盐酸美普他酚鼻用温敏型凝胶的制备及其体外释放度考察

Preparation of Nasal Thermosensible Gels of Meptazinol Hydrochloride and Its Release Behavior in Vitro

目的:制备盐酸美普他酚鼻用温敏型凝胶并考察其体外释放特性。方法:以盐酸美普他酚为主药,泊洛沙姆P407为凝胶材料制备凝胶;以影响制剂胶凝温度的泊洛沙姆P407、P188及PEG6000用量为考察因素,胶凝温度为考察指标进行正交试验优选处方;同时采用改良的Franz扩散池法,以生理盐水为介质进行体外释放特性评价。结果:以处方中含有泊洛沙姆P407为20%、泊洛沙姆P188为3%、PEG6000为2%为最佳处方,平均胶凝温度为32.4℃。所制制剂15min即释药约25%,体外释药行为符合Higuchi方程。结论:该制剂处方设计和工艺方法可行,并具有一定的缓释特性,适合鼻腔给药。

OBJECTIVE： To prepare the nasal thermosensible gels of meptazinol hydrochloride and to study its release behavior in vitro. METHODS： The gels were prepared using meptazinol as main component and P407 as gel matrix. The formulation of gels was optimized by orthogonal test using amount of P407, P188 and PEG6000 as factors and gelatination temperature as index. Modified Franz diffusion cell was used to investigate its release behavior in vitro with normal saline as medium. RESULTS： Optimized formulation of gels was as follows： P407 accounting for 20%, P188 for 3%, PEG6000 for 2%, the gelatination temperature of preparation was 32.4 ℃. Release percentage of gels was about 25% within 15 min. Release behavior of gels in vitro was in line with Higuchi equation. CONCLUSION： The formulation design and preparation technology of the gels are feasible and preparation is sustained-release gels with nasal administration.