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

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.

Formulation and Optimization of Rifampicin and Quercetin Laden Liquisolid Compact: In-Vitro and In-Vivo Study

“…The transparent drug solution was diluted with methanol before being examined by a UV spectrophotometer (Shimadzu Corp., Japan) at 365 cm and 470 cm for QUE and RIF, respectively. Three copies of each sample were analyzed [20][21][22][23][24][25].…”

“…The independent variables were Tween 20, PEG 200, and propylene glycol (X1, X2, and X3). The response variables for both medications' solubility in mg/ml and their percentage CDR at 60 minutes in 0.1 M hydrochloric acid were selected because they were viewed as crucial elements for Liqui-solid Compact to improve oral absorption of the poorly water-soluble drug [20][21][22][23][24][25].…”

“…The angle of the slide was defined as the angle created between the plate and the ground. The ideal flowable attribute of a powder excipient in relation to the specific liquid vehicle being employed is an angle of slide value of roughly 33 [20][21][22][23][24][25].…”

“…The surplus liquid that was left on the carrier material's surface is further absorbed by the coating layer, leaving the entire system dry and free-flowing. The liquisolid approach has produced encouraging results for a variety of medications [20][21][22][23][24][25]. Therefore, the Liquisolid compacts that contain insoluble pharmaceuticals encourage dissolution by facilitating the wetting process by increasing the net effective surface area, which leads to an increase in the availability of the drug for dissolution media [20][21][22][23][24][25].…”

“…The liquisolid approach has produced encouraging results for a variety of medications [20][21][22][23][24][25]. Therefore, the Liquisolid compacts that contain insoluble pharmaceuticals encourage dissolution by facilitating the wetting process by increasing the net effective surface area, which leads to an increase in the availability of the drug for dissolution media [20][21][22][23][24][25]. A semi-synthetic antibiotic called rifampicin is made from Streptomyces mediterranei.…”