Biopharmaceutics and Pharmacokinetics by Venkateswarlu: Basics and Advanced Topics PDF
anomalous dissolution of insoluble drug forms an inclusion complex with water-soluble polymers. the dissolution profile of ibuprofen may be changed by complexation with excipients such as polyethylene glycols, arginine, glucose, sodium chloride, taurine, and trehalose. in addition, modified release of ibuprofen is achieved with a combination of polymers and surfactants. the dissolution of mebendazole decreased in a ph-dependent manner when it is complexed with hp-beta-cd. however, the addition of hp-beta-cd was reported to be unstable when mebendazole was complexed with another water-soluble derivative of beta-cyclodextrin, sulfobutylether beta-cyclodextrin, and the drug precipitation was prevented with the addition of polyethylene glycol. solubility of curcumin and fluconazole can be increased with the formation of inclusion complexes. the complexes of filipin and cholesterol facilitated cholesterol-dependent membrane localization of filipin and diffusion of filipin from the membrane to the interior of the cell. this formed a lipid raft scaffold and changed the cholesterol-dependence of endocytosis of filipin. the interaction of cholesterol with beta-cyclodextrin improved the solubility of bovine serum albumin. half-life of cimetidine is prolonged with the formation of inclusion complex with beta-cyclodextrin and hydroxypropyl-beta-cyclodextrin. change of pharmacokinetics caused by changes in the solubility of a drug is often reported. an example of a successful case is clopidogrel-loaded poly(d,l-lactide-co-glycolide) nanoparticles; the dissolution rate of the clopidogrel-loaded nanoparticles was slower than the free clopidogrel. an increased f and half-life of clopidogrel were obtained with decreasing the particle size of nanoparticles. simultaneous loading of the poorly soluble drug bicalutamide and clopidogrel into plga and poly(d,l-lactide-co-glycolide) nanoparticles also increased the f and half-life of clopidogrel.
biopharmaceutics and pharmacokinetics by venkateswarlu pdf download