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胆汁酸(Bile acids)用于治疗血脂异常已超过25年,其与不可吸收的树脂在肠腔内结合形成胆汁酸螯合物BAS(考来烯胺、考来维仑、colestimide、考来替泊)调节胆汁酸代谢,BAS经便排泄,并经由肠肝循环重吸收。胆汁酸可通过影响核受体FXR和TGR5调节肝糖代谢、外周胰岛素敏感性和能量代谢等。临床研究表明胆汁酸能够降低LDL,有利于预防冠心病。另外,2008年已证明BAS盐酸考来维仑(colesevelam HCl)联合饮食控制和运动疗法可改善T2DM血糖控制。最早Garg A等1994年一项为期6周的随机双盲交叉对照证明,盐酸考来烯胺降低血糖和HbA1c,随后2008年Goldberg RB等对胰岛素治疗DM控制不满意的患者、Fonseca等对二甲双胍或磺脲类药物(SUs)治疗DM控制不满意的患者研究发现,盐酸考来维仑均可改善这些患者的血糖控制情况。
Bile acids have been used for the treatment of dyslipidemia for more than 25 years and bind to non-absorbable resins in the intestine to form the bile acid chelate BAS (testosterone, colestimide, Parker) regulate bile acid metabolism, BAS excretion, and re-absorption through the enterohepatic circulation. Bile acids regulate hepatic glucose metabolism, peripheral insulin sensitivity and energy metabolism by affecting nuclear receptors FXR and TGR5. Clinical studies have shown that bile acids can reduce LDL, is conducive to the prevention of coronary heart disease. In addition, colesevelam HCl combined with dietary control and exercise therapy has been shown to improve T2DM glycemic control in 2008. The earliest Garg A et al., 1994, a 6-week, randomized, double-blind crossover study demonstrated that cholestyramine hydrochloride lowered blood glucose and HbA1c followed by Goldberg RB in 2008 who were dissatisfied with insulin-controlled DM control. Fonseca et al. Studies of sulfonylureas (SUs) in patients who were unsatisfied with DM control found that colesevelam hydrochloride improves glycemic control in these patients.