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Methods for the preparation of injectable depot compositions

  • US 10,058,504 B2
  • Filed: 11/30/2012
  • Issued: 08/28/2018
  • Est. Priority Date: 05/31/2010
  • Status: Active Grant
First Claim
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1. An injectable depot composition consisting of risperidone, and a polymeric solution of DMSO and PLGA copolymer, wherein:

  • the content of risperidone is 13% wt±

    10%, based upon the weight of the composition, and the risperidone possesses a particle distribution selected from;

    a. not more than 10% of the total volume of the particles is smaller than 10 microns, not more than the 10% of the total volume of particles is greater than 225 microns, and the d0.5 is in the range of 10-200 microns;

    b. not more than 10% of the total volume of the particles is less than the range 1-10 μ

    m, not more than the 10% of the total volume of particles is greater than the range 225-400 μ

    m, and the d0.5 of the size distribution is in the range of about 40-200 μ

    m;

    orc. expressed as volume, d0.9 is about 150 to about 400 μ

    m, d0.5 is about 40 to about 200 μ

    m and d0.1 is about 10 to about 60 μ

    m;

    the mass ratio of DMSO to risperidone is 4.66±

    10%;

    1;

    the mass ratio of polymeric solution to risperidone is about 6.66±

    10%;

    1;

    the PLGA copolymer is an end-capped biodegradable poly(lactide-co-glycolide) copolymer having a monomer ratio of lactic acid to glycolic acid of 50;

    50 and an inherent viscosity in the range of 0.20±

    10% dl/g to 0.50±

    10% dl/g as measured in chloroform at 25°

    C. at a concentration of 0.1% wt/v with a Ubbelohde size 0c glass capillary viscometer;

    the polymeric solution has a viscosity in the range of 0.5-3.0 Pa·

    s; and

    the amount of risperidone dissolved in the injectable composition is 20% wt.

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