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Pharmacokinetics - An important perspective in drug research
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Drug discovery and drug research have become fast growing fields of research. As more and more new prospective drugs appear, pharmacology starts playing a major role in the discovery process. The prospective drugs undergo a number of high-throughput screening processes after which they ultimately become potential drugs.

Pharmacology deals with the effect of the compounds within the body thereby affecting the function of the biological system. It covers mainly two areas: pharmacokinetics and pharmacodynamics. While the latter deals with the effect of the drug on the body, the former deals with the effect of the biological system of the body on the drug. Both determine the fate of the prospective compounds in becoming potential drugs. Among them, Pharmacokinetics plays a vital role in drug discovery in which the drug-like properties of the prospective compounds are tested in both in-vitro and in-vivo environment.

Pharmacokinetics is the study of the concentration time course of a compound and its metabolite within the body based on the ADME-Tox properties of the compound. After ingestion, the compound undergoes a series of changes within the body starting from the solubilisation of the compound, absorption, digestion, metabolism, and ultimately excretion from the body. After ingestion, the concentration of the compound firstly increases within the blood stream with time due to the solubilisation of the compound and then, after metabolism, the concentration decreases with time with an increase in the corresponding metabolite of the compound. The Pharmacokinetics of a compound is studied based on a number of pharmacokinetic or PK parameters like clearance, half-life, etc., measured with the help of invitro experiments, which may be cell-based or non-cell based. The concentration of the compounds and their corresponding metabolites is measured in an HPLC or LC/MS after conducting the experiments. After the compounds are screened based on invitro experiments, they are tested on animals like rats, mice, etc., which is known as animal pharmacokinetics. In this process, blood or serum of the animal is collected at various time-intervals after the ingestion of the compound. The concentration of the compound and its metabolite is measured with the help of LC/MS. LC/MS is usually used in the measurement of the compound and its metabolite after proper extraction procedure, as it can measure very low amounts of the same present in the biological fluids with minimal interference from the proteins, etc present in the fluids. After proper statistical analysis of the data, the PK parameters are measured. Based on this data, the potential drug-like compounds are screened for further tests.

The PK parameters of the compounds are greatly affected due to the plasma protein binding of the compounds within the body. These plasma proteins bind the compounds and thereby reduce their bioavailability in the body. Moreover, the different barriers in the body like intestinal barrier, BBB, etc also reduce the bioavailability of the compounds in many cases. Hence, along with the usual tests of solubility, metabolism, etc of the compound, a study is carried out regarding the effects of plasma proteins and various barriers within the body on the compounds in order to get a clearer idea of the bioavailability of the compounds. The combined study gives a true picture regarding the PK parameters of the compounds. These tests are also performed invitro in the drug discovery lab. In the preliminary screening, the toxicity studies also form a very vital part, as a compound may have drug-like properties and be toxic too which thereby rejects it during the screening process.

Although, the entire process may seem like a simple one, but it is a long drawn process whereby, both the chemistry and biology departments are involved and go hand in hand to make drug discovery a success. Even though some compounds may be selected to be having drug-like properties in the first range of tests, but they then undergo even further chemical modifications in their structure to make them more potential in nature. These structural modifications depend on their nature of solubility, metabolism, and bioavailability. If they possess further enhanced drug-like properties after structural modification, then they undergo different cell assays and series of tests on animals before undergoing tests on human trials, which forms the last stage in drug discovery process.
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Pharmacokinetics - An important perspective in drug research00