MICROCRYSTALLINE DIKETOPIPERAZINE COMPOSITIONS AND METHODS

A method of making microcrystalline diketopiperazine particles substantially uniform in size having a hollow spherical structure and comprising a shell comprising crystallites of the diketopiperazine that do not self-assemble in suspension, wherein the particles are suitable for pulmonary administra...

Full description

Saved in:
Bibliographic Details
Main Authors Guarneri, Joseph J, Wilson, Bryan R, Grant, Marshall L
Format Patent
LanguageEnglish
Published 14.11.2019
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
Online AccessGet full text

Cover

More Information
Summary:A method of making microcrystalline diketopiperazine particles substantially uniform in size having a hollow spherical structure and comprising a shell comprising crystallites of the diketopiperazine that do not self-assemble in suspension, wherein the particles are suitable for pulmonary administration as a dry powder comprising: a) forming diketopiperazine crystallites in a surfactant-free suspension; wherein the crystallites have a size distribution as a bimodal curve as measured by laser diffraction having a first peak of crystallites of the bimodal distribution having an average size of 0.2 pm to 0.4 pm and a second peak of crystallites having an average size of 2.1 pm to 2.4 pm b) atomizing the suspension using a spray dryer under an air or gas stream, and c) forming a dry powder comprising the microcrystalline diketopiperazine particles having hollow spheres and a having a volumetric median geometric diameter of less than equal to 5 pm WO 2014/144895 PCT/US2014/029491 FIG, A FI, I4 IMMEN[ Ia INE 048- - R 0,2 -20 0.0 0.10 1.'00 10.00 100.00 diameter (pm).
Bibliography:Application Number: AU20180253545