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首页> 外文期刊>The Journal of Clinical Pharmacology: Official Journal of the American College of Clinical Pharmacology >Effects of extensive and poor gastrointestinal metabolism on the pharmacodynamics of pravastatin.
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Effects of extensive and poor gastrointestinal metabolism on the pharmacodynamics of pravastatin.

机译：胃肠道广泛和不良代谢对普伐他汀药效学的影响。

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摘要

The enhanced nonenzymatic isomerization of pravastatin to SQ 31,906, a relatively inactive metabolite, has been demonstrated to occur on exposure to gastric acidity in humans. However, the effect of gastric metabolism on the pharmacodynamics of pravastatin has not been studied. In addition, it was hypothesized that some individuals may be more extensive gastric metabolizers than others. Sixteen men received 4 weeks of oral therapy with pravastatin 10 mg after a 6-week drug washout diet run-in period. Pharmacokinetic and pharmacodynamic parameters were determined after 8 hours of serum sampling on the final day of therapy. Patients with a metabolic ratio for area under the concentration-time curve (AUC0-8 of pravastatin/AUC0-8 of SQ 31,906) of less than 1.6 had a significantly lower reduction in total and low-density lipoprotein (LDL) cholesterol compared with those with a ratio > 1.6. An enteric formulation of pravastatin should increase the bioavailability of pravastatin and enhanced lipid-lowering efficacy.
机译：普伐他汀增强的非酶异构化为SQ 31,906（一种相对无活性的代谢物），已证明在人体暴露于胃酸时会发生。但是，尚未研究胃代谢对普伐他汀药效学的影响。另外，假设某些人可能比其他人更广泛地代谢胃。在经过6周的药物洗脱饮食磨合期后，有16名男性接受了普伐他汀10 mg口服治疗4周。在治疗的最后一天从血清中取样8小时后，确定药代动力学和药效学参数。浓度-时间曲线下的面积代谢比（普伐他汀的AUC0-8 / SQ 31,906的AUC0-8）低于1.6的患者与总胆固醇和低密度脂蛋白（LDL）胆固醇相比，其胆固醇降低显着更低比率> 1.6。普伐他汀的肠溶制剂应增加普伐他汀的生物利用度并增强降脂功效。

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