Formulations of indol-3-yl-2-oxoacetamide compounds
This invention relates to an oral formulation containing an effective amount of the compound of the following formula I: d-alpha-tocopheryl polyethylene glycol 1000 succinate (“TPGS”); and 2-(2-ethoxyethoxy)ethanol (“Transcutol”). R 1 through R 4 and n are defined herein. Also disclosed is a method of treating cancer by administering this formula to a subject orally.
1. A pharmaceutical formulation comprising:
15-80% by weight d-alpha-tocopheryl polyethylene glycol 1000 succinate (“TPGS”);
20-30% by weight 2-(2-ethoxyethoxy)ethanol (“Transcutol”); and
N-(3-methylisothiazol-5-yl)-2-[1-(3-methylisoxazol-5-ylmethyl)-1H-indol-3-yl]-2-oxoacetamide.
2. The formulation of claim 1 , wherein the TPGS is 70-80% by weight.
3. The formulation of claim 1 , further comprising polyethylene glycol (“PEG”) having a molecular weight ranging from 300 to 6000.
4. The formulation of claim 3 , wherein the PEG has a molecular weight ranging from 400 to 1000.
5. The formulation of claim 3 , wherein the PEG is 10-65% by weight.
6. The formulation of claim 5 , wherein the PEG is 30-65% by weight and the TPGS is 15-50% by weight.
7. The formulation of claim 6 , wherein the PEG is 40-65% by weight, the TPGS is 15-40% by weight, and the Transcutol is 20-25% by weight.
8. The formulation of claim 1 , wherein the formulation is encapsulated in a capsule.
9. The formulation of claim 8 , wherein the capsule is formed of at least one polymer selected from the group consisting of porcine collagen material, bovine collagen material, gelatin, gum arabic, pectin, poly(ethylene-co-maleic anhydride), poly(vinvlmethylether-co-maleic anhydride), carrageenan, and agar-agar.
10. The formulation of claim 1 , wherein the formulation is free of glyceride, fatty acid, and fatty acid ester.
11. The formulation of claim 10 , wherein the TPGS is 70-80% by weight.
12. The formulation of claim 10 , further comprising polyethylene glycol (PEG) having a molecular weight ranging from 300 to 6000.
13. The formulation of claim 12 , wherein the PEG has a molecular weight ranging from 400 to 1000.
14. The formulation of claim 13 , wherein the PEG is 10-65% by weight.
15. The formulation of claim 14 , wherein the PEG is 40-65% by weight, the TPGS is 15-40% by weight, and the Transcutol is 20-25% by weight.
16. A method for treating cancer, the method comprising administering orally to a subject in need thereof an effective amount of the formulation of claim 1 , wherein the cancer is leukemia, colorectal, nasopharyngeal, lung, or cervical cancer.