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本文报道了一种简便、灵敏度较高的一叶萩碱(SCRN)制剂体内吸收的生物测定法。此法根据SCRN在血液中的浓度达到一定水平时会引起动物抽搐的特征,测得本批实验用鼠静注SCRN硝酸盐时的半数抽搐量(CD_(50)~(1v))为3.98mg/kg,并以此为基准比较了4种SCRN制剂在肌注或口服后进入血液的速度、所能达到的血药水平及其时间效应。试验结果表明:肌注SCRN硝酸盐的CD_(50)为15mg/kg。它能很快被吸收,但3h后血药水平就很低。肌注SCRN油剂则与之相反,给药量虽高达26mg/kg,也只能使3h后出现的血药水平峰值为24.6%,但它有长效作用,10h后才降至5.8%。初步临床试验的结果也表明后者的有效率略为高些。此外,还试验和讨论了某些口服制剂的吸收效果。
In this paper, we report a simple and sensitive bioassay method for the in vivo absorption of a mucopolysaccharide (SCRN) preparation. This method according to the concentration of SCRN in the blood reaches a certain level will cause animal convulsions characteristics measured in this batch of experimental mice intravenous sedation SCRN nitrate half of the amount of seizures (CD_ (50) ~ (1v)) was 3.98mg / kg, and used as a benchmark to compare the four kinds of SCRN formulations into the bloodstream after intramuscular or oral administration, the achievable blood level and its time effect. The experimental results showed that: CD_ (50) of intramuscular injection of SCRN nitrate was 15 mg / kg. It can be quickly absorbed, but blood levels are low after 3h. On the contrary, intramuscular injection of SCRN oil, although the dose was as high as 26 mg / kg, only caused the peak blood level after 3 h to reach 24.6%. However, it had a long-lasting effect and decreased to 5.8% after 10 h. The results of the preliminary clinical trial also showed that the latter was slightly more effective. In addition, the absorption effect of certain oral preparations was also tested and discussed.