Zhikang Granules (ZKG) is a traditional Chinese medicine prescription for the treatment of hyperlipidemia symptoms. In this study, the effect of extraction solvents-namely, acetone, ethanol, and water-on the recovery of a bioactive ingredient-namely, chrysophanol-and on the bioactivity of this herbal formulation was investigated. Although the solubility of chrysophanol is highest in acetone, the amount of chrysophanol extracted from Semen Cassiae is lowest in this solvent. Water was found to play an important role in the release of chrysophanol from Semen Cassiae. Two alternative ZKG processing methods are proposed based on the findings of bench-scale extraction tests. The resulting products were analyzed by both Chemical analyses and biological assays. One of the products offered the same level of bioactivity while using only 10% of the original amount of Semen Cassiae.