Pharmacodynamic activity of lipoprotein lipase and hepatic lipase, and pharmacokinetic parameters measured in normolipidaemic subjects receiving ciprofibrate (100 or 200 mg/day) or micronised fenofibrate (200 mg/day) therapy for 23 days
Pharmacodynamic activity of lipoprotein lipase and hepatic lipase, and pharmacokinetic parameters measured in normolipidaemic subjects receiving ciprofibrate (100 or 200 mg/day) or micronised fenofibrate (200 mg/day) therapy for 23 days
复制标题
DOI：
10.1016/s0021-9150(96)90508-0
复制
发表时间：
1996-07-01
期刊：
影响因子：
5.3
通讯作者：
Harvengt, C
中科院分区：
文献类型：
--
作者：
Desager, JP;Horsmans, Y;Harvengt, C
分别用环丙贝特（100 mg或200 mg）和非诺贝特（200 mg）治疗23 d后测定脂蛋白脂酶（LPL）和肝脂酶（HL）活性。在一项双盲、双安慰剂、交叉研究中，三组6名健康志愿者接受100 mg环丙贝特/天接着200 mg非诺贝特“高生物利用度”（HB）/天，或反之亦然（A组），200 mg环丙贝特/天接着200 mg非诺贝特HB/天，或反之亦然（B组），或100 mg环丙贝特/天接着200 mg环丙贝特/天，反之亦然（C组）。在治疗前后评价空腹血脂水平和安全性指标。发现100毫克环丙贝特/天治疗在改变脂质谱方面与200毫克非诺贝特HB/天治疗大约一样有效。在用200 mg环丙贝特/天治疗后获得LPL的最高活化。100或200 mg环丙贝特治疗后发现HL活性适度但具有统计学显著性增加。环丙贝特和非诺贝酸的药代动力学研究显示，与非诺贝贝特相比，环丙贝特制剂达到血浆峰浓度的时间较短，但消除半衰期较长。在增加LPL和HL活性方面，200 mg环丙贝特/天的剂量比100 mg环丙贝特/天更有效;然而，200 mg环丙贝特/天也与安全性参数的潜在有害变化相关。200 mg非诺贝特HB/天治疗可能是100 mg环丙贝特/天治疗糖尿病患者的替代疗法。
The activities of lipoprotein lipase (LPL) and hepatic lipase (HL) were investigated after 23 days of ciprofibrate (100 mg or 200 mg) therapy or fenofibrate (200 mg) therapy. In a double-blind, double-placebo, cross-over study, three groups of six healthy volunteers received either 100 mg ciprofibrate/day followed by 200 mg fenofibrate 'high bioavailability' (HB)/day, or vice versa (group A), 200 mg ciprofibrate/day followed by 200 mg fenofibrate HB/day, or vice versa (group B), or 100 mg ciprofibrate/day followed by 200 mg ciprofibrate/day, or vice versa (group C). Fasting plasma lipid levels and safety parameters were evaluated before and after treatment. One hundred milligrams ciprofibrate/day therapy was found to be approximately as effective as 200 mg fenofibrate HB/day therapy in altering the lipid profile. The highest activation of LPL was obtained after treatment with 200 mg ciprofibrate/day. A modest, but statistically significant, increase in HL activity was found after 100 or 200 mg ciprofibrate treatment. Investigation of the pharmacokinetics of ciprofibrate and fenofibric acid revealed a shorter time to reach peak plasma levels, but a longer elimination half life for the ciprofibrate preparations in comparison with fenofibrate. A dose of 200 mg ciprofibrate/day is more effective than 100 mg ciprofibrate/day at increasing LPL and HL activity; however, 200 mg ciprofibrate/day is also associated with a potentially detrimental change in safety parameters. Two hundred milligrams fenofibrate HB/day therapy may represent an alternative therapy to 100 mg ciprofibrate/day for hyperlipidaemic patients.