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By Joseph Robinson, Vincent H. L. Lee

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Additional info for Controlled Drug Delivery: Fundamentals and Applications, Second Edition

Example text

Indeed, it is not unusual for a disease state to act as a stimulus for development of a controlled release drug delivery system. A case in point is rheumatoid arthritis, for which aspirin is still the drug of choice [194] . Normally, aspirin would not be considered to be a likely candidate for sustained release because its biological half-life is 6 hr [195]. However, a sustained release product would be advantageous to maintain therapeutic concentrations, particularly 34 J Li et al. throughout the night, thus alleviating morning stiffness [196].

However, the absorptive surfaces of most routes are impermeable to macromolecules or other targeted delivery systems, thereby necessitating either intravascular or intraarterial administration. Acute or chronic therapy: Consideration of whether one expects to achieve cure or control of a condition and the expected length of drug therapy are important factors in designing controlled release systems. Attempts to generate a one year contraceptive implant presents significantly different problems in design than does an antibiotic for acute infection.

One aspect of this distribution is binding of drug to tissues and proteins in blood. An extensive discussion of this phenomenon can be found in a series of papers by Kruger-Thiemer et al. [77-81]. In general, the bound portion of a drug can be considered inactive and unable to cross membranes. At high binding one sees prolonged drug action. The apparent volume of distribution of a drug is frequently used to describe the magnitude of distribution, including binding, within the body. Conceptually, this pharmacokinetic parameter can be viewed as a proportionality constant relating plasma or serum concentration of drug to total amount of drug in the body.

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