Chemistry: fertilizers – Processes and products – Forms or conditioning
Patent
1987-07-23
1989-12-12
Bond, Robert T.
Chemistry: fertilizers
Processes and products
Forms or conditioning
71 95, 71 94, 514946, 514947, 514183, 514212, 514328, 514425, 8564, 8568, 8574, A01N 4336, A01N 4340, A01N, A01N
Patent
active
048865451
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
This invention relates to compositions comprising a physiologically-active agent and a 1-alkyl azacycloalkane, which is substituted by oxygen or sulfur atoms pendant from any of the carbon atoms alpha to the nitrogen atom, including the 1-alkyl alpha carbon atom, in an amount effective to enhance the penetration of the physiologically-active agent through the skin or other membrane of the body of an animal.
Other compositions of 1-substituted azacycloalkane and their uses relate to an improved method of dyeing fibers, improved delivery of plant nutrients, improved plant pest control, improved delivery of plant growth regulations, improved acid-catalyzed conversion of a reactant to a reaction product and an improved insect repellant.
BACKGROUND OF THE ART
As hereinabove indicated, the present invention includes a number of uses in which it provides an advantage. Each of these uses will be hereinafter addressed in the order of their recital beginning with the use of the composition of the present invention in the enhancement of the penetration of a physiologically-active agent through the skin or other membranes of body.
It is well known that many physiologically-active agents are best applied topically to obtain desirable results. Topical application, as contrasted to systemic application, can avoid metabolic degradation of the agents, largely avoids side effects of the agents and permits high local concentrations of the agents.
The greatest problem in applying physiologically active agents topically is that the skin is such an effective barrier to penetration. The epidermis of the skin has an exterior layer of dead cells called the stratum corneum which is tightly compacted and oily and which provides an effective barrier against gaseous, solid or liquid chemical agents, whether used alone or in water or oil solutions. If a physiologically active agent penetrates the stratum corneum, it can readily pass through the basal layer of the epidermis and into the dermis.
Although the effectiveness of the stratum corneum as a barrier provides great protection, it also frustrates efforts to apply beneficial agents directly to local areas of the body. The inability of physiologically active agents to penetrate the stratum corneum prevents their effective use to treat such conditions as inflammation, acne, psoriasis, herpes simplex, eczema, infections due to fungus, virus, or other microorganisms, or other disorders or conditions of the skin or mucous membranes, or of conditions beneath the exterior surface of the skin or mucous membranes. The stratum corneum also prevents the skin from absorbing and retaining cosmetic-type materials such as sunscreens, perfumes, mosquito repellants and the like.
Physiologically active agents may be applied to locally affected parts of the body through the vehicle system described herein. Vehicles such as USP cold cream, ethanol and various ointments, oils, solvents, and emulsions have been used heretofore to apply physiologically active ingredients locally. Most such vehicles are not effective to carry significant amounts of physiologically active agents through the skin. One such vehicle is dimethyl sulfoxide.
The 1-lower alkyl substituted azacyclopentan-2-ones having 1-4 carbon atoms in the alkyl group are known to moderately enhance percutaneous absorption of chemicals, e.g., drugs. It was earlier recognized that it would be desirable to obtain the same or higher level of percutaneous absorption with substantially lower concentrations of the penetration-enhancing compound. Therefore, a new class of N-substituted azacycloalkan-2-ones were invented having the desired properties. This new class of penetration-enhancing agents are described in U.S. Pat. Nos. 3,989,815; 3,989,816; 3,991,203; 4,122,170; 4,316,893; 4,405,616; 4,415,563; 4,423,040; 4,424,210; and 4,444,762, which are hereby incorporated by reference.
It is an object of this invention to provide new penetration-enhancing agents having the desirable property of enhancing the percutaneous absorpti
REFERENCES:
patent: 4415363 (1983-11-01), Radjadhyaksha
patent: 4424210 (1984-01-01), Radjadhyaksha
patent: 4525199 (1985-06-01), Radjadhyaksha
patent: 4755535 (1988-07-01), Minaskainian et al.
patent: 4762549 (1988-08-01), Radjadhyaksha
Minaskanian Gevork
Peck James V.
Baran Robert J.
Bond Robert T.
Hackler Walter A.
Nelson Research & Development Company
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