US4168308A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Composition for enhancing the administration of pharmacologically active agents
Assignee: Pfizer Health AB
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Filing: 1977-11-23
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Granted: 1979-09-18
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Expires: 1997-11-23
Abstract
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.
Inventors
- 👤 Karl A. J. Wretlind
- 👤 Stellan Ljungberg
- 👤 Ivan Hakansson
- 👤 Bengt M. Ajaxon
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 13:31
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/10; A61K9/107; A61K9/1075
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
107 words
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 central depressants, analgesics, spasmolytics, muscle relaxants and vasodepressants.
Claim 2
Dependent Claim
107 words
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 central depressants, analgesics, spasmolytics, muscle relaxants and vasodepressants.
Claim 3
Dependent Claim
29 words
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.
Claim 4
Dependent Claim
26 words
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.
Claim 5
Dependent Claim
28 words
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.
Claim 6
Dependent Claim
25 words
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.
Claim 7
Dependent Claim
25 words
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.
Claim 8
Dependent Claim
21 words
A composition as defined in claim 1, wherein the oil-soluble pharmacological agent is a muscle relaxant from the compounds of phenyramidol.
Claim 9
Dependent Claim
117 words
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, chloroalose, tribromoethanol, pentazocine, phenylbutazone, cyclandelate, benzocaine, secobarbital, quatacaine, lidocaine, thiopental, pentobarbital, diazepam, and methoxyflurane.
Claim 10
Dependent Claim
117 words
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, chloroalose, tribromoethanol, pentazocine, phenylbutazone, cyclandelate, benzocaine, secobarbital, quatacaine, lidocaine, thiopental, pentobarbital, diazepam, and methoxyflurane.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-09-17 | 1983-03-19 | 1983-09-18 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-09-17 | 1987-03-19 | 1987-09-18 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-09-17 | 1991-03-19 | 1991-09-18 | $7700.00 | Window Closed / Lapsed |