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Development of Salbutamol Sulphate Sublingual Films in Pullulan Matrix for Enhanced Bioavailability & Clinical Efficacy

[ Vol. 14 , Issue. 4 ]

Author(s):

Nahed Mohamed Sallam, Rania Abdel-Basset Sanad*, Rasha Mohamed kharshoom and Mokhles Abdelfadil Zeneldin   Pages 503 - 515 ( 13 )

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.

Keywords:

Clinical evaluation, maltodextrin, pharmacokinetics, pullulan, sublingual films, ZAN spirometry.

Affiliation:

Department of Pharmaceutics, National Organization for Drug Control and Research (NODCAR), Cairo, 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, Department of Pharmaceutics, Faculty of Pharmacy, Beni-Sueif University, Beni-Sueif, Department of Chest Diseases, Faculty of Medicine, Al-Azhar University, Damietta

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