抗生素89－07在大鼠体内组织分布及与正常人血浆蛋白结合率研究

Comparison tissue distribution in rat and plasma protein binding between antibiotic 89-07 and gentamicin

本文报道抗生素８９－０７在大鼠体内组织分布及与人血浆蛋白结合率，并与庆大霉素作比较，以了解抗生素８９－０７与庆大霉素在以上特性中的差异，对其进行药理学评价。结果表明：抗生素８９－０７和庆大霉素在大鼠体内各组织中以肾脏中药物含量最高，３ｍｉｎ时分别为９．４８±２．１７和６．２１±３．１０μｇ／ｇ，３０ｍｉｎ分别为９．７５±２．４５和１０．４５±３．３３μｇ／ｇ，２４０ｍｉｎ分别为１２．２７±７．３４和１３．８５±７．１７μｇ／ｇ。另外还测定了脑、心、胃肠道、胰、脾、肝、生殖腺、肌肉、脂肪和血中的浓度。抗生素８９－０７与人血浆蛋白结合率为２３．２１％±１．５３％；庆大霉素为２５．５１％±１．０２％，两者间无显著性差异（Ｐ＞０．０５）。由研究结果可以看出，抗生素８９－０７在大鼠体内组织分布及与正常人血浆蛋白结合率与庆大霉素相似。

Plasma protein binding of antibiotic 89-07 was compared with that ofgentamicin by using the equilibrium dialysis technique。 The plasma protein binding rate ofantibiotic 89-07 were 25. 38%±4. 59%,22.13%±3.21%, 22. 12%±5. 26%with serumconcentration 10,4,2mg/L respectively. The plasma protein binding rate of gentamicin were25. 89%±2. 46%, 26. 53%±1.32%,24. 12%±3. 94%at the same serum concentration。The differences between them were not significant(P>0.05). Tissuedistribution in rat was studied by bioassay. The concentrations of antibiotic89-07 in kidney at three time intervalsweredetermined as the following9.48±2. 17μg/gat3min,9. 75 ±2. 45μg/gat30min, 12. 27 ± 7.34μg/g at 240min , compared with that of gentamicin 6. 21 ±3 . 10μg/g at3min,10. 45 ± 3. 33μg/g at 30min, 13. 85 ± 7. 17μg/g at 240min, In this experiment, 11kinds of organs have been studied. Results showed effective diffusion and combination ofantibiotic 89-07 with kidney。 The differences between these two regimens of tissueconcentration were not significant.