黄芩苷及其磷脂复合物药效学对比研究——在体鼻黏膜吸收及不同给药途径抗大鼠脑水肿和神经功能损伤对比

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目的:对比研究黄芩苷及其磷脂复合物的大鼠在体鼻黏膜吸收情况,并比较黄芩苷磷脂复合物经舌下静脉及鼻腔给药之不同给药途径对脑缺血损伤致大鼠脑水肿和神经功能损伤的影响。方法:通过大鼠在体鼻黏膜吸收试验比较黄芩苷及其磷脂复合物经鼻吸收的差异,采用紫外分光光度法测定0~120 min黄芩苷累计吸收量,并计算其吸收速率常数;采用线栓法制备大鼠大脑中动脉缺血再灌注损伤模型,观察经舌下静脉给药(给药剂量以黄芩苷计为7.5 mg.kg-1)及经鼻给药(给药剂量以黄芩苷计为7.5 mg·kg-1)后黄芩苷磷脂复合物不同给药途径对脑水肿和神经功能评分的防治效果。结果:黄芩苷磷脂复合物大鼠鼻黏膜吸收速率明显大于黄芩苷,其吸收速率常数分别为[(12.2±2.04)×10-3·min-1,(9.60±1.34)×10-3·min-1],且经鼻给药防治脑缺血损伤致大鼠脑水肿和神经功能损伤的效果优于舌下静脉给药,其神经功能评分结果分别为(1.66±0.68)分和(1.78±0.78)分;脑组织含水量分别为(79.10±0.65)%和(79.48±0.76)%。结论:黄芩苷制备成磷脂复合物后体内吸收及药效优于黄芩苷,且经鼻给药优于舌下静脉给药。 OBJECTIVE: To compare the nasal mucosal absorption of baicalin and its phospholipid complex in rats and to compare the different route of administration of baicalin phospholipid complex via the sublingual vein and nasal cavity. Effects of edema and neurological impairment. Methods: The difference of nasal absorption between baicalin and its phospholipid complex in rat nasal mucosa absorption test was compared. The absorbance of baicalin from 0 to 120 min was measured by ultraviolet spectrophotometry, and the absorption rate constant was calculated. The middle cerebral artery occlusion (MCAO) injury model was established by the method of suppository. The rats were given sublingual (7.5 mg.kg-1) baicalin and nasal administration (baicalin Calculated as 7.5 mg · kg-1) baicalin phospholipid complex route of administration of cerebral edema and neurological function of the prevention and treatment. Results: The absorption rate of nasal mucosa of baicalin phospholipid complex rats was significantly higher than that of baicalin, and the absorption rate constants were (12.2 ± 2.04) × 10-3 · min-1 and (9.60 ± 1.34) × 10-3 · min -1], and nasal administration of cerebral ischemia injury prevention and treatment of cerebral edema and nerve function damage is better than sublingual vein administration, the neurological function score was (1.66 ± 0.68) points and (1.78 ± 0.78). The brain water content was (79.10 ± 0.65)% and (79.48 ± 0.76)% respectively. CONCLUSION: Baicalin is superior to baicalin in its absorption and pharmacodynamics after being prepared into phospholipid complex, and its nasal administration is superior to sublingual intravenous administration.
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