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Patent US4567161A successfully refreshed from Google Patents.
US4567161A
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US
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Liquid active ingredient concentrates for preparation of microemulsions
Assignee: A Natterman und Cie GmbH
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Filing: 1983-06-28
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Granted: 1986-01-28
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Expires: 2003-06-28
Abstract
Abstract Liquid, active substance formulations containing an active substance insoluble or poorly soluble in water, or a mixture, a phospholipid, a special co-emulsifier (glycerinester in which the 1 or 2 OH groups have been esterized with hydrocarbon atoms of 8-16, preferably 8-10, C atoms by means of fatty acids and the 3 or remaining OH group of the glycerin body has been etherized with polyethyleneglycol, specifically, with 6-30, preferably 6-15 ethyleneoxide units) and a liquid carrier, the molar ratio of phospholipid to co-emulsifier being from 1:1 to 1:4, and the formulations being such that when added to water they form a transparent liquid system in the form of a microemulsion, with a degree of fineness of 10-200 nm in the lipid phase.
Inventors
- 👤 Ulrich Posanski
- 👤 Miklos Ghyczy
- 👤 Kurt-Heinz Bauer
- 👤 Armin Wendel
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 12:35
CPC Classifications
A; A01; A01N; A01N25/00; A01N25/02; A61; A61K; A61K9/00; A61K9/10; A61K9/107; A61K9/1075; C; C09; C09K; C09K23/00; C09K23/017
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
155 words
Liquid formulations which contain a component or mixture of components selected from the group consisting of one or more pharmaceutically active substance, said component being insoluble or poorly soluble in water, and conventional additives and auxiliary substances in a lipophilic liquid or in a liquid mixture with a phospholipid selected from the group consisting of phosphatidyl choline, phosphatidyl ethanol amine, phosphatidic acid, phosphatidyl inositol, N-acylphosphatidyl ethanol amine and mixtures thereof, and an ethoxylated derivative of glycerin ester, with fatty acids as co-emulsifier, wherein the lipophilic liquid contains a lipophilic carrier liquid and the first or second OH groups of the glycerin or the glycerin ester are esterized by means of the fatty acids with hydrocarbon chains of from 8 to 16 C atoms and the third of remaining OH group of the glycerin body is etherized with the polyethyleneglycol with 6-30 ethyleneoxide units, the molar ratio of phospholipid to co-emulsifier being from 1:1 to 1:4.
Claim 2
Dependent Claim
155 words
Liquid formulations which contain a component or mixture of components selected from the group consisting of one or more pharmaceutically active substance, said component being insoluble or poorly soluble in water, and conventional additives and auxiliary substances in a lipophilic liquid or in a liquid mixture with a phospholipid selected from the group consisting of phosphatidyl choline, phosphatidyl ethanol amine, phosphatidic acid, phosphatidyl inositol, N-acylphosphatidyl ethanol amine and mixtures thereof, and an ethoxylated derivative of glycerin ester, with fatty acids as co-emulsifier, wherein the lipophilic liquid contains a lipophilic carrier liquid and the first or second OH groups of the glycerin or the glycerin ester are esterized by means of the fatty acids with hydrocarbon chains of from 8 to 16 C atoms and the third of remaining OH group of the glycerin body is etherized with the polyethyleneglycol with 6-30 ethyleneoxide units, the molar ratio of phospholipid to co-emulsifier being from 1:1 to 1:4.
Claim 3
Dependent Claim
21 words
Liquid formulations as set forth in claim 1, wherein the molar ratio of phospholipid to co-emulsifier is from 1:1 to 1:2.
Claim 4
Dependent Claim
18 words
Liquid formulations as set forth in claim 1, wherein the molar ratio of phopholipid to co-emulsifier is 1:2.
Claim 5
Dependent Claim
24 words
Liquid formulations as set forth in claim 1, wherein said formulations contain mixtures of glycerides, fatty acids, and organic solvents as a carrier liquid.
Claim 6
Dependent Claim
43 words
Liquid formulations as set forth in claim 1, wherein said formulations consist of 5-50 wght.% phospholipids 5-80 wght.% co-emulsifer 10-60 wght.% carrier liquid 0.1-50 wght.% component or mixture of components insoluble or poorly soluble in water 0.1-10 wght.% other additives and auxiliary substances.
Claim 7
Dependent Claim
34 words
Liquid formulations as set forth in claim 1, wherein said formulations contain a biologically active substance or a mixture of such substances as component or mixture of components insoluble or poorly soluble in water.
Claim 8
Dependent Claim
19 words
Liquid formulations as set forth in claim 6 wherein said component is a pharmaceutically active substance insoluble in water.
Claim 9
Dependent Claim
32 words
Liquid formulations as set forth in claim 7, wherein said formulations contain acetylsalicylic acid, ibuprofen, benzodiazepine, nitroglycerin, isosorbiddinitrate, corticoide, chloramphenicol, dexamesthson, mebendazol, grieseofulvin, miconazol, nitrofurantoin, furosemid, clotrimazol, or metronidazol as said component.
Claim 10
Dependent Claim
29 words
Application of liquid formulations as set forth in claim 1 for the production of transparent, aqueous liquid systems, in which the lipid phase has a fineness of 10-200 nm.
References Cited (Backward Citations)
US3203862A
Cited
US3169094A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1989-01-27 | 1989-07-29 | 1990-01-28 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1993-01-27 | 1993-07-29 | 1994-01-28 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1997-01-27 | 1997-07-29 | 1998-01-28 | $7700.00 | Window Closed / Lapsed |