EP0041795A2
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EP
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Injectable composition of rapamycin
Assignee: Wyeth Canada Inc
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Filing: 1981-05-27
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Granted: —
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Expires: 2001-05-27
Abstract
Abstract Described is an injectable composition comprising rapamycin and a nonionic surfactant selected from polyoxyethylated fatty acids, polyoxyethylated fatty alcohols or polyoxyethylated glycerine hydroxy fatty acid esters and a method of preparing said compositions. The composition provides enhanced blood levels of rapamycin in a mammal following injected administration thereof.
Inventors
- 👤 Surendra Nath Sehgal
- 👤 Harold Arthur Baker
- 👤 Anne Marie Sidorowicz
- 👤 Claude Vezina
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-31 21:41
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/70; A61K47/00; A61K47/06; A61K47/08; A61K47/10; A61K47/14; A61K47/44; A61K9/00; A61K9/0012; A61K9/0019; A61P; A61P31/00; A61P31/04; A61P31/10
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
42 words
An injectable composition of rapamycin, suitable for intravenous administration, which comprises about 1 to 20 milligrams of rapamycin per millilitre of the composition and a nonionic surfactant selected from polyoxyethylated fatty acids, polyoxyethylated fatty alcohols and polyoxyethylated glycerine hydroxy fatty acid esters.
Claim 2
Dependent Claim
42 words
An injectable composition of rapamycin, suitable for intravenous administration, which comprises about 1 to 20 milligrams of rapamycin per millilitre of the composition and a nonionic surfactant selected from polyoxyethylated fatty acids, polyoxyethylated fatty alcohols and polyoxyethylated glycerine hydroxy fatty acid esters.
Claim 3
Dependent Claim
21 words
A composition of Claim 1 containing an aqueous solution of about 1 to 50 percent by weight of the nonionic surfactant.
Claim 4
Dependent Claim
21 words
A composition of Claim 1 containing an aqueous solution of about 1 to 20 percent by weight of the nonionic surfactant.
Claim 5
Dependent Claim
23 words
A composition as claimed in Claim 1 or Claim 2 wherein the nonionic surfactant is polyoxyethylated castor oil or polyoxyethylated hydrogenated castor oil.
Claim 6
Dependent Claim
41 words
A composition of Claim 1 containing about 1 to 20 milligrams of rapamycin per millilitre of an aqueous solution of about 1 to 20 percent by weight of a nonionic surfactant selected from polyoxyethylated castor oil and polyoxyethylated hydrogenated castor oil.
Claim 7
Dependent Claim
112 words
A process for preparing an injectable composition, suitable for intravenous administration, comprising about 1 to 20 milligrams of rapamycin per millimeter of an aqueous solution of a nonionic surfactant selected from polyoxyethylated fatty acids, polyoxyethylated fatty alcohols and polyoxyethylated glycerin hydroxy fatty acid esters, which comprises dissolving rapamycin in an organic solvent which is capable of dissolving rapamycin and is miscible with the nonionic surfactant, and either (i) adding the nonionic surfactant, if required removing some or all of the organic solvent, and adding water; or (ii.) adding a solution of nonionic surfactant in water; the amounts of rapamycin and nonionic surfactant being predetermined to give the desired concentrations in the composition.
Claim 8
Dependent Claim
112 words
A process for preparing an injectable composition, suitable for intravenous administration, comprising about 1 to 20 milligrams of rapamycin per millimeter of an aqueous solution of a nonionic surfactant selected from polyoxyethylated fatty acids, polyoxyethylated fatty alcohols and polyoxyethylated glycerin hydroxy fatty acid esters, which comprises dissolving rapamycin in an organic solvent which is capable of dissolving rapamycin and is miscible with the nonionic surfactant, and either (i) adding the nonionic surfactant, if required removing some or all of the organic solvent, and adding water; or (ii.) adding a solution of nonionic surfactant in water; the amounts of rapamycin and nonionic surfactant being predetermined to give the desired concentrations in the composition.
Claim 9
Dependent Claim
16 words
A process as claimed in Claim 6 wherein the organic solvent is acetone, methanol or ethanol.
Claim 10
Dependent Claim
23 words
A process as claimed in Claim 6 or Claim 7 wherein the nonionic surfactant is polyoxyethylated castor oil or polyoxyethylated hydrogenated castor oil.
Claim 11
Dependent Claim
28 words
A process as claimed in any one of Claims 6, 7 and 8 wherein the aqueous solution comprises about 1.0 to 20 percent by weight of nonionic surfactant.
Claim 12
Dependent Claim
35 words
An intravenously injectable composition as claimed in any one of Claims 1 to 5 for use as an agent for enhancing blood levels of rapamycin or for providing rapamycin in the brain of a mammal.
Claim 13
Dependent Claim
3 words
CLAIMS FOR AUSTRIA
Claim 14
Dependent Claim
112 words
A process for preparing an injectable composition, suitable for intravenous administration, comprising about 1 to 20 milligrams of rapamycin per millimeter of an aqueous solution of a nonionic surfactant selected from polyoxyethylated fatty acids, polyoxyethylated fatty alcohols and polyoxyethylated glycerin hydroxy fatty acid esters, which comprises dissolving rapamycin in an organic solvent which is capable of dissolving rapamycin and is miscible with the nonionic surfactant, and either (i) adding the nonionic surfactant, if required removing some or all of the organic solvent, and adding water; or (ii) adding a solution of nonionic surfactant in water; the amounts of rapamycin and nonionic surfactant being predetermined to give the desired concentrations in the composition.
Claim 15
Dependent Claim
112 words
A process for preparing an injectable composition, suitable for intravenous administration, comprising about 1 to 20 milligrams of rapamycin per millimeter of an aqueous solution of a nonionic surfactant selected from polyoxyethylated fatty acids, polyoxyethylated fatty alcohols and polyoxyethylated glycerin hydroxy fatty acid esters, which comprises dissolving rapamycin in an organic solvent which is capable of dissolving rapamycin and is miscible with the nonionic surfactant, and either (i) adding the nonionic surfactant, if required removing some or all of the organic solvent, and adding water; or (ii) adding a solution of nonionic surfactant in water; the amounts of rapamycin and nonionic surfactant being predetermined to give the desired concentrations in the composition.
Claim 16
Dependent Claim
16 words
A process as claimed in Claim 1 wherein the organic solvent is acetone, methanol or ethanol.
Claim 17
Dependent Claim
23 words
A process as claimed in Claim 1 or Claim 2 wherein the nonionic surfactant is polyoxyethylated castor oil or polyoxyethylated hydrogenated castor oil.
Claim 18
Dependent Claim
25 words
A process as claimed in Claim 1 or Claim 2 wherein the aqueous solution comprises about 1.0 to 20 percent by weight of nonionic surfactant.
Claim 19
Dependent Claim
34 words
A process as claimed in Claim 1 in which the aqueous solution comprises about 1 to 20 percent by weight of a nonionic surfactant selected from polyoxyethylated castor oil and polyoxyethylated hydrogenated castor oil.
References Cited (Backward Citations)
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