盐酸沙拉沙星胶囊在蚕体内的药物动力学研究

Studies on the Pharmacokinetics of Sarafloxacin Hydrochloride Capsules in Silkworm

[目的]研究盐酸沙拉沙星胶囊在蚕体内的药物代谢动力学特征。[方法]采用微生物法测定家蚕食下不同浓度的盐酸沙拉沙星胶囊后不同时间血液中的药物含量。[结果]分别给5龄家蚕添食51、02、0 mg/kg盐酸沙拉沙星后,AIC值分别为-37.72547、11.076 95和27.447 15,拟合度良好;主要药动学参数吸收速率常数ka分别为0.835、0.8200、.653 h-1,达峰时间Tmax分别为2.8872、.7372、.765 h,最高血药浓度Cmax分别为3.9106、.609、11.032μg/ml。蚕食盐酸沙拉沙星后蚕体内的血药浓度-时间曲线符合一级吸收一室开放式模型,盐酸沙拉沙星在蚕体内吸收迅速、达峰时间短(2.8 h左右),最高血药浓度与添食剂量成正比、消除半衰期较短的药物代谢动力学特征,适合日内多次给药。[结论]该研究为制定蚕病的临床合理用药方案提供了药物动力学依据。

[Objective]The research aimed to study the pharmacokinetics characteristics of sarafloxacin hydrochloride capsule in silkworm.[Method]Using microbial method,the content of sarafloxacin hydrochloride in the blood of silkworm after feeding different concentrations of sarafloxacin hydrochloride capsule was determined.[Result]After the administration of 5,10,20 mg/kg sarafloxacin hydrochloride to 5th-instar silkworm,AIC values were-37.725 47、11.076 95 and 27.447 15 respectively,with good fitting degree.The major pharmacokinetic parameters were as follows： the absorption rate constant（ka） was 0.835,0.820 and 0.653 h respectively;The peak time（Tmax） was 2.887,2.737 and 2.765 h respectively;The maximal blood concentration（Cmax） was 3.910、6.609 and 11.032 μg/ml respectively.The drug concentration-time curve of sarafloxacin hydrochloride in silkworm body fitted to the first order absorption kinetics and one compartment open model.Sarafloxacin hydrochloride had the pharmacokinetic properties including quick absorption inside the larval body,short time to reach peak value（about 2.8 h）,the maximal blood concentration being proportional to the administered dosage,and shorter elimination half-life,being suitable for multiple administrations within one day.[Conclusion]The research provided pharmacokinetics basis for making the reasonable administration scheme for silkworm diseases in the clinic.