US4861580A
Expired / Lapsed
US
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Composition using salt form of organic acid derivative of alpha-tocopheral
Assignee: Elan Pharmaceuticals LLC
•
Filing: 1986-09-24
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Granted: 1989-08-29
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Expires: 2006-09-24
Abstract
Abstract Methods and compositions are described for the preparation of alpha-tocopherol vesicles, the bilayers of which comprise a salt form of an organic acid derivative of alpha-tocopherol such as the Tris salt form of alpha-tocopherol hemisuccinate. The method is rapid and efficient and does not require the use of organic solvents. The alpha-tocopherol vesicles may be used to entrap compounds which are insoluble in aqueous solutions. Such preparations are especially useful for entrapping bioactive agents of limited solubility, thus enabling administration in vivo.
Inventors
- 👤 Andrew S. Janoff
- 👤 Lois E. Bolcsak
- 👤 Alan L. Weiner
- 👤 Paul A. Tremblay
- 👤 Michael V. W. Bergamini
- 👤 Robert L. Suddith
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-25 00:47
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/10; A61K9/127; A61K9/1277; A61K31/00; A61K31/33; A61K31/335; A61K31/35; A61K31/352; A61K31/353; A61K31/355; A61K9/1271; A61K9/1272; A61P; A61P25/00; A61P25/04; A61P27/00; A61P27/02; A61P29/00; A61P31/00; A61P31/04; A61P31/10; A61P31/12; A61P33/00; A61P33/10; A61P37/00; A61P37/02; A61P37/06; Y; Y10; Y10S; Y10S436/00; Y10S436/829; Y10T; Y10T428/00; Y10T428/29; Y10T428/2982; Y10T428/2984
Claims Analysis
Total Claims: 53
Claim 1
Independent Claim
23 words
A composition comprising a tris(hydroxymethyl)aminomethane, a 2-amino-2-methyl-1,3-propanediol, a 2-aminoethanol, a bis-tris-propane, or a triethanolamine salt form of an organic acid derivative of alpha-tocopherol.
Claim 2
Dependent Claim
23 words
A composition comprising a tris(hydroxymethyl)aminomethane, a 2-amino-2-methyl-1,3-propanediol, a 2-aminoethanol, a bis-tris-propane, or a triethanolamine salt form of an organic acid derivative of alpha-tocopherol.
Claim 3
Dependent Claim
12 words
The composition according to claim 1 in which the alpha-tocopherol is D-alpha-tocopherol.
Claim 4
Dependent Claim
17 words
A pharmaceutical composition comprising the composition according to claim 2 and a pharmaceutically acceptable carrier or diluent.
Claim 5
Dependent Claim
19 words
The composition according to claim 1 comprising a tris(hydroxymethyl)aminomethane salt form of an organic acid derivative of a alpha-tocopherol.
Claim 6
Dependent Claim
23 words
The composition according to claim 1 in which the organic acid derivative comprises a carboxylic acid, a dicarboxylic acid or a polycarboxylic acid.
Claim 7
Dependent Claim
22 words
The composition according to claim 5 in which the carboxylic acid is an aliphatic carboxylic acid containing up to five carbon atoms.
Claim 8
Dependent Claim
16 words
The composition according to claim 5 in which the dicarboxylic acid comprises an aliphatic dicarboxylic acid.
Claim 9
Dependent Claim
18 words
The composition according to claim 7 in which the aliphatic dicarboxylic acid contains up to seven carbon atoms.
Claim 10
Dependent Claim
15 words
The composition according to claim 8 in which the aliphatic dicarboxylic acid is succinic acid.
Claim 11
Dependent Claim
22 words
The composition according to claim 1 in which the organic acid is an hydroxy acid, an amino acid or a polyamino acid.
Claim 12
Dependent Claim
17 words
The composition according to claim 1 comprising the tris(hydroxymethyl)aminomethane salt form of a hemisuccinate derivative of alpha-tocopherol.
Claim 13
Dependent Claim
15 words
The composition, according to claim 1 in which the composition additionally comprises a bioactive agent.
Claim 14
Dependent Claim
24 words
The composition according to claim 12 in which the bioactive agent is selected from the group consisting of antibacterial, antifungal, antiviral and antiparasitic compounds.
Claim 15
Dependent Claim
32 words
The composition according to claim 13 in which the antifungal compound is miconazole, terconazole, econazole, isoconazole, tioconazole, bifonazole, clotrimazole, ketoconazole, butaconazole, itraconazole, oxiconazole, fenticonazole, nystatin, naftifine, amphotericin B, zinoconazole or ciclopirox olamine.
Claim 16
Dependent Claim
23 words
The composition according to claim 12 in which the bioactive agent is selected from the group consisting of peptides, proteins, glycoproteins and lipoproteins.
Claim 17
Dependent Claim
14 words
The composition according to claim 15 in which the bioactive agent comprises growth hormone.
Claim 18
Dependent Claim
25 words
The composition according to claim 12 in which the bioactive agent is selected from the group consisting of dyes, radiolabels, radio-opaque compounds and fluorescent compounds.
Claim 19
Dependent Claim
25 words
The composition according to claim 12 in which the bioactive agent is selected from the group consisting of anti-inflammatory, antiglaucoma, mydriatic, analgesic and anesthetic compounds.
Claim 20
Dependent Claim
13 words
The composition according to claim 12 in which the bioactive agent comprises pilocarpine.
Claim 21
Dependent Claim
19 words
The composition according to claim 12 in which the bioactive agent comprises a narcotic, a psychoactive or anxiolytic agent.
Claim 22
Dependent Claim
14 words
The composition according to claim 12 in which the bioactive agent comprises a vitamin.
Claim 23
Dependent Claim
14 words
The composition according to claim 12 in which the organic acid is succinic acid.
Claim 24
Dependent Claim
24 words
A composition comprising a salt form of an organic acid derivative of alpha-tocopherol wherein the salt form is derived from an ionizable bioactive agent.
Claim 25
Dependent Claim
24 words
A composition comprising a salt form of an organic acid derivative of alpha-tocopherol wherein the salt form is derived from an ionizable bioactive agent.
Claim 26
Dependent Claim
14 words
The composition according to claim 23 in which the organic acid is succinic acid.
Claim 27
Dependent Claim
15 words
The composition according to claim 23 in which ionizable bioactive agent comprises an antifungal compound.
Claim 28
Dependent Claim
32 words
The composition according to claim 23 in which the antifungal compound is miconazole, terconazole, econazole, isoconazole, tioconazole, bifonazole, clotrimazole, ketoconazole, butaconazole, itraconazole, oxiconazole, fenticonazole, nystatin, naftifine, amphotericin B, zinoconazole or ciclopirox olamine.
Claim 29
Dependent Claim
28 words
The composition according to claim 23 in which the ionizable bioactive agent is a peptide, protein, glycoprotein or lipoprotein salt form of an organic acid derivative of alpha-tocopherol.
Claim 30
Dependent Claim
24 words
The composition according to claim 23 in which the ionizable bioactive agent is a pilocarpine salt form of an organic acid derivative of alpha-tocopherol.
Claim 31
Dependent Claim
14 words
The composition according to claim 28 additionally comprising a mucomimetic agent and a preservative.
Claim 32
Dependent Claim
26 words
The composition according to claim 29 wherein the mucomimetic agent is selected from the group consisting of hyaluronic acid, chondroitin sulfate, hydroxylpropyl methylcellulose, and polyvinyl alcohol.
Claim 33
Dependent Claim
16 words
The composition according to claim 30 wherein the mucomimetic agent is hydroxypropyl methylcellulose or polyvinyl alcohol.
Claim 34
Dependent Claim
21 words
A method of treating glaucoma comprising administering an anti-glaucoma-effective amount of the pharmaceutical composition according to claim 30 to a subject.
Claim 35
Dependent Claim
16 words
The composition according to claim 29 wherein the preservative is sorbic acid EDTA or benzylkonium chloride.
Claim 36
Dependent Claim
25 words
A composition comprising a salt form of an organic acid derivative of a sterol and a salt form of an organic acid derivative of alpha-tocopherol.
Claim 37
Dependent Claim
25 words
A composition comprising a salt form of an organic acid derivative of a sterol and a salt form of an organic acid derivative of alpha-tocopherol.
Claim 38
Dependent Claim
11 words
The composition according to claim 34 additionally comprising a bioactive agent.
Claim 39
Dependent Claim
23 words
The composition according to claim 35 wherein the bioactive agent is selected from the group consisting of peptides, polypeptides, proteins, glycoproteins, and lipoproteins.
Claim 40
Dependent Claim
13 words
The composition according to claim 36 wherein the polypeptide is an immunosuppressive agent.
Claim 41
Dependent Claim
12 words
The composition according to claim 36 wherein the polypeptide is cyclosporin A.
Claim 42
Dependent Claim
18 words
A composition according to claim 34 in which at least one salt form comprises an ionizable bioactive agent.
Claim 43
Dependent Claim
23 words
The composition according to claim 34 wherein the bioactive agent is selected from the group consisting of antibacterial, antifungal, antiviral and antiparasitic compounds.
Claim 44
Dependent Claim
24 words
The composition according to claim 34 wherein the bioactive agents is selected from the group consisting of dyes, radiolabels, radio-opque compounds and fluorescent compounds.
Claim 45
Dependent Claim
24 words
The composition according to claim 34 wherein the bioactive agent is selected from the group consisting of anti-inflammatory, antiglaucoma, mydriatic, analgesic, and anesthetic compounds.
Claim 46
Dependent Claim
17 words
A pharmaceutical composition comprising the composition according to claim 34 and a pharmaceutically acceptable carrier or diluent.
Claim 47
Dependent Claim
20 words
The composition according to claim 34 wherein the sterol is cholesterol hemisuccinate tris(hydroxymethyl)aminomethane and the alpha-tocopherol is alpha-tocopherol hemisuccinate tris(hydroxymethyl)aminomethane.
Claim 48
Dependent Claim
11 words
The composition according to claim 44 additionally comprising a bioactive agent.
Claim 49
Dependent Claim
16 words
A pharmaceutical composition comprising the composition of claim 44 and a pharmaceutically acceptable carrier or diluent.
Claim 50
Dependent Claim
22 words
The composition according to claim 34 wherein the salt form of the sterol or the alpha-tocopherol is a bioactive agent salt form.
Claim 51
Dependent Claim
11 words
A composition/comprising cholesterol hemisuccinate tris(hydroxymethyl)aminomethane, alpha-tocopherol hemisuccinate tris(hydroxymethyl)aminomethane, and cyclosporin A.
Claim 52
Dependent Claim
11 words
A composition/comprising cholesterol hemisuccinate tris(hydroxymethyl)aminomethane, alpha-tocopherol hemisuccinate tris(hydroxymethyl)aminomethane, and cyclosporin A.
Claim 53
Dependent Claim
17 words
A pharmaceutical composition comprising the composition according to claim 48 and a pharmaceutically acceptable carrier or diluent.
References Cited (Backward Citations)
US3136695A
Cited
US3993754A
Cited
US4145410A
Cited
US4224179A
Cited
US4235871A
Cited
US4193983A
Cited
US4271196A
Cited
US4342739A
Cited
US4411894A
Cited
US4438052A
Cited
US4376118A
Cited
US4522803A
Cited
WO1985000968A1
Cited
US4721612A
Cited
US4665204A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1992-08-28 | 1993-02-27 | 1993-08-29 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-08-28 | 1997-02-27 | 1997-08-29 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-08-28 | 2001-02-27 | 2001-08-29 | $7700.00 | Window Closed / Lapsed |