Characterization of drug penetration to the brain for preventing development of symptoms and progress of the aging disease

这项研究描述了几种药物对大脑的渗透，以防止症状的发展和老年病的进展。(1)姜黄素在牛脑微血管内皮细胞中的渗透性，在高效液相色谱-紫外检测法中不能以检出限进行测定。(2)[3^H]氟伐他汀转运到牛脑微血管内皮细胞参与了载体介导的机制。(3)有机阳离子敏感转运系统参与了[3^H]金刚烷胺向大鼠脑微血管内皮细胞的转运。在大鼠大脑中微量注射金刚烷胺后，约50%的金刚烷胺在60分钟内下降得相对较慢。(4)提示帕金森病患者左旋多巴转运体干预转运效率略有下降。(5)通过人脑微血管内皮细胞和脑灌流技术的实验，证实P-糖蛋白参与了金刚烷胺在血脑屏障的转运，这是一种简单的扩散机制，对金刚烷胺的血脑屏障转运没有影响。(7)磺胺甲恶唑-甲氧苄啶(SMX-TMP)联合用药后，74岁和75岁患者的血肌酐(Scr)显著升高(P&lt；0.05)，无论男女，总剂量为8~96g。总剂量为？8g(平均29.8g)组Scr增加18.4%(P=0.002)，而？7g(平均5.3g)组仅增加4.5%。数据显示，治疗期间总剂量为30g左右(约2.4g为TMP)时，Scr增加约20%，表明总剂量对治疗后Scr增加的贡献大于年龄和性别。

This study characterized penetration of several drugs to the brain for preventing development of symptoms and progress of the aging disease. (1) Curcumin permeation into bovine brain microvascular endothelial cells could not determine with limitation of detection in HPLC-UV method. (2) Transport of [3^H]fluvastatin into bovine brain microvascular endothelial cells was involved in the carrier-mediated mechanism. (3) Transport of [3^H]amantadine into rat brain microvascular endothelial cells was involved in the organic cation-sensitive transport system. About 50% of amantadine decreased comparatively slowly in 60 minutes after the microinject in a rat cerebrum. (4) It was suggested that the transporter intervention transport efficiency of levodopa decreases slightly in Parkinson's disease. (5) Participation of a simple diffusion mechanism and P-glycoprotein in the transport of mazindol at the blood-brain barrier, and (6) no influences of P-glycoprotein at the blood-brain barrier transport of amantadine, were demonstrated from experiments using human brain microvascular endothelium cells or the brain perfusion technique. (7) Serum creatinine (SCr) increased significantly following sulfamethoxazole-trimethoprim (SMX-TMP) combination product use in patients ?74 years of age and ?75 years of age, in both males and females, and in patients with a total dose of ?8 g (8 to 96 g) (P<0.05). The group with a total dose of ?8 g (mean 29.8 g) had a significant SCr increase of 18.4% (P=0.002), while the increase in the ?7 g (mean 5.3 g) group was only 4.5%. The data showed that SCr increased byabout 20% when the total dose taken over the treatment period was around 30 g (about2.4 g as TMP) and indicated that total dose contributes more than age and sex to the post-treatment increase in SCr.