Aliberti G, D'Erasmo E, Oddo C M, Vecci E
Clinica Medica, University of Rome, La Sapienza, Italy.
Cardiovasc Drugs Ther. 1991 Aug;5(4):697-9. doi: 10.1007/BF03029743.
The purpose of this study has been to compare the acute antihypertensive effect of a dose of 20 mg of ketanserin in 18 patients after sublingual administration and in 19 after oral administration. In three patients ketanserin and ketanserin-ol plasma levels were measured after both sublingual and oral administration. The results showed a more rapid, considerable antihypertensive effect after sublingual administration. In addition, the high plasma levels of ketanserin-ol, the metabolite produced by hepatic reduction of ketanserin, reached after sublingual administration, rather than transmucosal absorption, indicate that the clinical effect observed is due to more rapid dissolution of the tablet formulation and liberation of the active drug.
本研究的目的是比较18例患者舌下含服20 mg酮色林和19例患者口服该剂量后的急性降压效果。对3例患者在舌下含服和口服酮色林后均测定了酮色林和酮色林醇的血浆水平。结果显示，舌下含服后降压作用起效更快且更显著。此外，舌下含服后达到的酮色林醇（酮色林经肝脏还原产生的代谢产物）高血浆水平，而非经黏膜吸收，表明观察到的临床效果是由于片剂制剂溶解更快以及活性药物释放所致。
