Ofoefule Sabinus I, Obodo Chioma E, Orisakwe Orish E, Afonne Johnson O, Ilondu Ndidiamaka A, Agbasi Patrick U, Anusiem Chikere A, Maduka Steve O, Ilo Cajetan E
Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Enugu State, Nigeria.
Am J Ther. 2002 Jan-Feb;9(1):15-8. doi: 10.1097/00045391-200201000-00004.
Salivary and urinary excretion and plasma-saliva concentration ratios of isoniazid (INH) in the absence and presence of ciprofloxacin (CP) were investigated in healthy female volunteers. Results obtained indicated an absorption form of interaction between INH and CP. This led to delay in gastric emptying and onset of absorption of INH in the upper part of the gastrointestinal tract, resulting in a corresponding delay in the onset of salivary and urinary excretion of the drugs. There was a 1-hour reduction in the time to attain peak saliva concentration of INH (tmax), an insignificant difference in peak saliva concentration (Cmax), and a significant (P = 0.05) increase in AUC(0-24h) of INH in the presence of CP. Cumulative amount of INH excreted in the urine increased approximately 38% in the presence of CP. The calculated plasma-saliva concentration ratios of INH were reduced in the presence of CP and were slightly lower than the experimental values. This indicates increased amount of the drug secreted into saliva in the presence of CP and possible buccal partitioning of the drug. Overall, results of the current study indicate that CP delayed the onset but not the extent of INH absorption. Therefore, concurrent administration of the two drugs was considered relatively safe, and the absorption interaction that may have occurred may not be of reasonable clinical consequence.
在健康女性志愿者中，研究了在不存在和存在环丙沙星（CP）的情况下异烟肼（INH）的唾液和尿液排泄以及血浆-唾液浓度比。所得结果表明INH与CP之间存在吸收形式的相互作用。这导致胃排空延迟以及INH在胃肠道上部的吸收开始延迟，从而导致药物唾液和尿液排泄的开始相应延迟。在存在CP的情况下，达到INH唾液峰值浓度的时间（tmax）减少了1小时，唾液峰值浓度（Cmax）无显著差异，而INH的AUC(0-24h)显著增加（P = 0.05）。在存在CP的情况下，尿液中排泄的INH累积量增加了约38%。在存在CP的情况下，计算得出的INH血浆-唾液浓度比降低，且略低于实验值。这表明在存在CP的情况下药物分泌到唾液中的量增加，并且药物可能存在颊部分布。总体而言，当前研究结果表明CP延迟了INH吸收的开始，但未延迟吸收程度。因此，两种药物同时给药被认为相对安全，并且可能发生的吸收相互作用可能没有合理的临床后果。
