Production of ultrafine sumatriptan succinate particles for pulmonary delivery.
OBJECTIVE
Drug particle physical properties are critical for the efficiency of a drug delivered to the lung. The purpose of this study was to produce ultrafine sumatriptan succinate particles for inhalation.


METHODS
Sumatriptan succinate particles were produced via reactive precipitation without any surfactants. Several low toxic organic solvents such as acetone, isopropanol, and tetrahydrofuran were investigated as the reaction medium. And the dry powder was obtained via spray drying. FT-IR, HPLC, SEM and XRD were exploited to characterize the physicochemical properties of the ultrafine sumatriptan succinate dry powder. The aerosol performance of the powder was evaluated using an Aeroliser connected to a multi stage liquid impinger operating at 60 l/min.


RESULTS
The mean particle size of the ultrafine sumatriptan succinate particles obtained under optimum conditions was in the range of 630-679 nm and consequently they were in the respirable range. The spray-dried powder whose fine particle fraction was increased up to 50.6 +/- 8.2% showed good aerosol performance whereas the vacuum-dried powder was approximate 18.2 +/- 3.0%.


CONCLUSIONS
Good aerosol performance ultrafine sumatriptan succinate particles could be produced by reactive precipitation without any additives followed by spray drying at the optimum parameters.
Yang
Zong-Yang
ZY
Sin-China Nano Technology Center, Key Lab for Nanomaterials, Ministry of Education, Beijing University of Chemical Technology, Beijing, 100029, People's Republic of China.
Le
Yuan
Y
Hu
Ting-Ting
TT
Shen
Zhigang
Z
Chen
Jian-Feng
JF
Yun
Jimmy
J
D000280:Administration, Inhalation; D000336:Aerosols; D011232:Chemical Precipitation; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D018360:Crystallography, X-Ray; D006801:Humans; D008855:Microscopy, Electron, Scanning; D009330:Nebulizers and Vaporizers; D010316:Particle Size; D011208:Powders; D017366:Serotonin Receptor Agonists / Q000008:administration & dosage / Q000737:chemistry*; D012995:Solubility; D012997:Solvents / Q000737:chemistry; D017550:Spectroscopy, Fourier Transform Infrared; D018170:Sumatriptan / Q000008:administration & dosage / Q000737:chemistry*; D013499:Surface Properties; D013678:Technology, Pharmaceutical / Q000379:methods; D013696:Temperature
D000336:Aerosols; D011208:Powders; D017366:Serotonin Receptor Agonists; D012997:Solvents; D018170:Sumatriptan