Oxazolidines have been described as potential pro-drugs having the amino- alcohol moiety. These would include many of the adrenergic agonists and beta blockers. These pro-drugs may enhance ocular, oral, dermal, nasal or pulmonary absorption of the parent drugs, as well as lessen first-pass raised about the formulation of these compounds, due to their instability in aqueous media. The purpose of the study is to investigate methods of stabilizing aqueous solutions of oxazolidines, which could perhaps lead to successful formulation procedures. Stabilization could either be accomplished by decreasing hydrolysis rate or shifting the equilibrium formed between oxazolidine, drug, and aldehyde to the left. The effects of pH and cyclodextrin (CD) analogs on hydrolysis rates and equilibria will be measured for ten oxazolidines using spectrophotometric and HPLC methods. An animal model will be used to identify conditions which lessen dosage requirements for pharmacological responses.
