Formulation and evaluation of liquisolid compact of azithromycin dihydrate

Abstract

Azithromycin dihydrate is a macrolide antibiotic and belongs to BCS class II drugs. The present study aims at the preparation of liquisolid compact of azithromycin dihydrate with an aim to improve the solubility of the drug. The liquid solid system uses a nonvolatile solvent to dissolve the drug. The solution or suspension of drug is converted into a free flowing dry and compressible powder in an admixture of coating and carrier material calculated mathematically. In this study Avicel PH102 and Aerosil 200 were used as carrier and coating material respectively. Propylene glycol was used as the nonvolatile solvent. Using different excipient ratio six formulations were made and evaluated for flowability and compressibility characteristics. Drug excipient interaction study was performed through Fourier transform infrared spectroscopy (FTIR). The formulations were subjected to statistical analysis. Optimization of the formulation was done through JMP V8.0 software. The optimized formulations were evaluated for flowability, compressibility study, thermal analysis by differential scanning calorimetry (DSC) and comparative dissolution study with pure drug. The optimized formulations showed a good flow property and compression characteristics. The FTIR study revealed no physical interaction of the drug with the excipient. The DSC thermograms proved the conversion of crystalline structure of the drug into its amorphous form. The comparative dissolution study of the optimized formulations with the pure drug revealed significant improvement of solubility of azithromycin dihydrate in liquid solid compact. Therefore, it can be concluded that a free flowing, non-adherent, dry and compressible powder of azithromycin dihydrate can be prepared using liquid solid compact technology.

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“…Such liquid medication can be converted into nonadherent, dry-looking, free-flowing and readily compressible powders by a simple admixture process with selected powder excipients referred to as carrier (having good absorption properties) and coating materials carrier (having good adsorption properties). However, the drug will be molecularly distributed in the liquisolid compact and enhance dissolution, and improves oral bioavailability 10 .…”