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

摘要

Methods are provided for drying a particle. Specifically, there is provided a spray-dried diketopiperazine-insulin particle formulation having improved aerodynamic performance and in which the active agent is more stabile and efficiently delivered as compared to that of the lyophilized diketopiperazine-insulin formulation. The dry powders have utility as pharmaceutical formulations for pulmonary delivery.

主权项

1. A dry powder medicament with an improved pharmaceutic property, made by a process comprising
a) forming microparticles comprising a diketopiperazine by adjusting the pH of a solution comprising a diketopiperazine having acidic or basic side chains, resulting in a suspension of microparticles of the diketopiperazine with acidic or basic side chains in a solvent, and optionally 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, increased aerodynamic performance of the powder, or improved stability of the active agent, if present.