Removal of inhaled 99mTc-labelled particles of disodium cromoglycate from the lungs.
Disodium cromoglycate particles were labelled with 99mTc by spray-drying technique. The in vitro dissolution profile as well as the leakage of radioactivity from the drug particles were determined using a through-flow cell method. The radioactive drug particles were mixed with a lactose carrier and inhaled from a dry powder device by five healthy volunteers. The removal of the inhaled drug particles from the lungs was evaluated by a gamma camera. A close relationship between the dissolution of the drug as such and the leakage of radioactivity was noted. Gamma scintigraphy indicated a biphasic exponential removal of radioactivity from the lung region. The slow component with the halftime of about 55 min was mainly due to the dissolution of drug particles in the lungs. The halftime of the fast component describing mucociliary clearance was less than 10 min. This process was the dominating one for the removal of the drug from the lungs. The experiment thus showed that the main fraction of the inhaled dose was deposited in the tracheobronchial region. Accordingly, only a small portion of the dose initially deposited in the lung can be absorbed and induce a therapeutic effect.
Vidgren
P
P
Department of Pharmaceutical Technology, University of Kuopio, Finland.
Vidgren
M
M
Paronen
P
P
Vainio
P
P
Karjalainen
P
P
Nuutinen
J
J
D000336:Aerosols; D004205:Cromolyn Sodium / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006801:Humans; D008168:Lung / Q000378:metabolism*; D013667:Technetium
D000336:Aerosols; D013667:Technetium; D004205:Cromolyn Sodium