Systems for transdermal administration of medicaments

• US 5,324,521 A
• Filed: 08/18/1992
• Issued: 06/28/1994
• Est. Priority Date: 12/18/1989
• Status: Expired due to Term

• Current Assignee: Transdermal Biotechnology, Inc.
• Original Assignee: DermaMed s.r.o.
• Inventors: Rubinstein, Yosef, Gertner, Avi
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): BAWA, RAJ
• Application Number:
  US07/929,485
• Time in Patent Office: 679 Days
• Field of Search: 424/449, 424/447, 424/443, 424/444, 424/484, 604/304
• US Class Current: 424/449
• CPC Class Codes: A61D 9/00 Bandages, poultices, compresses specially adapted to veterinary purposes fetlock-joint protecting rings A01K13/00
• CPC Class Codes: A61K 9/70 Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug hollow drug-filled fibres A61K9/0092
• CPC Class Codes: A61K 9/703 characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches

Abstract

A non-adhesive matrix for use as a dosage form in the transdermal administration of a medicament to a mammal comprises a porous, non-adhesive, absorbent perforate solid support having absorbed thereon a mixture comprising a medicament adapted for transdermal administration and a pharmaceutically acceptable carrier for the medicament. The carrier consists essentially of at least one compound selected from esters of C_8-24 fatty acids, pharmaceutically acceptable aliphatic polyhydroxy compounds and non-volatile paraffins.

Claims

1. In a non-adhesive matrix for use as a dosage form in the transdermal administration of a medicament to a mammal which comprises a porous, non-adhesive, absorbent perforate solid support having absorbed thereon a mixture comprising a medicament adapted for transdermal administration and a pharmaceutically acceptable carrier for the medicament, the improvement being that the carrier consists essentially of at least one compound selected from the group consisting of esters of C_8-24 fatty acids with at least one aliphatic hydroxy compound containing 2-12 carbon atoms and 2-3 hydroxy groups;

and

the acid component of the ester is selected from the group consisting of caprylic, capric, lauric, palmic, stearic, arachidic, behenic, lignoceric, oleic, elaidic, petroselinic, linoleic, alpha-linolenic, gamma-linolenic, linolelaidic, arachidic, 11-eicosenoic, 11,14-eicosadienoic, 11,14,17-eicosatrienoic, 8,11,14-eicosatrienoic, arachidonic, 5,8,11,14,17-eicosapentaenoic, erucic and nervonic acids;

provided that when said hydroxy compound is glycerol the esters thereof are selected from diglycerides and triglycerides of at least one C_8-24 fatty acid,

whereby said medicament is detectable in the bloodstream within two hours after administration thereof.

2. A matrix according to claim 1, wherein the medicament comprises at least one member selected from the group consisting of growth promoters, fertility agents, micronutritional supplements, anti-inflammatory agents, anthelmintics, antibiotics and antiparasitics.

3. A matrix according to claim 1, which contains an additional medicament selected from antiinflammatory agents and antihistamines.

4. A matrix according to claim 1, wherein the medicament comprises at least one member selected from the group consisting of:

(a) fertility and growth promoting agents;

estradiol, flugestone acetate, medroxyprogesterone, medroxyprogesterone acetate, megestrol acetate, progesterone, proligestone, melengestrol acetate, testosterone, trenbulone, zeranol;

(b) anthelmintics;

albendazole, febantel, fenbendazole, flubendazole, ivermectin, levamisole, mebendazole, oxybendazole, oxfendazole, thiabendazole, tricalbendazole, pyrantel, morantel;

(c) antibiotics;

semisynthetic penicillins, tetracyclines and cephalosporins;

(d) antiparasitics;

cythioate, fenthion;

(e) antiinflammatory agents;

betamethazone, flumethazone, dexamethazone;

(f) micronutrients;

selenium disulfide, iron dextran.