Title:Development of Salbutamol Sulphate Sublingual Films in Pullulan Matrix for Enhanced Bioavailability & Clinical Efficacy
Volume: 14
Issue: 4
Author(s): Nahed Mohamed Sallam, Rania Abdel-Basset Sanad*, Rasha Mohamed kharshoom and Mokhles Abdelfadil Zeneldin
Affiliation:
- Department of Pharmaceutics, National Organization for Drug Control and Research (NODCAR), Cairo, Egypt; Postal address: Department of Pharmaceutics, National Organization of Drug Control and Research (NODCAR), 6 Abou Hazem Street, Pyramids, Giza,Egypt
Keywords:
Clinical evaluation, maltodextrin, pharmacokinetics, pullulan, sublingual films, ZAN spirometry.
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.
Method: 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.
Conclusion: FDSFs significantly improved the bioavailability of SS and resulted in dramatic improvement
in its clinical efficacy.
