Multiparticulate crystalline drug compositions having controlled release profiles
AssigneePfizer Inc.
InventorsLeah E. Appel, Roderick J. Ray, David K. Lyon, James B. West, Scott B. McCray, Marshall D. Crew, Dwayne T. Friesen, Scott M. Herbig, Julian B. Lo
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Abstract
A multiparticulate for controlled release of a drug comprises crystalline drug, a glyceride having at least one alkylate substituent of at least 16 carbon atoms, and a poloxamer, wherein at least 70 wt % of the drug in the multiparticulate is crystalline.
Claims15
A pharmaceutical composition providing controlled release of azithromycin, comprising a plurality of multiparticulates, said multiparticulates comprising said azithromycin wherein at least 70 wt % of said azithromycin is crystalline, a poloxamer and a glyceride having at least one alkylate substituent of at least 16 carbon atoms, wherein the weight ratio of poloxamer to glyceride ranges from about 0.01 to 0.50, and wherein said multiparticulates comprise crystalline azithromycin suspended in a mixture of said glyceride and poloxamer.
A process for forming multiparticulates, comprising:
- (a) forming a molten mixture comprising azithromycin, a poloxamer and a glyceride having at least one alkylate substituent of at least 16 carbon atoms, wherein said molten mixture has a viscosity less than about 20,000 cp and comprises crystalline azithromycin suspended in a mixture of said glyceride and poloxamer;
- (b) forming droplets from said molten mixture;
- and
- (c) solidifying said droplets to form multiparticulates
- wherein at least 70 wt % of said azithromycin in said multiparticulates is crystalline, and
- wherein the ratio of poloxamer to glyceride ranges from about 0.01 to 0.50.
A method for controlling the release rate of azithromycin from a multiparticulate, comprising:
- (a) determining a desired release rate of said azithromycin from said multiparticulate;
- (b) forming multiparticulates comprising
- (1) forming a molten mixture comprising crystalline azithromycin suspended in a mixture of a poloxamer and a glyceride having at least one alkylate substituent of at least 16 carbon atoms;
- (2) forming droplets from said molten mixture;
- and
- (3) solidifying said droplets to form multiparticulates wherein at least 70 wt % of said azithromycin in said multiparticulates is crystalline;
- and
- (c) prior to (b) selecting a weight ratio of said poloxamer to said glyceride to achieve said desired release rate, wherein the weight ratio of poloxamer to glyceride ranges from about 0.01 to 0.50.
Dependencies are inferred from the claim text.