Evaluation of Dissolution Enhancement of Aprepitant Drug in Ternary Pharmaceutical Solid Dispersions with Soluplus® and Poloxamer 188 Prepared by Melt Mixing

Abstract

In the present study Aprepitant (APT) ternary solid dispersions (SDs) were developed and evaluated for the first time. Specifically, ternary SDs of APT with Poloxamer 188 and Soluplus® (SOL) were prepared via melt mixing and compared to binary APT/Poloxamer 188 and APT/SOL SDs. Initially, combined thermo-gravimetric and hot-stage polarized light microscopy studies indicated that all tested compounds were thermally stable up to 280 °C, while Poloxamer 188 acted as a plasticizer to SOL by significantly reducing the temperature required to fully solubilize the API during SD preparation. Differential scanning calorimetry combined with wide angle X-ray diffraction studies showed that crystalline API was dispersed in both binary and ternary SDs, while Fourier transformation-infrared spectroscopy studies revealed no molecular interactions among the components. Scanning electron microscopy combined with EDAX element analysis showed that the API was dispersed in nano-scale within the polymer matrices, while increasing APT content led to increasing API nano-crystals within the SDs. Finally, dissolution studies showed that the prepared formulations enhanced dissolution of Aprepitant and its mechanism analysis was further studied. A mathematical model was also investigated to evaluate the drug release mechanism.

Electrospinning as a method for preparation of redispersible dry product with high content of magnetic nanoparticles

“…Thermogravimetric analysis revealed that the MNP contents in the dry electrospun products of formulations F e 4 and F w 2 were (50.5 ± 0.3) % (w/w) and (50.9 ± 0.5) % (w/w), respectively. The MNP content in the dry electrospun product was determined based on the fact that both polymers, namely PEO and P188, undergo complete thermal decomposition in the temperature range from 400 to 500 • C (Gordon Cameron et al, 1989;Nanaki et al, 2019), whereas the MNPs are not susceptible to thermal decomposition in this temperature range. As the theoretical content of MNPs in the dry product was 50 % (w/w), the thermogravimetric analysis confirmed that MNPs were incorporated in the dry product without any loss.…”

A Micro-Configured Multiparticulate Reconstitutable Suspension Powder of Fixed Dose Rifampicin and Pyrazinamide: Optimal Fabrication and In Vitro Quality Evaluation

“…The initiation of xylitol thermal decomposition was observed at 200 °C and total weight loss recorded at 300 °C ( Figure 3 A) [ 75 ]. Both methylcellulose and Kolliphor ® showed their final thermal decomposition at temperatures greater than 400 °C with an onset of thermal events only displayed at higher heat levels (i.e., 300 °C and 330 °C, respectively) ( Figure 3 D,E)) [ 76 , 77 ]. The onset of thermal decomposition for Primellose ® , polyvinylpyrrolidone, magnesium stearate, potassium chloride and sodium chloride were noted at 258 °C, 360 °C, 87 °C, 340 °C, and 400 °C, respectively while their final decomposition were recorded at temperatures of 600 °C and above ( Figure 3 B,C,F–H) showing their high resistance to thermal deformation as separate entities.…”

Determination of Alteration in Micromeritic Properties of a Solid Dispersion: Brunauer-Emmett-Teller Based Adsorption and Other Structured Approaches

“…In TGA analysis, it was observed that the solid dispersions prepared with MLBG polymer showed minor fluctuations in mass loss, indicating increased thermal stability of dispersion at higher temperature when the percentage of mass loss were compared among both optimized dispersions, which might be due to interactions. TGA thermograms of BEX-polymer systems, indicated that the presence of BEX has minimal effect on the thermal profile of the polymeric carriers, a characteristic that strongly implies a favorable interface between drug and polymers [59][60][61].…”