Carlos Samour - Bedford MA, US Scott Krauser - Tyngsboro MA, US Robert Gyurik - Exeter NH, US
International Classification:
A61K009/70
US Classification:
424/449000
Abstract:
Topical alcoholic or aqueous alcoholic gels containing ibuprofen or other NSAIDs, such as, naproxen, in substantially neutral salt form, have enhanced penetration through skin and may provide rapid pain/inflammation relief by including in the formulation 2-n-nonyl-1,3-dioxolane or other hydrocarbyl derivative of 1,3-dioxolane-or 1,3-dioxane or acetal, as skin penetration enhancing compound. The amount of propylene glycol may be varied to adjust the initial flux of the NSAID through the skin, especially for ibuprofen, naproxen, and ketorolac.
Ibuprofen Salt Emulsifiers And Cream Formulations Containing Same
Emulsions and creams containing ibuprofen effective for topical administration of the ibuprofen are provided without the presence of conventional O/W emulsifying agent. The emulsions and creams are formed by using the ibuprofen, in the form of its salt, as the O/W emulsifying agent. A minor amount of a W/O emulsifying agent may be included in the composition. Percutaneous delivery of ibuprofen is improved by using a skin penetration enhancing compound, such as 2-n-nonyl-1,3-dioxolane or decanaldimethyl acetal, as the oily phase of the emulsion.
Non-Steroidal Anti-Inflammatory Drug Formulations For Topical Applications To The Skin
Carlos Samour - Bedford MA, US Scott Krauser - Tyngsboro MA, US Robert Gyurik - Exeter NH, US
Assignee:
MacroChem Corporation - Lexington MA
International Classification:
A61K 31/192 A61F 13/02
US Classification:
424448000, 514569000
Abstract:
Topical alcoholic or aqueous alcoholic gels containing ibuprofen or other NSAIDs, such as, naproxen, in substantially neutral salt form, have enhanced penetration through skin and may provide rapid pain/inflammation relief by including in the formulation 2-n-nonyl-1,3-dioxolane or other hydrocarbyl derivative of 1,3-dioxolane or 1,3-dioxane or acetal, as skin penetration enhancing compound. The amount of propylene glycol may be varied to adjust the initial flux of the NSAID through the skin, especially for ibuprofen, naproxen, and ketorolac.
Pharmaceutical Compositions For Topical Application
Compounds of Formula I are useful as skin penetration enhancing agents: (I) wherein: R represents a linear, saturated or unsaturated, substituted or unsubstituted hydrocarbyl radical; and X represents a —(CO)O—, —O(CO)—, C═O, CONH, O, NHCONH, S, or S═O radical. Compositions and methods using these compounds are also described.
Non-Steroidal Antiinflammtory Drug Formulations For Topical Application To The Skin
Carlos M. Samour - Bedford MA Scott F. Krauser - Tyngsboro MA Robert J. Gyurik - Exeter NH
Assignee:
MacroChem Corporation - Lexington MA
International Classification:
A61K 4710 A61K 4722 A61K 910
US Classification:
424449
Abstract:
Topical alcoholic or aqueous alcoholic gels containing ibuprofen or other NSAIDs, such as, naproxen, in substantially neutral salt form, have enhanced penetration through skin and may provide rapid pain/inflammation relief by including in the formulation 2-n-nonyl-1,3-dioxolane or other hydrocarbyl derivative of 1,3-dioxolane or 1,3-dioxane or acetal, as skin penetration enhancing compound. The amount of propylene glycol may be varied to adjust the initial flux of the NSAID through the skin, especially for ibuprofen, naproxen, and ketorolac.
Cationic Film-Forming Polymer Compositions, And Use Thereof In Topical Agents Delivery System And Method Of Delivering Agents To The Skin
Carlos M. Samour - Newport RI Scott F. Krauser - Methuen MA
Assignee:
MacroChem Corporation - Lexington MA
International Classification:
C08G 1850
US Classification:
528 49
Abstract:
A mixture of lipophilic and amphiphilic/hydrophilic film-forming polymers of the formula (I)
R--(CO). sub. m Y. sup. 1 --(CH. sub. 2 CHR. sup. 1 O). sub. n --�CONH--Z--NHCO(OCH. sub. 2 CHR. sup. 2). sub. n' --Y. sup. 2 --(CH. sub. 2 CHR. sup. 2 O). sub. n" !. sub. p --CONH--Z--NHCO--(OCH. sub. 2 CHR. sup. 1). sub. n --Y. sup. 1 (CO). sub. m R (I)
where R represents (i) an alkyl, alkenyl or alkaryl group of from 1 to 30 carbon atoms or (ii) a polypropylene oxide group or polybutylene oxide group; R. sup. 1 and R. sup. 2, each, independently, represent a hydrogen atom, or a methyl or ethyl group; Z represents a divalent linking hydrocarbyl group; m is 0 or 1; when m=0, Y. sup. 1 represents O, NR. sup. 3 or N. sup. + R. sup. 3 R. sup. 4 X. sup. - and when m=1 Y. sup.
Hormone Replacement Therapy Drug Formulations For Topical Application To The Skin
Carlos M. Samour - Bedford MA Scott F. Krauser - Tyngsboro MA Robert J. Gyurik - Exeter NH
Assignee:
MacroChem Corporation - Lexington MA
International Classification:
A61K 3156
US Classification:
514177
Abstract:
Topical alcoholic or aqueous alcoholic gels containing testosterone, progesterone, estradiol or other hormones have enhanced penetration through skin by including in the formulation 2-n-nonyl-1,3-dioxolane or other hydrocarbyl derivative of 1,3-dioxolane or 1,3-dioxane or acetal, as skin penetration enhancing compound.
Composition And Method For Treating Penile Erectile Dysfunction
Carlos M. Samour - Bedford MA Scott F. Krauser - Tyngsboro MA Robert J. Gyurik - Exeter NH
Assignee:
MacroChem Corporation - Lexington MA
International Classification:
A61K 31557 A61K 31495 A61K 3150 A61K 31415
US Classification:
514573
Abstract:
A composition for the topical transdermal administration to the penis is based on prostaglandin E. sub. 1. The composition is non-irritating and effective for relieving erectile impotence or other penile erectile dysfunction. A penetration enhancing effective amount of a dioxolane, dioxane, or acetal skin penetration enhancing compound in a pharmaceutically acceptable aqueous alcoholic carrier is used to facilitate the penetration of the prostaglandin E. sub. 1 active ingredient through the skin. Phentolamine or prazosin may be used in combination with prostaglandin E. sub. 1.