Compositions and method of controlling transdermal penetration of topical and systemic agents

• US 4,692,462 A
• Filed: 03/18/1985
• Issued: 09/08/1987
• Est. Priority Date: 03/18/1985
• Status: Expired due to Fees

• Current Assignee: Menley & James Laboratories Limited
• Original Assignee: Menley & James Laboratories Limited
• Inventors: Banerjee, Pradip K.
• Primary Examiner(s): Rose, Shep K.
• Application Number:
  US06/713,068
• Time in Patent Office: 904 Days
• Field of Search: 424/28, 424/79, 514/449
• US Class Current: 424/444
• CPC Class Codes: A61K 47/585 Ion exchange resins, e.g. polystyrene sulfonic acid resin
• 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

Compositions and methods useful for improved and controlled transdermal and transmembrane drug delivery of topical and systemic agents. The compositions and methods comprise a pharmacologically active drug together with a non-toxic pharmaceutically acceptable ion exchange resin, and a salt in a gel-forming vehicle and topically administering to human or animal skin or other membranes the resulting compositions. If desired, a penetration enhancer may also be employed in the compositions of this invention.

Claims

1. A pharmaceutical composition for the controlled transdermal delivery of one or more pharmacologically active systemic drugs comprising a safe and effective amount of a systemic drug-ion exchange resin complex and a salt effective to control the drug release note, containing the appropriate counter ion for the ion-exchange resin, selected from the group consisting of sodium chloride, monobasic sodium phosphate, dibasic sodium phosphate, zinc sulfate, magnesium chloride, calcium chloride, potassium chloride, sodium sulfate, sodium acetate, magnesium acetate and sodium citrate in a gel-forming vehicle.

2. The composition of claim 1 wherein the drug is pseudoephedrine.

3. The composition of claim 1 wherein the ion exchange complex contains the systemic drugs pseudoephedrine and chlorpheniramine.

4. The composition of claim 1 wherein the ion exchange resin is a carboxylic acid resin.

5. The composition of claim 4 wherein the salt is sodium chloride.

6. The composition of claim 1 in which the gel-forming vehicle comprises the gel-forming substances selected from the group consisting of gelatin, hydroxypropyl methylcellulose, polvvinylpyrrolidone and a quaternary nitrogen containing cellulose ether mixed with water.

7. A method for controlling the transdermal penetration of one or more non-toxic pharmacologically active systemic drugs to a patient which comprises applying to said patient a composition comprising a systemic drug-ion exchange resin complex and a salt effective to control the drug release note, containing the appropriate counter ion for the ion-exchange resin, selected from the group consisting of sodium chloride, monobasic sodium phosphate, dibasic sodium phosphate, zinc sulfate, magnesium chloride, calcium chloride, potassium chloride, sodium sulfate, sodium acetate, magnesium acetate and sodium citrate in a gel-forming vehicle.

8. The method of claim 7 wherein the ion exchange complex contains the systemic drugs pseudoephedrine and chlorpheniramine.

9. In a device for use in the controlled transdermal delivery of pharmacologically active systemic drugs provided with a cavity having an inert backing member which is impermeable to said systemic drugs, the improvement comprising said cavity containing a composition comprising a systemic drug-ion exchange resin complex and a salt effective to control the drug release note, containing the appropriate counter ion for the ion-exchange resin, selected from the group consisting of sodium chloride, monobasic sodium phosphate, dibasic sodium phosphate, zinc sulfate, magnesium chloride, calcium chloride, potassium chloride, sodium sulfate, sodium acetate, magnesium acetate and sodium citrate in a gel-forming vehicle.

10. A device for use in the controlled transdermal administration of pharmacologically active systemic drugs comprising a cavity, a backing member impermeable to said systemic drugs surrounding said cavity, an adhesive layer on said backing member, said cavity containing a composition comprising a systemic drug ion exchange resin complex and a salt effective to control the drug release note, containing the appropriate counter ion for the ion-exchange resin, selected from the group consisting of sodium chloride, monobasic sodium phosphate, dibasic sodium phosphate, zinc sulfate, magnesium chloride, calcium chloride, potassium chloride, sodium sulfate, sodium acetate, magnesium acetate and sodium citrate in a gel forming vehicle which provides a controlled rate of systemic drug release.

11. The device of claim 10 in which the backing member is a plastic film.