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Pharmaceutical compositions

Assignee: Glaxo Laboratories Ltd
•
Filing: 1972-11-20
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Granted: 1975-08-19
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Expires: 1992-11-20
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Abstract

Abstract An anaesthetic composition for use by intravenous injection containing a water-soluble steroidal anaesthetic and a parenterally acceptable non-ionic surface active agent.

Inventors

  • 👤 Benjamin Davis
  • 👤 Derek Roger Pearce

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-27 21:36
CPC Classifications
A; A61; A61K; A61K47/00; A61K47/06; A61K47/08; A61K47/10; A61K47/14; A61K47/24; A61K47/26; A61K47/44; A61K9/00; A61K9/0012; A61K9/0019; C; C07; C07J; C07J41/00; C07J41/0033; C07J41/005

Claims Analysis

Total Claims: 16
Claim 1
Independent Claim 79 words
AN AQUEOUS SOLUTION ADAPTED FOR USE IN MEDICINE TO PRODUCE ANAESTHESIA BY INTRAVENOUS INJECTION, SAID SOLUTION CONSISTING ESSENTIALLY OF FROM 0.1-20% BY WEIGHT OF A STEROIDAL ANAESTHETIC HAVING A SOLUBILITY IN WATER AT 20*C OF AT LEAST 1 MG/ML AND FROM 0.1-50% BY WEIGHT OF A VEIN-DAMAGE REDUCING SUBSTANCE CONSISTING OF A PARENTERALLY ACCEPTABLE NONIONIC SURFACE ACTIVE COMPONENT HAVING AN HLB VALUE ABOVE 9 AND NOT MORE THAN 30, WHEREBY THE PHYSIOLOGICAL COMPATIBILITY OF SAID STEROIDAL ANAESTHETIC IS IMPROVED.
Claim 2
Dependent Claim 79 words
AN AQUEOUS SOLUTION ADAPTED FOR USE IN MEDICINE TO PRODUCE ANAESTHESIA BY INTRAVENOUS INJECTION, SAID SOLUTION CONSISTING ESSENTIALLY OF FROM 0.1-20% BY WEIGHT OF A STEROIDAL ANAESTHETIC HAVING A SOLUBILITY IN WATER AT 20*C OF AT LEAST 1 MG/ML AND FROM 0.1-50% BY WEIGHT OF A VEIN-DAMAGE REDUCING SUBSTANCE CONSISTING OF A PARENTERALLY ACCEPTABLE NONIONIC SURFACE ACTIVE COMPONENT HAVING AN HLB VALUE ABOVE 9 AND NOT MORE THAN 30, WHEREBY THE PHYSIOLOGICAL COMPATIBILITY OF SAID STEROIDAL ANAESTHETIC IS IMPROVED.
Claim 3
Dependent Claim 16 words
A solution as claimed in claim 1 wherein the HLB value is from 12.5 to 18.
Claim 4
Dependent Claim 116 words
A solution as claimed in claim 1 wherein the surface active component comprises a polyoxyethylated derivative of a fatty glyceride oil, having 12-20 carbon atoms, and containing 35 to 45 oxyethylene groups per mole of fatty oil; a polyoxyethylene ether of an alcohol having 12-18 carbon atoms and containing 10-30 oxyethylene groups; a polyoxyethylene-polyoxypropylene ether containing 15-150 oxyethylene groups and 15 to 50 oxypropylene groups; a polyoxyethylated fatty acid (having 12-18 carbon atoms) ester of sorbitan or mannitan containing 15-30 oxyethylene groups; a polyethylene glycol ester of a fatty acid having 12-18 carbon atoms and containing 6-40 oxyethylene groups; an ester of a fatty acid having 12-18 carbon atoms of sorbitan or mannitan; or a phospholipid.
Claim 5
Dependent Claim 23 words
A solution as claimed in claim 1 wherein the surface active component is present in an amount of 2 to 5% by weight.
Claim 6
Dependent Claim 22 words
A solution as claimed in claim 1 wherein the steroidal anaesthetic is present in an amount of 1 to 10% by weight.
Claim 7
Dependent Claim 25 words
A solution as claimed in claim 1 wherein the steroidal anaesthetic is a salt formed between the steroid and a physiologically acceptable anion or cation.
Claim 8
Dependent Claim 20 words
A solution as claimed in claim 6 wherein the ionic substituent is a carboxylate, carbonate, phosphate, pyrophosphate or basis substituent.
Claim 9
Dependent Claim 31 words
A solution as claimed in claim 6 wherein the steroidal anaesthetic is a member of the pregnane series said salt being a salt of an ionic substituent carried at the 21-position.
Claim 10
Dependent Claim 24 words
A solution as claimed in claim 6 wherein said salt being a salt of an ionic substituent is carried at the 2 Beta -position.
Claim 11
Dependent Claim 33 words
A solution as claimed in claim 6 wherein the steroidal anaesthetic is a member of the androstane series said salt being a salt of an ionic substituent carried at the 17 Beta -position.
Claim 12
Dependent Claim 20 words
A solution as claimed in claim 6 said salt being a salt of an ionic substituent carried at the 3-position.
Claim 13
Dependent Claim 67 words
A solution as claimed in claim 1 wherein the steroidal anaesthetic is 21-hydroxy-5 Beta -pregnane-3,20-dione 21-hemisuccinate sodium; 21-hydroxy-5 Beta -pregnane-3,20-dione 21-phosphate sodium; 3 Alpha -hydroxy-5 Beta -pregnane-11,20-dione 3-hemisuccinate sodium; 3 Alpha -hydroxy-5 Beta -pregnane -20-one 3-hemisuccinate sodium; 3 Alpha -hydroxy-5 Alpha -pregnane-11,20-dione 3-hemisuccinate sodium; 3 Alpha -hydroxy-5 Beta -pregnane-11,20-dione 3-hemiglutarate sodium; 3 Alpha -hydroxy-16 Beta -methyl-5 Beta -pregnane-11,20-dione 3-hemisuccinate sodium; or 3 Alpha -hydroxy-5 Beta -pregnane-11,20-dione 3-amino-acetate-hydrochloride.
Claim 14
Independent Claim 83 words
A method of inducing anaesthesia in an individual, man or animal, whereby the tendency to cause vein damage is reduced, comprising intravenously administering to said individual an aqueous solution consisting essentially of from 0.1 -20% by weight of a steroidal anaesthetic having a solubility in water at 20*C of at least 1 mg/ml and from 0.1-50% by weight of a vein-damage reducing substance consisting of a parenterally acceptable nonionic surface active component having an HLB value above 9 and not more than 30.
Claim 15
Independent Claim 83 words
A method of inducing anaesthesia in an individual, man or animal, whereby the tendency to cause vein damage is reduced, comprising intravenously administering to said individual an aqueous solution consisting essentially of from 0.1 -20% by weight of a steroidal anaesthetic having a solubility in water at 20*C of at least 1 mg/ml and from 0.1-50% by weight of a vein-damage reducing substance consisting of a parenterally acceptable nonionic surface active component having an HLB value above 9 and not more than 30.
Claim 16
Dependent Claim 16 words
The method of claim 13 wherein said solution contains 2%-5% by weight of surface active component.

References Cited (Backward Citations)

US2708651A Cited
US2880138A Cited
US3180797A Cited
US3337400A Cited
US3714352A Cited
US3781435A Cited
US3816624A Cited
US3763195A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1978-08-18 1979-02-17 1979-08-19 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1982-08-18 1983-02-17 1983-08-19 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1986-08-18 1987-02-17 1987-08-19 $7700.00 Window Closed / Lapsed

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