title: 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 Tmax(p < .05) and higher Cmax(p < .01) than those of free drug. The AUC0→∞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.
authors.affiliation: a Department of Pharmaceutics , State Key Laboratory of Natural Medicines, China Pharmaceutical University , Nanjing , Jiangsu Province , PR China.
authors.forename: Weiqin
authors.initials: W
authors.lastname: Wang
authors.affiliation: a Department of Pharmaceutics , State Key Laboratory of Natural Medicines, China Pharmaceutical University , Nanjing , Jiangsu Province , PR China.
authors.forename: Changchang
authors.initials: C
authors.lastname: Cui
authors.affiliation: a Department of Pharmaceutics , State Key Laboratory of Natural Medicines, China Pharmaceutical University , Nanjing , Jiangsu Province , PR China.
authors.forename: Mengying
authors.initials: M
authors.lastname: Li
authors.affiliation: a Department of Pharmaceutics , State Key Laboratory of Natural Medicines, China Pharmaceutical University , Nanjing , Jiangsu Province , PR China.|b Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine , Nanjing , Jiangsu Province , PR China.
authors.forename: Zhenhai
authors.initials: Z
authors.lastname: Zhang
authors.affiliation: a Department of Pharmaceutics , State Key Laboratory of Natural Medicines, China Pharmaceutical University , Nanjing , Jiangsu Province , PR China.
authors.forename: Huixia
authors.initials: H
authors.lastname: Lv
mesh_terms: D001682:Biological Availability; D002152:Calorimetry, Differential Scanning; D004355:Drug Stability; D009828:Oleanolic Acid / Q000008:administration & dosage* / Q000737:chemistry; D011205:Povidone / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D012995:Solubility
chemical_list: C077842:polyvinylpolypyrrolidone; D009828:Oleanolic Acid; D011205:Povidone
keywords: Solid dispersion; dissolution rate; oleanolic acid; polyvinylpolypyrrolidone; stability