Khan Muhammad Khalid, Khan Muhammad Farid, Mustafa Ghulam, Sualah Mohammed
Gomal University, Dera Ismail Khan, Pakistan.
Pak J Pharm Sci. 2012 Jan;25(1):81-8.
Ciprofloxacin was given orally to 28 healthy male volunteers for single oral dose of 500mg; Plasma samples were collected at different time's interval between 0 and 12h and analyzed both by high pressure liquid chromatography and by a microbiological assay. The detection limits (LOD) were 0.02μg/ml and 0.1μg/ml, for both methods respectively. For each method, coefficients of variation (R(2)) were 0.9995 and 0.9918 in plasma and limit of quantitation (LOQ).02 and 0.5μg/ml. The Comparison of means maximum concentration 2.68 μg/ml at 1.5 hr for test and 2.43 μg/ml are attain in HPLC method of Reference at 2hrs respectively. The plasma concentrations measured by microbiological assay of reference tablet are 3.95μg/ml (mean ± SE) at 1 hour and 3.80μg/ml (mean ± SE) at 1 hour. The concentrations in plasma measured by microbiological method were markedly higher than the high-pressure liquid chromatography values which indicates the presence of antimicrobially active metabolites. The mean ± SE values of pharmacokinetic parameters calculated by HPLC method, for total area under the curve (AUC 0-oo) were 13.11, and 11.91 h.mg/l for both test and reference tablets respectively. The mean ± SE values of clearance measured in l/h were 44.91 and 48.42 respectively. The elimination rate constant Kel [l/h] showed 0.17 l/h for test and 0.15 l/h reference tablets and likewise, absorption half-life expressed in hours shown 0.67 h for test and 1.04 h for reference respectively. The Mean Residence Time for test is 5.48 h and 5.49 h for reference. The mean ± SE values of pharmacokinetic parameters (Microbiological assay) for total area under the curve (AUC 0-oo) were 22.11 and 19.33 h.mg/l for both test and reference tablets respectively. The mean ± SE values of clearance measured in l/h were 29.02 and 31.63 respectively. The elimination rate constant Kel [l/h] showed 0.21 l/h for test and 0.20 l/h reference tablets and likewise, absorption half-life expressed in hours shown 0.86h for test and 0.56 h for reference respectively. The Mean Residence Time for test is 5.27 h and 4.67 h for reference. Significant difference observed between two methods.
对28名健康男性志愿者口服环丙沙星，单次口服剂量为500mg；在0至12小时的不同时间间隔采集血浆样本，并通过高压液相色谱法和微生物测定法进行分析。两种方法的检测限（LOD）分别为0.02μg/ml和0.1μg/ml。对于每种方法，血浆中的变异系数（R(2)）分别为0.9995和0.9918，定量限（LOQ）分别为0.02和0.5μg/ml。测试药物在1.5小时时的平均最大浓度为2.68μg/ml，参比药物在2小时时通过高效液相色谱法测得的平均最大浓度为2.43μg/ml。参比片剂微生物测定法测得的血浆浓度在1小时时为3.95μg/ml（平均值±标准误），在1小时时为3.80μg/ml（平均值±标准误）。微生物法测得的血浆浓度明显高于高压液相色谱法的值，这表明存在具有抗菌活性的代谢物。通过高效液相色谱法计算的药代动力学参数，测试片和参比片的曲线下总面积（AUC 0-∞）的平均值±标准误分别为13.11和11.91 h.mg/l。以l/h为单位测得的清除率平均值±标准误分别为44.91和48.42。测试片和参比片的消除速率常数Kel [l/h]分别为0.17 l/h和0.15 l/h，同样，以小时表示的吸收半衰期测试片为0.67小时，参比片为1.04小时。测试片的平均驻留时间为5.48小时，参比片为5.49小时。两种方法之间观察到显著差异。通过微生物测定法计算的药代动力学参数，测试片和参比片的曲线下总面积（AUC 0-∞）的平均值±标准误分别为22.11和19.33 h.mg/l。以l/h为单位测得的清除率平均值±标准误分别为29.02和31.63。测试片和参比片的消除速率常数Kel [l/h]分别为0.21 l/h和0.20 l/h，同样，以小时表示的吸收半衰期测试片为0.86小时，参比片为0.56小时。测试片的平均驻留时间为5.27小时，参比片为4.67小时。两种方法之间观察到显著差异。
