健康人应用4种不同剂型茶碱的药代动力学及生物利用度研究

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通过荧光偏振免疫法测定10名健康人血清中茶碱浓度,对口服茶碱控释片、茶碱缓释片、氨茶碱片及静脉注射氨茶碱进行了药代动力学及生物利用度的研究。结果:控释片达峰时间(tp=6.00±0.93h)与缓释片达峰时间(tp=6.00±1.11h)均慢于氨茶碱片(tp=1.83±0.38h);清除率(Cl=0.40±0.11、Cl=0.41±0.09ml/min·kg)也均小于氨茶碱片(Cl=0.64±0.12ml/min·kg),控释与缓释片的生物利用度分别为94.0±15.7%、94.8±17.2%,高于氨茶碱片(F=87.7±19.5%)。控释片、缓释片与普通片各药代动学参数及绝对生物利用度间差异均有显著性,而控释片与缓释片间无显著性差异,说明茶碱控释片与缓释片具有满意的缓释特性,保证可靠的完全吸收,减小峰谷浓度落差,并可减少给药次数,降低毒副反应的发生率,提高临床治疗效果。 Fluorescence polarization immunoassay was used to determine the theophylline concentration in 10 healthy volunteers. Pharmacokinetics and bioavailability of theophylline controlled-release tablets, theophylline sustained-release tablets, aminophylline tablets and intravenous aminophylline were investigated. Research. Results: The peak time of controlled release tablets (tp = 6.00 ± 0.93h) and the peak time of sustained release tablets (tp = 6.00 ± 1.11h) were slower than those of aminophylline tablets (tp = 1.83 ± 0.38h). The clearance rates (Cl = 0.40 ± 0.11, Cl = 0.41 ± 0.09ml / min · kg) were also less than that of aminophylline tablets (Cl = 0.64 ± 0.12ml / Min · kg). The bioavailability of controlled release and sustained release tablets were 94.0 ± 15.7% and 94.8 ± 17.2%, respectively, higher than that of aminophylline tablets (F = 87.7 ± 19 .5%). Controlled release tablets, sustained release tablets and ordinary tablets of each pharmacokinetic parameters and absolute bioavailability differences were significant, and controlled release tablets and sustained release tablets no significant difference, indicating that theophylline controlled release tablets and slow Release tablets with satisfactory sustained-release properties, to ensure reliable and complete absorption, reduce the peak-to-valley concentration drop, and can reduce the frequency of administration, reduce the incidence of adverse reactions and improve clinical treatment.
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