ABSTRACT

VINCENT H. K. LI and JOSEPH R. ROBINSON / Universi ty of Wisconsin , Madison, Wisconsin

VINCENT H. L. LEE / Universi ty of Southern California, Los Angeles , California

I . In t roduct ion 4

II . Terminology 5

I I I . Rationale of Susta ined/Control led D r u g Delivery 7

IV. Factors Influencing the Design and Performance of Susta ined/Control led Release Products 9

V. Physicochemical Proper t i es of a D r u g Influencing Design and Performance 12

A. Aqueous Solubility 13 B . Part i t ion Coefficient and Molecular Size 14 C. D r u g Stability 14 D . Protein Binding 15

VI. Biological Factors Influencing Design and Performance of Susta ined/Control led Release Produc ts 15

A. Absorption 16 B . Dis t r ibut ion 18 C. Metabolism 23 D . Duration of Action 26 E. Side Effects 30 F . Margin of Safety 31

G. Role of Disease State 33 H. Role of Circadian Rhythm 35

VII . Selected Routes of D r u g Administration 36

VIII .