New Formulation Technique for Solubility and Dissolution Rate Enhancement of Poorly Soluble Drugs

Аннотация

Ebastine (EBS) is a second-generation non-sedating antihistamine used for the prevention and treatment of allergic rhinitis and chronic idiopathic urticaria. It is BCS class II drug exhibiting low aqueous solubility and poor oral bioavailability. The present work was aimed at enhancing the dissolution rate of EBS by formulating it in the form of a liquisolid (LS) system using Tween 20 (non-volatile solvent), Avicel PH 102 (carrier material) and Aerosil 200 (coating material). Various batches of LS powder system were formulated by adopting a mathematical model for calculating required quantities of excipients. The absence of interaction between drug and excipients was checked by Fourier transform IR spectroscopy and differential scanning calorimetry studies. Formulated EBS tablets were evaluated for post compression parameters. X-ray powder diffraction studies and scanning electron microscopy showed the loss of EBS crystallinity in LS formulations. Formulation F9 was considered as optimum, showing a higher drug release of up to 99.06% in comparison to marketed tablet formulations. Stability of the optimized formulation was confirmed by results of the accelerated aging study. Thus, it is concluded that LS formulation is a favorable method of EBS solubility enhancement.