术前服用盐酸安妥沙星后患者被切除肺组织中药物浓度分析

Concentrations of Preoperative Oral Antofloxacin Hydrochloride in Patients after Resection of Lung Tissue were Analyzed

目的研究盐酸安妥沙星口服400 mg在肺组织中药物浓度,初步评价术前应用口服单剂盐酸安妥沙星400 mg作为肺叶切除术预防感染用药的可靠性。方法选取2011年1月至2013年8月肺叶切除术患者48例,按距离支气管离断前时间不同随机分为4、8、12、24 h给药共4组,口服盐酸安妥沙星400 mg,收集血液标本和肺组织标本,采用高效液相色谱法测定血浆及肺组织中药物浓度。结果 4、8、12、24 h组血浆和肺组织中药物浓度分别为(3.281±0.817)μg·mL-1和(5.992±3.228)μg·g-1、(3.192±0.953)μg·mL-1和(5.885±2.952)μg·g-1、(1.712±0.576)μg·mL-1和(3.419±1.107)μg·g-1、(0.431±0.095)μg·mL-1和(1.258±0.306)μg·g-1。结论口服盐酸安妥沙星后药物在肺组织中药物清除时间大于血浆药物清除时间,肺叶切除术术前12 h内口服单剂盐酸安妥沙星400 mg在肺组织中的药物浓度可以达到有效抗菌作用,理论上肺叶切除术术前12 h内口服盐酸安妥沙星400 mg可以作为感染预防用药。

OBJECTIVE To determine the concentrationsof antofloxacin hydrochloride in the lung tissuesafter single dose preoperative oral administration of 400 mg in patientsreceiving pulmonry lobectomy for,preliminary evaluation of the rationality of this regimen to prevent infection. METHODS Forty-eight patients with no clinical evidence of preoperative infection undergoing pulmonary lobectomy were selected and randomized into four treatment groups. 400 mg antofloxacin hydrochloride was administered orally at 4,8, 12,and 24 h before the removal of the bronchi. Blood samples and lung tissues were collected after operation. The antofloxacin hydrochloride in blood serum and lung tissues was determined by high performance liquid chromatogram. RESULTS The average concentrations of antofloxacin hydrochloride in serum andlung tissuesin the four groupswere（ 3. 281 ± 0. 817） μg · mL- 1and（ 5. 992 ± 3. 228） μg·g- 1,（ 3. 192 ±0. 953） μg·mL- 1and（ 5. 885 ± 2. 952） μg·g- 1,（ 1. 712 ±0. 576） μg·mL- 1and（ 3. 419 ± 1. 107） μg·g- 1,and（ 0. 431 ±0. 095） μg·mL- 1and（ 1. 258 ± 0. 306） μg·g- 1,respectively. CONCLUSION The clearance time of oral antofloxacin hydrochloride in lung tissue was longer than that in serum. Single dose administration of oral antofloxacin hydrochloride 400mg within 12 h before operation can achieve effective bactericidal levels in serum and lung tissues,which could be a method to prevent infection for pulmonary lobectomy.