Formulation Development of Mirtazapine Liquisolid Compacts: Optimization Using Central Composite Design

Molecules. 2022 Jun 22;27(13):4005. doi: 10.3390/molecules27134005.

Abstract

Mirtazapine is a tetracyclic anti-depressant with poor water solubility. The aim of this study was to improve the dissolution rate of mirtazapine by delivering the drug as a liquisolid compact. Central composite design (CCD) was employed for the preparation of mirtazapine liquisolid compacts. In this, the impacts of two independent factors, i.e., excipient ratio (carrier:coating) and different drug concentration on the response of liquisolid system were optimized. Liquisolid compacts were prepared using propylene glycol as a solvent, microcrystalline cellulose as a carrier, and silicon dioxide (Aerosil) as the coating material. The crystallinity of the formulated drug and the interactions between the excipients were examined using X-ray powder diffraction (XRD) and Fourier-transform infrared spectroscopy (FTIR), respectively. The dissolution study for the liquisolid compact was carried out as per FDA guidelines. The results showed loss of crystallinity of the mirtazapine in the formulation and was completely solubilized in non-volatile solvent and equally dispersed throughout the powder system. Moreover, drug dissolution was found to be higher in liquisolid compacts than the direct compressed conventional tablets (of mirtazapine). The liquisolid technique appears to be a promising approach for improving the dissolution of poorly soluble drugs like mirtazapine.

Keywords: dissolution enhancement; green products; in vitro characterization; mental disease; mirtazapine; poorly water-soluble drugs; sustainable manufacturing.

MeSH terms

  • Excipients* / chemistry
  • Mirtazapine
  • Powders
  • Silicon Dioxide* / chemistry
  • Solubility
  • Solvents / chemistry
  • Tablets / chemistry

Substances

  • Excipients
  • Powders
  • Solvents
  • Tablets
  • Silicon Dioxide
  • Mirtazapine

Grants and funding

This research received no external funding.