的药代动力学性质单一,反复给药舌下片剂舒芬太尼在健康志愿者。
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Willsie SK, Evashenk妈,哈默尔LG、黄党卫军,蒋介石即,帕默页
的药代动力学性质单一,反复给药舌下片剂舒芬太尼在健康志愿者。
其他。2015年1月1;37 (1):145 - 55。doi: 10.1016 / j.clinthera.2014.11.001。Epub 2014年12月24日。
- PubMed ID
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25544247 (在PubMed]
- 文摘
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用途:是一种mu-opioid舒芬太尼受体激动剂治疗指数高的临床前研究,没有活跃的代谢产物,它是高度亲脂性的,从而使transmucosal路线的管理。后迅速分布的等离子体静脉管理结果舒芬太尼在短时间的行动要求过多的重复剂量如果用于术后镇痛。舌下片舒芬太尼系统(太平洋)是一个手持,预编的,病人自控镇痛系统旨在让病人用药15-mug舒芬太尼平板电脑在他们的舌头二十分钟停摆。舒芬太尼的药代动力学(PK)特点,由不同的路线单一和重复后的交付和舌下(SL)管理、检查2的研究。方法:一项随机、非盲、交叉研究在健康受试者评估的PK 15杯由不同的路线:舒芬太尼静脉,SL,颊(BU)和PO。第二个非盲、交叉研究在健康受试者评估PK参数单一,重复剂量(全太平洋药物连续40盒SL剂量每20分钟)15-mug SL舒芬太尼的平板电脑。剂量是自行使用太平洋。结果:给药途径研究(n = 25),意味着与第四政府Cmax值最高,和生物利用度的值是:SL, 59%;但是,78%;阿宝,9%。 The absorption across the oral mucosa was associated with a median plasma half-time (time from Cmax to 50% of Cmax) that was 25-fold longer (2.5 hours) with SL versus IV administration (0.1 hours). In the single- and repeated-dose study (n = 38), mean AUC0-infinity was 125.5 h . pg/mL, and Cmax was 35.0 pg/mL, with a median Tmax of 0.8 hours after the administration of a single sufentanil SL tablet. With 40 consecutive doses, Cmax was 8-fold higher compared with that of a single dose, and steady state was achieved after the 13th dose. Median plasma half-time after the 40th dose was not statistically longer than that after a single dose (2.7 vs 2.2 hours, respectively), and the median Tmax was 0.3 hours after the last repeated dose. IMPLICATIONS: These study results support the viability of the SSTS for use in patient-controlled analgesia. The wide range of mean drug concentrations achieved after repeated dosing at 20-minute intervals compared with those with a single dose suggests the flexibility of patient-controlled dosing to meet individual analgesic requirements. The prolonged plasma half-time with SL administration is expected to provide a more appropriate duration of analgesia compared with that of IV administration, and the PK properties of repeated-dose administration support a 20-minute lockout interval.
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