药物动力学的倍他米松在单剂磷酸肌内倍他米松管理局和倍他米松醋酸健康受试者。
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萨勒姆二世,纳吉布NM
药物动力学的倍他米松在单剂磷酸肌内倍他米松管理局和倍他米松醋酸健康受试者。
其他。2012年1月,34 (1):214 - 20。doi: 10.1016 / j.clinthera.2011.11.022。Epub 2011年12月9日。
- PubMed ID
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22154197 (在PubMed]
- 文摘
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背景:倍他米松用于其抗炎和免疫抑制作用在许多器官系统的疾病。然而,倍他米松在等离子体肌内注射后的药代动力学性质的倍他米松磷酸钠和倍他米松醋酸双作用悬架需要进一步调查。目的:本研究的主要目的是确定倍他米松的药代动力学参数,倍他米松乙酸酯和倍他米松磷酸后管理单个肌内剂量的双作用悬浮健康志愿者。方法:两个不同的研究进行了健康的男性。志愿者判断健康的根据他们的病史,体检,实验室测试结果。在监禁之前,所有志愿者测试酒精和毒品的滥用自由。10小时通宵禁食后,单一剂量的1毫升的双作用悬架包含3毫克的倍他米松磷酸和3毫克的倍他米松醋酸是由肌内注射。血液采样48小时。在第二项研究中获得的血浆样品是倍他米松酯的稳定,使药代动力学分析。结果:24名健康男性的意思是27(6.62)岁(SD)参与研究。 No incidences of serious adverse events were recorded during the studies. Six mild adverse events were reported in 2 subjects in the second study. One subject suffered from pain at the injection site and insomnia, and another subject complained of heartburn and drowsiness. Betamethasone phosphate appeared to be readily absorbed with a mean AUC(0-t) of 96.01 ng/h/mL and an AUC(0-infinity) of 97.96 (23.38) ng/h/mL. Betamethasone peak plasma concentration reached a mean t((1/2)) of 12.92 hours. Betamethasone acetate was not detected in the volunteers' plasma in either study (total of 2208 plasma samples). CONCLUSION: The observed pharmacokinetic parameters suggested that the acetate ester, and not the phosphate ester, of betamethasone acts as a prodrug or reservoir for betamethasone, conferring on it sustained- and extended-release characteristics.
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