Cg. Peng et al., Study of the hygroscopic properties of selected pharmaceutical aerosols using single particle levitation, PHARM RES, 17(9), 2000, pp. 1104-1109
Purpose. To use a single particle levitation technique to investigate the e
quilibrium water sorption characteristics in both the evaporation and growt
h of four respiratory drugs at 37 degreesC: atropine sulfate (AS), isoprote
renol hydrochloride (IPHC) and isoproterenol hemisulfate (IPHS) and disodiu
m cromoglycate (DSCG).
Methods. The equilibrium water content was measured as a function of relati
ve humidity (RH) by a single particle levitation technique using an electro
dynamic balance (EDB). The change of water content was determined by the vo
ltage required to balance the weight of the levitated particle electrostati
cally. The water activities of bulk samples were also measured. Growth rati
os were determined and compared with values in the literature.
Results Crystallization or deliquescence was not observed for AS, IPHC and
IPHS. The hysteresis in the water cycle was not observed for any of the dru
gs. At RH similar to 0%, AS particles still contain about 5% water but IPHC
and IPHS particles do not contain any residual water. The aerodynamic grow
th ratio from RH 0% to 99.5% is 2.60, 2.86, 2.42 and 1.26 for AS, IPHC, IPH
S and DSCG, respectively. Supersaturated droplets of IPHC and IPHS are expe
cted to exist in the ambient conditions. DSCG is in a solid state in the RH
range of 10-90%.
Conclusions. It is expected that some aerosolized drugs of low solubility m
ay experience supersaturation before they enter the human body and this cou
ld exert a significant influence both on particle loss before inhalation an
d on the deposition of the drugs in the lungs. The EDB is a convenient and
reliable tool for studying the hygroscopic properties of pharmaceutical aer
osols, especially for supersaturated solutions.