US5364632A
Expired / Lapsed
US
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Medicinal emulsions
Assignee: Yissum Research Development Co of Hebrew University of Jerusalem
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Filing: 1993-03-09
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Granted: 1994-11-15
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Expires: 2013-03-09
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.
Inventors
- 👤 Simon Benita
- 👤 Menashe Levy
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 11:39
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/10; A61K9/107; A61K9/1075
Claims Analysis
Total Claims: 35
Claim 1
Independent Claim
84 words
In a pharmaceutical composition consisting essentially of a hydrophobic drug and a carrier, the improvement being in a carrier which is an oil-in-water emulsion of droplet sizes of 0.1 to 0.27 μm consisting essentially of: (i) about 3-50% (w/v) of an oily carrier consisting of a medium chain triglyceride (MCT) oil or (ii) 0.5-20% (w/v) phospholipids; (iii) about 0.3-10% (w/v) of a non-ionic surfactant; and (iv) about 0.5-5% (w/v) of a ionic surfactant selected from the group consisting of cholic acid and deoxycholic acid.
Claim 2
Dependent Claim
84 words
In a pharmaceutical composition consisting essentially of a hydrophobic drug and a carrier, the improvement being in a carrier which is an oil-in-water emulsion of droplet sizes of 0.1 to 0.27 μm consisting essentially of: (i) about 3-50% (w/v) of an oily carrier consisting of a medium chain triglyceride (MCT) oil or (ii) 0.5-20% (w/v) phospholipids; (iii) about 0.3-10% (w/v) of a non-ionic surfactant; and (iv) about 0.5-5% (w/v) of a ionic surfactant selected from the group consisting of cholic acid and deoxycholic acid.
Claim 3
Dependent Claim
105 words
A pharmaceutical carrier consisting essentially of a hydrophobic drug and a carrier, wherein said carrier is an oil-in-water pharmaceutical composition of a droplet size of about 0.1-0.27 μm (i) about 3.50% (w/v) of an oily carrier consisting of a medium chain triglyceride (MCT) oil and up to 50% (w/v) of at least one vegetable oil selected from the group consisting of soybean oil, cotton seed oil, olive oil and sesame oil; (ii) 0.5-20% (w/v) phospholipids; (iii) about 0.3-10% (w/v) of a non-ionic surfactant; and (iv) about 0.5-5% (w/v) of a ionic surfactant selected from the group consisting of cholic acid deoxycholic acid and salts thereof.
Claim 4
Dependent Claim
105 words
A pharmaceutical carrier consisting essentially of a hydrophobic drug and a carrier, wherein said carrier is an oil-in-water pharmaceutical composition of a droplet size of about 0.1-0.27 μm (i) about 3.50% (w/v) of an oily carrier consisting of a medium chain triglyceride (MCT) oil and up to 50% (w/v) of at least one vegetable oil selected from the group consisting of soybean oil, cotton seed oil, olive oil and sesame oil; (ii) 0.5-20% (w/v) phospholipids; (iii) about 0.3-10% (w/v) of a non-ionic surfactant; and (iv) about 0.5-5% (w/v) of a ionic surfactant selected from the group consisting of cholic acid deoxycholic acid and salts thereof.
Claim 5
Dependent Claim
13 words
A carrier according to claim 1 in a form suitable for parenteral administration.
Claim 6
Dependent Claim
13 words
A carrier according to claim 1 in a form suitable for topical administration.
Claim 7
Dependent Claim
13 words
A carrier according to claim 1 in a form suitable for oral administration.
Claim 8
Dependent Claim
13 words
A carrier according to claim 1 in a form suitable for occular administration.
Claim 9
Dependent Claim
32 words
A carrier according to claim 2, in which the proportion of the non aqueous phase which comprises said oily carrier, phospholiplids, non-ionic surfactant and said ionic surfactant does not exceed 30% (w/v).
Claim 10
Dependent Claim
18 words
A carrier according to claim 7 in which the proportion of said non-aqueous phase does not exceed 25%.
Claim 11
Dependent Claim
18 words
A carrier according to claim 1, wherein the relative proportions of the oily carrier is about 10-20% (w/v).
Claim 12
Dependent Claim
17 words
A carrier according to claim 1, wherein the relative proportions of the phospholipid is about 0.5-2% (w/v).
Claim 13
Dependent Claim
17 words
A carrier according to claim 10, wherein the relative proportion of the phospholipid is about 0.75% (w/v).
Claim 14
Dependent Claim
18 words
A carrier according to claim 1, wherein the proportion of the said ionic surfactant is about 4-6.6% (w/v).
Claim 15
Dependent Claim
13 words
A carrier according to claim 1, wherein the non ionic surfactant is Poloxamer.
Claim 16
Dependent Claim
26 words
A carrier according to claim 1, wherein the said ionic surfactant is selected from the group consisting of cholic acid, deoxycholic acid and their sodium salt.
Claim 17
Dependent Claim
36 words
A composition according to claim 1 wherein said hydrophobic drugs are selected from the group consisting of antibiotics or narcotic drugs or non-steroidal anti-inflammatory hydrophobic drugs, hydrophobic steroids, hydrophobic azoles, hydrophobic polypeptides, hydrophobic cephalosporines and dimercaptol.
Claim 18
Dependent Claim
36 words
A carrier according to claim 14, wherein said drug is selected from the group consisting of amphotericin B, morphine-base, diazepam, fluphenazine deconate, lorazepam, piroxicam, indomethacin, progesterone, testosterone propionate, miconazole, clotrimazole, cyclosporine, deoxycortone, calciferol, cephalosporine and dimercaptol.
Claim 19
Dependent Claim
13 words
A carrier according to claim 16, wherein said hydrophobic drug is amphotericin B.
Claim 20
Dependent Claim
12 words
A Composition according to claim 16, wherein said hydrophobic drug is diazepam.
Claim 21
Dependent Claim
16 words
A carrier according to claim 16, wherein said hydrophobic drug is morphine, indomethacin, cyclosporine or miconazole.
Claim 22
Dependent Claim
135 words
A pharmaceutical composition comprising a drug and a carrier wherein the carrier is an oil-in-water pharmaceutical composition consisting essentially of: (i) about 3-50% (w/v) of (a) a first component of a medium chain triglyceride (MOT) oil; or (b) a mixture of the first component with a second component of a vegetable oil, wherein the amount of the second component of the mixture is present in an equal or lesser amount compared to the first component; (ii) about 0.5-20% (w/v) of a third component of a phoepholipid; (iii) about 0.3-10% (w/v) of a non-ionic surfactant; and (iv) about 0.5-5% (w/v) of an ionic surfactant selected from the group consisting of cholic acid, deoxycholic acid, a taurocholate, or a salt thereof; wherein the pharmaceutical composition has a droplet size of between about 0.05 to about 0.27 μm.
Claim 23
Dependent Claim
135 words
A pharmaceutical composition comprising a drug and a carrier wherein the carrier is an oil-in-water pharmaceutical composition consisting essentially of: (i) about 3-50% (w/v) of (a) a first component of a medium chain triglyceride (MOT) oil; or (b) a mixture of the first component with a second component of a vegetable oil, wherein the amount of the second component of the mixture is present in an equal or lesser amount compared to the first component; (ii) about 0.5-20% (w/v) of a third component of a phoepholipid; (iii) about 0.3-10% (w/v) of a non-ionic surfactant; and (iv) about 0.5-5% (w/v) of an ionic surfactant selected from the group consisting of cholic acid, deoxycholic acid, a taurocholate, or a salt thereof; wherein the pharmaceutical composition has a droplet size of between about 0.05 to about 0.27 μm.
Claim 24
Dependent Claim
25 words
The pharmaceutical composition of claim 20 wherein the first component or mixture of first and second components is present in an amount of about 5-25%.
Claim 25
Dependent Claim
22 words
The pharmaceutical composition of claim 20 wherein the second component of the mixture is present in an amount of 10% or less.
Claim 26
Dependent Claim
25 words
The pharmaceutical composition of claim 20 wherein the first component or mixture of first and second components is present in an amount of about 10-20%.
Claim 27
Dependent Claim
21 words
The pharmaceutical composition of claim 20 wherein the cholic acid or deoxycholic acid is in the form of the sodium salt.
Claim 28
Dependent Claim
20 words
The pharmaceutical composition of claim 20 wherein the vegetable oil is soybean oil, cottonseed oil, olive oil or sesame oil.
Claim 29
Dependent Claim
19 words
The pharmaceutical composition of claim 20 wherein the phospholipids are present in an amount of about 0.75 to 2%.
Claim 30
Dependent Claim
26 words
The pharmaceutical composition of claim 20 wherein the phospholipids are selected from the group consisting of lecithin, mixtures of lecithin, and phosphatidylethanolamine, or soybean oil phospholipids.
Claim 31
Dependent Claim
17 words
The pharmaceutical composition of claim 20 wherein the non-ionic surfactant is a copolymer of polyoxyethylene and polyoxypropylene.
Claim 32
Dependent Claim
20 words
The pharmaceutical composition of claim 20 wherein the non-ionic surfactant is present in an amount of about 0.5 to 2%.
Claim 33
Dependent Claim
20 words
The pharmaceutical composition of claim 20 wherein the ionic surfactant is present in an amount of about 0.5 to 2%.
Claim 34
Dependent Claim
11 words
The pharmaceutical composition of claim 20 wherein the drug is hydrophobic.
Claim 35
Dependent Claim
15 words
The pharmaceutical composition of claim 20 wherein the ionic surfactant is an alkali metal salt.
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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) | 1997-11-14 | 1998-05-16 | 1998-11-15 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2001-11-14 | 2002-05-16 | 2002-11-15 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2005-11-14 | 2006-05-16 | 2006-11-15 | $7700.00 | Window Closed / Lapsed |