Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 8 of 8 for “"Intrinsic clearance"”.
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First-principle based pharmacokinetic modeling
… and experimental results indicate that apparent intrinsic clearance and intrinsic clearance could be affected by blood flow and protein binding. In Chapter 3, I discuss permeability limited hepatic elimination under perfusion steady state. Permeability limited elimination is classified to …
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Impact of CYP2C8 single nucleotide polymorphisms on in-vitro metabolism of imatinib to N-desmethyl imatinib
… (median ± SD K𝚖 = 6 ± 2 vs 11 ± 2 μM, p=0.04). Intrinsic clearance (Cl𝚒𝚗𝚝) was higher in CYP2C8*1/*3 HLMs compared to CYP2C8*1/*1 (median ± SD Cl𝚒𝚗𝚝 = 19 ± 8 vs 13 ± 2 μl/min/mg, p = 0.25). CYP2C8*3/*3 (pooled HLM) showed highest binding affinity (K𝚖 = 3.6 μM) and weak autoinhibition (K𝚒 = 449 …
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The Comparison of Rat and Human Intestinal and Hepatic Glucuronidation of Enterolactone Derived from Flaxseed Lignans
… microsomal fractions from both human and rat. An intrinsic clearance (CLint) value was calculated using the substrate depletion approach. In addition to monitoring substrate depletion, high-pressure liquid chromatography (HPLC) analysis allowed detection of EL glucuronides, which were further …
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Interspecies Pharmacokinetic Scaling and Metabolism of Alcohols and Glycols
… substrates: Enzyme affinity (1/Km) and in-vitro intrinsic clearance (CLintin-vitro) correlated positively with logP values; glycols showed lower CLintin-vitro values than straight-chain alcohols. In-vitro hepatic cytosol studies yielded acceptable in-vivo predictions for the metabolic clearance …
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Pharmacokinetics, pharmacogenetics and optimisation of treatment with non-nucleoside reverse transcriptase inhibitors in HIV-infected African children
… predictor of between-subject variability in clearance (89% and 68% decrease between fastest/slowest CYP2B6 metabolic subgroups for efavirenz and nevirapine, respectively). PK was affected by weight, described with allometric scaling. Nevirapine intrinsic clearance displayed diurnal variations …
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Lignocaine extraction ratio and clearance as an indicator of hypoxic hepatic injury : a study using the in situ and the isolated perfused pig liver
… and whether lignocaine extraction ratio and clearance could be used as an indicator of hepatic function. This was studied using the isolated pig liver perfused via the hepatic artery and portal vein. To establish whether the pig liver could be used as a possible human model for this …
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Hit to Lead Stage Optimization of Orally Efficacious β-Carboline Antimalarials
… less than or close to 100 nM. Unfortunately, the intrinsic clearance rate of several selected compounds was found to be higher than MMV1803522. These results left us with scope for the development of new analog compounds. The emerging structure-activity relationship within this scaffold and …
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Relationship Between Flavonoid Structure And Phase-II Metabolism
… was used along with in vitro glucuronidation intrinsic clearance values in recombinant human UGT isoforms. For objectives 4, 5 and 6, intact Caco-2 cell monolayers was used as the transport model, and Caco-2 cell lysate was used for measuring glucuronide formation rates. Results: 1) To …