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|Title:||ENHANCING TISSUE PENETRATION OF PHYSIOLOGICALLY ACTIVE STEROIDAL AGENTS WITH DMSO|
|Abstract:||A method of enhancing tissue penetration of physiologically active steroidal agents by conjointly applying them to the tissue with dimethyl sulfoxide. Penetration of the skin and the mucous membranes of the body cavities by these agents may be enhanced by cojoint application of such agents and dimethyl sulfoxide directly to such membranes. Preferably, for penetration of these agents through the skin compositions of DMSO at concentrations of 50 percent and above are employed and for penetration through mucous membranes, compositions including DMSO at concentrations of 10 percent and above are employed. Steroidal Agents may be advantageously administered by injection with DMSO in concentrations preferably up to 20 percent by weight to enhance penetration of internal tissue membranes barriers to achieve better distribution of these agents.|
|Inventor(s):||Herschler; Robert John (Camas, WA)|
|Assignee:||Crown Zellerbach Corporation (San Francisco, CA)|
|Filing Date:||Sep 02, 1970|
|Claims:||1. A method of enhancing the penetration into and across an external membrane barrier of a human or animal subject of a physiologically active glucocorticoid steroidal agent capable of eliciting a physiological effect upon topical application thereof, which comprises the concurrent topical administration to the external membrane of an amount of said steroidal agent effective to produce the desired physiological effect and an amount of DMSO sufficient to effectively enhance penetration of said steroidal agent to achieve the desired physiological effect. |
2. A method as in claim 1 and wherein the said agent is applied to the intact skin in a composition which includes said DMSO and wherein the DMSO in said composition is at least about 50 percent by weight of the composition.
3. A method as in claim 1 and wherein said agent is applied to induce at least a physiological effect locally to the site of application.
4. A method as in claim 1 and wherein said glucocorticoid is a 3-keto, .DELTA. 4, 11-oxygen function, 20-keto steroid of the pregnane series.
5. A method as in claim 4 and wherein said glucocorticoid is a 11-hydroxy steroid.
6. A method as in claim 1 and wherein said agent is applied to said membrane in a composition which includes said DMSO.
7. A method as in claim 6 and wherein said composition contains a pharmaceutically acceptable thickening agent in an amount sufficient to materially increase the viscosity thereof, whereby to facilitate topical application.
8. A method as in claim 7 wherein said composition is in the form of an ointment.
9. A method as in claim 7 and wherein said composition is in the form of a lotion.