Cocrystal of phloretin with isoniazid: preparation, characterization, and evaluation

Abstract

Phloretin and isoniazid formed new cocrystal and the structure, solubility and antitumor activities were study.

Pharmaceutical Properties of the Phloretin–4,4′-Bipyridine Cocrystal: Structure Analysis, Drug Release Profile, and Antioxidant Activity Research

“…The solubility and dissolution rate of solid drugs were changed due to the formation of cocrystals, which affected the release and absorption of drugs in vivo. The solubility results of pure Phl were selected from the last experimental data . According to the powder dissolution curve of the Phl–4B cocrystal (Figure ), the cocrystal reached equilibrium solubility (49.93 ± 9.69 μg·mL –1 , P > 0.05) in pH 1.2 buffer for 540–1440 min.…”

“…In vitro simulated digestion experiments of Phl and Phl–4B cocrystal were performed in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF). The release rule of pure Phl was selected from the last experimental data . According to Figure , the release rates of Phl and Phl–4B cocrystal at 120 min were 10.78% and 15.18%, respectively, during the incubation stage of gastric digestion, and the Phl–4B cocrystal release rate was significantly higher than that of the Phl raw material at this stage ( P < 0.05).…”

“…Subsequently, the Phl concentration declined after reaching its peak, a phenomenon known as the The release rule of pure Phl was selected from the last experimental data. 16 According to Figure 12, the release rates of Phl and Phl−4B cocrystal at 120 min were 10.78% and 15.18%, respectively, during the incubation stage of gastric digestion, and the Phl−4B cocrystal release rate was significantly higher than that of the Phl raw material at this stage (P < 0.05). However, the release rate of the Phl raw material was very low in the first 30 min and began to rise rapidly to 10.78% after 30 min.…”

“…Our research group is committed to using this strategy to improve the water solubility of natural compounds. In the preliminary experiment, our research group found that phloretin could form a cocrystal with isoniazid (Figure ). After the cocrystal formation of phloretin and isoniazid, the water solubility of phloretin improved.…”

Antioxidant Activity of Trilobatin and Its Inhibitory Effects on Oxidative Damage of Biological Macromolecules

“…1B, within the range of experimental concentration trilobatin showed the same strong ABTS free radical scavenging ability as Vc. Previous research showed that phloretin also had significant DPPH and ABTS radical scavenging activities (Lu et al, 2023). The similar effects of trilobatin and phloretin on DPPH and ABTS free radicals might be due to their similar structures.…”