Uematsu M
Shikwa Gakuho. 1989 Jan;89(1):127-53.
The author attempted to determine the feasibility of monitoring blood concentration of antimicrobial agents by estimating blood levels of the agents on the basis of their content in saliva. Since it is difficult to determine drug tissue-penetration degree in humans, at present, tissue concentrations must be estimated from corresponding blood concentration. In the case of orally administered drugs exhibiting great individual differences in absorption by the gastrointestinal tract, frequent blood collection is required for blood-concentration monitoring. Noninvasive and very simple saliva collection, on the other hand, has already been used for monitoring concentrations of such drugs as carbamazepine and antiepileptics. PPA, ENX, NFLX, and OFLX are pyridonecarboxylic acid antimicrobial agents of great usefulness because of their expanded antimicrobial spectrum and their effectiveness even against gram-negative bacteria that exhibit no adequate response to other oral antimicrobial agents. After PPA, ENX, NFLX, and OFLX were administered orally to healthy volunteers, serum and saliva samples were collected. The samples were then centrifuged, deproteinized, and freeze-dried. 1. After the freeze-dried samples were dissolved to give tenfold to twentyfold concentrated solutions, levels of agents were bioassayed by means of the thin-layer-disc method. On the basis of the data obtained in this way, pharmacokinetic analyses were performed according to the one compartment model of Imoto and Yamaoka. A personal computer (NEC-8801, 9801) was used in drawing simulated curves. 2. Percentages of salivary as compared to serum concentrations were as follows: PPA (500 mg)-70, ENX (300 mg)-75, ENX (200 mg)-78, NFLX (200 mg)-35, and OFLX (200 mg)-105. Corresponding values for pharmacokinetic data were as follows: PPA (500 mg)-77.2, ENX (300 mg)-74.2, ENX (200 mg)-85.0, NFLX (200 mg)-30.0, and OFLX (200 mg)-91.6. Coefficients of correlation (r =) between salivary and serum concentrations in measured data were as follows: PPA (500 mg)-0.915, ENX (300 mg)-0.989, ENX (200 mg)-0.953, NFLX (200 mg)-0.887, and OFLX (200 mg)-0.886.(ABSTRACT TRUNCATED AT 400 WORDS)
作者试图通过根据唾液中抗菌药物的含量来估算其血药浓度，从而确定监测抗菌药物血药浓度的可行性。由于难以确定人体中药物的组织穿透程度，目前，必须根据相应的血药浓度来估算组织浓度。对于口服给药后在胃肠道吸收方面存在很大个体差异的药物，进行血药浓度监测时需要频繁采血。另一方面，非侵入性且非常简单的唾液采集已被用于监测卡马西平和抗癫痫药物等的浓度。吡哌酸（PPA）、依诺沙星（ENX）、诺氟沙星（NFLX）和氧氟沙星（OFLX）是吡啶酮羧酸类抗菌药物，因其抗菌谱扩大且对其他口服抗菌药物无充分反应的革兰氏阴性菌也有效而非常有用。在对健康志愿者口服PPA、ENX、NFLX和OFLX后，采集血清和唾液样本。然后将样本离心、去蛋白并冻干。1. 将冻干样本溶解制成浓度为原来10至20倍的溶液后，采用薄层圆盘法对药物水平进行生物测定。基于以这种方式获得的数据，根据井本和山冈的单室模型进行药代动力学分析。绘制模拟曲线时使用了个人计算机（NEC - 8801、9801）。2. 唾液浓度与血清浓度的百分比分别如下：PPA（500毫克） - 70、ENX（300毫克） - 75、ENX（200毫克） - 78、NFLX（200毫克） - 35、OFLX（200毫克） - 105。药代动力学数据的相应值如下：PPA（500毫克） - 77.2、ENX（300毫克） - 74.2、ENX（200毫克） - 85.0、NFLX（200毫克） - 30.0、OFLX（200毫克） - 91.6。实测数据中唾液浓度与血清浓度之间的相关系数（r =）如下：PPA（500毫克） - 0.915、ENX（300毫克） - 0.989、ENX（200毫克） - 0.953、NFLX（200毫克） - 0.887、OFLX（200毫克） - 0.886。（摘要截取自400字）
