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

Divya Harmalkar, Soraiya Godinho, Prashant Jivaji Bhide, Lalit Kumar, Rupesh Kalidas Shirodkar

Research output: Contribution to journalArticle

Abstract

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.

Original languageEnglish
JournalPharmaceutical Chemistry Journal
DOIs
Publication statusAccepted/In press - 01-01-2019

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Solubility
Pharmaceutical Preparations
Excipients
Tablets
Powder Diffraction
Polysorbates
Histamine Antagonists
Urticaria
Differential Scanning Calorimetry
Fourier Analysis
Drug Interactions
Cellulose
X-Ray Diffraction
Silicon Dioxide
Electron Scanning Microscopy
Powders
Biological Availability
Spectrum Analysis
Theoretical Models
ebastine

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Drug Discovery

Cite this

Harmalkar, Divya ; Godinho, Soraiya ; Bhide, Prashant Jivaji ; Kumar, Lalit ; Shirodkar, Rupesh Kalidas. / New Formulation Technique for Solubility and Dissolution Rate Enhancement of Poorly Soluble Drugs. In: Pharmaceutical Chemistry Journal. 2019.
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New Formulation Technique for Solubility and Dissolution Rate Enhancement of Poorly Soluble Drugs. / Harmalkar, Divya; Godinho, Soraiya; Bhide, Prashant Jivaji; Kumar, Lalit; Shirodkar, Rupesh Kalidas.

In: Pharmaceutical Chemistry Journal, 01.01.2019.

Research output: Contribution to journalArticle

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