title: Development of Salbutamol Sulphate Sublingual Films in Pullulan Matrix for Enhanced Bioavailability & Clinical Efficacy.
abstract: BACKGROUND
  Salbutamol sulphate (SS) is a model short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm having poor bioavailability (50%) due to its extensive first-pass effect.
  
  
  OBJECTIVE
  Formulation of SS as fast dissolving sublingual films (FDSFs) using a biocompatible and biodegradable Pullulan polymer to bypass its metabolism in liver and offers a fast relieve of asthma.
  
  
  METHODS
  Films were prepared by solvent casting technique adopting 32 factorial design to study the effect of two independent variables namely; polymer type (HPMC E5, Pullulan, and L-HPC) and polymer to Maltodextrin ratio (3:0, 3:1 or 5:1). Films physicomechanical properties, disintegration time and in-vitro dissolution of the prepared formulations were evaluated.
  
  
  RESULTS
  Formula F3 containing Pullulan with Maltodextrin in a ratio 3:1 has the least disintegration time (26±2.6 seconds) and the highest dissolution rate (100%±0.5%) after four minutes. Pharmacokinetic study of the optimum formula F3 in healthy human volunteers revealed a shorter tmax (0.75±0.25 hour) compared to Ventolin® tablet 2 mg (2.1±0.37 hour). Clinical evaluation of F3 in 14 male asthmatic patients using ZAN Spirometry showed clinical improvement in lung function parameters when compared with Ventolin® tablets.
  
  
  CONCLUSIONS
  FDSFs significantly improved the bioavailability of SS and resulted in dramatic improvement in its clinical efficacy.
authors: Department of Pharmaceutics, National Organization for Drug Control and Research (NODCAR), Cairo, Egypt.
authors: Nahed Mohamed
authors: NM
authors: Sallam
authors: Department of Pharmaceutics, National Organization for Drug Control and Research (NODCAR), Cairo, Egypt.
authors: Rania Abdel-Basset
authors: RA
authors: Sanad
authors: Department of Pharmaceutics, Faculty of Pharmacy, Beni-Sueif University, Beni-Sueif, Egypt.
authors: Rasha Mohamed
authors: RM
authors: Kharshoom
authors: Department of Chest Diseases, Faculty of Medicine, Al-Azhar University, Damietta, Egypt.
authors: Mokhles Abdelfadil
authors: MA
authors: Zeneldin
mesh_terms: D000284:Administration, Oral; D000328:Adult; D000420:Albuterol / Q000008:administration & dosage* / Q000493:pharmacokinetics; D001249:Asthma / Q000188:drug therapy*; D001682:Biological Availability; D018592:Cross-Over Studies; D005936:Glucans / Q000737:chemistry*; D006801:Humans; D008297:Male; D065568:Oral Mucosal Absorption; D012995:Solubility; D013431:Sulfates; D013607:Tablets; D016896:Treatment Outcome
chemical_list: D005936:Glucans; D013431:Sulfates; D013607:Tablets; C009109:pullulan; D000420:Albuterol
keywords: Clinical evaluation; ZAN spirometry; maltodextrin; pharmacokinetics; pullulan; sublingual films