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目的:考察羟萘甲酸沙美特罗的平喘作用,并与硫酸沙丁胺醇进行比较。方法:采用离体豚鼠气管螺旋条法和在体豚鼠药物引喘法。结果:羟萘甲酸沙美特罗具有松弛豚鼠气管平滑肌作用,pD2为9.04±0.12;非竞争性拮抗乙酰胆碱(Ach)所致的豚鼠离体气管平滑肌收缩,IC50为(15.7±1.64)×10-10mol/L;延长Ach和His所致豚鼠哮喘的潜伏期。其作用呈现剂量依赖性,用药后0.5,1.5,6h对于豚鼠喘息性抽搐保护作用的ED50及其95%的可信限分别每只为6.79(3.91~9.98),5.16(2.94~9.07),5.92(3.40~9.31)μg。结论:羟萘甲酸沙美特罗具有平喘作用,其作用强度和作用时间均显著强于硫酸沙丁胺醇(P<0.05)。
OBJECTIVE: To investigate the antiasthmatic effect of salmeterol xinafoate and compare it with salbutamol sulfate. Methods: The guinea pig trachea spiral strip method and in vivo guinea pig drug asthma method. RESULTS: Salmeterol xinafoate had the effect of relaxing the bronchial smooth muscle of guinea pigs with a pD2 of 9.04 ± 0.12. The non-competitive antagonism of acetylcholine (Ach) induced guinea pig tracheal smooth muscle contraction with IC50 of (15.7 ± 1.64) × 10-10mol / L; prolonged Ach and His-induced guinea pig asthma latency. The effect was dose-dependent. The ED50 and 95% confidence limits of 0.5, 1.5, and 6 h for the protection of asthmatic convulsions in guinea pigs were 6.79 (3.91-9.98 ), 5.16 (2.94 ~ 9.07), 5.92 (3.40 ~ 9.31) μg. Conclusion: Salmeterol xinafoate has an antiasthmatic effect, its intensity and action time are significantly stronger than salbutamol sulfate (P <0.05).