Patent US5616342A successfully refreshed from Google Patents.
US5616342A
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Emulsioin suitable for administering a poorly water-soluble photosensitizing compound and use thereof
Assignee: Pfizer Health AB
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Filing: 1995-04-11
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Granted: 1997-04-01
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Expires: 2015-04-11
Abstract
Abstract Emulsion comprising a lipoid as a hydrophobic phase dispersed in a hydrophilic phase, a poorly water-soluble photosensitizing compound, surfactant, and as a cosurfactant a salt of a bile acid is provided that is suitable for administering to a patient.
Inventors
- 👤 Robert T. Lyons
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 03:34
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/40; A61K31/409; A61K41/00; A61K41/0057; A61K41/0071; A61K9/00; A61K9/10; A61K9/107; A61K9/1075
Claims Analysis
Total Claims: 32
Claim 1
Independent Claim
89 words
An emulsion for administering a poorly water-soluble, pharmacologically active, photosensitizing pyrrole-based macrocyclic compound to a patient comprising a pharmacologically acceptable lipid as a hydrophobic phase dispersed in a hydrophilic phase, an effective amount of said photosensitizing pyrrole-based macrocyclic compound, a phospholipids stabilizer, and as a costabilizer, a pharmaceutically acceptable salt of a bile acid selected from the group consisting of cholic acid, deoxycholic acid, glycocholic acid; and mixtures thereof, and wherein the concentration of said pharmaceutically acceptable salt is about 0.01 to about 1.0 g/100 ml of the emulsion.
Claim 2
Dependent Claim
89 words
An emulsion for administering a poorly water-soluble, pharmacologically active, photosensitizing pyrrole-based macrocyclic compound to a patient comprising a pharmacologically acceptable lipid as a hydrophobic phase dispersed in a hydrophilic phase, an effective amount of said photosensitizing pyrrole-based macrocyclic compound, a phospholipids stabilizer, and as a costabilizer, a pharmaceutically acceptable salt of a bile acid selected from the group consisting of cholic acid, deoxycholic acid, glycocholic acid; and mixtures thereof, and wherein the concentration of said pharmaceutically acceptable salt is about 0.01 to about 1.0 g/100 ml of the emulsion.
Claim 3
Dependent Claim
45 words
The emulsion of claim 1 wherein said lipoid is selected from the group consisting of soybean oil, safflower oil, marine oil, black currant seed oil, borage oil, palm kernel oil, sunflower oil, cotton seed oil, olive oil, coconut oil and physical or interesterified mixtures thereof.
Claim 4
Dependent Claim
22 words
The emulsion of claim 1 wherein said lipoid is a triglyceride having a fatty acid chain length of 8 to 10 carbons.
Claim 5
Dependent Claim
15 words
The emulsion of claim 1 wherein said lipoid is the triglycerides distilled from coconut oil.
Claim 6
Dependent Claim
12 words
The emulsion of claim 1 wherein said stabilizer is egg yolk phospholipids.
Claim 7
Dependent Claim
17 words
The emulsion of claim 1 wherein the particles have a mean diameter of less than 5 mlcrons.
Claim 8
Dependent Claim
13 words
The emulsion of claim 1 wherein said diameter is 0.5 mlcrons or less.
Claim 9
Dependent Claim
51 words
The emulsion of claim 1 wherein the amount of said photosensitizing compound is about 0.01 to about 1 g/100 ml, the amount of said lipoid is about 5 to about 40 g/100 ml, and the amount of said salt of a bile acid is about 0.05 to about 0.4 g/100 ml.
Claim 10
Dependent Claim
19 words
The emulsion of claim 1 wherein the amount of said stabilizer is about 0.3 to about 3 g/100 ml.
Claim 11
Dependent Claim
11 words
The emulsion of claim 1 which further includes an isotonic agent.
Claim 12
Dependent Claim
22 words
The emulsion of claim 10 wherein said isotonic agent is present in an amount of about 0.4 to about 4 g/100 ml.
Claim 13
Dependent Claim
11 words
The emulsion of claim 10 wherein said isotonic agent is glycerin.
Claim 14
Dependent Claim
10 words
The emulsion of claim 1 which further includes an antioxidant.
Claim 15
Dependent Claim
21 words
The emulsion of claim 13 wherein the antioxidant is present in an amount of about 0.02 to about 0.2 g/100 ml.
Claim 16
Dependent Claim
10 words
The emulsion of claim 14 wherein said antioxidant is α-tocopherol.
Claim 17
Dependent Claim
18 words
The emulsion of claim 1 wherein said salt of a bile acid is a salt of cholic acid.
Claim 18
Dependent Claim
11 words
The emulsion of claim 16 wherein said salt is sodium cholate.
Claim 19
Dependent Claim
10 words
The emulsion of claim 1 which further includes ethyl alcohol.
Claim 20
Dependent Claim
20 words
The emulsion of claim 18 wherein the amount of said ethyl alcohol is about 0.2 to about 2 grams/100 ml.
Claim 21
Dependent Claim
45 words
The emulsion of claim 1 wherein said pyrrolic macrocyclic compound is selected from the group consisting of at least one of naturally occurring or synthetic porphyrins, naturally occurring or synthetic chlorins, naturally occurring or synthetic bacteriochlorins, synthetic isobacteriochlorins, phthalocyanines, naphthalocyanines, and expanded pyrrole-based macrocyclic systems.
Claim 22
Dependent Claim
14 words
The emulsion of claim 20 wherein said pyrrolic macrocyclic compound is tin ethyl etiopurpurin.
Claim 23
Dependent Claim
13 words
The emulsion of claim 20 wherein said pyrrolic macrocyclic compound is zinc phthalocyanine.
Claim 24
Dependent Claim
13 words
The emulsion of claim 20 wherein said pyrrolic macrocyclic compound is benzoporphyrin derivative.
Claim 25
Dependent Claim
14 words
The emulsion of claim 20 wherein said pyrrolic macrocyclic compound is meso-tetra (hydroxyphenyl) chlorin.
Claim 26
Dependent Claim
21 words
A method for treating a patient with a photosensitizing compound which comprises administering to said patient the emulsion of claim 1.
Claim 27
Dependent Claim
10 words
The method of claim 25 wherein said administering is intravenously.
Claim 28
Dependent Claim
23 words
The method of claim 25 which further comprises exposing said pyrrolic macrocyclic compound to light after administering in order to activate said compound.
Claim 29
Dependent Claim
48 words
A method for diagnosing a patient for tumors which comprises administering to said patient the emulsion of claim 1 and then exposing said patient to light of a suitable wavelength that would induce fluorescence of any photosensitizing compound preferentially maintained by hyperproliferating or abnormal cells in said patient.
Claim 30
Dependent Claim
14 words
The emulsion of claim 1 having a pH of about 7.5 to about 9.5.
Claim 31
Dependent Claim
22 words
The emulsion of claim 20 wherein said expanded pyrrole-base macrocyclic systems is selected from the group consisting of porphycenes, sapphyrins and texaphyrins.
Claim 32
Dependent Claim
47 words
The emulsion of claim 1 wherein said stabilizer consists of phospholipids in an amount of about 0.3 to about 3 g/100 ml of said emulsion and said costabilizer consists of said salt of a bile acid in an amount of about 0.05 to about 0.4 g/100 ml.
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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) | 2000-03-31 | 2000-09-30 | 2001-04-01 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2004-03-31 | 2004-09-30 | 2005-04-01 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2008-03-31 | 2008-09-30 | 2009-04-01 | $7700.00 | Window Closed / Lapsed |