静脉注射和口腔给药后咪达唑仑的药代动力学。
Midazolam pharmacokinetics following intravenous and buccal administration.
作者信息
Schwagmeier R, Alincic S, Striebel H W
机构信息
Department of Anaesthesiology and Intensive Care Medicine, Benjamin Franklin Medical Center, Free University of Berlin, Germany.
出版信息
Br J Clin Pharmacol. 1998 Sep;46(3):203-6. doi: 10.1046/j.1365-2125.1998.00781.x.
AIMS
Midazolam has good anxiolytic qualities and is a well established premedication agent before anaesthesia or short surgical procedures. The objective of the present study was to determine pharmacokinetic data from individual plasma concentration profiles obtained following intravenous and buccal administration of midazolam.
METHODS
Eight young healthy volunteers received single doses of 5 mg midazolam i.v. and after a period of 1 week buccally in a cross over manner. Blood samples were obtained up to 480 min. The measurement of plasma midazolam concentrations was by gas-chromatography.
RESULTS
The maximum plasma concentration was 55.9 ng ml(-1) (range 35.6-77.9 ng ml(-1)) at 30 min (range 15-90 min) following buccal administration. AUC was calculated to be 15016 ng ml(-1) min (s.d. 3778 ng ml(-1) min) following i.v. and 11191 ng ml(-1) min (s.d. 1777 ng ml(-1) min) following buccal midazolam. This gave a mean midazolam bioavailability of 74.5%.
CONCLUSIONS
The pharmacokinetic data presented in this study demonstrate a high bioavailability and reliable plasma concentrations following buccal midazolam. The clinical benefit of buccal midazolam may be in particular patient controlled premedication or sedation in adults.
目的
咪达唑仑具有良好的抗焦虑特性，是麻醉或短时间外科手术前常用的术前用药。本研究的目的是通过静脉注射和口腔给药后获得的个体血浆浓度曲线来确定咪达唑仑的药代动力学数据。
方法
8名年轻健康志愿者以交叉方式接受单剂量5mg咪达唑仑静脉注射，1周后口腔给药。在480分钟内采集血样。血浆咪达唑仑浓度的测定采用气相色谱法。
结果
口腔给药后30分钟（范围15 - 90分钟）血浆最大浓度为55.9ng/ml（范围35.6 - 77.9ng/ml）。静脉注射后AUC计算为15016ng/ml·min（标准差3778ng/ml·min），口腔给药咪达唑仑后为11191ng/ml·min（标准差1777ng/ml·min）。这使得咪达唑仑的平均生物利用度为74.5%。
结论
本研究中呈现的药代动力学数据表明，口腔给药咪达唑仑后具有高生物利用度和可靠的血浆浓度。口腔给药咪达唑仑的临床益处可能尤其体现在成人患者自控的术前用药或镇静方面。
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