摘要
用四氧嘧啶（ａｌｌｏｘａｎ）引起的大鼠糖尿病模型，观察糖尿病早期对头孢噻肟（ＣＴＸ）药代动力学和药效学的影响。ＨＰＬＣ方法测定ＣＴＸ的血药浓度，用计算机计算各项药代参数。糖尿病组动物的血药峰浓度和ＡＵＣ值明显低于对照组，但两组的Ｔ１／２ｋａ和Ｔ１／２ｋｅ无明显差别，提示糖尿病早期不影响ＣＴＸ的吸收和消除速度。但由于ＣＴＸ的蛋白结合率降低，游离药物浓度增加，大量游离药物进入组织液，可使血中药物总浓度降低。ＣＴＸ对两组动物肺炎球菌感染的ＰＤ５０无明显差别，可能与糖尿病大鼠血中游离的药浓度提高有关。
The present paper describes the pharmacokindtics and
pharmacodynamics of CTX in both normal control rats and early
alloxan-diabetic rats in vivo. The plasma concentrations of CTX were
determined with HPLC. The main pharmacokinetic parameters of the two
groups were calculated with computer.Compared with the control group,
t冰Cand AUC in the diabetic group decreased significantly. Most of
the free drug was distributed to tissue fluid because the protein
binding of CTX decreased. But ,the T1/2 ka and T1/2 ke of the two
groups were not significantly different. It was suggested that the
absorption and elimination rate of CTX were not affected in early
diabetic rats. The PD50 of CTX against S. Pneumonias infection was
not different significantly between the two groups.This implies that
the therapeutic effect of CTX was enhanced as the plasma free
concentration could be increased in diabetic ratts.
出处
《药学学报》
CAS
CSCD
北大核心
1995年第7期495-499,共5页
Acta Pharmaceutica Sinica
