Alprazolam Kinetics Following Sublingual and Oral Administration
Alprazolam Kinetics Following Sublingual and Oral Administration
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舌下和口服给药后的阿普唑仑动力学
DOI：
10.1097/00004714-198710000-00008
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发表时间：
1987
影响因子：
2.9
通讯作者：
R. Shader
中科院分区：
文献类型：
--
作者：
J. Scavone;D. Greenblatt;R. Shader
13 名健康志愿者通过舌下和口服途径两次随机服用 1 毫克阿普唑仑（市售口服片剂）。通过电子捕获气相色谱法测量每次给药后 48 小时内的血浆阿普唑仑浓度。舌下给药后的血药峰浓度高于口服给药后（17.3 vs. 14.9 ng/ml），并且舌下给药后达到峰浓度的时间（给药后1.17 vs. 1.73小时）。然而，这些差异并未达到统计学显着性。舌下给药的血浆浓度曲线下平均总面积略大于口服给药后的血浆浓度曲线下总面积（203.7 vs. 194.4 ng/ml），舌下给药和口服剂量之间没有发现消除半衰期（11.7 vs. 11.8 小时）或清除率（86.4 vs. 92.4 ml/min）的显着差异。因此，舌下给药后的阿普唑仑吸收与空腹口服给药后的吸收一样快，并且吸收的完全性相当。在临床方面，阿普唑仑的舌下含服和口服剂量可能具有相同的治疗效果。对于无法吞咽药片或在给药时无法获得液体的恐慌症患者来说，舌下给药可能是一种有用的替代方案。 （临床精神药理学杂志 1987 年；7：332–334）
Thirteen healthy volunteers received 1 mg of alprazolam, as the commercially available oral tablet, by sublingual and oral routes on two occasions in random sequence. Plasma alprazolam concentrations during 48 hours after each dose were measured by electron-capture gas-liquid chromatography. The peak plasma concentration after sublingual dosage was higher than after oral administration (17.3 vs. 14.9 ng/ml), and the time of peak concentration following sublingual administration was reached (1.17 vs. 1.73 hours after dose). However, these differences did not reach statistical significance. The mean total area under the plasma concentration curve for sublingual administration was slightly but not significantly larger than that following oral dosage (203.7 vs. 194.4 hr. ng/ml) and no significant differences between sublingual and oral dosage were found for elimination half-life (11.7 vs. 11.8 hours) or for clearance (86.4 vs. 92.4 ml/min). Thus, alprazolam absorption following sublingual administration is as rapid as after oral dosage on an empty stomach, and completeness of absorption is comparable. In clinical terms, sublingual and oral dosages of alprazolam are likely to be therapeutically equivalent. The sublingual route may be a useful alternative for panic disorder patients who cannot swallow pills or for those who do not have access to a liquid at the time of dosing. (J Clin Psychopharmacol 1987;7:332–334)