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目的考察大鼠鼻腔给药后血和脑脊液中盐酸美普他酚(MEP)的浓度,并与口服比较。方法采用连续采集法收集脑脊液样品,用HPLC荧光检测器测定各生物样品中MEP的浓度。结果鼻腔给药后药物迅速吸收入血,并在血和脑脊液中达到高浓度,而MEP口服后体内药浓很低。鼻腔给药后血和CSF的AUC值分别为口服的7.375和15.6倍。结论MEP鼻腔给药具有起效快、生物利用度高的特点,有望成为口服的替代途径。
Objective To investigate the concentration of meptapaclol hydrochloride (MEP) in blood and cerebrospinal fluid (CSF) after nasal administration in rats and compare it with that of oral administration. Methods Cerebrospinal fluid (CSF) samples were collected by continuous collection and the concentration of MEP in each sample was determined by HPLC fluorescence detector. Results After nasal administration, the drug quickly absorbed into the blood and reached high levels in the blood and cerebrospinal fluid. However, the drug concentration in the body after oral administration of MEP was very low. The AUC values of blood and CSF after nasal administration were 7.375 and 15.6 times, respectively, orally. Conclusion MEP nasal administration has the characteristics of fast onset and high bioavailability, and is expected to be an alternative oral route.