Molecular transdermal transport system

• US 5,853,751 A
• Filed: 06/09/1997
• Issued: 12/29/1998
• Est. Priority Date: 06/23/1993
• Status: Expired due to Term

• Current Assignee: BioChemics, Inc.
• Original Assignee: John J. Masiz
• Inventors: Masiz, John J.
• Primary Examiner(s): BROUILLETTE, D GABRIELLE
• Application Number:
  US08/871,156
• Time in Patent Office: 568 Days
• Field of Search: 424/449, 424/448, 514/946, 514/947
• US Class Current: 424/449
• CPC Class Codes: A61K 47/44 Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14
• 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 9/7023 Transdermal patches and similar drug-containing composite devices, e.g. cataplasms galenical aspects of iontophoretic devices A61K9/0009; microneedle arrays A61K9/0021; buccal patches A61K9/006

Abstract

An efficient transdermal delivery system for delivering an active ingredient to the blood supply of a living body, comprising a vasodilator, an active ingredient, a permeation enhancer for the active ingredient, and a water soluble gum for binding the foregoing. A non-breathable layer also can be used for controlling the microenvironment at the transport site. Compression can be used to further enhance the blood supply at the transport site.

Claims

1. A transdermal delivery system for delivering an active ingredient through the skin of a living body, comprising:

a. an active ingredient;

b. a vasodilator;

c. first means for enhancing the permeation of said active ingredient through said skin; and

d. second means for binding said active ingredient and said vasodilator and first means into a singular transport vehicle, said second means releasing said active ingredient upon contact with a bodily fluid having a non-neutral pH.

2. The transdermal delivery system of claim 1, wherein said first means for enhancing the permeation comprises a vegetable oil.

3. The transdermal delivery system of claim 1, wherein said first means is selected from the group consisting of peanut oil, olive oil, sunflower oil, soybean oil, monoi oil, macadamia oil and a vegetable oil/alcohol mix.

4. The transdermal delivery system of claim 1, wherein said second means comprises a water-soluble gum.

5. The transdermal delivery system of claim 2, wherein said second means comprises a water-soluble gum.

6. The transdermal delivery system of claim 3, wherein said second means comprises a water-soluble gum.

7. The transdermal delivery system of claim 4, wherein said water-soluble gum is selected from the group consisting of agar, arabic, carob, CMC, carrageenans, ghatti, guar, karaya, kadaya, locust bean, tragacanth and xanthan gum.

8. The transdermal delivery system of claim 5, wherein said water-soluble gum is selected from the group consisting of agar, arabic, carob, CMC, carrageenans, ghatti, guar, karaya, kadaya, locust bean, tragacanth and xanthan gum.

9. The transdermal delivery system of claim 6, wherein said water-soluble gum is selected from the group consisting of agar, arabic, carob, CMC, carrageenans, ghatti, guar, karaya, kadaya, locust bean, tragacanth and xanthan gum.

10. The transdermal delivery system of claim 1, further comprising means for controlling the temperature and humidity at the site of transport of said active ingredient through said skin.

11. The transdermal delivery system of claim 10, wherein said means for controlling the temperature and humidity comprises a non-breathable layer.

12. The transdermal delivery system of claim 1, wherein said non-neutral medium is selected from the group consisting of blood, interstitial fluid, sweat, saliva, mucoid secretions, lymphatic fluid, sinovial fluid, endolymph, perilymph, synaptic fluid, intersynaptic fluid, and spinal fluid.

13. A method of delivering an active ingredient through the skin of a living body, comprising:

a. placing the active ingredient on the skin at a transport site;

b. enhancing the blood supply to the site of transport of said active ingredient through said skin by applying a vasodiloator to said site;

c. enhancing the permeation of said active ingredient through said skin by binding said active ingredient to a carrier with a water-soluble gum; and

d. allowing said active ingredient to be released from said carrier upon contact with a bodily fluid having a non-neutral pH.

14. The method of claim 13, further comprising controlling the temperature and humidity at said transport site.

15. The method of claim 14, wherein said temperature and humidity are controlled by covering said transport site with a non-breathable material.

16. The method of claim 13, wherein said non-neutral medium is selected from the group consisting of blood, interstitial fluid, sweat, saliva, mucoid secretions, lymphatic fluid, sinovial fluid, endolymph, perilymph, synaptic fluid, intersynaptic fluid, and spinal fluid.