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目的:研究以TMC-P407-P188-卡波姆为基质的天麻素鼻腔温敏凝胶的药动学参数,初步研究其脑靶向性。方法:以大鼠为动物模型,实验组天麻素鼻腔原位凝胶给药,对照组静注天麻素注射液,给药后分别取两组大鼠体内血液与脑组织(大脑和小脑),采用HPLC法分别测定两组血液中的天麻素含量和脑组织中天麻苷元的浓度,绘制药时曲线,计算曲线下面积(AUC)和平均滞留时间(MRT)等药动学参数,比较两组生物利用度F(%)和脑靶向性参数(BTI)。结果:与静注天麻素注射液相较,经鼻给予天麻素温敏凝胶的大鼠脑组织中的天麻苷元含量显著增加(P<0.05),大脑和小脑的药时曲线下面积显著增加,BTI分别为2.38和1.93,药物平均滞留时间MRT增加了近2倍。生物利用度F(%)也较大的增加。结论:以TMC-P407-P188-卡波姆为基质的天麻素鼻腔温敏凝胶能很好的发挥药效作用,且具有一定的脑靶向性和药物缓释性。
OBJECTIVE: To study the pharmacokinetic parameters of gastrodin thermo-sensitive gels based on TMC-P407-P188-carbomer and to study its brain targeting. Methods: The rats were used as the animal model, the experimental group was given gastrodin gel in situ and the control group was given gastrodin injection. Blood and brain tissues (cerebrum and cerebellum) The content of gastrodin and the concentration of gastrodin in brain tissue were determined by HPLC respectively. The pharmacokinetic parameters such as the curve of drugmedication, areas under the curve (AUC) and mean retention time (MRT) were calculated. Group bioavailability F (%) and brain-targeting parameters (BTI). Results: Compared with the injection of gastrodin injection, the content of gastrodin in the brain tissue of rats receiving gastrodin thermo-sensitive gel significantly increased (P <0.05), and the area under the curve of drug-capillaries increased significantly. BTI were 2.38 and 1.93, the average MRT of drug increased nearly 2 times. Bioavailability F (%) also increased significantly. CONCLUSION: Gastrodin thermo-sensitive gel with TMC-P407-P188-carbomer can play a good pharmacodynamic effect, and has certain brain targeting and drug release.