Evaluation of pharmaceutical excipients as cosolvents in 4-methyl umbelliferone glucuronidation in human liver microsomes: applications for compounds with low solubility.

@article{Argikar2011EvaluationOP,
  title={Evaluation of pharmaceutical excipients as cosolvents in 4-methyl umbelliferone glucuronidation in human liver microsomes: applications for compounds with low solubility.},
  author={Upendra A Argikar and Guiqing Liang and Jennifer L Bushee and Vinayak P Hosagrahara and Wendy S. C. Lee},
  journal={Drug metabolism and pharmacokinetics},
  year={2011},
  volume={26 1},
  pages={102-6}
}
Standard incubation procedures for carrying out microsomal assays involve the use of less than 1% w/v organic solvents to minimize the potential inhibitory effects of organic solvents on metabolic activity. This presents a practical limitation for poorly soluble xenobiotics, which cannot be incubated at concentrations high enough to obtain a V(max), and therefore subsequent values for K(m) and Cl(int) cannot be calculated. Our goal was to study the application of a variety of pharmaceutical… CONTINUE READING

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