摘要
８名健康志愿者自身交叉对照，比较单次口服长效头孢氨苄颗粒２ｇ（含头孢氨苄１ｇ）与头孢氨苄片０．５ｇ×２（两次间隔５ｈ）的体内动力学，血药浓度测定用微生物法。结果表明：长效制剂（Ａ）及普通片剂（Ｂ）在０→１２ｈ的血药浓度时程曲线中出现双峰现象。第一峰浓度（Ｃｍａｘ＿１）比较，Ａ、Ｂ分别为８．８１±１．９４ｍｇ／１及１３．２１±２．１ｍｇ／１（Ｐ＜０．０５），第二峰（Ｃｍａｘ＿２）Ａ、Ｂ分别为７．４０±２．３９ｍｇ／ｌ及１０．１８±２．９０ｍｇ／ｌ（Ｐ＞０．０５）；在餐后，Ｂ制剂的Ｔｍａｘ＿２延长及Ｃｍａｘ降低，Ａ、Ｂ制剂的ＡＵＣ＿０→１２ｈ及ＭＲＴ间无显著性差异，提示单次口服Ａ制剂２ｇ，可具有Ｂ的双峰现象及约维持１２ｈ有效血浓度，Ａ制剂是一种长效的控释剂，有可能每天用药两次即可达到治疗效果。
Comparision of the pharmacokinetics of 2 g single dose of long acting cephalexin granules (A) (including cephalexin 1 g) with 1 g Cephalexin tablets (B) (divided in two times, the internal was 5 hours) was studie in 8 healthy volunteers (randomly cross-over). The plasma levels of Cephalexin were detected with bioassay method.Two peaks were showed in the concertration curve(0→12h) of A and B preparations. The main parameters of A and B were as follows: the first Cmax were 8.81±1.94 mg/l and 13.21±2.1 mg/l (P<0.05), the second Cmax were 7.40±2.39 mg/l and 10.18±2.90mg /l, respectively. After the meal, the second Cmax of B were decreased and the second Tmax of B were prolonged. The AUC0→12 and MRT of A and B were not statistically significant. This suggested that A preparation is a long acting controled released preparation, which has two peaks and the effective concerntration was maintained in 12 h duration, when it was given in single dose in 2 g, the level of the antibiotic was the same of ephalexin tablets of 0.5 g given twice in 12 h.. So,preparation A may be effective when administered orally 2 g twice a day.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
1995年第1期16-19,共4页
The Chinese Journal of Clinical Pharmacology
