ABSTRACT

I. Introduction......................................................................................................................... 92

II. Potential Benefits from Lung Targeting of Drugs Via Pro-Drugs.................................92 A. Improved Selectivity of Action in Lung Relative to Effects on Other

Organs........................................................................................................................ 92 1. DipivaloyI Isoproterenol......................................................... 92 2. Bitolterol......................................................................................................... 92

B. Prolongation of Therapeutic E ffect........................................................................ 92 C. Conferral of Pulmonary Activity or Enhancement of Pulmonary Activity........ 93

III. Desirable Attributes for a Pulmonary Pro-Drug............................................................. 94 A. Lung Uptake............................................................................................................. 94 B. Lung Metabolic Capability to Convert Pro-Drug to Active Drug M oiety......... 99 C. Retention of Parent Drug in Lung Tissue after Release from Pro-Drug.............99