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目的探讨盐酸曲马多微球缓释片的制备方法,并对微球缓释片在家犬体内药动学进行研究。方法以乙基纤维素作为包裹材料,运用喷雾干燥法制备盐酸曲马多缓释微球,直接压片得到盐酸曲马多微球缓释片。对微球缓释片和市售缓释片进行家犬体内单剂量给药实验,建立高效液相分析方法。结果 HPLC显示方法精密度、回收率、专属性都符合要求。市售缓释片和微球缓释片的药动学参数Cmax分别为(322±16)ng·mL-1和(346±11)ng·mL-1;Tmax分别为(2.5±0.3)h和(1.5±0.4)h;t1/2分别为(4.31±0.84)h和(4.95±0.79)h,AUC0→t分别为(2 940.8±32.1)ng·h·mL-1和(3 560.9±18.6)ng·h·mL-1,相对生物利用度为121.09%,不同释放时间点,盐酸曲马多微球缓释片的体内吸收与体外释放都具有良好的相关性。结论盐酸曲马多微球缓释片具有缓释效果。
Objective To study the preparation of tramadol hydrochloride microspheres sustained-release tablets and study the pharmacokinetics of microspheres sustained-release tablets in dogs. Methods Ethylcellulose was used as the coating material, and tramadol hydrochloride microspheres were prepared by spray drying method. The microspheres sustained-release tablets and commercially available sustained-release tablets dogs domestic single-dose administration experiments, the establishment of high performance liquid chromatography. Results HPLC showed that the precision, recovery and specificity of the methods met the requirements. The pharmacokinetic parameters Cmax were (322 ± 16) ng · mL-1 and (346 ± 11) ng · mL-1, respectively, and the Tmax were (2.5 ± 0.3) h (1.5 ± 0.4) h and (4.31 ± 0.84) h and (4.95 ± 0.79) h, respectively. The AUC0 → t were (2940.8 ± 32.1) ng · h · mL-1 and 18.6) ng · h · mL-1, the relative bioavailability was 121.09%. At different time points, the absorption of tramadol hydrochloride microspheres in vivo was related to the release in vitro. Conclusion Tramadol hydrochloride microspheres sustained-release tablets with sustained-release effect.