Plant-derived active ingredients with hepatoprotective activity have been used extensively in the treatment of various liver diseases. These compounds are used either in their natural form or the chemical constituents present therein serve as templates for the development of synthetic-based therapeutic entities. Current research interests are focused on formulation development and pharmacokinetic studies of herbal medicines. This article provides a comprehensive review on formulation influences on the preclinical/clinical pharmacokinetics of selected hepatoprotectants such as silymarin, curcumin, glycyrrhizin, andrographolide, phyllanthin, hypophyllanthin, and picroside I and II. Both the formulation and pharmacokinetic factors could affect the target-site concentrations of the active herbal components and, thus, the therapeutic responses. This review contributes to the establishment of a comprehensive understanding of the influence of formulation/dosage form on the pharmacokinetic profile of the hepatoprotective compounds.