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蟾皮制剂有Ⅰ号(水溶性成分)和Ⅱ号(水脂混合成分)两种注射剂.1.急性毒性:给小鼠快速静脉注射Ⅰ号(50毫升/公斤),24小时未见异常反应.给小鼠静脉注射Ⅱ号,LD50=3.81±0.22毫升/公斤.给小鼠腹腔注射Ⅱ号,LD50=26.27±0.31毫升/公斤.Ⅰ号、Ⅱ号对大鼠均可引起心电图异常,但未见死亡.2.安全试验:对家兔局部刺激性试验和小鼠致敏试验发现,Ⅰ号未见异常而Ⅱ号则略有反应.3.中枢神经系统药理作用:①镇痛作用:Ⅰ号对小鼠热板法测定痛阈提高百分率,3小时后仍为65.6%(P<0.01).②镇静,催眠作用:Ⅱ号对小鼠可显著提高阈剂量水合氯醛的入睡率和睡眠时间(P<0.01)而Ⅰ号作用不显著(P>0.05)③抗痉作用:Ⅰ号、Ⅱ号对小鼠电惊厥均无明显影响.结果表明:Ⅰ号注射液急性毒性极低,并有温和持久的镇痛作用,可供临床用.但应注意对心脏的影响.Ⅱ号注射液虽在毒性和安全试验上存在一定的问题,但由于具有显著增强催眠作用,提示蟾皮制剂在改进工艺和提高有效成分等方面尚有一定的余地.
Toad skin preparation has two kinds of injections Ⅰ (water-soluble component) and Ⅱ (water-fat mixed component) .Acute toxicity: The mice were given iv (50ml / kg) .Intravenous injection of mouse No. II, LD50 = 3.81 ± 0.22 ml / kg intraperitoneal injection to mice No. Ⅱ, LD50 = 26.27 ± 0.31 ml / kg.Ⅰ, Ⅱ rats can cause ECG abnormalities, but No death .2 safety test: Local irritation test in rabbits and mice sensitization test found that no abnormality of No. Ⅰ and No. 2 is a slight reaction.3 Central nervous system pharmacological effects: ① analgesic effect: Ⅰ on the hot plate method for the determination of pain threshold increased percentage, 65.6% after 3 hours (P <0.01). ② sedation, hypnosis effect: Ⅱ mice can significantly increase the threshold dose of chloral hydrate sleep rate and (P <0.01), while the effect of I was not significant (P> 0.05) ③ Antispasmodic effect: Ⅰ and Ⅱ had no significant effect on electric shock in mice.The results showed that: Ⅰ acute toxicity was very low, And a moderate and lasting analgesic effect for clinical use, but should pay attention to the impact on the heart. Although the No. 2 injection toxicity and safety tests there is a certain However, due to the significant enhancement of hypnotic effect, it is suggested that there is still some room for improvement of the process and improvement of the active ingredients of the toad preparation.