This study employed hot-melt extrusion technology to prepare berberrubine solid dispersions using Soluplus® as the carrier, aiming to enhance its solubility, improve oral bioavailability. The solid dispersions were characterized by DSC, XRD, SEM, and FI-IR. Solubility and in vitro dissolution studies were conducted. The results indicated that the drug was highly dispersed in the carrier in an amorphous state. The solid dispersions significantly increased drug solubility, particularly showing a 2.59-fold enhancement in pH 6.8 phosphate buffer.Moreover, the solid dispersions with the two drug-carrier ratios exhibited distinct composition-dependent release characteristics, respectively. An LC-MS/MS method was established to determine berberrubine in rat plasma, and the oral pharmacokinetics of the solid dispersions in rats were investigated. The results showed that the AUC0-t of the solid dispersions was 12.9 times higher than that of pure berberrubine (p < 0.01), indicating a significant improvement in oral bioavailability. Therefore, solid dispersions can significantly enhance drug solubility and oral bioavailability. Moreover, solid dispersions with different drug-carrier ratios exhibit distinct immediate-release or sustained-release characteristics, providing valuable insights for formulation development. Depending on the therapeutic strategy and clinical requirements of the disease, different release behaviors can be selected to guide formulation design studies.
Zhao et al. (Mon,) studied this question.