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US4370322A Expired / Lapsed US ⏱️ 0.0 years remaining

Topically administrable pharmaceutical compositions containing anti-inflammatory steroids

Assignee: Glaxo Group Ltd
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Filing: 1981-10-05
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Granted: 1983-01-25
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Expires: 2001-10-05
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Abstract

Abstract Pharmaceutical compositions such as ointments and creams are provided by admixture of anti-inflammatory steroids active on topical application with a liquid oily phase containing at least one oil possessing a viscosity less than 10 centistokes and in which the steroid has a solubility of at least 0.5% by weight at 25 DEG C., the degree of unsaturation of the steroid in the liquid oily phase of the composition at 25 DEG C., being at least 3. Examples of steroids which may be used are betamethasone, beclomethasone and clobetasol derivatives. Suitable oils include esters of mono- and dibasic aliphatic acids. The compositions may include further oils such as liquid paraffin and conventional additives used in the preparation of ointments and creams. The local anti-inflammatory effect of the steroids is maintained in such formulations but systemic side effects are decreased.

Inventors

  • 👤 Michael J. Busse
  • 👤 Kenneth A. Lees

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-06 15:44
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/06; A61K31/00; A61K31/56; A61K31/57; A61K47/00; A61K47/06; A61K47/08; A61K47/14; A61K9/0012; A61K9/0014; A61P; A61P29/00

Claims Analysis

Total Claims: 15
Claim 1
Independent Claim 79 words
A pharmaceutical composition comprising an anti-inflammatory steroid selected from beclomethasone 17,21-dipropionate, betamethasone 17-valerate, betamethasone 17,21-dipropionate, clobetasol 17-propionate, clobetasone 17-butyrate and chloromethyl 17α-acetoxy-9α-fluoro-11β-hydroxy-16β-methyl-3-oxoandrosta-1,4-diene-17β-carboxylate dissolved in a liquid oily phase containing at least one oil possessing a viscosity less than 10 centistokes and in which the steroid has a solubility of at least 0.5% by weight at 25° C., the degree of unsaturation of the steroid in the liquid oily phase of the composition at 25° C. being at least 3.
Claim 2
Dependent Claim 79 words
A pharmaceutical composition comprising an anti-inflammatory steroid selected from beclomethasone 17,21-dipropionate, betamethasone 17-valerate, betamethasone 17,21-dipropionate, clobetasol 17-propionate, clobetasone 17-butyrate and chloromethyl 17α-acetoxy-9α-fluoro-11β-hydroxy-16β-methyl-3-oxoandrosta-1,4-diene-17β-carboxylate dissolved in a liquid oily phase containing at least one oil possessing a viscosity less than 10 centistokes and in which the steroid has a solubility of at least 0.5% by weight at 25° C., the degree of unsaturation of the steroid in the liquid oily phase of the composition at 25° C. being at least 3.
Claim 3
Dependent Claim 37 words
A pharmaceutical composition according to claim 1 wherein the liquid oily phase contains at least one oil selected from the esters of mono- and dibasic aliphatic acids, the said esters having from 6 to 18 carbon atoms.
Claim 4
Dependent Claim 31 words
A pharmaceutical composition according to claim 2 wherein the liquid oily phase contains at least one oil selected from the butyl and isopropyl esters of adipic, lauric, palmitic and myristic acids.
Claim 5
Dependent Claim 15 words
A pharmaceutical composition according to claim 3 wherein the liquid oily phase contains dibutyl adipate.
Claim 6
Dependent Claim 11 words
A pharmaceutical composition according to claim 4 which contains clobetasol 17-propionate.
Claim 7
Dependent Claim 11 words
A pharmaceutical composition according to claim 4 which contains betamethasone 17-valerate.
Claim 8
Dependent Claim 11 words
A pharmaceutical composition according to claim 4 which contains beclomethasone 17,21-dipropionate.
Claim 9
Dependent Claim 15 words
A pharmaceutical composition according to claim 1 wherein the liquid oily phase contains further oils.
Claim 10
Dependent Claim 22 words
A pharmaceutical composition according to claim 8 wherein the liquid oily phase contains liquid paraffin having a viscosity of about 7 centistokes.
Claim 11
Dependent Claim 22 words
A pharmaceutical composition according to claim 1 wherein the degree of unsaturation of the steroid is in the range 3.0 to 5.0.
Claim 12
Dependent Claim 23 words
A pharmaceutical composition according to claim 1 wherein the concentration of the steroid is from 0.02 to 1.5% by weight of the composition.
Claim 13
Dependent Claim 15 words
A pharmaceutical composition according to claim 1 in the form of an ointment or cream.
Claim 14
Dependent Claim 25 words
A pharmaceutical composition according to claim 12 containing, as additional ingredients, substances selected from solid wax, emulsifying agents, preservatives, buffers, stabilisers and other conventional additives.
Claim 15
Dependent Claim 25 words
A method of treatment of inflammatory dermatoses of humans and animals comprising topically administering to the affected skin a pharmaceutical composition according to claim 1.

References Cited (Backward Citations)

US3856828A Cited
US4070462A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1986-01-24 1986-07-26 1987-01-25 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1990-01-24 1990-07-26 1991-01-25 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1994-01-24 1994-07-26 1995-01-25 $7700.00 Window Closed / Lapsed

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