Müller S, Mayer J M, Etter J C, Testa B
Ecole de Pharmacie, Université de Lausanne, Switzerland.
Chirality. 1990;2(2):74-8. doi: 10.1002/chir.530020203.
Ibuprofen was used to demonstrate that isolated rat hepatocytes offer a suitable in vitro model to investigate the metabolic chiral inversion of anti-inflammatory 2-arylpropionic acids (profens). The inversion of the pharmacologically inactive (-)-(R)-ibuprofen to the active (+)-(S)-ibuprofen was shown to obey apparent first-order kinetics during 5 h and to increase linearly with increasing hepatocyte concentration up to 4 x 10(5) cells/ml. No elimination of (R)-ibuprofen by routes other than inversion was seen, whereas the elimination of (S)-ibuprofen appeared to be saturable.
布洛芬被用于证明分离的大鼠肝细胞提供了一个合适的体外模型，以研究抗炎性2-芳基丙酸（profens）的代谢手性转化。药理活性不高的(-)-(R)-布洛芬向活性的(+)-(S)-布洛芬的转化在5小时内符合表观一级动力学，并且随着肝细胞浓度增加至4×10⁵个细胞/毫升呈线性增加。未观察到除转化以外的其他途径对(R)-布洛芬的消除，而(S)-布洛芬的消除似乎具有饱和性。
