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Method for improving the pharmaceutic properties of microparticles comprising diketopiperazine and an active agent

  • US 10,130,581 B2
  • Filed: 12/16/2015
  • Issued: 11/20/2018
  • Est. Priority Date: 02/22/2006
  • Status: Active Grant
First Claim
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1. A method for forming a dry powder medicament with an improved pharmaceutic property, comprising a) a step for forming microparticles comprising a diketopiperazine with acidic or basic side chains, resulting in a suspension of microparticles of the diketopiperazine with acidic or basic side chains in an appropriate solvent, and optionally a step for loading said microparticles with an active agent, then b) removing solvent by spray drying to obtain a dry powder, wherein the dry powder has an improved pharmaceutic property as compared to a dry powder obtained by removing solvent by lyophilization, and wherein the improved pharmaceutic property is increased density of the powder, and wherein said dry powder has a bulk density from 0.15 to 0.20 g/cc.

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