Methods for reducing vein irritation

Abstract

The present invention provides compositions for delivering highly water-soluble drugs (such as vinca alkaloids) and methods of using such compositions.

1 - 20 . (canceled) 
     
     
         21 . A method for treating cancer while reducing vein irritation, said method comprising administering a composition comprising a triglyceride oil, an emulsifier, a stabilizer, water, and a highly water soluble drug, wherein (a) the composition is an emulsion having an oil and an aqueous phase, and (b) the drug is substantially in the oil phase, to treat cancer. 
     
     
         22 . The method of  claim 21 , wherein the emulsion is at a pH range of 3 to 5. 
     
     
         23 . The method of  claim 21 , wherein the drug alone is venous toxic. 
     
     
         24 . The method of  claim 21 , wherein the drug is weakly basic. 
     
     
         25 . The method of  claim 21 , wherein the drug is selected from the group consisting of dopamine, ciprofloxacin, vancomycin, norvancomycin, doxorubicin, daunorubicin, vinca alkaloids, and pharmaceutically acceptable salts thereof. 
     
     
         26 . The method of  claim 21 , wherein said drug is vinorelbine bitartrate having the chemical name of 3′,4′-didehydro-4′-deoxy-C′-norvincaleukoblastine [R-(R*,R*)-2,3-dihydroxybutanedioate (1:2)(salt)] and the following structure: or another pharmaceutically acceptable salt of vinorelbine. 
     
     
         27 . The method of  claim 21 , wherein the triglyceride oil is a triglyceride having long chain fatty acids, a triglyceride having medium chain fatty acids, or a mixture thereof. 
     
     
         28 . The method of  claim 21 , wherein the emulsifier is egg lecithin, soy lecithin, a synthetic phospholipid, or a mixture thereof. 
     
     
         29 . The method of  claim 21 , wherein the stabilizer is a fatty acid, riboflavin-5-phosphate, vitamin-E succinate, cholesterol sulfate, or a mixture thereof. 
     
     
         30 . The method of  claim 29 , wherein the fatty acid is oleic acid or a pharmaceutically acceptable salt thereof. 
     
     
         31 . The method of  claim 21 , wherein the drug has an aqueous solubility of over 50 mg/ml. 
     
     
         32 . The method of  claim 21 , wherein the drug has an aqueous solubility of over 100 mg/ml. 
     
     
         33 . The method of  claim 21 , wherein the drug has an aqueous solubility of over 500 mg/ml. 
     
     
         34 . The method of  claim 21 , wherein the drug has an aqueous solubility of over 1000 mg/ml. 
     
     
         35 . The method of  claim 21 , wherein the charge ratio of the drug to the stabilizer is 1:1 to 1:10. 
     
     
         36 . The method of  claim 21 , wherein no less than 90% of the drug is present in the oil phase of the emulsion. 
     
     
         37 . The method of  claim 21 , wherein no less than 95% of the drug is present in the oil phase of the emulsion. 
     
     
         38 . The method of  claim 21 , wherein the drug in the composition is in a concentration range of 1 to 50 mg/mL.