Preparation of Efavirenz resinate by spray drying using response surface methodology and its physicochemical characterization for taste masking

Abstract

In the present study, taste masked drug–resin complex (DRC) of efavirenz (EFV) was prepared by spray drying technique. The DRC was then incorporated in to a fast dissolving tablet dosage form. EFV is antiretroviral agent of very bitter taste and low oral bioavailability. To investigate the influence of the independent variables on encapsulation efficiency (EE) as well as on the bitter taste of EFV, response surface methodology was employed. Ion-exchange resin (tulsion-335) and amount of solvent were selected as the independent variables while the EE was selected as the dependent variable. DRC was characterized for EE, X-ray diffraction, particle size distribution, Fourier transform infrared spectroscopy, surface morphology, and in vitro dissolution study. The spectrophotometric method was used for the evaluation of bitter taste of EFV. The EE was found to be 37–84%. The compressed tablets were evaluated for the hardness, Friability, wetting time, disintegration time and in vitro drug release studies. This study confirmed that complexation of the drug with an ion-exchange resin can effectively mask the bitter taste of the drug in combination with production of fast dissolving tablets.

Keywords:

• Efavirenz
• drug–resin complex
• spray drying
• encapsulation efficiency
• taste masking

Acknowledgment

The work is supported by University Grants Commission, New Delhi through National Fellowship and Cipla Limited, Mumbai, India for providing gift sample of Efavirenz.

Disclosure statement

No potential conflict of interest was reported by the authors.