Pharmacokinetics Research Service

Instruction manual

First Edition (Revised on April, 2016)

Pharmacokinetics Research Service

【Service Content】

Pharmacokinetics mainly study dynamic changes of drug metabolism in body, including drug absorption, distribution and excretion. The research will analyze the drugs and their metabolites by collecting samples in different tissues, organs at different time point. The pharmacokinetic experiments in vivo and in vitro can be designed according to customers’ requirements.

【Service Items】

1. Research evaluation in vivo

Plasma dynamics research, tissue distribution research and excretion research are included.

Detection method: LC-MS/MS, RT-PCR, ELISA, Isotopic labeling, etc.

Species: Dog, mouse, rat, rabbit, etc.

Drug administration: Intraperitoneal injection, intravenous injection, Intragastric administration, subcutaneous injection, intramuscular injection, intravenous infusion, subcutaneous infusion, nasal cavity and lateral ventricle injection, etc.

Sample collection: Blood sampling from caudal vein, dorsalis pedis vein, femoral vein,  eye socket and cheek; the collection of cerebrospinal fluid, tear, lymphatic fluid, urine, stool, bile, etc.

2. Research evaluation in vitro

Plasma protein binding rate, plasma stability, CYP450 inhibition and induction, liver microsomal metabolism test; metabolic products and pathways prediction and confirmation; transmembrane transport test, drug drug interaction detection, metabolic phenotype study and liver cell metabolism stability test are included.

In vitro Experiments can be divided into:

(1) Absorption tests

Intestinal absorption/Pgp binding experiment: Caco-2/PAMPA, bidirectional transport analysis, intestinal permeability analysis, Pgp substrate/inhibitor confirmation.

Transdermal absorption experiment: Skin, skin permeability.

(2) Distribution tests

Plasma protein binding rate: Plasma of different species, balanced dialysis/ultra filtration, molecular-exclusion chromatography (SHPLC, macromolecule), drug stability, comparative study of different species.

Blood distribution experiment: Drug concentration analysis (total blood and plasma concentration ratio), blood drug stability.

(3) Metabolic studies

Cytochrome P450 inhibition test: Human liver microsome and cDNA expression enzyme; CYP subtype: 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, D6, 2E1 & 3A4; standard substrate, IC50, time-dependent inhibition (TDI).

Cytochrome P450 induction test: Fresh liver and human hepatocytes; CYP isozyme, etc.

Drug metabolites research: Hepatocytes of different species; stability study of liver metabolism, metabolites identification and structure confirmation, comparative study of different species.

Detection method: Cell proliferation inhibition assay, chicken embryo angiogenesis inhibition assay, anti-bacteria and anti-virus detection in vitro, FCM, ELISPOT test, ELISA, etc.

【Customer Supply】

1. Cells; if the customers need common human, mouse or rat cell lines, we can offer them for free.

2. Related drugs and experimental scheme.

【Service Results】

1. Provide complete experimental data and charts.

2. Provide specific experimental report.