抄録
The blood level and tissue distributions (tongue, gingiva, submandibular gland, parotid gland, cervical lymphonodi, liver and kidney) of peroral PCs, ampicillin and amoxicillin, were bioassayed using NZW rabbits weighing 2.5-3.5kg.
Samples were collected 10 times from 0.25 to 5 hours after oral administration for determination of the blood level, and 6 times from 0.5 to 5 hours after oral administration for determination of the tissue distributions.
Using 2 compartment model based on the measurement data, the pharmacokinetic pa-rameters of the blood level and tissue distributions in the tongue, gingiva, submandibular gland, parotid gland and cervical lymphonodi were determined and drew a simulation curve.
On comparing the Cmax and AUC of the blood level between ampicillin and amoxicillin from the pharmacokinetic parameters found as reliable from actual measurement, at the same dose amoxicillin showed the Cmax and AUC 2.00 and 2.47 times higher respectively than those of ampicillin.
On comparing the tissue distributions in the tongue, gingiva, submandibular gland, parotid gland and cervical lymphonodi from the same compartment model, the Cmax and AUC obtained with amoxicillin amounted 1.44 to 2.60 times and 1.49 to 2.21 times those of ampicillin respectively at the same dose.
On examining the calculation of ampicillin in the tongue, gingiva, submandibular gland, parotid gland and cervical lymphonodi in comparison with the blood level, the Cmax and AUC of tissue calculation amounted to 30.0-70.0% and 46.4-85.7% respectively of the blood level.
In the tissue calculation of amoxicillin in the tongue, gingiva, submandibular gland, parotid gland and cervical lymphonodi as compared to the blood level, the Cmax and AUC amounted to 24.1-54.9% and 39.3-70.0% respectively of the blood level.
