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首页> 外文期刊>The Journal of Clinical Pharmacology: Official Journal of the American College of Clinical Pharmacology >Comparative target site pharmacokinetics of immediate- and modified-release formulations of cefaclor in humans.
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Comparative target site pharmacokinetics of immediate- and modified-release formulations of cefaclor in humans.

机译：头孢克洛的即时和调释制剂在人体内的比较靶点药代动力学。

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摘要

Optimal dosing of beta-lactam antibiotics aims at maximizing the time at which drug levels in the interstitial spacefluid (ISF)--the fluid that surrounds the causative microorganisms at the target site--exceed the minimal inhibitory concentration (MIC). One potentially attractive strategy to achieve this goal is to administer antibiotics as oral sustained-release formulations. The present study was designed to test the hypothesis that sustained-release formulations could lead to a more suitable pharmacokinetic profile in the ISF at the relevant target site. For this purpose, time versus cefaclor concentration profiles attained in the ISF were measured following administration of two formulations, an immediate- (500 mg IR) and a modified-release formulation in two different doses (500 mg MR and 750 mgMR) in a three-way crossover study of healthy male volunteers (n = 12). For the measurement of unbound cefaclor concentrations in the ISF of human skeletal muscle, the in vivo microdialysis technique was employed. For all three formulations, unbound cefaclor concentration in the ISF closely followed individual plasma concentration profiles in a dose-dependent pattern, with ISF to unbound plasma ratios ranging from 0.67 to 0.73. The mean residence time was found to be significantly longer for the MR formulations versus the IR formulation. The data of the present study indicate that time above MIC values at the target site can be substantially prolonged if an antibiotic is administered as a sustained-release product.
机译：β-内酰胺类抗生素的最佳剂量旨在最大程度地延长间隙空间流体（ISF）中的药物水平（最小化靶标浓度（MIC）），该时间是目标部位周围引起病原微生物的液体。实现该目标的一种潜在有吸引力的策略是将抗生素作为口服缓释制剂给药。本研究旨在测试以下假设：缓释制剂可以在相关目标部位的ISF中导致更合适的药代动力学特征。为此，在两种制剂中，分别以两种不同剂量（500 mg MR和750 mgMR）以三种剂量给药后，立即测定（500 mg IR）和调释制剂后在ISF中获得的时间与头孢克洛浓度曲线健康男性志愿者的双向交叉研究（n = 12）。为了测量人骨骼肌的ISF中未结合的头孢克洛浓度，采用了体内微透析技术。对于所有三种制剂，ISF中未结合的头孢克洛浓度均以剂量依赖的方式密切跟踪各个血浆的浓度曲线，ISF与未结合的血浆比率为0.67至0.73。发现与IR制剂相比，MR制剂的平均停留时间明显更长。本研究的数据表明，如果将抗生素作为缓释产品给药，则靶点高于MIC值的时间会大大延长。

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