Analysis of the importance of pharmacokinetics in preclinical studies

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 In the process of new drug development, it is necessary to conduct pharmacokinetic studies to analyze the pharmacokinetic parameters of drugs in vivo and use them as their outstanding advantages and effects. 

Generally speaking, drugs with exceptional benefits should have shallow toxic side effects, good pharmacodynamic and pharmacokinetic properties, high efficiency of utilization and absorption, high solubility, and low toxicity of metabolites in vivo, etc., which can be used to guide new drug development and clinical drug use.

The drug’s utilization and absorption efficiency are relatively high, and it has relatively high solubility. Moreover, the toxicity of metabolites in the body is relatively low, which can be used to guide the development of new drugs and clinical medication.

Pharmacokinetics is a discipline that adopts mathematical principles and methods to quantitatively analyze and describe the dynamic processes of drugs and their regularity in vivo, which can quantitatively study the absorption, distribution, metabolism, and excretion patterns of drugs in living organisms. Mediiclon Pharmacokinetics Lab has passed the  GLP  certification by  NMPA. Following the guiding principles of ICH,  NMPA  and FDA. The lab offers in vivo and in vitro pharmacokinetic tests according to the needs of our clients and provides them with complete sets of pharmacokinetic evaluation and optimization services.

1. The application of pharmacokinetics in pharmacological research

A drug needs to maintain the corresponding concentration and reach the related target site and the affiliated site of action for effective binding, to produce drug-receptor interactions and the corresponding pharmacological effects. The strength of the pharmacological effect is critical and related to the relevant factors, mainly the concentration of the drug at the site of action. 


For example, the strength of Furosemide diuretic has a linear relationship with Na+ excretion, urine flow, and blood concentration; salicylic acid has an analgesic effect when it reaches 50-100mg/L in the body anti-rheumatic effect when the attention is more significant than 250mg/L, anti-inflammatory effect when the concentration is 350-450mg/L; toxic side effects will occur when the concentration is more important than 500mg/L; toxic death will happen when the attention is 1600mg/L-1800mg/L. The study of pharmacokinetics can further investigate the pharmacological effects of the drug to guide the clinical use of the drug.

2. Application of pharmacokinetics to toxicology studies

In toxicology research, drug metabolism kinetics and toxicity tests are fully integrated and linked to explore the laws of adverse reactions and drug toxicity to guide toxicology research. Toxicokinetics is the link between clinical and non-clinical trials, mainly to determine the relationship between comparative systemic toxicity, exposure, and toxicokinetic data over time. It can be used to explain the toxicological findings or changes in the drug in the trial, thus providing a basis for preclinical toxicity testing through the study of metabolites and revealing the mechanism of action of toxicity.


3. The application of pharmacokinetics in formulation research

High-quality drug dosage forms have distinct advantages and characteristics, including safety, stability, etc. The practical application of pharmacokinetics positively affects the acute and effective screening and evaluation of drugs. On this basis, it provides an essential guarantee for the scientific and rational use of clinical medicines to ensure the safety of clinical drug use. In China and abroad, comprehensive and in-depth research has been conducted on targeted and controlled release formulations, which have become a hot issue of great concern. They can maintain the effective concentration of drugs, reduce the number of doses to a certain extent, and reduce their side effects. Through a comprehensive and in-depth study of the pharmacokinetics of formulations, we can effectively evaluate various dosage forms of drugs and effectively combine and link them with the relevant regulations and requirements.

The biological activity and activity intensity of drugs in vivo are closely related to their absorption, distribution, metabolism, and excretion processes and characteristics in vivo, so the in-depth study of drug metabolism kinetics has specific hints and guidance to reveal their biological effects and mechanisms of action in vivo. With the development of the discipline and the improvement of research technology, the impact of drugs on the drug disposal system of organisms such as transporters and metabolic enzymes also belongs to the research of drug metabolism kinetics. The disposition of drugs in the organism determines to a certain extent, the strength of its efficacy or toxicity, so the study of pharmacokinetics has a vital role and significance in the process of innovative drug development.

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