鼻腔给药促进盐酸美普他酚在大鼠体内的吸收及脑转运

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。

SHI Zhen-qi,et al:Enhancement of systemic and CNS delivery of meptazinol hydrochloride by intranasal administration to ratsEnhancement of systemic and CNS delivery of meptazinol hydrochloride by intranasal administration to rats

Aim To investigate the extent of systemic absorption and uptake of meptazinol (MEP) hydrochloride in cerebrospinal fluid (CSF) after intranasal administration on rats and compare with oral administration. Methods CSF samples were collected by a serial sampling method. The concentration of MEP in the biological samples was measured by HPLC with fluorescence detector. Results Rapid and significant levels of MEP in plasma and CSF can be achieved after nasal administration whereas the oral administration resulted in considerably lower drug concentrations. AUC in plasma and CSF from the nasal route are 7.375 and 15.6 folds compared with those of the oral route, respectively. Conclusion Intranasal MEP is able to show quick absorption and improve the bioavailability, which could be a promising alternative to oral administration.