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US4017615A Expired / Lapsed US ⏱️ 0.0 years remaining

Propylene carbonate ointment vehicle

Assignee: Syntex Pharmaceuticals International Ltd
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Filing: 1975-12-11
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Granted: 1977-04-12
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Expires: 1995-12-11
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Abstract

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.

Inventors

  • 👤 Subramaniam Shastri
  • 👤 Zafaruzzaman I. Shaikh

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-24 19:48
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/06; A61K47/00; A61K47/06; A61K47/22; A61K9/0012; A61K9/0014

Claims Analysis

Total Claims: 8
Claim 1
Independent Claim 100 words
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 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.
Claim 2
Dependent Claim 100 words
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 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.
Claim 3
Dependent Claim 14 words
The ointment of claim 1 wherein the medicament is a topically active anti-inflammatory steroid.
Claim 4
Dependent Claim 313 words
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 11 and R 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 3 ' is hydrogen, hydroxy, chloro or fluoro; at position C-16, hydrogen, methyl, hydroxy or conventional hydrolyzable esters thereof, at position C-17α, hydrogen, hydroxy, conventional hydrolyzable esters thereof, or when taken together with C-16α, a group having the formula ##STR7## wherein R 6 is hydrogen or alkyl of up to 8 carbons, and R 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 11 and R 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 3 ' is hydrogen, hydroxy, chloro or fluoro; at position C-16, hydrogen, methyl, hydroxy or conventional hydrolyzable esters thereof, at position C-17α, hydrogen, hydroxy, conventional hydrolyzable esters thereof, or when taken together with C-16α, a group having the formula ##STR10## wherein R 6 is hydrogen or alkyl of up to 8 carbons, and R 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.
Claim 5
Dependent Claim 10 words
The ointment of claim 3 wherein the steroid is 6α,9α-difluoro-11β-hydroxy-16α,17α-isopropylidenedioxy-21-acetoxypregna-1,4-diene-3,20-dione.
Claim 6
Dependent Claim 10 words
The ointment of claim 3 wherein the steroid is 6α,9α-difluoro-11β,21-dihydroxy-16α,17α-isopropylidenedioxypregna-1,4-diene-3,20-dione.
Claim 7
Dependent Claim 10 words
The ointment of claim 3 wherein the steroid is 6α-fluoro-9α,11β-dichloro-16α,17α-isopropylidenedioxy-21-hydroxypregna-1,4-diene-3,20-dione.
Claim 8
Dependent Claim 10 words
The ointment of claim 3 wherein the steroid is 9α,11β-dichloro-6α,21-difluoro-16α,17α-isopropylidenedioxypregna-1,4-diene-3,20-dione.

References Cited (Backward Citations)

US3185627A Cited
US3178352A Cited
US3136696A Cited
FR1448042A Cited
GB1096753A Cited
US3592930A Cited
US3924004A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1980-04-11 1980-10-11 1981-04-12 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1984-04-11 1984-10-11 1985-04-12 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1988-04-11 1988-10-11 1989-04-12 $7700.00 Window Closed / Lapsed

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