Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Web – sheet or filament bases; compositions of bandages; or...
Patent
1993-10-21
1997-06-24
Phelan, D. Gabrielle
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Web, sheet or filament bases; compositions of bandages; or...
424449, 514946, 514947, A61L 1516
Patent
active
056415044
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
This invention relates to the transdermal delivery of drugs or other biologically active agents and more particularly to methods and compositions for enhancing the percutaneous absorption of drugs or other agents when incorporated in transdermal drug delivery systems or devices.
BACKGROUND OF THE INVENTION
The transdermal route of parenteral delivery of drugs provides many advantages, and transdermal systems for delivering a wide variety of drugs or other beneficial agents are described in U.S. Pat. Nos. 3,598,122, 3,598,123, 4,379,454, 4,286,592, 4,314,557 and 4,568,343, for example, all of which are incorporated herein by reference. In many cases, drugs which would appear to be ideal candidates for transdermal delivery are found to have such low permeability through intact skin that they cannot be delivered in therapeutically effective amounts from reasonably sized devices.
The terms "therapeutically effective rate" and "therapeutically effective amount", as used herein, refer to a rate or an amount of drug or other agent which provides a therapeutic effect or result.
The term "reasonable size", as used herein, refers to a device of a size with a base surface area (that area in contact with the skin site) that is from about 1 cm.sup.2 to about 50 cm.sup.2, preferably from about 5 cm.sup.2 to about 25 cm.sup.2. While devices of as large as 200 cm.sup.2 can be considered to be of "conventional" size, such large sizes are not generally acceptable to people, as a practical matter.
In an effort to increase skin permeability so that drugs can be delivered in therapeutically effective amounts, it has been proposed to pretreat the skin with various chemicals or to concurrently deliver the drug in the presence of a permeation enhancer. Various materials have been suggested for this purpose as described in U.S. Pat. Nos. 4,299,826, 4,343,798, 4,046,886, 4,130,643, 4,405,616, 4,335,115, 4,130,667, 3,903,256, 4,379,454, 3,527,864, 3,952,099, 3,896,238, 3,472,931, 4,788,062, 4,746,515, 4,863,738 and 4,863,970; British Pat. No. 1,011,949; and Idson, "Percutaneous Absorption," J. Pharm. Sci. (1975) 64:901-924.
It is often difficult to predict which compounds will work as permeation enhancers and which permeation enhancers will work for particular drugs. In systemic drug delivery applications, a compound that enhances the permeability of one drug or a family of drugs may not necessarily enhance the permeability of another drug or family of drugs. Therefore, the usefulness of a particular compound as a permeation enhancer must be analyzed carefully.
DISCLOSURE OF THE INVENTION
According to the present invention, it has been discovered that glycerol monolinoleate (GMLO) is effective in enhancing the permeation of drugs through body surfaces and membranes generally, and through skin in particular. Importantly, glycerol monolinoleate is able to enhance the permeability of these drugs such that they can be delivered at therapeutically effective rates with reasonably sized transdermal delivery devices.
Accordingly, the present invention provides a composition of matter for application to a body surface or membrane to deliver at least one drug, in a therapeutically effective amount, by permeation through the body surface or membrane comprising a least one drug and a permeation-enhancing amount of glycerol monolinoleate. The invention further provides a method for the transdermal coadministration of a therapeutically effective amount of a drug together with a skin permeation-enhancing amount of glycerol monolinoleate.
The system of the invention is a transdermal drug delivery device comprising a matrix adapted to be placed in drug- and permeation enhancer-transmitting relation with the skin or mucosa site. The matrix contains sufficient amounts of glycerol monolinoleate and of a drug to continuously coadminister to the skin for a predetermined period of time the drug and the permeation enhancer to provide a therapeutic effect. The device is of a reasonable size useful for the application of the dru
REFERENCES:
patent: 3472931 (1969-10-01), Stoughton
patent: 3527864 (1970-09-01), MacMillan et al.
patent: 3598122 (1971-08-01), Zaffaroni
patent: 3598123 (1971-08-01), Zaffaroni
patent: 3896238 (1975-07-01), Smith
patent: 3903256 (1975-09-01), MacMillan et al.
patent: 3952099 (1976-04-01), Smith
patent: 4046886 (1977-09-01), Smith
patent: 4130643 (1978-12-01), Smith
patent: 4130667 (1978-12-01), SDmith
patent: 4144317 (1979-03-01), Higuchi et al.
patent: 4286592 (1981-09-01), Chandrasekaran
patent: 4299826 (1981-11-01), Luedders
patent: 4314557 (1982-02-01), Chandrasekaran
patent: 4335115 (1982-06-01), Thompson et al.
patent: 4343798 (1982-08-01), Fawzi
patent: 4379454 (1983-04-01), Campbell et al.
patent: 4405616 (1983-09-01), Rajadhyaksha
patent: 4568343 (1986-02-01), Leeper et al.
patent: 4746515 (1988-05-01), Cheng et al.
patent: 4788062 (1988-11-01), Gale et al.
patent: 4863738 (1989-09-01), Taskovich
patent: 4863970 (1989-09-01), Patel et al.
Idson,Percutaneous Absorption, J. Pharm. Sci. (1975) 64:901-924.
Chemical Abstracts, vol. 112, No. 20, (14 May 1990), Abstract No. 185809T.
Lee Eun Soo
Nedberge Diane E.
Yum Su Il
ALZA Corporation
Cagan Felissa H.
Phelan D. Gabrielle
Rafa Michael J.
Stone Steven F.
LandOfFree
Skin permeation enhancer compositions using glycerol monolinolea does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Skin permeation enhancer compositions using glycerol monolinolea, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Skin permeation enhancer compositions using glycerol monolinolea will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-147787