Iontophoretic administration of drugs

• US 5,383,848 A
• Filed: 04/04/1991
• Issued: 01/24/1995
• Est. Priority Date: 04/12/1990
• Status: Expired due to Fees

• Current Assignee: Gensia Pharmaceuticals, Inc. (Teva Pharmaceutical Industries Limited)
• Original Assignee: Gensia Inc (Teva Pharmaceutical Industries Limited)
• Inventors: Pawelchak, John M., Hillman, Robert S.
• Primary Examiner(s): Yasko, John D.
• Assistant Examiner(s): Rafa, Michael
• Application Number:
  US07/680,577
• Time in Patent Office: 1,391 Days
• Field of Search: 128/798, 128/802, 128/803, 128/898, 604/20, 607/149-153
• US Class Current: 604/20
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/415 1,2-Diazoles
• CPC Class Codes: A61K 31/455 Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
• CPC Class Codes: A61K 31/60 Salicylic acid; Derivatives thereof
• CPC Class Codes: A61K 31/621 having the hydroxy group in position 2 esterified, e.g. benorylate
• CPC Class Codes: A61K 36/81 Solanaceae (Potato family), e.g. tobacco, nightshade, tomato, belladonna, capsicum or jimsonweed
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 9/0009 involving or responsive to electricity, magnetism or acoustic waves; Galenical aspects of sonophoresis, iontophoresis, electroporation or electroosmosis microelectromechanical systems A61K9/0097

Abstract

Methods, formulations, and a system for improved iontophoretic administration of a drug, by, preferably, topical administration of a formulation containing an active vasodilator, rubefacient, or counterirritant agent such as capsaicin on the skin at the electrode site, or, iontophoretic administration of a vasodilator formulation or alpha blocker prior to iontophoretic administration of the drug.

Claims

1. An improved method of iontophoretic administration of a drug to a subject comprising the steps of:

selecting a site on the subject'"'"'s skin for iontophoretic administration of the drug;

administering a formulation capable of increasing blood flow to the subject'"'"'s skin near the site and prior to iontophoretic administration of the drug;

allowing sufficient time to pass for the formulation to effect increased flow of blood in the skin near the site on the subject'"'"'s skin; and

iontophoretically administering the drug to the subject at the site;

wherein said formulation includes from about 0.1 to about 5% methyl nicotinate and from about 0.02% to about 0.3% capsaicin in a vehicle of which comprises a short chain aliphatic alcohol, light mineral oil or propylene glycol and methyl salicylate, in a ratio which comprises about 2 to about 6 parts alcohol and about 1 to about 4 parts mineral oil or propylene glycol per part methyl salicylate.

2. A method according to claim 1 wherein said vehicle comprises 2.9 parts ethyl alcohol and 2.0 parts propylene glycol per part methyl salicylate.

3. The method according to claim 2 wherein said formulation comprises about 0.27% (w/w) methyl nicotinate and about 0.028% capsaicin.

4. A method according to claim 1 wherein said vehicle comprises 2.9 parts isopropyl alcohol and 2.0 parts mineral oil per part methyl salicylate.

5. The method according to claim 4 wherein said formulation comprises 0.27% (w/w) methyl nicotinate and 0.028% capsaicin.

6. An improved method of iontophoretic administration of a drug to a subject comprising the steps of:

selecting a site on the subject'"'"'s skin for iontophoretic administration of the drug;

administering a formulation capable of increasing blood flow to the subject'"'"'s skin near the site and prior to iontophoretic administration of the drug;

allowing sufficient time to pass for the formulation to effect increased flow of blood in the skin near the side on the subject'"'"'s skin; and

iontophoretically administering the drug to the subject at the site;

wherein said formulation contains methyl salicylate, 17.5%;

histamine dihydrochloride, 0.02%;

methyl ester of nicotinic acid, 0.27%; and

capsicum oleoresin, 0.24% in an isopropyl alcohol and water vehicle.

7. An improved method of iontophoretic administration of a drug to a subject comprising the steps of:

selecting a site on the subject'"'"'s skin for iontophoretic administration of the drug;

administering a formulation capable of increasing blood flow to the subject'"'"'s skin near the site and prior to iontophoretic administration of the drug;

allowing sufficient time to pass for the formulation to effect increased flow of blood in the skin near the side on the subject'"'"'s skin; and

iontophoretically administering the drug to the subject at the site;

wherein said formulation contains methyl salicylate, 15%;

capsaicin, 0.025%; and

camphor, 3.6% in 70% alcohol with acetone.

8. An improved method of iontophoretic administration of a drug to a subject comprising the steps of:

selecting a site on the subject'"'"'s skin for iontophoretic administration of the drug;

administering a formulation capable of increasing blood flow to the subject'"'"'s skin near the site and prior to iontophoretic administration of the drug;

allowing sufficient time to pass for the formulation to effect increased flow of blood in the skin near the side on the subject'"'"'s skin; and

iontophoretically administering the drug to the subject at the site;

wherein said formulation includes 0.24% capsaicin and 0.27% methyl nicotinate by weight.