硫酸沙丁胺醇微球缓释片的制备及初步药动学研究

Study on Preparation and Pharmacokinetics of Salbutamol Sulfate Microspheres Sustained Release Tablets

摘要: 目的探讨硫酸沙丁胺醇微球缓释片的制备方法，并对微球缓释片在家犬体内的药动学进行初步研究。方法运用喷雾干燥法制备硫酸沙丁胺醇缓释微球，直接压片得到硫酸沙丁胺醇微球缓释片。对微球缓释片和市售普通片进行家犬体内单剂量给药实验，建立了血药浓度测定的高效液相色谱法。结果普通片和微球缓释片的药动学参数C_max分别为(155.1±3.4)和(126.7±1.9)ng·mL^-1；T_max分别为(1.5±0.6)和(4.1±0.8)h；t_1/2分别为(4.12±0.93)和(5.73±0.64)h，相对生物利用度为109.7%。结论硫酸沙丁胺醇微球缓释片具有缓释效果。

Abstract: OBJECTIVE To explore the methods to prepare salbutamol sulfate microspheres sustained-release tablets, and study its pharmacokinetics and relative bioavailability in dogs. METHODS Salbutamol sulfate sustained release microspheres were prepared of by spray drying method, and then direct tabletting. The microspheres sustained release tablets and commercial tablets in dogs were performed single dose experiments by HPLC. RESULTS The pharmacokinetic parameters for the single dose of commercial tablets and tested tablets were C_max (155.1±3.4) and (126.7±1.9)ng·mL^-1, T_max(1.5±0.6) and (4.1±0.8)h; t_1/2 (4.12±0.93) and (5.73±0.64)h, the relative bioavailability was 109.7%. CONCLUSION Salbutamol sulfate microspheres sustained-release tablets is sustained-release preparation.