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目的:对芷冰鼻腔原位凝胶剂的药效学及鼻纤毛毒性进行研究。方法:50只小鼠随机分为5组,空白组给予0.8 g.kg-1生理盐水,对照组(灌胃给予阿司匹林0.04 g.kg-1),芷冰鼻腔原位凝胶剂(ZBISG)低、中、高剂量组(0.4,0.8,1.2 g.kg-1),在给药5 min后ip 0.6%醋酸溶液10 mL.kg-1。观察并记录出现扭体的时间及20 min内出现扭体反应的次数,计算镇痛率。用热板法测定小鼠给药前及给药后15,30,60,90 min痛反应潜伏期,计算痛阈提高率。采用在体蟾蜍上颚模型,生理盐水0.5 mL作为对照,考察凝胶的鼻纤毛毒性。结果:与空白组相比,各给药组小鼠的扭体次数均有显著性下降(P<0.01),与阿司匹林组相比,低剂量组无显著差异,而中、高剂量组差异显著(P<0.01),随着剂量的增加,ZBISG的止痛作用增强;小鼠出现扭体的时间各给药组与空白组相比,均有显著性差异(P<0.01),随着剂量的增加,ZBISG的抑制出现疼痛反应的作用增强。各给药组与空白对照组相比,各时间点的热痛阈提高率均有显著性差异(P<0.01),ZBISG组各时间点的痛阈提高率均高于阿司匹林组(P<0.01);ZBISG低、中剂量组与高剂量组相比,各个时间点的痛阈提高率均有显著性差异(P<0.01)。芷冰鼻用原位凝胶剂对纤毛运动基本无影响。结论:芷冰鼻用原位凝胶剂为1种有效安全的新型制剂。
Objective: To study the pharmacodynamics and nasal cilia toxicity of Angelica nasal in situ gel. Methods: Fifty mice were randomly divided into five groups. The rats in the blank group were treated with 0.8 g · kg-1 normal saline, and the control group (aspirin 0.04 g.kg-1 intragastrically), Zibing nasal in situ gel (ZBISG) Low, medium and high dose group (0.4,0.8,1.2 g.kg-1), 5 min after administration ip 0.6% acetic acid solution 10 mL.kg-1. Observed and recorded writhing time and torsion reaction within 20 min the number of times to calculate the analgesic rate. The hot-plate method was used to determine the latency of pain reaction before and 15, 30, 60, and 90 min after administration, and the rate of improvement of pain threshold was calculated. In vivo toad palate model, saline 0.5 mL as a control to investigate the nasal ciliotoxicity of the gel. Results: Compared with the blank group, the number of writhing in each administration group was significantly decreased (P <0.01), compared with the aspirin group, there was no significant difference in the low dose group, but the middle and high dose group was significantly different (P <0.01). The analgesic effect of ZBISG increased with the increase of dose. The writhing time in each group was significantly different (P <0.01) Increase, ZBISG inhibit the emergence of the role of pain response. Compared with the blank control group, the improvement rate of the heat pain threshold at each time point was significantly different (P <0.01), and the improvement rate of pain threshold at each time point in ZBISG group was higher than that of aspirin group (P <0.01) ). Compared with the high-dose ZBISG low and medium dose groups, the improvement rates of pain threshold at all time points were significantly different (P <0.01). Zhibing nasal gel in situ with no effect on ciliary movement. Conclusion: Angelica nasal in situ gel is an effective and safe new preparation.