摘要
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。
A study on the pharmacokinetics and bioavilability of theophylline controlled release tablet (Theo-CR),theophylline sustained release tablet(Theo-SR), ordinary aminophylline tablet (Amino-Tab)and intravenous aminophylline was carried out by determination of serum theophylline concentrations with fluorescence polarization immuno-assay on 10 healthy volunteers. The results showed that total body theophylline clearance(Cl), time to peak level(tp) and absolute bioavailability(F) of Theo-CR were 0.4±0.11ml/min·kg,6.00±0.93h and 94.0±15.7% respectively, those of Theo-SR were 0.41±0.09ml/min·kg,6.00±1.11h and 94.8±17.2% respectively, those of Amino-Tab. were 0.64±0.12ml/min·kg,1.83±0.38h and 87.7±19.5% respectively. The results showed that the rates of absorption and elimination of Theo-CR and Theo-SR were slower and the absolute bioavailability was higher than those of Amino-Tab with statistically significant difference. This study demonstrated that Theo-CR and Theo-SR may provide an effective and safe therapeutic concentration.
出处
《中国药房》
CAS
CSCD
1994年第5期32-33,共2页
China Pharmacy
关键词
茶碱
药代动力学
控释
缓释
生物学效用
theophpylline pharmacokinetics controlled release sustained release biological effect
