Butylphthalide Intravenous Emulsion and Application Thereof

Abstract

The present invention discloses a butylphthalide intravenous emulsion for intravenous injection or infusion, containing butylphthalide or derivatives thereof as an active ingredient in an amount of 0.01˜50 wt % and an excipient in an amount of 50˜99.99 wt %, based on the total weight of the emulsion.

1 . A butylphthalide intravenous emulsion comprising butylphthalide or derivatives thereof as an active ingredient in an amount of 0.01˜50 wt % and an excipient in an amount of 50˜99.99 wt %, based on the total weight of the emulsion. 
   
   
       2 . The butylphthalide intravenous emulsion according to  claim 1 , wherein the butylphthalide or derivatives thereof is a raceme of butylphthalide or derivatives thereof, or l-butylphthalide or derivatives thereof. 
   
   
       3 . The butylphthalide intravenous emulsion according to  claim 1  or  2 , wherein the excipient comprises an oil phase in an amount of 0˜50 wt %, an aqueous phase in an amount of 50˜98 wt %, an emulsifier in an amount of 0.01˜50 wt %, a stabilizer in an amount of 0˜50 wt %, and an osmoregulation agent in an amount of 0˜10 wt %, based on the total weight of the excipient. 
   
   
       4 . The butylphthalide intravenous emulsion according to  claim 3 , wherein the oil phase comprises a natural vegetable oil with long chain fatty acid ester groups, or a vegetable oil or fatty acid ester being subjected to structure modification and hydrolysis, or glyceride with a chain length of C 6 ˜C 12  fatty acid, or a mixture thereof. 
   
   
       5 . The butylphthalide intravenous emulsion according to  claim 4 , wherein the oil phase is one of or a mixture of soybean oil, castor oil, tea-seed oil, peanut oil, cottonseed oil, sesame oil, rape oil, safflower oil, olive oil, coconut oil, palm oil, cacao oil, Arlacel 80, Arlacel 86, Capmul MCM, Captex 200 (oil), Captex 355 (oil), Miglyol 812 (oil), Myvacet (oil), Myverol 18-92, glyceride oleate, glyceride linoleate, macrogol glyceryl laurate, ethyl oleate, ethyl linoleate, and caprylocaproyl triglyceride,. 
   
   
       6 . The butylphthalide intravenous emulsion according to  claim 3 , wherein the emulsifier comprises one of or a mixture of nonionic surfactants and anionic surfactants. 
   
   
       7 . The butylphthalide intravenous emulsion according to  claim 6 , wherein the emulsifier is one of or a mixture of soybean lecithin or modified soybean lecthin, ovolecithin or modified ovolecithin, Ophase 31, Poloxamer 108, Poloxamer 188, Poloxamer 407, polyoxyethylene (hydrogenated) castor oil, water soluble VE (TPGS), Solutol HS-15, PEG-400 monostearate, PEG-1750 monostearate, Tween-80, Tween-20, and Span-20. 
   
   
       8 . The butylphthalide intravenous emulsion according to  claim 3 , wherein the stabilizer is one of or a mixture of oleic acid, sodium oleate, sodium caprylate, cholesterol, cholic acid, deoxycholic acid and sodium salt thereof, vitamin A, vitamin C, and vitamin E. 
   
   
       9 . The butylphthalide intravenous emulsion according to  claim 3 , wherein the osmoregulation agent is one of or a mixture of sodium chloride, glucose, sorbitol, xylitol, mannitol, and glycerol. 
   
   
       10 . The butylphthalide intravenous emulsion according to  claim 1 , which is administered by intravenous injection or infusion.