means by which the system is attached to the skin.
Inventor(s): Chandrasekaran; Santosh K. (Palo Alto, CA), Darda; Siegfried (Ingelheim am Rhein, DE), Michaels; Alan S. (Atherton, CA), Cleary; Gary W. (Palo Alto, CA)
Assignee: ALZA Corporation (Palo Alto, CA) Boehringer Ingelheim GmbH (Ingelheim am Rhein, DE)
Application Number:05/815,033
Patent Claims: 1. A therapeutic system in the form of a skin patch for administering clonidine continuously and transdermally through a predetermined area of unbroken skin in a controlled manner for a prolonged time period to effect central alpha-adrenergic stimulation comprising:

(a) a backing that is substantially impermeable to clonidine, one face of which forms the top of the patch;

(b) a clonidine reservoir adjacent the opposite face of the backing that contains an amount of clonidine sufficient to provide clonidine for said prolonged time period at a central alpha-adrenergic stimulating rate;

(c) means for releasing clonidine from the reservoir at said rate to said predetermined area of skin; and

(d) means for affixing the patch to said predetermined area of skin.

2. The therapeutic system of claim 1 wherein the central alpha-adrenergic stimulating rate is one that provides hypertension therapy.

3. A therapeutic system in the form of a skin patch for administering 2,6-dichloro-N-2-imidazolidinylidene benzeneamine continuously and transdermally through a predetermined area of unbroken skin in a controlled manner for a prolonged time period to effect central alpha-adrenergic stimulation comprising a sandwich-type laminate of:

(a) a backing lamina that is substantially impermeable to the benzeneamine, one face of which forms the top of the patch;

(b) a benzeneamine reservoir lamina adjacent the opposite face of the backing lamina comprising:

(i) an amount of said benzeneamine at least equal to that required to provide said benzeneamine for said prolonged time period at a central alpha-adrenergic stimulating rate, dispersed in

(ii) a carrier that is permeable to said benzeneamine;

(c) a microporous membrane lamina adjacent and below the benzeneamine reservoir lamina through which the benzeneamine is released from the reservoir lamina at said rate after the skin patch is affixed to the skin; and

(d) a contact adhesive lamina adjacent and below the microporous membrane lamina by which the patch is affixed to the skin comprising:

(i) a contact adhesive that is permeable to the benzeneamine; and

(ii) an amount of benzeneamine that constitutes at least a substantial portion of the quantity of the benzeneamine that is immobilized by said predetermined area of skin.

4. The therapeutic system of claim 3 wherein the rate is one that provides hypertension therapy.

5. The therapeutic system of claim 4 wherein said rate is in the range of 0.1 to 100 mcg/hr and said amount of benzeneamine in said contact adhesive lamina is 10 to 300 mcg/cm.sup.2 of said predetermined area of skin.

6. The therapeutic system of claim 4 wherein said rate is in the range of 0.2 to 70 mcg/hr and said amount of benzeneamine in the contact adhesive lamina is 150 to 250 mcg/cm.sup.2 of said predetermined area of skin.

7. The therapeutic system of claim 4 including:

(e) a strippable coating lamina adjacent and below the contact adhesive lamina that is substantially impermeable to the components of the contact adhesive lamina and is adapted to be stripped off the patch before the patch is affixed to the skin.

8. The therapeutic system of claim 4 wherein the carrier and the contact adhesive comprise a gelled mixture of mineral oil of about 10 to about 100 cp at 25.degree. C. and polyisobutene.

9. The therapeutic system of claim 8 wherein the polyisobutene is a blend of a first polyisobutene having a viscosity average molecular weight of 35,000 to 50,000 and a second polyisobutene having a viscosity average molecular weight of 1,000,000 to 1,500,000.

10. The therapeutic system of claim 9 wherein the mineral oil constitutes 35% to 65% by weight of the gelled mixture, the first polyisobutene constitutes 10% to 40% by weight of the gelled mixture and the second polyisobutene constitutes 10% to 40% by weight of the gelled mixture.

11. The therapeutic system of claim 4 wherein the microporous membrane lamina has a porosity of about 0.1 to 0.85, a tortuosity of about 1 to 10 and a thickness of about 10.sup.-3 to 10.sup.-2 cm.

12. The therapeutic system of claim 11 wherein the microporous membrane lamina is made of polypropylene.

13. The therapeutic system of claim 12 wherein the backing layer is made of aluminized polyethylene terephthalate.

14. The therapeutic system of claim 4 including:

(e) a strippable coating lamina adjacent and below the contact adhesive lamina that is substantially impermeable to the components of the contact adhesive lamina and is adapted to be stripped off the patch before the patch is affixed to the skin, and wherein said rate is in the range of 0.2 to 70 mcg/hr, the amount of the benzeneamine in the contact adhesive lamina is 150 to 250 mcg/cm.sup.2 of skin, the particle size of the undissolved benzeneamine present in the reservoir lamina and contact adhesive lamina being in the range of about 5 to 20 microns, the carrier comprises a gelled mixture of 35% to 65% by weight mineral oil of about 10 to about 100 cp at 25.degree. C., 10% to 40% by weight polyisobutene having a viscosity average molecular weight of 35,000 to 50,000, and 10% to 40% by weight polyisobutene having a viscosity average molecular weight of 1,000,000 to 1,500,000, the contact adhesive is made of said gelled mixture, the microporous membrane lamina is made of polypropylene, and the backing layer is made of aluminized polyethylene terephthalate.
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