Emulsion vehicle for poorly soluble drugs

Abstract

An emulsion of α-tocopherol, stabilized by biocompatible surfactants, as a vehicle or carrier for therapeutic drugs, which is substantially ethanol free and which can be administered to animals or humans various routes is disclosed. Also included in the emulsion is PEGylated vitamin E PEGylated α-tocopherol includes polyethylene glycol subunits attached by a succinic acid diester at the ring hydroxyl of vitamin E and serves as a primary surfactant, stabilizer and a secondary solvent in emulsions of α-tocopherol.

1 - 24 . (Canceled)  
     
     
         25 . A method of administering a chemotherapeutic agent to a subject in need there of, comprising: 
 providing a pharmaceutical composition comprising a chemotherapeutic agent and a tocopherol, wherein the chemotherapeutic agent is at least one of a taxoid, a taxane, or a taxine, and wherein the concentration of the chemotherapeutic agent is at least about 5 mg/ml; and    administering the pharmaceutical composition in a therapeutically effective amount to a subject in need thereof.    
     
     
         26 . The method of  claim 25 , wherein the chemotherapeutic agent is paclitaxel.  
     
     
         27 . The method of  claim 26 , wherein the concentration of the paclitaxel in the composition is at least about 10 mg/ml.  
     
     
         28 . The method of  claim 26 , wherein the concentration of the paclitaxel in the composition is at least about 20 mg/ml.  
     
     
         29 . The method of  claim 28 , wherein the tocopherol is α-tocopherol.  
     
     
         30 . The method of  claim 25 , wherein the composition further comprises a tocopherol polyethylene glycol derivative.  
     
     
         31 . The method of  claim 30 , wherein the tocopherol polyethylene glycol derivative is d-α-tocopherol polyethylene glycol 1000 succinate.  
     
     
         32 . The method of  claim 25 , wherein the composition further comprises polyethylene glycol.  
     
     
         33 . The method of  claim 25 , wherein the composition further comprises a polyoxypropylene-polyoxyethylene glycol nonionic block co-polymer.  
     
     
         34 . The method of  claim 25 , wherein the composition is stable for at least 3 months.  
     
     
         35 . The method of  claim 25 , wherein the composition is administered parentally.  
     
     
         36 . The method of  claim 25 , wherein the composition is administered by intravenous infusion over a period of less than 3 hours.  
     
     
         37 . The method of  claim 25 , wherein the composition is administered by bolus injection.  
     
     
         38 . A method of administering a chemotherapeutic agent to a subject in need there of, comprising: 
 providing a pharmaceutical composition comprising a chemotherapeutic agent, a tocopherol, and a tocopherol polyethylene glycol derivative, wherein the chemotherapeutic agent is at least one of a taxoid, a taxane, or a taxine; and    administering the pharmaceutical composition in a therapeutically effective amount to a subject in need thereof.    
     
     
         39 . The method of  claim 38 , wherein the chemotherapeutic agent is paclitaxel.  
     
     
         40 . The method of  claim 39 , wherein the concentration of the paclitaxel in the composition is at least about 5 mg/ml.  
     
     
         41 . The method of  claim 39 , wherein the concentration of the paclitaxel in the composition is at least about 10 mg/ml.  
     
     
         42 . The method of  claim 39 , wherein the concentration of the paclitaxel in the composition is at least about 20 mg/ml.  
     
     
         43 . The method of  claim 38 , wherein the tocopherol is α-tocopherol.  
     
     
         44 . The method of  claim 38 , wherein the tocopherol polyethylene glycol derivative is tocopherol polyethylene glycol succinate.  
     
     
         45 . The method of  claim 38 , wherein the composition further comprises polyethylene glycol.  
     
     
         46 . The method of  claim 38 , wherein the composition further comprises a polyoxypropylene-polyoxyethylene glycol nonionic block co-polymer.  
     
     
         47 . The method of  claim 38 , wherein the composition is administered parentally.  
     
     
         48 . The method of  claim 38 , wherein the composition is administered by intravenous infusion over a period of less than 3 hours.  
     
     
         49 . The method of  claim 38 , wherein the composition is administered by bolus injection.  
     
     
         50 . A method of treating a carcinoma in a subject suffering therefrom, comprising: 
 providing a pharmaceutical composition comprising a chemotherapeutic agent and a tocopherol, wherein the chemotherapeutic agent is at least one of a taxoid, a taxane, or a taxine, and wherein the concentration of the chemotherapeutic agent is at least about 5 mg/ml; and    administering the pharmaceutical composition in a therapeutically effective amount to a subject suffering from a carcinoma.    
     
     
         51 . The method of  claim 60 , wherein the chemotherapeutic agent is paclitaxel.  
     
     
         52 . The method of  claim 61 , wherein the concentration of the paclitaxel in the composition is at least about 10 mg/ml.  
     
     
         53 . The method of  claim 61 , wherein the concentration of the paclitaxel in the composition is at least about 20 mg/ml.  
     
     
         54 . The method of  claim 60 , wherein the tocopherol is α-tocopherol.  
     
     
         55 . The method of  claim 60 , wherein the composition further comprises a tocopherol polyethylene glycol derivative.  
     
     
         56 . The method of  claim 65 , wherein the tocopherol polyethylene glycol derivative is d-α-tocopherol polyethylene glycol 1000 succinate.  
     
     
         57 . The method of  claim 60 , wherein the composition further comprises polyethylene glycol.  
     
     
         58 . The method of  claim 60 , wherein the composition further comprises a polyoxypropylene-polyoxyethylene glycol nonionic block co-polymer.  
     
     
         59 . The method of  claim 60 , wherein the composition is stable for at least 3 months.  
     
     
         60 . The method of  claim 60 , wherein the composition is administered parentally.  
     
     
         61 . The method of  claim 60 , wherein the composition is administered by intravenous infusion over a period of less than 3 hours.  
     
     
         62 . The method of  claim 60 , wherein the composition is administered by bolus injection.  
     
     
         63 . The method of  claim 60 , wherein the carcinoma is a breast carcinoma.  
     
     
         64 . The method of  claim 60 , wherein the carcinoma is a lung carcinoma.  
     
     
         65 . The method of  claim 60 , wherein the carcinoma is a skin carcinoma.  
     
     
         66 . The method of  claim 60 , wherein the carcinoma is a uterus carcinoma.  
     
     
         67 . A method for treating a carcinoma in a subject suffering therefrom, comprising: 
 providing a pharmaceutical composition comprising a chemotherapeutic agent, a tocopherol, and a tocopherol polyethylene glycol derivative, wherein the chemotherapeutic agent is at least one of a taxoid, a taxane, or a taxine; and    administering the pharmaceutical composition in a therapeutically effective amount to a subject suffering from a carcinoma.    
     
     
         68 . The method of  claim 77 , wherein the chemotherapeutic agent is paclitaxel.  
     
     
         69 . The method of  claim 78 , wherein the concentration of the paclitaxel in the composition is at least about 5 mg/ml.  
     
     
         70 . The method of  claim 78 , wherein the concentration of the paclitaxel in the composition is at least about 10 mg/ml.  
     
     
         71 . The method of  claim 78 , wherein the concentration of the paclitaxel in the composition is at least about 20 mg/ml.  
     
     
         72 . The method of  claim 77 , wherein the tocopherol is α-tocopherol.  
     
     
         73 . The method of  claim 77 , wherein the tocopherol polyethylene glycol derivative is tocopherol polyethylene glycol succinate.  
     
     
         74 . The method of  claim 77 , wherein the composition further comprises polyethylene glycol.  
     
     
         75 . The method of  claim 77 , wherein the composition further comprises a polyoxypropylene-polyoxyethylene glycol nonionic block co-polymer.  
     
     
         76 . The method of  claim 77 , wherein the composition is administered parentally.  
     
     
         77 . The method of  claim 77 , wherein the composition is administered by intravenous infusion over a period of less than 3 hours.  
     
     
         78 . The method of  claim 77 , wherein the composition is administered by bolus injection.  
     
     
         79 . The method of  claim 77 , wherein the carcinoma is a breast carcinoma.  
     
     
         80 . The method of  claim 77 , wherein the carcinoma is a lung carcinoma.  
     
     
         81 . The method of  claim 77 , wherein the carcinoma is a skin carcinoma.  
     
     
         82 . The method of  claim 77 , wherein the carcinoma is a uterus carcinoma.