Abstract: Oral Chinese herbal medicines (OCHMs) are administered as chemically and physically complex preparations, but the pharmacological entity that reaches a colorectal cancer (CRC)-relevant biological interface may differ substantially from the ingredient list of the administered product. This critical narrative review applies a single organizing hierarchy: material form is the primary pharmacological variable; anatomical compartment constrains exposure; evidence level determines the strength of inference; and the colorectal tumor ecosystem is the downstream site of pharmacodynamic convergence. Five post-oral material forms are distinguished: blood-accessible small molecules; intestinally available parent compounds and microbial transformation products; polysaccharides and glycoconjugates; plant-derived vesicle-like nanoparticles; and decoction-derived supramolecular or self-assembled aggregates. Across these categories, the decisive question is whether a defined entity reaches a relevant compartment at sufficient concentration and duration to produce a reproducible pharmacodynamic effect. Evidence is most mature for selected small-molecule pharmacology and a limited set of clinical outcomes, intermediate for structure-resolved polysaccharide–microbiota mechanisms, and preliminary for natural vesicles and decoction-derived assemblies. We therefore propose four linked validation gates—material identity, compartment-specific exposure, causal pharmacodynamics, and clinical reproducibility—to discipline interpretation and translation. This framework converts the generic language of multicomponent and multitarget action into experimentally testable pharmacology.