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The initial absorption phase of thezolpidem-MR formulation was as fast as that of zolpidem-IR with no significant difference in t(max). With zolpidem-MR 12.5 mg, C(max) was moderately lower than with zolpidem-IR (ratio of 0.82), and plasma zolpidem concentrations were maintained above those observed with zolpidem-IR for a longer period of time, particularly from 3 to 6 h post-dose. This was confirmed by an increase in half-value duration (HVD) from 2.3 h with zolpidem-IR to 4.6 h with zolpidem-MR 12.5 mg. The mean terminal half-life was similar between formulations. Zolpidem-MR 12.5 mg provides the appropriate pharmacokinetic characteristics to extend plasma zolpidemconcentrations into the middle of the night (3-6 h post-dose), while retaining the same t(max) and terminal half-life.
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RXMCDM: 金币+1, 多谢应助! 2014-10-16 23:29:53
xiaowanzi9: 金币+20, 翻译EPI+1, ★★★★★最佳答案 2014-10-17 08:55:25
唑吡坦-MR制剂的初始吸收阶段和唑吡坦-IR一样快,t(最大)没有显著差异。用12.5毫克唑吡坦-MR时,C(最大值)比唑吡坦-IR适度降低(比值为0.82),血浆唑吡坦的浓度高于用唑吡坦-IR得到的浓度,且维持更长的时间,特别是在用药后3至6个小时。这也由半值时间(HVD)增加得到进一步证实:在使用12.5毫克时,唑吡坦-IR的HVD为2.3ħ,而带唑吡坦-MR的HVD则增加至4.6小时。两种制剂的平均终末半衰期相似。12.5毫克唑吡坦-MR提供了适当的药代动力学特性,使血浆唑吡坦浓度可以持续到半夜(用药后3-6小时),同时维持相同的t(max)和终末半衰期。
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