Delivery, drug design metabolism

Barbizhayev, M. A. (2008). Ocular drug metabolism of the bioactivating antioxidant N-acetylcamosine for vision in ophthalmic prodrug and codrug design and delivery. Drug Dev. Ind. Pharm. 34,1071-1089. 

Figure 15.1. The retrometabolic drug design loop, includingchemical delivery system (CDS) design and soft drug (SD) design. A schematic representation of possible metabolic pathways for drugs in general is also included (see text for details).

Meijer DKF, Groothuis GMM, Mulder GJ, Swart PJ. The isolated perfused rat liver as a tool to study drug transport, drug metabolism and cell spediic drug delivery. In In Vitro and Ex Vivo Test Systems to Rationalize Drug Design and Delivery, Crommelin D, Couvreur P, Duchene D, Eds. Edition de Sante, Paris, 1994, pp. 17—31. 

The pharmacist should certainly know which drug dosage forms have been designed as delivery systems for prodrugs and also understand the mechanism whereby the active form is made available within the body. Only then can the pharmacist counsel the physician about why a certain product may be inappropriate for such individuals as an achlorhydric patient, a patient with a gastrectomy, or even possibly a patient with a hepatoportal bypass, if liver metabolism... 

The frequently used acronym LADME, which stands for liberation, absorption, distribution, metabolism, and excretion, broadly describes the various biopharmaceutical processes influencing the pharmacokinetics of a drug. Since each of aspect of LADME can influence the pharmacokinetics of a drug and ultimately the design of controlled release delivery devices, this section will review and explain the relationship between LADME processes and eight common pharmacokinetic parameters (F, K, Vd, tm, Cl, ha, tmax, Cp jnax). 

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