Setnikar I, Arigoni R, Chisté R, Makovec F, Revel L
Rotta Research Laboratorium, Monza/Milano, Italy.
Arzneimittelforschung. 1987 Jun;37(6):698-702.
The absolute bioavailability of 1H-indole-3-acetic acid, 1-(4-chlorobenzoyl)-5-methoxy-2-methyl 2-[4-[4-[[4-(benzoylamino)-1,5-dioxopentyl]oxy]propyl]-1- piperazinyl]-ethyl ester (+/-) (proglumetacin, CR 604) was studied in 12 dogs, in a triple cross-over experiment with single doses of i.v. proglumetacin diphosphate, oral proglumetacin diphosphate or oral proglumetacin dimaleate. Determined were proglumetacin, 2'-[4-(3-hydroxypropyl)-piperazin-1-yl]-ethyl-(1-p- chlorobenzoyl-5-methoxy-2-methylindol-3-yl)-acetic acid (CR 1015), indometacin and proglumide in plasma. Proglumetacin and CR 1015 were found in plasma only after the i.v. administration. Conversely indometacin and proglumide were found after all administration routes. The areas under the curve of indometacin and of proglumide did not differ significantly after the three treatments, as shown by the analysis of variance.
在一项三交叉试验中，对12只犬单次静脉注射二磷酸普罗谷美辛、口服二磷酸普罗谷美辛或口服马来酸普罗谷美辛，研究了1H-吲哚-3-乙酸、1-(4-氯苯甲酰基)-5-甲氧基-2-甲基2-[4-[4-[[4-(苯甲酰氨基)-1,5-二氧代戊基]氧基]丙基]-1-哌嗪基]-乙酯(±)(普罗谷美辛，CR 604)的绝对生物利用度。测定血浆中的普罗谷美辛、2'-[4-(3-羟丙基)-哌嗪-1-基]-乙基-(1-对氯苯甲酰基-5-甲氧基-2-甲基吲哚-3-基)-乙酸(CR 1015)、吲哚美辛和丙谷胺。仅在静脉注射后血浆中发现普罗谷美辛和CR 1015。相反，在所有给药途径后均发现吲哚美辛和丙谷胺。方差分析表明，三种治疗后吲哚美辛和丙谷胺的曲线下面积无显著差异。
