Study of a novel disintegrable oleanolic acid-polyvinylpolypyrrolidone solid dispersion

Abstract

Novel solid dispersions of oleanolic acid-polyvinylpolypyrrolidone (OLA-PVPP SDs) were designed and prepared to improve the apparent solubility of drug, as well as to improve the stability, fluidity and compressibility of SDs. Disintegrable OLA-PVPP SDs were then evaluated both in vitro and in vivo. DSC, XRD, IR and SEM analysis proved the formation of OLA-PVPP SD and its amorphous state. The results of fluidity study, moisture absorption test and stability test showed that OLA-PVPP SD with good fluidity and qualified stability was successfully obtained. Meanwhile excellent dissolution rate was achieved for in vitro studies; dissolution test showed that ∼50–75% of OLA was dissolved from SDs within the first 10 min, which is about 10–15 times of free OLA. In vivo study indicated that the formation of solid dispersion could largely improve the absorption of OLA, resulting in a much shorter T_max (p < .05) and higher C_max (p < .01) than those of free drug. The AUC_0→∞ of OLA-PVPP SDs (1:6) were 155.4 ± 37.24 h·ng/mL compared to the 103.11 ± 26.69 h·ng/mL and 94.92 ± 13.05 h·ng/mL of OLA-PVPP physical mixture (1:6) and free OLA, respectively. These proved PVPP could be a promising carrier of solid dispersions and was industrially feasible alternative carrier in the manufacture of solid dispersions.

Keywords:

• Solid dispersion
• oleanolic acid
• polyvinylpolypyrrolidone
• dissolution rate
• stability

Disclosure statement

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this article.

Additional information

Funding

The National Natural Science Foundation of China (No. 81673830) is gratefully acknowledged for financial support.