Study of a novel disintegrable oleanolic acid- polyvinylpolypyrrolidone solid dispersion.

Study of a novel disintegrable oleanolic acid- polyvinylpolypyrrolidone solid dispersion.

Drug Dev Ind Pharm. 2017 Mar 02;:1-24

Authors: Wang W, Cui C, Li M, Zhang Z, Lv H

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 in vitro studies; dissolution test showed that approximately 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 Tmax (p < 0.05) and higher Cmax (p < 0.01) than those of free drug. The AUC0→∞ of OLA-PVPP SDs (1:6) were 155.4±37.24 h·ng/mL comparing 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.

PMID: 28277846 [PubMed - as supplied by publisher]

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