The complexity of traditional Chinese medicines (TCMs) is related to their multi-component\nsystem. TCM aqueous decoction is a common clinical oral formulation. Between molecules in\nsolution, there exist intermolecular strong interactions to form chemical bonds or weak non-bonding\ninteractions such as hydrogen bonds and Van derWaals forces, which hold molecules together to form\nââ?¬Å?molecular aggregatesââ?¬Â. Taking the TCM Puerariae lobatae Radix (Gegen) as an example, we explored\nfour Gegen decoctions of different concentration of 0.019, 0.038, 0.075, and 0.30 g/mL, named G-1,\nG-2, G-3, and G-4. In order of molecular aggregate size (diameter) the four kinds of solution were\nranked G-1 < G-2 < G-3 < G-4 by Flow Cell 200S IPAC image analysis. A rabbit vertebrobasilar artery\ninsufficiency (VBI) model was set up and they were given Gegen decoction (GGD) at a clinical dosage\nof 0.82 g/kg (achieved by adjusting the gastric perfusion volume depending on the concentration).\nThe HPLC fingerprint of rabbit plasma showed that the chemical component absorption into blood in\norder of peak area values was G-1 < G-2 > G-3 > G-4. Puerarin and daidzin are the major constituents\nof Gegen, and the pharmacokinetics of G-1 and G-2 puerarin conformed with the two compartment\nopen model, while for G-3 and G-4, they conformed to a one compartment open model. For all four\nGGDs the pharmacokinetics of daidzin complied with a one compartment open model. FQ-PCR\nassays of rabbitsââ?¬â?¢ vertebrobasilar arterial tissue were performed to determine the pharmacodynamic\nprofiles of the four GGDs. GGD markedly lowered the level of AT1R mRNA, while the AT2R mRNA\nlevel was increased significantly vs. the VBI model, and G-2 was the most effective. In theory the\ndosage was equal to the blood drug concentration and should be consistent; however, the formation\nof molecular aggregates affects drug absorption and metabolism, and therefore influences drugsââ?¬â?¢\neffects. Our data provided references for the rational use of Chinese medicines in the clinic, such as\nthe best oral preparation and decoction concentration.
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