Compositions for delivering highly water soluble drugs
The present invention provides compositions for delivering highly water-soluble drugs (such as vinca alkaloids) and methods of using such compositions.
1. A method for treating breast cancer, said method comprising:
administering to a patient in need thereof a composition, wherein said composition comprises
vinorelbine bitartrate in an oil-in-water emulsion having an oil phase and an aqueous phase, wherein the oil phase comprises a triglyceride oil having medium chain fatty acids, soy lecithin, and oleic acid, and the aqueous phase comprises water, sucrose, and disodium edetate (EDTA) dihydrate, wherein in excess of 80% of the vinorelbine bitartrate is dissolved and remains in the oil phase,
and wherein:
(a) vinorelbine bitartrate is at a concentration of 1.4% (w/w);
(b) triglyceride oil having medium chain fatty acids is at a concentration of 15% (w/w);
(c) soy lecithin is at a concentration of 7.5% (w/w);
(d) oleic acid is at a concentration of 1.5% (w/w);
(e) sucrose is at a concentration of 15% (w/w);
(f) disodium edetate (EDTA) dihydrate is at a concentration of 0.005% (w/w);
(g) vinorelbine bitartrate to oleic acid is in a 1:4 molar ratio;
(h) the composition is at a pH of 3.7; and
(i) water to q.s., thereby treating breast cancer.
2. The method of claim 1 , wherein no less than 90% of the drug is present in the oil phase of the emulsion.
3. The method of claim 1 , wherein no less than 95% of the drug is present in the oil phase of the emulsion.
4. The method of claim 1 , wherein the drug in the composition is in a concentration range of 1 to 50 mg/mL.
5. The method of claim 1 , wherein the composition is administered intravenously.
6. The method of claim 1 , wherein the composition is administered intramuscularly or intraarterially.
7. A method for treating non-small cell lung cancer, said method comprising:
administering to a patient in need thereof a composition, wherein said composition comprises:
vinorelbine bitartrate in an oil-in-water emulsion having an oil phase and an aqueous phase, wherein the oil phase comprises a triglyceride oil having medium chain fatty acids, soy lecithin, and oleic acid, and the aqueous phase comprises water, sucrose, and disodium edetate (EDTA) dihydrate, wherein in excess of 80% of the vinorelbine bitartrate is dissolved and remains in the oil phase,
and wherein:
(a) vinorelbine bitartrate is at a concentration of 1.4% (w/w);
(b) triglyceride oil having medium chain fatty acids is at a concentration of 15% (w/w);
(c) soy lecithin is at a concentration of 7.5% (w/w);
(d) oleic acid is at a concentration of 1.5% (w/w);
(e) sucrose is at a concentration of 15% (w/w);
(f) disodium edetate (EDTA) dihydrate is at a concentration of 0.005% (w/w);
(g) vinorelbine bitartrate to oleic acid is in a 1:4 molar ratio;
(h) the composition is at a pH of 3.7; and
(i) water to q.s., thereby treating non-small cell lung cancer.
8. The method of claim 7 , wherein no less than 90% of the drug is present in the oil phase of the emulsion.
9. The method of claim 7 , wherein no less than 95% of the drug is present in the oil phase of the emulsion.
10. The method of claim 7 , wherein the drug in the composition is in a concentration range of 1 to 50 mg/mL.
11. The method of claim 7 , wherein the composition is administered intravenously.
12. The method of claim 7 , wherein the composition is administered intramuscularly or intraarterially.