US2003096797A1PendingUtilityA1
Novel pharmaceutical formulations comprising aminoalkyl phosphorothioates
Est. expiryJun 15, 2019(expired)· nominal 20-yr term from priority
A61K 31/66
55
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Claims
Abstract
The present invention provides novel pharmaceutical compositions comprising aminoalkyl phosphorothioate compounds in combination with surfactants, hydrotropes and chelating agents. The compositions are well-suited for subcutaneous administration.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A pharmaceutical composition comprising an amount of an aminoalkyl phosphorothioate and a surfactant which enhances the biological activity of the composition.
2 . The pharmaceutical composition of claim 1 , wherein the amount of aminoalkyl phosphorothioate is from about 10 mg to about 3000 mg.
3 . The pharmaceutical composition of claim 1 , wherein the amount of surfactant is added in the form of an aqueous dispersion, said dispersion having a concentration of from about 0.1 mg/ml to about 20 mg/ml.
4 . The pharmaceutical composition of claim 1 , wherein the biological activity is cytoprotection, radio- or chemo-protection.
5 . The pharmaceutical composition of claim 1 , wherein the aminoalkyl phosphorothioate is amifostine or S-3-(3-methylaminopropylamino)-3-propyl dihydrogen phosphorothioate.
6 . The pharmaceutical composition of claim 4 , wherein the aminoalkyl phosphorothioate is amifostine.
7 . The pharmaceutical composition of claim 1 , wherein the surfactant is selected from the group consisting of cholic acid, a salt of cholic acid, deoxycholic acid, a salt of deoxycholic acid, taurocholic acid, polyvinylpyrrolidone, a salt of taurocholic acid, TWEEN 80 and sodium dodecylsulfate.
8 . The pharmaceutical composition of claim 5 , wherein the surfactant is sodium deoxycholate.
9 . The pharmaceutical composition of claim 1 , wherein said composition is freeze-dried or lyophilized.
10 . The pharmaceutical composition of claim 1 , wherein said composition is a liquid.
11 . A pharmaceutical composition which comprises a therapeutically effective amount of amifostine and sodium deoxycholate.
12 . A pharmaceutical composition comprising an amount of an aminoalkyl phosphorothioate and a hydrotrope.
13 . The pharmaceutical composition of claim 1 , further comprising a hydrotrope.
14 . The pharmaceutical composition of claim 13 , wherein the hydrotrope is added in the form of an aqueous solution, having a concentration of from about 0.5 mg/ml to about 100 mg/ml.
15 . The pharmaceutical composition of claim 13 , wherein the hydrotrope is selected from the group consisting of sorbitol, mannitol, nicotinic acid, nicotinamide, 2,5-dihydroxybenzoic acid, ascorbic acid, ascorbyl dipalmitate, fructose, glucose, glucose glutamate, glucuronic acid, glycerin, 1,2,6-hexanetriol, hydroxystearyl methylglucamine, inositol, lactose, maltitol, sorbeth-20, sucrose, thioglycerin, tris(hydroxymethyl)nitromethane, tromethamine and xylitol.
16 . The pharmaceutical composition of claim 13 , wherein the hydrotrope is a polyhydroxylated alcohol.
17 . The pharmaceutical composition of claim 16 , wherein the polyhydroxylated alcohol is sorbitol.
18 . The pharmaceutical composition of claim 13 , wherein said composition is freeze-dried or lyophilized.
19 . The pharmaceutical composition of claim 13 , wherein said composition is a liquid.
20 . A pharmaceutical composition comprising an amount of an aminoalkyl phosphorothioate, a hydrotrope and a chelating agent.
21 . The pharmaceutical composition of claim 20 , wherein the chelating agent is added in the form of an aqueous dispersion, said dispersion having a concentration of from about 0.5 mg/ml to about 100 mg/ml.
22 . The pharmaceutical composition of claim 20 , wherein the aminoalkyl phosphorothioate is amifostine or S-3-(3-methylaminopropylamino)-3-propyl dihydrogen phosphorothioate..
23 . The pharmaceutical composition of claim 20 , wherein the hydrotrope is selected from the group consisting of sorbitol, mannitol, nicotinic acid, nicotinamide, 2,5-dihydroxybenzoic acid, ascorbic acid, ascorbyl dipalmitate, fructose, glucose, glucose glutamate, glucuronic acid, glycerin, 1,2,6-hexanetriol, hydroxystearyl methylglucamine, inositol, lactose, maltitol, sorbeth-20, sucrose, thioglycerin, tris(hydroxymethyl)nitromethane, tromethamine and xylitol.
24 . The pharmaceutical composition of claim 20 , wherein the hydrotrope is sorbitol.
25 . The pharmaceutical composition of claim 20 , wherein the chelating agent is EDTA or DTPA.
26 . The pharmaceutical composition of claim 20 , wherein the chelating agent is EDTA.
27 . The pharmaceutical composition of claim 20 , wherein said composition is freeze-dried or lyophilized.
28 . The pharmaceutical composition of claim 20 , wherein said composition is a liquid.
29 . A pharmaceutical composition which comprises a therapeutically effective amount of amifostine, an amount of sorbitol and an amount of EDTA.
30 . The pharmaceutical composition of claims 1 or 13 , further comprising a chelating agent.
31 . The pharmaceutical composition of claim 30 , wherein the chelating agent is EDTA.
32 . The pharmaceutical composition of claim 30 , wherein said composition is freeze-dried or lyophilized.
33 . The pharmaceutical composition of claim 30 , wherein said composition is a liquid.
34 . A pharmaceutical composition comprising an amount of an aminoalkyl phosphorothioate and a chelating agent, wherein said pharmaceutical composition is adapted for use via subcutaneous administration.
35 . The pharmaceutical composition of claim 34 , wherein the aminoalkyl phosphorothioate is amifostine or S-3-(3-methylaminopropylamino)-3-propyl dihydrogen phosphorothioate.
36 . The pharmaceutical composition of claim 20 , wherein the chelating agent is EDTA.
37 . A pharmaceutical composition which comprises a therapeutically effective amount of amifostine, an amount of sodium deoxycholate, an amount of sorbitol and an amount of EDTA.
38 . The pharmaceutical composition of claim 1 , 11 , 12 , 13 , 20 or 34 wherein the composition has a pH of between about 6 and about 8.
39 . The pharmaceutical composition of claim 1 , wherein said pharmaceutical composition is adapted for use via subcutaneous administration.
40 . A pharmaceutical composition adapted for use via subcutaneous administration, comprising amifostine and a compound selected from the group consisting of 0.075% Sodium Deoxycholate, 2% Sorbitol, 2% Edetate Disodium, 0.2% Edetate Disodium, 1% Tween 80, 1% Choline Chloride, 0.02% Sodium Dodecyl Sulfate, WR-1065 and mixtures thereof, and wherein the composition has a pH of between about 6 and about 8.
41 . The pharmaceutical composition of claim 1 , wherein said pharmaceutical composition is adapted for use via intravenous administration.
42 . The pharmaceutical composition of claim 1 , wherein said pharmaceutical composition is adapted for use via oral administration.
43 . A unit dosage form which comprises a pharmaceutical composition of claim 1 , 11 , 12 , 13 , 20 , or 34 .
44 . A method of treating a patient having cancer from the toxicities associated with radio- or chemotherapy, using the pharmaceutical composition of claim 1 , 11 , 12 , 13 , 20 or 34 .
45 . A method of protecting a patient having cancer from the toxicities associated with radio- or chemotherapy, using the pharmaceutical composition of claim 1 , 11 , 12 , 13 , 20 or 34 .
46 . A method of treating a patient having MDS, using the pharmaceutical composition of claim 1 , 11 , 12 , 13 , 20 or 34 .
47 . A method of protecting a patient having MDS, using the pharmaceutical composition of claim 1 , 11 , 12 , 13 , 20 or 34 .Join the waitlist — get patent alerts
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