[Design, preparation, and evaluation of orally disintegrating antiviral granules]

This study reformulated antiviral granules into orally disintegrating granules to achieve instant dissolution and water-free administration and improve compliance and convenience of drug administration for patients. The type of hydrophilic excipients, the ratio of drug-to-excipient, and the grinding time were optimized by a vibration mill to prepare orally disintegrating powder. With the powder used as the raw material, the heating temperature and time were investigated to obtain the optimal granulation process. The differences before and after the preparation of orally disintegrating powder and granules were evaluated by a laser particle size analyzer, an X-ray diffractometer, a scanning electron microscope, and a multiple light scattering analyzer. The results showed that the orally disintegrating powder obtained by grinding the extract powder and xylitol at a ratio of 1∶1 for 3 min had the best instant solubility and taste. The optimal molding rate, instant solubility, and taste of the orally disintegrating granules were obtained by heating the orally disintegrating powder at 90 ℃ for 10 min. Compared with those of the extract powder, the particle size d_(0.9) of the orally disintegrating powder decreased from 846.29 to 44.57 μm; the specific surface area increased from 0.27 to 0.50 m~2·g~(-1), and the total adsorption volume increased from 0.001 5 to 0.002 6 cm~3·g~(-1). The multiple light scattering analysis showed that the orally disintegrating powder could be better dispersed in water. The X-ray diffraction experiment indicated that the crystal structure of xylitol did not change significantly before and after the preparation of orally disintegrating powder and the hot melt bonding process. Scanning electron microscopy showed that the spherical structure of the extract powder was broken into larger irregular fragments, and smaller xylitol particles were adsorbed and wrapped on the surface of the extract powder. After hot melt bonding, the surface or edges of xylitol were melted, and the surrounding extract powder was bonded together, thereby achieving bonding granulation. The orally disintegrating granules catered to the properties of granules, and the taste score and in vitro and in vivo instant solubility were better. In summary, by proposing a new molding process based on instant formulation and hot melt bonding granulation technology and preparing orally disintegrating antiviral granules, the study improves the convenience and compliance of drug administration for patients and provides a useful exploration of the innovation and improvement of traditional Chinese medicine forms.