Tamassia V, Jannuzzo M G, Moro E, Stegnjaich S, Groppi W, Nicolis F B
Int J Clin Pharmacol Res. 1984;4(3):223-30.
Indoprofen, a non-steroidal analgesic and antiinflammatory drug whose activity and safety in man have been established in a large number of studies, has an asymmetric carbon atom and can therefore occur as either the (+) or the (-) enantiomer. As it has been shown that its pharmacological effects are almost entirely due to the (+) isomer (d-indoprofen), some pharmacokinetic properties of the latter have been studied in man in comparison with the racemic mixture given by oral administration, d-indoprofen is cleared from plasma and excreted in urine (as unchanged plus conjugated drug) at a slower rate than l-indoprofen. Moreover, no stereospecific inversion of d-indoprofen to the inactive enantiomer occurs after either single or repeated (one week) administration. The pharmacokinetic behaviour of d-indoprofen in the human organism appears to be the same after administration of the racemic form or of the dextro-enantiomer, when the latter is given at half the dose.
吲哚洛芬是一种非甾体类镇痛抗炎药，其在人体中的活性和安全性已在大量研究中得到证实。它含有一个不对称碳原子，因此可以以（+）或（-）对映体的形式存在。已有研究表明其药理作用几乎完全归因于（+）异构体（d-吲哚洛芬），与口服给予的外消旋混合物相比，已对后者在人体中的一些药代动力学特性进行了研究。d-吲哚洛芬从血浆中清除并以尿液（以未改变的药物加上结合药物的形式）排泄的速度比l-吲哚洛芬慢。此外，单次或重复（一周）给药后，d-吲哚洛芬不会立体定向转化为无活性对映体。当以半剂量给予右旋对映体时，给予外消旋形式或右旋对映体后，d-吲哚洛芬在人体中的药代动力学行为似乎相同。
