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首页> 外文期刊>Journal of Young Pharmacists >Modulation of the P-Glycoproein-Mediated Intestinal Secretion of Glibenclamide: In Vitro and In Vivo Assessments
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Modulation of the P-Glycoproein-Mediated Intestinal Secretion of Glibenclamide: In Vitro and In Vivo Assessments

机译：P-糖蛋白介导的格列本脲肠分泌的调节：体外和体内评估。

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The everted gut sac method was used to assess the role of the P-glycoprotein (P-gp) on the intestinal secretion of glibenclamide, a prototype of drug used to treat diabetic mellitus. The study included the evaluation of a P-gp modulator carbamazepine used at equimolar doses in the rat. Furthermore, the influence of carbamazepine on the disposition kinetics of glibenclamide in plasma was characterized. For the in vitro experiments, ileal sacs were incubated with glibenclamide in the presence or absence of carbamazepine. In the in vivo experiments, albino rats of either sex were randomly allocated to two groups (n = 6) and oral treatment with glibenclamide (3.6 mg/kg), alone and coadministration with carbamazepine (90 mg/kg). Blood samples were collected at an interval of 1, 2, 4, 6, and 8 h, respectively. Glibenclamide concentrations in both in vitro and in vivo samples were estimated by a sensitive RP-HPLC method. The rate of glibenclamide accumulation in the intestine wall of everted sacs was significantly lower after its incubation with carbamazepine when compared to glibenclamide alone treated. In the agreement with the in vivo and in vitro experiments, the presence of carbamazepine induced an enhancement in the concentrations of glibenclamide in plasma and gastrointestinal tract. The results obtained in this study, both under in vivo and in vitro conditions confirm the relevance of P-gp-mediated transport to the intestinal secretion of glibenclamide.
机译：外翻肠囊法用于评估P-糖蛋白（P-gp）在格列本脲（一种用于治疗糖尿病的药物原型）的肠分泌物中的作用。该研究包括对大鼠等摩尔剂量使用的P-gp调节剂卡马西平的评估。此外，表征了卡马西平对血浆中格列本脲的处置动力学的影响。对于体外实验，在存在或不存在卡马西平的情况下，将回肠囊与格列本脲一起孵育。在体内实验中，将任意性别的白化病大鼠随机分为两组（n = 6），分别口服格列苯脲（3.6 mg / kg）和卡马西平（90 mg / kg）共同给药。分别在1、2、4、6和8小时的间隔内采集血液样本。通过灵敏的RP-HPLC方法估算体外和体内样品中的格列本脲浓度。与单用格列本脲相比，格列本脲与卡马西平一起孵育后，倾斜囊的肠壁中格列本脲的累积速率显着降低。与体内和体外实验一致，卡马西平的存在诱导了血浆和胃肠道中格列本脲的浓度增加。这项研究在体内和体外条件下获得的结果证实了P-gp介导的转运与格列本脲肠道分泌的相关性。

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