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Chapter
Introduction to Pharmacokinetics
Pharmacokinetics (drug kinetics) deals with the in vivo fate or disposition processes of the drug (i.e., how the body does to the drug) that determine drug exposure in the body and therefore pharmacological ef...
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Chapter
Circadian Clock and Non-CYP Phase I Metabolism
Circadian rhythms in drug metabolism by non-CYP phase I enzymes (i.e., MAOs) have been recognized since 1970s. The profound effects of the circadian clock on non-CYP phase I metabolism are highlighted recently...
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Chapter
Circadian Clock and Uptake Transporters
Transport of drugs across biological membranes is a critical step in pharmacokinetic processes. Uptake transporters are membrane proteins that mediate the transport of a large number of drugs into cells. Becau...
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Chapter
Circadian Clock and Phase II Metabolism
Circadian clock is an endogenous oscillator (consisting of multiple clock genes) that drives circadian rhythms. Phase II metabolism is referred to conjugation reactions through which parent compounds and certa...
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Chapter
Circadian Clock and Efflux Transporters
Efflux transporters from the ATP-binding cassette (ABC) and solute carrier (SLC) families [e.g., P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), multidrug resistance proteins (MRPs), and multid...
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Chapter
Introduction to Mammalian Circadian Clock System
Organisms on Earth are dictated by circadian changes (e.g., sunlight, humidity, and temperature) in the environment caused by the planet’s rotation around its own axis. All forms of life have evolved biologica...
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Article
Nanosuspensions Containing Oridonin/HP-β-Cyclodextrin Inclusion Complexes for Oral Bioavailability Enhancement via Improved Dissolution and Permeability
Chemotherapy via oral route of anticancer drugs offers much convenience and compliance to patients. However, oral chemotherapy has been challenged by limited absorption due to poor drug solubility and intestin...
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Article
Glucose-Based Mesoporous Carbon Nanospheres as Functional Carriers for Oral Delivery of Amphiphobic Raloxifene: Insights into the Bioavailability Enhancement and Lymphatic Transport
Oral therapy with raloxifene (RXF), an amphiphobic drug for remedy of the postmenopausal osteoporosis and estrogen-dependent breast cancer, is less effective due to its poor bioavailability (2% or so). This wo...
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Article
Erratum to: Regioselective Glucuronidation of Andrographolide and Its Major Derivatives: Metabolite Identification, Isozyme Contribution, and Species Differences
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Article
Regioselective Glucuronidation of Andrographolide and Its Major Derivatives: Metabolite Identification, Isozyme Contribution, and Species Differences
Andrographolide (AND) and two of its derivatives, deoxyandrographolide (DEO) and dehydroandrographolide (DEH), are widely used in clinical practice as anti-inflammatory agents. However, UDP-glucuronosyltransfe...
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Article
A New Strategy to Rapidly Evaluate Kinetics of Glucuronide Efflux by Breast Cancer Resistance Protein (BCRP/ABCG2)
The efflux transporter breast cancer resistance protein (BCRP/ABCG2) plays an important role in excretion of anionic drugs and metabolites including glucuronides in humans.
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Article
Accurate Prediction of Glucuronidation of Structurally Diverse Phenolics by Human UGT1A9 Using Combined Experimental and In Silico Approaches
Catalytic selectivity of human UGT1A9, an important membrane-bound enzyme catalyzing glucuronidation of xenobiotics, was determined experimentally using 145 phenolics and analyzed by 3D-QSAR methods.
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Article
Regioselective Glucuronidation of Flavonols by Six Human UGT1A Isoforms
Glucuronidation is a major barrier to flavonoid bioavailability; understanding its regiospecificity and reaction kinetics would greatly enhance our ability to model and predict flavonoid disposition. We aimed ...