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Physiologically based pharmacokinetic modeling of small molecules: How much progress have we made?
N Isoherranen - Drug Metabolism and Disposition, 2024 - Elsevier
Physiologically based pharmacokinetic (PBPK) models of small molecules have become
mainstream in drug development and in academic research. The use of PBPK models is …
mainstream in drug development and in academic research. The use of PBPK models is …
Innovations, opportunities, and challenges for predicting alteration in drug-metabolizing enzyme and transporter activity in specific populations
Drug-metabolizing enzymes and transporters (DMETs) are key regulators of the
pharmacokinetics, efficacy, and toxicity of therapeutics. Over the past two decades …
pharmacokinetics, efficacy, and toxicity of therapeutics. Over the past two decades …
Phase 1 pharmacokinetic and safety study of soticlestat in participants with mild or moderate hepatic impairment or normal hepatic function
W Yin, P Mitra, V Copalu, TC Marbury… - Pharmacology …, 2024 - Wiley Online Library
Abstract This phase 1, open‐label, three‐arm study (NCT05098054) compared the
pharmacokinetics and safety of soticlestat (TAK‐935) in participants with hepatic impairment …
pharmacokinetics and safety of soticlestat (TAK‐935) in participants with hepatic impairment …
Incorporation and performance verification of hepatic portal blood flow shunting in minimal and full PBPK models of liver cirrhosis
Patho‐physiological changes in liver cirrhosis create portacaval shunts that allow blood flow
to bypass the hepatic portal vein into the systemic circulation affecting drug …
to bypass the hepatic portal vein into the systemic circulation affecting drug …
Simultaneously predicting the pharmacokinetics of ces1-metabolized drugs and their metabolites using physiologically based pharmacokinetic model in cirrhosis …
X Luo, Z Zhang, R Mu, G Hu, L Liu, X Liu - Pharmaceutics, 2024 - mdpi.com
Hepatic carboxylesterase 1 (CES1) metabolizes numerous prodrugs into active ingredients
or direct-acting drugs into inactive metabolites. We aimed to develop a semi-physiologically …
or direct-acting drugs into inactive metabolites. We aimed to develop a semi-physiologically …
Toward improved predictions of pharmacokinetics of transported drugs in hepatic impairment: Insights from the extended clearance model
Abstract Hepatic impairment (HI) moderately (< 5‐fold) affects the systemic exposure (ie,
area under the plasma concentration–time curve [AUC]) of drugs that are substrates of the …
area under the plasma concentration–time curve [AUC]) of drugs that are substrates of the …
[HTML][HTML] Disposition of Oral Nalbuphine and Its Metabolites in Healthy Subjects and Subjects with Hepatic Impairment: Preliminary Modeling Results Using a …
S Nagar, A Hawi, T Sciascia, K Korzekwa - Metabolites, 2024 - mdpi.com
Nalbuphine (NAL) is a mixed κ-agonist/μ-antagonist opioid with extensive first-pass
metabolism. A phase 1 open-label study was conducted to characterize the …
metabolism. A phase 1 open-label study was conducted to characterize the …