药物动力学的tedizolid口服:单个和多个剂量,效果的食物,和比较两个固体形式的前体药物。
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弗拉纳根SD,好爸爸,穆尼奥斯KA, Minassian SL, Prokocimer PG
药物动力学的tedizolid口服:单个和多个剂量,效果的食物,和比较两个固体形式的前体药物。
药物治疗。2014年3月,34 (3):240 - 50。doi: 10.1002 / phar.1337。Epub 2013年8月7日。
- PubMed ID
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23926058 (在PubMed]
- 文摘
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目的:单和multiple-dose药物动力学(PK) tedizolid口服后检查tedizolid磷酸二钠(兼总经理),包括食物PK的影响。信息的相对生物利用度自由酸磷酸tedizolid决心桥这些和其他研究的结果的固体形式前体药物选择的进一步发展。设计:随机安慰剂对照,双盲单——multiple-ascending剂量研究和随机非盲、交叉食物效应和相对生物利用度研究。背景:临床研究单位。参与者:健康受试者。干预:研究tr701 40 - 101登记主体single-ascending剂量(200 - 1200 mg兼总经理或安慰剂)和40学科在21天的multiple-ascending剂量(200、300、或400毫克/天信息调用一次;600毫克/天linezolid两次;或安慰剂)武器。研究tr701 - 103是一个food-effect 12个受试者服用600毫克的一系列问题。研究tr701 - 108是一个相对生物利用度研究在12个受试者服用150毫克tedizolid等价物作为信息或tedizolid磷酸盐。测量及主要结果:等离子体浓度的药物前体tedizolid磷酸盐,其活跃的一部分tedizolid,和/或linezolid收集。 After administration of 200 to 600 mg TPD, tedizolid values increased approximately dose proportionally in area under the concentration-time curve (AUC) and maximum plasma concentration (Cmax ). Tedizolid half-life values were approximately 2-fold greater compared with linezolid. TPD administration with food delayed tedizolid absorption and reduced Cmax relative to the fasted state but did not alter AUC. Minimal accumulation was predicted and observed for tedizolid, whereas observed accumulation of linezolid exceeded predictions based on single-dose PK. Comparable PK of tedizolid was observed following oral administration of either TPD or tedizolid phosphate. In the multiple-ascending dose study, 3 of 24 tedizolid subjects were withdrawn under prespecified stopping rules (one each of elevated alanine aminotransferase, low reticulocyte count, or low white blood cell count), as was 1 of 8 linezolid subjects (low reticulocyte count). CONCLUSIONS: Overall, tedizolid has a favorable PK profile, a half-life that supports once daily administration, and no nonlinearities at steady state. Tedizolid phosphate can be administered without regard to food.
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