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Claims for Patent: RE32393

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Claims for Patent: RE32393

Title: Composition for enhancing the administration of pharmacologically active agents
Abstract:According to the invention, the parenteral administration of water-insoluble pharmacologically active agents is enhanced wherein the agents are administered in the lipoid phase of a carrier emulsion comprising a microemulsion of a finely dispersed lipoid in an aqueous phase. The lipoid preferably has a mean particle size below 1 micron. This makes it possible to administer water-insoluble agents in high concentrations, and thus a lower dose, whereby a rapid onset of the pharmacological effect is accompanied by a markedly reduced incidence of injury to body tissues.
Inventor(s): Wretlind; Karl A. J. (Stockholm, SE), Ljungberg; Stellan (Lidingo, SE), Hakansson; Ivan (Stockholm, SE), Ajaxon; Bengt M. (Upsala, SE)
Assignee: KabiVitrum AB (Stockholm, SE)
Application Number:06/605,760
Patent Claims: 1. A composition for enhancing .[.parenteral.]. .Iadd.intravenous .Iaddend.administration comprising a stable, oil-in-water emulsion .Iadd.capable of withstanding autoclaving, .Iaddend.containing a pharmacologically inert lipoid as a hydrophobic phase dispersed in a hydrophilic phase and an effective dose of a pharmacologically active, oil-soluble agent predominantly dissolved in said lipoid at a fraction ratio thereto in the hydrophobic phase, said lipoid being dispersed in the emulsion as finely divided particles having a mean particle size less than 1 micron to achieve rapid onset of an acceptable therapeutic effect attributable to said effective dose of the active agent, said active, .Iadd.oil soluble .Iaddend.agent being selected from a class of substances consisting of central depressants, analgesics, .[.spasmolytics,.]. muscle relaxants, and vasodepressants. .[.2. A composition as defined in claim 1, wherein the oil-soluble pharmacological agent is a central depressant from a class of compounds consisting of: hexobarbital, secobarbital, thiopental, pentobarbital, and diazepam..]. .[.3. A composition as defined in claim 1, wherein the oil-soluble pharmacological agent is an anaesthetic from a class of compounds consisting of: hexylether, tribromoethanol and halothane..]. .[.4. A composition as defined in claim 1, wherein the oil-soluble pharmacological agent is an analgesic from a class of compounds consisting of: pentazocine, phenylbutazone, benzocaine, quatacaine, and lidocaine..]. .[.5. A composition as defined in claim 1, wherein the oil-soluble pharmacological agent is a spasmolytic from a class of compounds consisting of: mecamylamine and cyclandelate..]. .[.6. A composition as defined in claim 1, wherein the oil-soluble pharmacological agent is a vasodepressant from a class of compounds

consisting of: quinidine and cyclandelate..]. 7. A composition as defined in claim 1, wherein the .Iadd.pharmacologically active .Iaddend.oil-soluble .[.pharmacological.]. agent is .[.a muscle relaxant from the compounds of.]. phenyramidol. .[.8. A composition for enhancing parenteral administration comprising a stable, oil-in-water emulsion containing a pharmacologically inert lipoid as a hydrophobic phase dispersed in a hydrophilic phase and an effective dose of a pharmacologically active, oil-soluble agent predominantly dissolved in said lipoid at a fraction ratio thereto in the hydrophobic phase, said lipoid being dispersed in the emulsion as finely divided particles having a mean particle size less than 1 micron to achieve rapid onset of an acceptable therapeutic effect attributable to said effective dose of the active agent, said active agent being selected from a class of substances consisting of: phenyramidol, hexobarbital, mecamylamine, quinidine, chloralose, tribromoethanol, pentazocine, phenylbutazone, cyclandelate, benzocaine, secobarbital, quatacaine, lidocaine, thiopental, pentobarbital, diazepam, and methoxyflurane..]. .Iadd.9. The composition of claim 1 wherein said lipoid contains an oil from the group of soybean

oil, cottonseed oil, coconut oil, and olive oil. .Iaddend. .Iadd.10. The composition of claim 1 which contains a stabilizer component containing at least one member selected from the group of phosphatide, polypropylene glycol, polyethylene glycol, polyglycerol monooleate, and polyoxyethylene derivative of fatty acids..Iaddend. .Iadd.11. The composition of claim 10 wherein said stabilizer component includes a phosphatide..Iaddend. .Iadd.12. The composition of claim 10 wherein said member includes polyoxyethylene derivative of fatty acids..Iaddend. .Iadd.13. The composition of claim 1 wherein said active agent provides longer duration than for the corresponding water-soluble salts of the agent..Iaddend. .Iadd.14. The composition of claim 1 wherein said lipoid is soybean oil..Iaddend. .Iadd.15. The composition of claim 10 wherein said phosphatide is egg phosphatide..Iaddend. .Iadd.16. The composition of claim 1 which further contains glycerol..Iaddend. .Iadd.17. The composition of claim 16 wherein the amount of said glycerol is about 2.5% by weight per 100 ml of composition..Iaddend. .Iadd.18. The composition of claim 11 wherein said active agent is diazepam and said stabilizer component also contains acetylated monoglycerides..Iaddend. .Iadd.19. The composition of claim 18 wherein the amount of said diazepam is about 0.5 g/100 ml of composition; amount of said phosphatide is about 1.2 g/100 ml of composition; amount of said acetylated monoglyceride is about 5.0 g/100 ml; and said lipoid is about 15 g of soybean oil per 100 ml of composition..Iaddend. .Iadd.20. The composition of claim 19 which further contains about 2.5 grams of glycerol..Iaddend. .Iadd.21. A composition for enhancing intravenous administration comprising a stable, oil-in-water emulsion capable of withstanding autoclaving containing a pharmacologically inert lipoid as a hydrophobic phase dispersed in a hydrophilic phase and an effective dose of a pharmacologically active, oil-soluble agent predominantly dissolved in said lipoid at a fraction ratio thereto in the hydrophobic phase, said lipoid being dispersed in the emulsion as finely divided particles having a mean particle size less than 1 micron to achieve rapid onset of an acceptable therapeutic effect attributable to said effective dose of the active agent, wherein said active agent is selected from the group of chloralose, benzocaine, and secobarbitol; and a stabilizer component containing a monoglyceride..Iaddend. .Iadd.22. A composition for enhancing intravenous administration comprising a stable, oil-in-water emulsion capable of withstanding autoclaving containing a pharmacologically inert lipoid as a hydrophobic phase dispersed in a hydrophilic phase and an effective dose of a pharmacologically active, oil-soluble agent predominantly dissolved in said lipoid at a fraction ratio thereto in the hydrophobic phase, said lipoid being dispersed in the emulsion as finely divided particles having a mean particle size less than 1 micron to achieve rapid onset of an acceptable therapeutic effect attributable to said effective dose of the active agent, wherein said active agent is selected from the group of chloralose, pentazocine, cycloandelate, quatacaine, lidocaine, phenylbutazone, thiopental, and pentobarbitol; and a stabilizer component containing a block polymer of ethylene oxide and propylene oxide..Iaddend. .Iadd.23. The composition of claim 22 which further includes an acylated monoglyceride and wherein said active agent is selected from the group of phenylbutazone, lidocaine, thiopental, and pentobarbitol..Iaddend. .Iadd.24. A composition for enhancing intravenous administration comprising a stable, oil-in-water emulsion capable of withstanding autoclaving containing a pharmacologically inert lipoid as a hydrophobic phase dispersed in a hydrophilic phase and an effective dose of hexobarbitol predominantly dissolved in said lipoid at a fraction ratio thereto in the hydrophobic phase, said lipoid being dispersed in the emulsion as finely divided particles having a mean particle size less than 1 micron to achieve rapid onset of an acceptable therapeutic effect attributable to said effective dose of the hexobarbitol..Iaddend. .Iadd.25. The composition of claim 1 which is capable of withstanding freezing..Iaddend. .Iadd.26. A method for administrating an active agent to a patient which comprises intravenously administering a composition comprising a stable, oil-in-water emulsion capable of withstanding autoclaving, containing a pharmacologically inert lipoid as a hydrophobic phase dispersed in a hydrophilic phase and an effective dose of a pharmacologically active, oil-soluble agent predominantly dissolved in said lipoid at a fraction ratio thereto in the hydrophobic phase, said lipoid being dispersed in the emulsion as finely divided particles having a mean particle size less than 1 micron to achieve rapid onset of an acceptable therapeutic effect attributable to said effective dose of the active agent, said active agent being selected from a class of substances consisting of central depressants, analgesics, muscle relaxants, and vasodepressants..Iaddend. .Iadd.27. The method of claim 26 wherein said lipoid contains an oil from the group of soybean oil, cottonseed oil, coconut oil, and olive oil..Iaddend. .Iadd.28. The method of claim 26 wherein said composition contains a stabilizer component containing at least one member selected from the group of phosphatide, polypropylene glycol, polyethylene glycol, polyglycerol monooleate, and polyoxyethylene derivative of fatty acids..Iaddend. .Iadd.29. The method of claim 28 wherein said stabilizer component includes a phosphatide..Iaddend. .Iadd.30. The method of claim 28 wherein said member includes polyoxyethylene derivative of fatty acids..Iaddend. .Iadd.31. The method of claim 26 wherein said active agent provides longer duration than for the corresponding water-soluble salts of the agent..Iaddend. .Iadd.32. The method of claim 26 wherein said lipoid is soybean oil..Iaddend. .Iadd.33. The method of claim 28 wherein said phosphatide is egg phosphatide..Iaddend. .Iadd.34. The method of claim 26 wherein said

composition further contains glycerol..Iaddend. .Iadd.35. The method of claim 34 wherein the amount of said glycerol is about 2.5% by weight per 100 ml of composition..Iaddend. .Iadd.36. The method of claim 26 wherein said active agent is phenyramidol..Iaddend. .Iadd.37. The method of claim 29 wherein said active agent is diazepam and said stabilizer component also contains acetylated monoglycerides..Iaddend. .Iadd.38. The method of claim 37 wherein the amount of said diazepam is about 0.5 g/100 ml of composition; amount of said phosphatide is about 1.2 g/100 ml of composition; amount of acetylated monoglyceride is about 5.0 g/100 ml; and said lipoid is about 15 g of soybean oil per 100 ml of composition..Iaddend. .Iadd.39. The method of claim 38 wherein said composition further contains about 2.5 grams of glycerol..Iaddend. .Iadd.40. The method of claim 26 wherein said composition is capable of withstanding freezing..Iaddend. .Iadd.41. A method for administrating an active agent to a patient which comprises intravenously administering a composition comprising a stable, oil-in-water emulsion capable of withstanding autoclaving containing a pharmacologically inert lipoid as a hydrophobic phase dispersed in a hydrophilic phase and an effective dose of a pharmacologically active, oil-soluble agent predominantly dissolved in said lipoid at a fraction ratio thereto in the hydrophobic phase, said lipoid being dispersed in the emulsion as finely divided particles having a mean particle size less than 1 micron to achieve rapid onset of an acceptable therapeutic effect attributable to said effective dose of the active agent, wherein said active agent is selected from the group of chloralose, benzocaine, and secobarbitol; and a stabilizer component containing a monoglyceride..Iaddend. .Iadd.42. A method for administrating an active agent to a patient which comprises intravenously administering a composition comprising a stable, oil-in-water emulsion capable of withstanding autoclaving containing a pharmacologically inert lipoid as a hydrophobic phase dispersed in a hydrophilic phase and an effective dose of a pharmacologically active, oil-soluble agent predominantly dissolved in said lipoid at a fraction ratio thereto in the hydrophobic phase, said lipoid being dispersed in the emulsion as finely divided particles having a mean particle size less than 1 micron to achieve rapid onset of an acceptable therapeutic effect attributable to said effective dose of the active agent, wherein said active agent is selected from the group of chloralose, pentazocine, cycloandelate, quatacaine, lidocaine, phenylbutazone, thiopental, and pentobarbitol; and a stabilizer component containing a block polymer of ethylene oxide and propylene oxide..Iaddend. .Iadd.43. The method of claim 42 wherein said composition further includes an acylated monoglyceride and wherein said active agent is selected from the group of phenylbutazone, lidocaine, thiopental, and pentobarbitol..Iaddend. .Iadd.44. A method for administrating an active agent to a patient which comprises intravenously administering a composition comprising a stable, oil-in-water emulsion capable of withstanding autoclaving containing a pharmacologically inert lipoid as a hydrophobic phase dispersed in a hydrophilic phase and an effective dose of hexobarbitol predominantly dissolved in said lipoid at a fraction ratio thereto in the hydrophobic phase, said lipoid being dispersed in the emulsion as finely divided particles having a mean particle size less than 1 micron to achieve rapid onset of an acceptable therapeutic effect attributable to said effective dose of the hexobarbitol..Iaddend.
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