大鼠鼻腔对吲哚美辛的吸收
Absorption of indomethacin from nasal cavity in rats.
作者信息
Huang Z L, Kagoshima M, Kagawa E, Shimada H
机构信息
Department of Clinical Pharmacology, School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.
出版信息
Zhongguo Yao Li Xue Bao. 1995 Mar;16(2):117-20.
AIM
To investigate if identical bioavailability, rapid Tmax, and Cmax of indometacin (Ind) could be achieved when Ind is administered in rats via intranasal (ina) route.
METHODS
The pharmacokinetics of Ind solution at a dosage of 3 mg.kg-1 was studied after i.v., ina, and po in rats using HPLC.
RESULTS
It showed that the time to peak (Tmax) of ina Ind 3 mg.kg-1 solution was 0.08 h, approached that after i.v. route the peak concentration (Cmax) following ina was 20.0 mg.L-1, 2.4 times higher than po dosing.
CONCLUSION
It demonstrated that the ina administration of Ind was superior to po in rats, and that Ind absorption through nasal mucosa was a reasonable approach at lower doses.
目的
研究吲哚美辛（Ind）经鼻内（ina）途径给予大鼠时，是否能实现与静脉注射相同的生物利用度、快速的达峰时间（Tmax）和峰浓度（Cmax）。
方法
采用高效液相色谱法（HPLC）研究了大鼠静脉注射（i.v.）、经鼻内（ina）和口服（po）给予3 mg·kg-1剂量的Ind溶液后的药代动力学。
结果
结果显示，3 mg·kg-1剂量的ina Ind溶液的达峰时间（Tmax）为0.08小时，接近静脉注射后的达峰时间；ina给药后的峰浓度（Cmax）为20.0 mg·L-1，比口服给药高2.4倍。
结论
结果表明，在大鼠中，ina给予Ind优于po给药，且低剂量时通过鼻黏膜吸收Ind是一种合理的途径。
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