Study of the hygroscopic properties of selected pharmaceutical aerosols using single particle levitation.
OBJECTIVE
To use a single particle levitation technique to investigate the equilibrium water sorption characteristics in both the evaporation and growth of four respiratory drugs at 37 degrees C: atropine sulfate (AS), isoproterenol hydrochloride (IPHC) and isoproterenol hemisulfate (IPHS) and disodium cromoglycate (DSCG).


METHODS
The equilibrium water content was measured as a function of relative humidity (RH) by a single particle levitation technique using an electrodynamic balance (EDB). The change of water content was determined by the voltage required to balance the weight of the levitated particle electrostatically. The water activities of bulk samples were also measured. Growth ratios 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 drugs. At RH approximately 0%, AS particles still contain about 5% water but IPHC and IPHS particles do not contain any residual water. The aerodynamic growth ratio from RH 0% to 99.5% is 2.60, 2.86, 2.42 and 1.26 for AS, IPHC, IPHS and DSCG, respectively. Supersaturated droplets of IPHC and IPHS are expected 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 may experience supersaturation before they enter the human body and this could exert a significant influence both on particle loss before inhalation and on the deposition of the drugs in the lungs. The EDB is a convenient and reliable tool for studying the hygroscopic properties of pharmaceutical aerosols, especially for supersaturated solutions.
Peng
C
C
Department of Chemical Engineering, Hong Kong University of Science and Technology, Clear Water Bay, Kowloon.
Chow
A H
AH
Chan
C K
CK
D000336:Aerosols / Q000737:chemistry*; D001285:Atropine / Q000737:chemistry*; D004205:Cromolyn Sodium / Q000737:chemistry*; D006801:Humans; D006813:Humidity; D007545:Isoproterenol / Q000737:chemistry*; D014867:Water / Q000737:chemistry*; D017155:Wettability
D000336:Aerosols; D014867:Water; D001285:Atropine; D007545:Isoproterenol; D004205:Cromolyn Sodium