外周药物球囊在猪体内的药代动力学研究

发布时间：2018-01-20 02:17

本文关键词： 药物球囊药代动力学再狭窄　出处：《中国医疗器械信息》2016年10期 　论文类型：期刊论文

【摘要】：目的:将外周药物球囊在健康猪模型体内扩张后,通过LC/MS检测靶血管、脏器和血浆中药物含量,计算靶血管组织、主要器脏的药代动力学参数,以评估外周药物球囊产品的药效,局部和全身可耐受性。方法:用载药密度为2μg/mm2的药物球囊在健康猪髂/股动脉扩张后,分别在术后2h、7d、28d、90d时,取药物球囊治疗段、治疗段近端、治疗段远端的血管检测含药量;取重要生命器官(心、肺、肝、脾、肾)检测药物浓度;另在治疗后30min、2h、6h、12h、1d、3d、7d取血液,检测血浆中的药物浓度。结果:靶血管部位在T=2h时,药物含量到达峰值,达130μg/g以上,7D时8.59μg/g,28D时有约3.43μg/g,90D时仍有0.09μg/g,均高于最低治疗剂量0.047μg/g。其他组织和器官药物含量均非常低,未发现任何由药物涂层引起的不良事件,产品在局部和全身对紫杉醇是可耐受。结论:紫杉醇在靶血管的分布远大于主要脏器和血液,呈主要分布,在局部和全身对紫杉醇是可耐受。
[Abstract]:Objective: to investigate the pharmacokinetic parameters of target blood vessel, organ and plasma by LC/MS after the peripheral drug balloon was dilated in healthy pig model. To evaluate the efficacy, local and systemic tolerability of peripheral drug balloon products. Methods: the drug balloon with a drug density of 2 渭 g / mm2 was used to dilate the iliac / femoral artery of healthy pigs at 2 hours and 7 days after operation. After 28 days, 90 days, the drug balloon treatment segment was taken, the near end of the treatment segment, the blood vessel of the distal end of the treatment segment detected the drug content; Vital organs (heart, lung, liver, spleen, kidney) were taken to detect drug concentration. In addition, blood samples were collected 30 minutes after treatment for 2 h, 12 h, 12 h, 1 d and 3 d to detect the concentration of drugs in plasma. Results: the concentration of drugs reached the peak at 2 h after treatment. There are about 3.43 渭 g / g / g / 9D and 0.09 渭 g / g / g of 8.59 渭 g / g / 28D at 7D and above 130 渭 g / g / g / g respectively. The drug content in other tissues and organs was very low, and no adverse events caused by drug coating were found. Conclusion: the distribution of paclitaxel in the target vessels is much larger than that in the main organs and blood, and the taxol is tolerated in the local and whole body.
【作者单位】：先健科技(深圳)有限公司;
【基金】：深圳市科技创新委员会战略性新兴产业(生物产业发展)专项资金,项目编号:CXZZ20140813102720940,本项目进入国家食药监总局创新医疗器械特别审批绿色通道。创新医疗器械特别审批申请项目编号:2015061,审查结果公示(2016年第2号)
【分类号】：R965
【正文快照】： 1.研究背景外周动脉疾病(Peripheral arterial disease,PAD)又称为下肢动脉闭塞性病变,是指下肢血管的动脉粥样硬化而导致的动脉狭窄、闭塞、下肢远端组织缺血坏死[1]。目前裸球囊导管、裸支架、药物支架是主要治疗手段[2]。裸球囊扩张后,再狭窄率高,产品有效性难以令人满意;

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