Claims for Patent: 4,017,615

Summary for Patent: 4,017,615

Title:	Propylene carbonate ointment vehicle
Abstract:	An ointment vehicle containing from 0.5 to 30 percent propylene carbonate, from 30 to 99.5 weight percent petrolatum and/or polysiloxane, compatible cosolvent, the concentration of which in combination with propylene carbonate is from 0.5 to 70 percent, and, optionally, surfactants, thickeners, preservatives, and penetrants. This ointment is a suitable vehicle for all types of therapeutic agents for topical application including antibiotics, steroids, antihistamines, antiseptics, anesthetics, antibacterials, fungicides and the like, and has shown particular advantages with anti-inflammatory topical corticoids.
Inventor(s):	Shastri; Subramaniam (Cupertino, CA), Shaikh; Zafaruzzaman I. (Palo Alto, CA)
Assignee:	Syntex Corporation (Panama, PM)
Application Number:	05/639,740
Patent Claims:	1. An ointment comprising an ointment base consisting essentially of a. from 0.5 to 30 weight percent propylene carbonate; b. from 30 to 99.5 weight percent petrolatum, polysiloxane having a viscosity of from 0.5 to 10.sup.6 centistokes, or mixtures thereof; c. compatible co-solvent, the concentration of which in combination with the propylene carbonate is from 0.5 to 70 weight percent; d. from 0 to 45 weight percent pharmaceutically acceptable surfactant; e. from 0 to 20 weight percent thickener; and f. from 0 to 25 weight percent penetrant in combination with a therapeutically effective amount of a propylene carbonate soluble medicament. 2. The ointment of claim 1 wherein the medicament is a topically active anti-inflammatory steroid. 3. The ointment of claim 2 wherein the steroid is a. a pregn-4-ene-3,20-dione having at each of positions C-1,2 and C-6,7, a single bond, double bond or group having the formula ##STR5## wherein R.sub.11 and R.sub.12 each is hydrogen, chloro or fluoro; at position C-6, hydrogen, methyl, fluoro or chloro; at position C-9, hydrogen, chloro, or fluoro; at position C-11, keto or ##STR6## wherein R.sub.3 ' is hydrogen, hydroxy, chloro or fluoro; at position C-16, hydrogen, methyl, hydroxy or conventional hydrolyzable esters thereof, at position C-17.alpha., hydrogen, hydroxy, conventional hydrolyzable esters thereof, or when taken together with C-16.alpha., a group having the formula ##STR7## wherein R.sub.6 is hydrogen or alkyl of up to 8 carbons, and R.sub.7 is hydrogen, or alkyl or aryl having up to 8 carbons; and at position C-21, hydroxy, conventional hydrolyzable esters thereof, tetrahydropyranyloxy, tetrahydrofuranyloxy, 4'-(lower)alkoxytetrahydropyran-4'-yloxy, lower alkoxy, lower cycloalkoxy, lower cycloalkenyloxy, chloro or fluoro; or b. a 2'-substituted-pregn-4-en-20-one-[3,2-c]pyrazole or a 1'-substituted-pregn-4-en-20-one-[3,2-c]-pyrazole having at the respective N-2' or N-1' positions, hydrogen, methyl, phenyl, chlorophenyl, fluorophenyl, methylphenyl, or methoxyphenyl, and having at C-6,7, a single bond, double bond or group having the formula ##STR8## wherein R.sub.11 and R.sub.12 each is hydrogen, chloro or fluoro; at position C-6, hydrogen, methyl fluoro or chloro; at position C-9, hydrogen, chloro or fluoro; at position C-11, keto or ##STR9## wherein R.sub.3 ' is hydrogen, hydroxy, chloro or fluoro; at position C-16, hydrogen, methyl, hydroxy or conventional hydrolyzable esters thereof, at position C-17.alpha., hydrogen, hydroxy, conventional hydrolyzable esters thereof, or when taken together with C-16.alpha., a group having the formula ##STR10## wherein R.sub.6 is hydrogen or alkyl of up to 8 carbons, and R.sub.7 is hydrogen, or alkyl or aryl having up to 8 carbons; and at position C-21, hydroxy, conventional hydrolyzable esters thereof, tetrahydropyranyloxy, tetrahydrofuranyloxy, 4'-(lower)alkoxytetrahydropyran-4'-yloxy, lower alkoxy, lower cycloalkoxy, lower cycloalkenyloxy, chloro or fluoro. 4. The ointment of claim 3 wherein the steroid is 6.alpha.,9.alpha.-difluoro-11.beta.-hydroxy-16.alpha.,17.alpha.-isopropyli denedioxy-21-acetoxypregna-1,4-diene-3,20-dione. 5. The ointment of claim 3 wherein the steroid is 6.alpha.,9.alpha.-difluoro-11.beta.,21-dihydroxy-16.alpha.,17.alpha.-isopr opylidenedioxypregna-1,4-diene-3,20-dione. 6. The ointment of claim 3 wherein the steroid is 6.alpha.-fluoro-9.alpha.,11.beta.-dichloro-16.alpha.,17.alpha.-isopropylid enedioxy-21-hydroxypregna-1,4-diene-3,20-dione. 7. The ointment of claim 3 wherein the steroid is 9.alpha.,11.beta.-dichloro-6.alpha.,21-difluoro-16.alpha.,17.alpha.-isopro pylidenedioxypregna-1,4-diene-3,20-dione.