EP0391369B1
Expired / Lapsed
EP
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Medicinal emulsions
Assignee: Yissum Research Development Co of Hebrew University of Jerusalem
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Filing: 1990-04-04
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Granted: 1994-08-31
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Expires: 2010-04-04
Abstract
Abstract A pharmaceutical composition being an oil in water type emulsion which comprises an effective amount of a lypophilic drug is provided. The composition comprises a synergistic combination consisting of about 3-50% of an oily carrier consisting of MCT oil optionally in combination with vegetable oil, about 0.05%-20% of a phospholipid, about 0.03-10% of a non-ionic surfactant, and about 0.05-5% of an ionic surfactant selected from the group consisting of bile-duct surface active agent, cholic acid and their derivatives. Also provided is a novel method for preparing said composition.
Inventors
- 👤 Benita Simon
- 👤 Levy Menashe
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-23 14:54
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/10; A61K9/107; A61K9/1075
Claims Analysis
Total Claims: 23
Claim 1
Independent Claim
151 words
A process for the preparation of a composition of the oil-in-water type emulsion comprising an effective amount of a hydrophobic drug, about 3 to 50% (w/v) of an oily carrier consisting of medium chain triglyceride (MCT) oil, optionally in combination with vegetable oil, about 0.05 to 20% (w/v) of phospholipid, about 0.03 to 10% (w/v) of a non-ionic surfactant, and about 0.05 to 10% (w/v) of an ionic surfactant selected from bile-duct surface active agents, cholic acid and deoxycholic acid, and their surface active derivatives and salts, which process comprises: (a) preparing a liposome mixture comprising the phospholipids, the non-ionic surfactant, the said ionic surfactant, and where the drug has a poor oil solubility, also comprising said drug; (b) preparing an oily mixture comprising said oily carrier, and where the drug is lipophilic, also comprising said drug; (c) mixing said liposome mixture with said oily mixture, whereby said emulsion is obtained.
Claim 2
Dependent Claim
34 words
A process according to Claim 1, wherein the so obtained emulsion is subjected to further stages, in which smaller droplets in the emulsion are obtained and/or the homogeneity of the droplets' size is increased.
Claim 3
Dependent Claim
16 words
A process according to Claim 1 or 2, wherein said drug has a poor oil solubility.
Claim 4
Dependent Claim
18 words
A process according to any one of Claims 1 to 3 in a form suitable for parenteral administration.
Claim 5
Dependent Claim
18 words
A process according to any one of Claims 1 to 3 in a form suitable for topical administration.
Claim 6
Dependent Claim
18 words
A process according to any one of Claims 1 to 3 in a form suitable for oral administration.
Claim 7
Dependent Claim
18 words
A process according to any one of Claims 1 to 3 in a form suitable for ocular administration.
Claim 8
Dependent Claim
31 words
A process according to Claim 4, in which the relative proportion of the non-aqueous phase which comprises said oily carrier, phospholipids, non-ionic surfactant and said ionic surfactant does not exceed 30%.
Claim 9
Dependent Claim
19 words
A process according to Claim 8, in which the relative proportion of said non-aqueous phase does not exceed 25%.
Claim 10
Dependent Claim
23 words
A process according to any one of the preceding claims, wherein the relative proportion of the oily carrier is about 10 to 20%
Claim 11
Dependent Claim
22 words
A process according to any one of the preceding claims, wherein the relative proportion of the phospholipid is about 0.5 to 2%.
Claim 12
Dependent Claim
16 words
A process according to Claim 11, wherein the relative proportion of the phospholipid is about 0.75%.
Claim 13
Dependent Claim
23 words
A process according to any one of the preceding claims, wherein the relative proportion of the non-ionic surfactant is about 0.5 to 3%.
Claim 14
Dependent Claim
24 words
A process according to any one of the preceding claims, wherein the relative proportion of the said non-ionic surfactant is about 3 to 10%.
Claim 15
Dependent Claim
20 words
A process according to Claim 14, wherein the relative proportion of the said ionic surfactant is about 4 to 6.6%.
Claim 16
Dependent Claim
30 words
A process according to any one of Claims 1 and 4 to 15, wherein the vegetable oil is selected from soybean oil, cotton seed oil, olive oil and sesame oil.
Claim 17
Dependent Claim
17 words
A process according to any one of the preceding claims, wherein the non-ionic surfactant is a poloxamer.
Claim 18
Dependent Claim
26 words
A process according to any one of the preceding claims, wherein the said ionic surfactant is selected from cholic acid, deoxycholic acid and their sodium salts.
Claim 19
Dependent Claim
41 words
A process according to any one of the preceding claims, wherein said drug is selected from hydrophobic or lipophilic antibiotics or narcotic drugs, hydrophobic benzodiazepines, non-steroidal anti-inflammatory lipophilic drugs, lipophilic steroids, lipophilic azoles, lipophilic polypeptides, lipophilic sterols, lipophilic cephalosporines and dimercaptol.
Claim 20
Dependent Claim
32 words
A process according to Claim 19, wherein said drug is selected from amphotericin B, morphine-base, diazepam, fluphenazine deconate, lorazepam, piroxicam, indomethacin, progesterone, testosterone propionate, miconazole, clotrimazole, cyclosporine, deoxycortone, calciferol, cephalosporine and dimercaptol.
Claim 21
Dependent Claim
11 words
A process according to Claim 20, wherein said drug is morphine.
Claim 22
Dependent Claim
20 words
A process according to any one of the preceding claims, wherein the mean oily droplet diameter is below 0.2 µm.
Claim 23
Dependent Claim
18 words
A process according to Claim 22, wherein the mean oily droplet diameter is about 0.1 to 0.15 µm.
References Cited (Backward Citations)
No citation records indexed.
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