Explain following conditions in the equilibrium dialysis method while determining the protein binding of three different drugs (use appropriate diagrams for each case). Also give the inference for these cases. Give protein binding and volume of distribution values of these drugs in descending order. Cases after the period Concentration of drug in protein solution of internal compartment Concentration of free drug in external compartment Case I 1000 mg/ml 1000 mg/ml Case II 1500 mg/ml 500 mg/ml Case III 1100 mg/ml 900 mg/ml
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Answer:
evaluate by suitable rearrangement : 280+183+320+217
Answer:
The available techniques for the investigation of drug binding to plasma and tissues protein are reviewed and the advantages and disadvantages of the various techniques stated. A comparison of different plasma protein binding techniques is made which shows that the size of the unbound fraction of drug may be influenced by the method used. Protein binding may be assayed by methods including equilibrium dialysis, ultrafiltration, ultracentrifugation, gel filtration, binding to albumin microspheres and circular dichroism. Tissue binding techniques can involve testing binding to isolated organs, tissue slices, homogenates and isolated subcellular particles. Details of the available methods to compute pharmacokinetic constants are given. Stereoselective binding has been investigated for a limited number of drugs and the difference in the binding of 2 enantiomers is usually modest. The measurement of the binding constants is often required to characterise the drug-protein interaction. Mathematical and graphical methods to compute the pharmacokinetic parameters are discussed. The implications of binding on the volume of distribution and clearance of drugs are examined.
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