硫酸沙丁胺醇缓释片的研制及人体生物利用度

PREPARATION AND BIOAVAILABILITY OF SUSTAINED RELEASE TABLETS OF SALBUTEROL SULFATE

用羟丙甲纤维素制备硫酸沙丁胺醇缓释片。药物通过凝胶层扩散释放，可达８ｈ以上。溶出介质、搅拌转速对溶出影响不大。１２名健康自愿者单剂量、多剂量口服试验证明，缓释片相对于普通片的生物利用度为１０１．５％，缓释片达峰延缓，峰值降低。

The sustained release tablets of salbuterol sulfate were prepared using HPMC.The release properties in vitro and the pharmacokinetics and bioavailability in twelve young healthy volunteers were determined by HPLC.The results showed that the drug was slowly released from the gel layer out of the swelled tablets.The pharmacokinetic parameters of the sustained and the conventional tablets were as follows: AUC 89.67±12.10 and 88.03 ±11.11 ng·h·ml -1 , t 1/2 8.63±0.89 and 4.26±0.92 h, C max 9.02±1.09 and 14.68±1.48 ng/ml, T max 4.16±0.45 and 1.69±0.29 h;respectively.