US2015064283A1PendingUtilityA1

Pharmaceutical compositions for parenteral administration

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Assignee: WU NIANPriority: Jun 28, 2011Filed: Nov 7, 2014Published: Mar 5, 2015
Est. expiryJun 28, 2031(~5 yrs left)· nominal 20-yr term from priority
Inventors:Nian Wu
A61K 31/05A61K 47/26A61K 33/24A61K 31/496A61K 31/337A61K 31/506A61K 33/243A61K 9/0019A61K 47/14A61K 47/34A61K 9/1617A61K 9/1641A61K 9/08A61K 9/141
61
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Claims

Abstract

The invention comprises various aqueous PEG-carbohydrate-lipid based formulations of pharmaceutical active ingredients including compositions for intravenous injections. This invention relates to methods and compositions for improving solubility and the safety profile of pharmaceutical compounds. More particularly, the present invention relates to employing PEG-carbohydrate-lipid conjugates for formulating drug compositions having increased solubility or dispersivity and enhanced stability.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
         1 . A pharmaceutical composition for parenteral administration of a pharmaceutical active ingredient, the composition comprising:
 a) an aqueous solution or mixture;   b) a pharmaceutical active ingredient; and   c) a solubility enhancer comprising at least one of oleoyl-diethylenetriamine-PEG-lactobionate, oleoyl-N-(3-aminopropyl)propane-1,3-diamine-undecaethylene-glycol-methyl-ether-lactobionate, oleoy-(aminopropylamino)ethanoyl-mPEG-lactobionate, myristoyl-diethylenetriamine-dodecaethylene-glycol-lactobionate, myristoyl-triethylenetetramine-dodecaethylene-glycol-lactobionate, oleoyl-triethylenetetramine-dodecaethylene-glycol-lactobionate, and oleoyl-triethylenetetramine-pentadecaethylene-glycol-lactobionate.   
     
     
         2 . The pharmaceutical composition of  claim 1  comprising the pharmaceutical active ingredient at a concentration between about 0.05 mg/mL and about 50 mg/mL. 
     
     
         3 . The pharmaceutical composition of  claim 1  comprising a weight ratio of the solubility enhancer to the pharmaceutical active ingredient between about 0.2 and about 25. 
     
     
         4 . The pharmaceutical composition of  claim 1  wherein the pharmaceutical active ingredient is selected from the group consisting of propofol, cisplatin, docetaxel, paclitaxel, posaconazole, voriconazole, and combinations thereof. 
     
     
         5 . The pharmaceutical composition of  claim 4  wherein the pharmaceutical active ingredient comprises propofol at a concentration in the pharmaceutical composition of between about 0.2 mg/mL to about 25 mg/mL. 
     
     
         6 . The pharmaceutical composition of  claim 4  wherein the pharmaceutical active ingredient comprises cisplatin at a concentration in the pharmaceutical composition of between about 0.2 mg/mL to about 50 mg/mL. 
     
     
         7 . The pharmaceutical composition of  claim 4  wherein the pharmaceutical active ingredient comprises docetaxel at a concentration in the pharmaceutical composition of between about 0.2 mg/mL to about 25 mg/mL. 
     
     
         8 . The pharmaceutical composition of  claim 4  wherein the pharmaceutical active ingredient comprises paclitaxel at a concentration in the pharmaceutical composition of between about 0.2 mg/mL to about 25 mg/mL. 
     
     
         9 . The pharmaceutical composition of  claim 4  wherein the pharmaceutical active ingredient comprises posaconazole at a concentration in the pharmaceutical composition of between about 0.5 mg/mL to about 40 mg/mL. 
     
     
         10 . The pharmaceutical composition of  claim 4  wherein the pharmaceutical active ingredient comprises voriconazole at a concentration in the pharmaceutical composition of between about 0.5 mg/mL to about 40 mg/mL. 
     
     
         11 . The pharmaceutical composition of  claim 1  wherein the solubility enhancer comprises oleoyl-diethylenetriamine-PEG-lactobionate. 
     
     
         12 . The pharmaceutical composition of  claim 1  wherein the solubility enhancer comprises oleoyl-N-(3-aminopropyl)propane-1,3-diamine-undecaethylene-glycol-methyl-ether-lactobionate. 
     
     
         13 . The pharmaceutical composition of  claim 1  wherein the solubility enhancer comprises oleoy-(aminopropylamino)ethanoyl-mPEG-lactobionate. 
     
     
         14 . The pharmaceutical composition of  claim 1  wherein the solubility enhancer comprises myristoyl-diethylenetriamine-dodecaethylene-glycol-lactobionate. 
     
     
         15 . The pharmaceutical composition of  claim 1  wherein the solubility enhancer comprises myristoyl-triethylenetetramine-dodecaethylene-glycol-lactobionate. 
     
     
         16 . The pharmaceutical composition of  claim 1  wherein the solubility enhancer comprises oleoyl-triethylenetetramine-dodecaethylene-glycol-lactobionate. 
     
     
         17 . The pharmaceutical composition of  claim 1  wherein the solubility enhancer comprises oleoyl-triethylenetetramine-pentadecaethylene-glycol-lactobionate.

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