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制备了硫酸沙丁胺醇骨架型缓释片（８ｍｇ／片），以释放度为指标筛选出了适宜处方，并对该处方缓释片与市售普通片对照进行了健康人体单剂量及多剂量随机交叉给药药动学研究。用高效液相荧光色谱法测定了血浆中的药物浓度。缓释片的药动学参数Ｔｍａｘ，Ｃｍａｘ，ＡＵＣ０→∞及ＰＴＦ（波动分数）分别为（４．６±０．８）ｈ，（７．９±１．４）ｎｇ／ｍｌ，（１２１．１±１２．３）ｈ·ｎｇ／ｍｌ及０．９３±０．２６，而普通片的相应药动学参数则分别为（１．４±０．４）ｈ，（１５．１±２．４）ｎｇ／ｍｌ，（１０３．３±８．７）ｈ·ｎｇ／ｍｌ及１．３１±０．２７。经双单侧检验两制剂ＡＵＣ０→∞无显著性差异，而ＰＴＦ则有显著性差异。缓释片相对于普通片的生物利用度为１０６．０％。缓释片具有给药次数少（一日二次）、给药后血药浓度波动较小的特点。
A salbutamol Sulfate Sustained-release Tablets (8mg / tablet) was prepared, and the appropriate prescriptions were selected according to the release rate index. The healthy human single-dose and multi-dose random crossover Pharmacokinetics study. The plasma concentration of the drug was determined by high performance liquid chromatography. The pharmacokinetic parameters Tmax, Cmax, AUC0 → ∞ and PTF of the sustained release tablets were (4.6 ± 0.8) h and (7.9 ± 1.4) ng / ml, respectively. 1 ± 12.3) h · ng / ml and 0.93 ± 0.26, respectively, while the corresponding pharmacokinetic parameters of common tablets were (1.4 ± 0.4) h and (15.1 ± 2), respectively. 4) ng / ml, (103.3 ± 8.7) h · ng / ml, and 1.31 ± 0.27. There was no significant difference in AUC0 → ∞ between the two preparations, but there was a significant difference in PTF. Bioavailability of sustained release tablets relative to conventional tablets was 106.0%. Sustained-release tablets with less administration (twice a day), after administration of plasma concentration fluctuations less features.