Sì Miào San (SMS), containing Rhizoma Atractylodis, Radix Achyranthis, Cortex Phellodendri, and Semen Coicis, is a formulation used for the treatment of general infections and inflammatory diseases. In clinical practice this classical formulation has been advanced by replacing Radix Achyranthis with Rhizoma Coptidis (m1SMS). SMS has been modified a second time by replacing Radix Achyranthis with Fructus Chaenomelis (m2SMS). The first step was a survey conducted in a hospital among patients suffering from rheumatic diseases, about their knowledge and interest in complementary medicine with a focus on TCM. The surveyed persons were interested in alternative medicine, but did know only little about TCM. The main goal was the establishment of a chemical profile of SMS, the two modifications, and single plant components as well as the assessment of the bioactivities of these samples. Decoctions of the formulations and single plant components were prepared, separated and investigated by thin layer chromatography (TLC), high-performance liquid-chromatography (HPLC), and liquid chromatography ? mass spectrometry (LC-MS/MS) to obtain fingerprints. Therefore, LC-MS/MS and HPLC methods were developed and validated. A gradient system with water and acetonitrile turned out to be the optimal system for the separation. In addition, the formulations and single component herbs were extracted with organic solvents according to the PPRC monograph for Sì Miào San, leading to the result that water is not the most suitable solvent for the extraction. A quality assessment did not reveal any differences in the chemical composition of the single component herbs. The anti-inflammatory and antioxidant activities of the formulations, single plant components, and pure compounds were tested using in-vitro bioassays (inhibition of 2,2-diphenyl-1-picrylhydrazyl, tyrosinase, lipid-peroxidation, Src tyrosine kinase, Interleukin-6 production as well as cytotoxicity).