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

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.

Cite this article as:

Sallam Mohamed Nahed, Sanad Abdel-Basset Rania*, kharshoom Mohamed Rasha and Zeneldin Abdelfadil Mokhles, Development of Salbutamol Sulphate Sublingual Films in Pullulan Matrix for Enhanced Bioavailability & Clinical Efficacy, Current Drug Delivery 2017; 14 (4) . https://dx.doi.org/10.2174/1567201813666161024161308

DOI https://dx.doi.org/10.2174/1567201813666161024161308	Print ISSN 1567-2018
Publisher Name Bentham Science Publisher	Online ISSN 1875-5704