Skin permeation enhancer compositions using glycerol monolinoleate

• US 5,641,504 A
• Filed: 10/21/1993
• Issued: 06/24/1997
• Est. Priority Date: 06/09/1988
• Status: Expired due to Term

• Current Assignee: ALZA Corporation (Johnson & Johnson)
• Original Assignee: ALZA Corporation (Johnson & Johnson)
• Inventors: Lee, Eun Soo, Yum, Su Il, Nedberge, Diane E.
• Primary Examiner(s): BROUILLETTE, D GABRIELLE
• Application Number:
  US08/162,026
• Time in Patent Office: 1,342 Days
• Field of Search: 424/449, 424/447, 514/946, 514/947
• US Class Current: 424/447
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• CPC Class Codes: A61K 9/0014 Skin, i.e. galenical aspects of topical compositions non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00
• CPC Class Codes: A61K 9/1274 Non-vesicle bilayer structures, e.g. liquid crystals, tubules, cubic phases, cochleates; Sponge phases
• 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 9/7084 Transdermal patches having a drug layer or reservoir, and one or more separate drug-free skin-adhesive layers, e.g. between drug reservoir and skin, or surrounding the drug reservoir; Liquid-filled reservoir patches

Abstract

The present invention provides compositions and systems for the transdermal administration of a drug together with glycerol monolinoleate as a permeation enhancer. An example of a delivery system of the invention is a system (20) having a drug reservoir (22) containing together a drug to be delivered and glycerol monolinoleate permeation enhancer. Reservoir is sandwiched between a backing layer (24) and an in-line contact adhesive layer (28).

Claims

1. A non-aqueous composition of matter for the transdermal application to a body surface or membrane of at least one drug, at a therapeutically effective rate, the composition comprising, in combination, a therapeutically effective amount of at least one drug and a permeation-enhancing amount of glycerol monolinoleate.

2. A composition according to claim 1 further comprising a carrier having the drug and glycerol monolinoleate dispersed throughout.

3. A composition according to claim 1 wherein the body surface or membrane is intact skin.

4. A composition according to claim 1 which further comprises ethanol, in a permeation-enhancing amount.

5. A delivery system for the transdermal application to a body surface or membrane of at least one drug, at a therapeutically effective rate, the therapeutic system comprising a non-aqueous composition which comprises a permeation-enhancing amount of glycerol monolinoleate and a therapeutically effective amount of drug in a matrix or carrier.

6. A system according to claim 5 wherein the composition comprises 0.01-20 wt percent drug and 0.01-70 wt percent glycerol monolinoleate.

7. A system according to claim 5 further comprising:

a backing behind the skin distal surface of the composition; and

means for maintaining the composition in drug- and glycerol monolinoleate-transmitting relationship to the body surface or membrane.

8. A system according to claim 5 wherein the composition further comprises a permeation-enhancing amount of ethanol.

9. A system according to claim 5 wherein the body surface or membrane is skin.

10. A system according to claim 5, 6 or 7 wherein the matrix comprises ethylene vinyl acetate copolymer having from about 9 to 60% vinyl acetate.

11. A system according to claim 7 wherein the means for maintaining the composition in relation with the skin comprises an in-line adhesive layer on the skin-proximal surface of the reservoir.

12. A delivery system for the transdermal application to a body surface or membrane of at least one drug at a therapeutically effective rate, the therapeutic system comprising a non-aqueous composition which comprises a permeation-enhancing amount of glycerol monolinoleate and ethanol in combination and a therapeutically effective amount of a drug in a matrix or carrier.

13. A system according to claim 12 further comprising;

a backing behind the skin distal surface of the composition; and

means for maintaining the composition in drug- and glycerol monolinoleate-transmitting relationship to the body surface or membrane.