Bandage for transdermally administering scopolamine to prevent nausea

• US 4,031,894 A
• Filed: 09/07/1976
• Issued: 06/28/1977
• Est. Priority Date: 12/08/1975
• Status: Expired due to Term

• Current Assignee: ALZA Corporation (Johnson & Johnson)
• Original Assignee: ALZA Corporation (Johnson & Johnson)
• Inventors: Urquhart, John, Chandrasekaran, Santosh Kumar, Shaw, Jane Elizabeth
• Primary Examiner(s): Medbery, Aldrich F.
• Application Number:
  US05/721,602
• Time in Patent Office: 294 Days
• Field of Search: 128/156, 128/260, 128/268, 128/296, 424/19, 424/20, 424/28, 424/267
• US Class Current: 424/448
• CPC Class Codes: A61F 13/00063 comprising medicaments or additives, e.g. odor control, PH control, debriding, antimicrobic drug delivery dressings A61K9/70; chemical aspect of the additives A61L15/00
• CPC Class Codes: A61F 13/534 having an inhomogeneous composition through the thickness of the pad A61F13/538, A61F13/539 take precedence; homogeneous cores with tissue wrapping A61F13/53
• CPC Class Codes: A61F 13/8405 Additives, e.g. for odour, disinfectant or pH control
• CPC Class Codes: A61F 2013/00902 containing means
• CPC Class Codes: A61F 2013/00919 for physical therapy, e.g. cold or magnetic
• CPC Class Codes: A61F 2013/53445 from several sheets
• CPC Class Codes: A61F 2013/8479 including electric or magnetic devices
• CPC Class Codes: A61K 31/46 8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
• CPC Class Codes: A61K 9/7053 obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
• CPC Class Codes: A61K 9/7092 Transdermal patches having multiple drug layers or reservoirs, e.g. for obtaining a specific release pattern, or for combining different drugs

Abstract

Method and therapeutic system in the form of a bandage that administer scopolamine base transdermally in an initial pulse of 10 to 200 μg/cm² of skin that quickly brings the concentration of scopolamine in the plasma to a level at which emesis and nausea are inhibited without intolerable side effects, followed by a substantially constant dosage in the range of 0.3 to 15 μg/hr that holds said level. The bandage is a four-layer laminate of, from the top: a protective backing; a gelled, mineral oil-polyisobutene-scopolamine reservoir lamina that is the source of the constant dosage; a microporous membrane that controls the constant dosage rate; and a gelled, mineral oil-polyisobutene-scopolamine adhesive layer that is the source of the pulse dose and the means by which the bandage is attached to the skin.

Claims

1. A therapeutic system in the form of a bandage for administering scopolamine base through unbroken skin to inhibit emesis and nausea for a prolonged time period comprising a sandwich-type laminate of:

(a) a backing lamina that is substantially impermeable to scopolamine base, one face of which forms the top of the bandage;

(b) a scopolamine base reservoir lamina adjacent the opposite face of the backing lamina comprising

i. (c) 0.2 to about 3 mg scopolamine base dispersed in a gelled mixture of

(ii) mineral oil of about 10 to about 100 cp at 25°

C., and polyisobutene;

(c) a microporous membrane lamina adjacent and below the scopolamine reservoir lamina through which the scopolamine base is released from the reservoir lamina after the bandage is affixed to the skin at a substantially constant rate in the range of about 0.3 to about 15 μ

g/hr; and

(d) a contact adhesive lamina adjacent and below the microporous membrane lamina by which said bandage is affixed to the skin comprising about 10 to about 200 μ

g scopolamine base per cm² effective surface area dispersed in a gelled mixture of said mineral oil and said polyisobutene.

2. The therapeutic system of claim 1 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 bandage before the bandage is affixed to the skin.

3. The therapeutic system of claim 1 wherein the effective surface area of the bandage is about 0.5 to 4 cm² .

4. The therapeutic system of claim 1 wherein the mineral oil constitutes 35% to 65% by weight of the mixture and the polyisobutene constitutes 35% to 65% by weight of the mixture.

5. The therapeutic system of claim 1 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.

6. The therapeutic system of claim 5 wherein the mineral oil constitutes 35% to 65% by weight of the mixture, the first polyisobutene constitutes 10% to 40% by weight of the mixture and the second polyisobutene constitutes 20% to 40% by weight of the mixture.

7. The therapeutic system of claim 1 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.

8. The therapeutic system of claim 7 wherein the microporous membrane lamina is made of polypropylene.

9. The therapeutic system of claim 8 wherein the effective surface area of the patch is about 0.5 to 4 cm² and the microporous membrane lamina is made of polypropylene.

10. The therapeutic system of claim 9 wherein the backing lamina is made of aluminized polyethylene terephthalate.

11. The therapeutic system of claim 1 wherein said substantially constant rate is in the range of 5 to 15 μ

g/hr and said contact adhesive lamina comprises about 50 to about 150 μ

g scopolamine base per cm² of effective surface area dispersed in a gelled mixture of said mineral oil and said polyisobutene.

12. The therapeutic system of claim 1 wherein said substantially constant rate is in the range of 3 to 10 μ

g/hr and said contact adhesive lamina comprises about 50 to about 150 μ

g scopolamine base per cm² of effective surface area dispersed in a gelled mixture of said mineral oil and said polyisobutene.