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

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。

Pharmacodynamics Comparison for Effects of Baicalin and its Phospholipid Complex on Cerebral Edema and Neurologic Impairment by in vivo Nasal Mucosa Absorption and other Delivery Approaches

ObJective: To investigate in vivo nasal mucosa absorption of baicalin and its phospholipid complex in rats; to compare the effect of the baicalin-phospholipid complex on cerebral edema and neurological impairment by sublingual iv administration and intranasal administration. Method: The nasal absorption in vivo in rats was used to compare the intranasal absorption of baicalin and its phospholipid complex.The model of focal ischemic reperfusion inJury of middle cerebral artery was built in rats by placing an intraluminal suture and the prevention and treatment of baicalin phospholipid complex was observed after sublingual iv administration and intranasal administration. Result: The nasal mucosa absorption rate of baicalin-phospholipid complex in rat is significantly greater than that of baicalin, they are (12.2±2.04)×10^-3 ·min^-1 and(9.60±1.34)×10^-3 ·min^-1 accordingly. The neurologic function scores are 1.66±0.68 and 1.78±0.78 respectively. They manifest that prevention and treatment effect of baicalin-phospholipid complex by intranasal administration was better than by that of sublingual iv administration against cerebral edema and neurological impairment caused by cerebral ischemic inJury in rats. Moreover, the fresh content of brain tissue is (79.10±0.65)% and (79.48±0.76)% separately. Conclusion: The in vivo absorption and efficacy of baicalin-phospholipid complex was better than that of baicalin, and nasal intranasal administration is superior to sublingual iv administration.