Improved injectable dispersions of propofol

A - Human Necessities – 61 – K

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Details

A61K 9/107 (2006.01) A61K 31/05 (2006.01) A61K 31/14 (2006.01) A61K 47/10 (2006.01) A61K 47/12 (2006.01) A61K 47/14 (2006.01) A61K 47/24 (2006.01) A61K 47/26 (2006.01) A61K 47/44 (2006.01)

Patent

CA 2412905

A sterile, injectable homogenized dispersion of micromatrices or microdroplets having a mean diameter from about 50 nm to about 1000 nm comprising about 1 % to about 7.5 % of propofol, about 1 % to about 8 % of a propofol-soluble diluent, and about 0.67 % to about 5 % of a surface stabilizing amphiphilic agent suspended in an aqueous medium containing a synergetic quantity of antimicrobial agent and a tonicity modifying amount of a pharmaceutically acceptable water-soluble hydroxyl-group-containing excipient, wherein the ratio of propofol to diluent is in the range of about 0.25 to about 7.5 while the ratio of propofol to amphiphilic agent is in the range from about 0.4 to about 1.5, and wherein the viscosity of the dispersion is in the range of 1.1 to 8 cps, processes for the formation of the dispersion, and methods of use are disclosed.

La présente invention concerne une dispersion homogénéisée injectable et stérile de micromatrices ou de microgouttelettes d'un diamètre moyen compris entre environ 50nm et environ 1000nm, comprenant entre environ 1 % et environ 5,5 % de propofol, entre environ 1 % et environ 8 % d'un diluant soluble dans le propofol, et entre environ 0,67 % et environ 5 % d'un agent amphiphile et stabilisateur de surface en suspension dans un milieu aqueux contenant une quantité synergétique d'un agent antimicrobien, et une quantité modificatrice de tonicité d'un excipient contenant un groupe hydroxyle soluble dans l'eau répondant aux normes pharmacologiques. Le rapport du propofol sur le diluant est compris entre 0,25 environ et 7,5 environ tandis que le rapport du propofol sur l'agent amphiphile est compris entre 0,4 environ et 1,5 environ. La viscosité de cette dispersion est comprise entre 1,1 et 8 cps. Cette invention concerne aussi des processus de préparation de cette dispersion et des techniques d'utilisation de celle-là.

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