药物动力学和芬太尼剂量比例舌下喷:单剂量5维交叉研究。
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•帕里克以N, Goskonda V, Chavan Dillaha L
药物动力学和芬太尼剂量比例舌下喷:单剂量5维交叉研究。
中国药物Investig。2013年6月,33 (6):391 - 400。doi: 10.1007 / s40261 - 013 - 0079 - 8。
- PubMed ID
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23605506 (在PubMed]
- 文摘
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背景:芬太尼舌下喷的芬太尼是一种新型配方舌下交付,旨在提高吸收的速度和程度的芬太尼突破癌症疼痛管理(一共)。目的:本研究的主要目的是确定不同剂量的药物动力学和剂量比例5(100、200、400、600和800杯)的芬太尼舌下喷在健康受试者在禁食条件下(部分);二级目标是评估的影响在口腔温度和pH值的相对生物利用度芬太尼(B部分)。方法:分析进行静脉血样画5分钟后36小时以内芬太尼管理舌下喷(((R)),中高Insys疗法,Inc .,钱德勒,阿兹,美国)。这个阶段我研究的是一部分5-treatment, 5-sequence 5-period交叉研究,受试者接受了一个治疗每个5芬太尼的舌下喷剂量。剂量比例是评估使用方差分析和线性回归技术。B部分是5-treatment、2-sequence 5-period交叉研究中,受试者都分配一个剂量的芬太尼舌下喷200杯以下五个条件:没有预处理,与冷或热饮料预处理,预处理与低收入或减饮料。环丙甲羟二羟吗啡酮是管理阻止潜在的阿片类药物效应与芬太尼。不良事件(AEs)监测和记录在整个研究。结果:53科目(15人,38岁的女人;平均年龄31岁)参加a 14个主题部分(11人,3个女人; mean age, 32 years) were enrolled in part B. The first quantifiable mean plasma concentrations of fentanyl were observed at the first sample time (5 min) for all doses. Mean maximum plasma concentration (C(max)) increased with increases in dose, whereas median time to reach C max (t max) tended to decrease with increases in dose. The dose-normalized C(max), area under the plasma concentration-time curve from time zero to infinity (AUCinfinity), and AUC from time zero to time of last measurable concentration (AUClast) values were linear and consistent with dose proportionality across the 100-800 mug dose range. Pretreatment of the oral cavity with a cold or hot beverage, or low- or high-pH beverage, did not appreciably alter fentanyl absorption (C(max) and AUCinfinity values). The most commonly reported AEs were nausea and vomiting. CONCLUSIONS: In healthy subjects, administration of fentanyl sublingual spray produced a rapid rise in fentanyl plasma concentrations. Dose-dependent parameters (C max and AUC) showed dose proportionality across the range of 100-800 mug. Altering the local environment of the oral cavity (temperature and pH) showed no effects on the bioavailability of fentanyl. The rapid and predictable rise in plasma fentanyl concentrations following administration of fentanyl sublingual spray corresponds with the rapid onset and duration of many BTCP episodes.
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- 药物