Development of Salbutamol Sulphate fast disintegrating sublingual tablets with enhanced bioavailability and improved clinical efficacy for potential treatment of asthma

摘要: Abstract Salbutamol Sulphate (SS) as a model bronchodilator drug undergoes first pass metabolism in liver, which has an oral bioavailability of only 50% the administrated dose. Thus, aim this study was to attain rapid absorption and improved bioavailability, with subsequent immediate onset pharmacological effect. This work introduces new design SS fast disintegrating sublingual tablets (FDSTs) using full factorial (2 3 ) three independent variables: type superdisintegrant (Ac-di-sol or Polyplasdone-XL), its concentration (3% 5%w/w) binder (Avicel PH101 PEG6000). The formula T7 containing Polyplasdone-XL (5%w/w) Avicel (10%w/w) had least disintegration time (12.83 ± 0.7 s) highest dissolution rate (100 ± 2.6%), hence selected for pharmacokinetic human volunteers. showed C max 19.36 ± 2.64 μg/ml, t 1.33 ± 0.24 h; mean AUC (0-8) found be 75.059 ± 7.55 μg h/ml (0-∞) 90.554 ± 8.027 μg h/ml. relative 129.92% when compared Ventolin ® tablets. clinical evaluation fourteen asthmatic patients significant difference forced expiratory volume 1 s (FEV1), vital capacity (FVC) peak flow (PEFR) ZAN spirometry.