Formulation and Evaluation of Bronchodilator Preparations

Abstract

Salbutamol Sulphate is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease in both children and adults. It binds to β2-adrenergic receptors on bronchial smooth muscle leading to smooth muscle relaxation. It is commercially available as tablet, inhaler, injection, syrup and neubiliser. However, its commercial preparation (Ventrolin® tablets; GalaxoSmithkline Pharma-Egypt) has oral bioavailability of only 50% due to extensive first-pass metabolism. The sublingual route of administration produces faster onset of action than orally ingested tablets and the portion absorbed through the sublingual blood vessels by passes the hepatic first pass processes. The aim of this thesis is to formulate Salbutamol Sulphate in two different preparations, rapidly disintegrating sublingual tablets and fast dissolving sublingual films. Thus, the work is divided into three main chapters. Chapter 1: Formulation, evaluation of Salbutamol Sulphate rapidly disintegrating sublingual tablets and stability study of the best formula. Chapter 2: Formulation, evaluation of Salbutamol Sulphate fast dissolving sublingual films and stability study of the best formula. Chapter 3: Bioavailability and clinical study of the selected Salbutamol Sulphate rapidly disintegrating sublingual tablet and fast dissolving sublingual film in humans.