Amorphous solid dispersions of tegoprazan and three different polymers: In vitro/in vivo evaluation of physicochemical properties

Polymeric solid dispersion enhances the equilibrium solubility and oral bioavailability of tegoprazan

“…In DSC analysis, a pure crystalline drug typically exhibits a very intense and sharp endothermic peak, and when polymers are used as carriers for SD formulation, generally reduced and unclear peak is observed 21,22 . In the DSC results, a clear and sharp endothermic peak was observed from TPZ, while the typical endothermic peaks of TPZ were disappeared in F1–F4 SDs.…”

“…However, the PM showed a slightly shifted endothermic peak for the melting temperature ( T m ) of TPZ of approximately 200–225 °C (Figure 4). On the other hand, the typical peak of TPZ disappeared in TPZ SDs, which is presumed to be due to the amorphization of TPZ inside the polymer matrix 22 …”

“…These results confirmed that the prepared SDs may exist as an amorphous form. The melting point of pure crystalline TPZ was reported as 223.5 ± 1.3 °C 22 . However, the PM showed a slightly shifted endothermic peak for the melting temperature ( T m ) of TPZ of approximately 200–225 °C (Figure 4).…”

“…In addition, SD powders are known to exhibit typical halo‐like patterns of amorphous materials. On the other hand, PXRD patterns of PM are also known to maintain the crystalline peak of the drug 22 . In the PXRD analysis, the characteristic peaks of TPZ were observed at specific 2 theta values, including 12.59, 14.94, 15.57, 16.55, 17.20, 19.61, 23.12, and 24.22, which closely match those reported in paper 22 and previously filed patent for the crystalline form A, 23 indicating that the TPZ used in this study is also in crystalline form A.…”

“…On the other hand, PXRD patterns of PM are also known to maintain the crystalline peak of the drug 22 . In the PXRD analysis, the characteristic peaks of TPZ were observed at specific 2 theta values, including 12.59, 14.94, 15.57, 16.55, 17.20, 19.61, 23.12, and 24.22, which closely match those reported in paper 22 and previously filed patent for the crystalline form A, 23 indicating that the TPZ used in this study is also in crystalline form A. However, in F1–F4, the specific 2‐theta value, which is characteristic of the crystalline form, disappeared, and only a lump‐like shape, which is one of the characteristics of the amorphous form, was present.…”