Saffron as a medicinal plant has many therapeutic effects. Phytochemical studies have reported that saffron is composed of at least four active ingredients which include crocin, crocetin, picrocrocin and safranal. The carotenoids of saffron are sensitive to oxygen, light, heat and enzymatic oxidization. However, regulation of these factors is required for saffron quality. Some pharmacologic effects of saffron and its active compounds include cardioprotective, neuroprotective, memory enhancer, antidepressant and anxiolytic. Among more than 150 chemicals of saffron, the most biologically active components are two carotenoids including crocin and crocetin. Most of the pharmacokinetic studies are related to these compounds. The pharmacokinetic studies have shown that crocin is not available after oral administration in blood circulation. Crocin is converted to crocetin in intestine but after intravenous injection, the level of crocetin in plasma is low. Crocetin can distribute in different tissues because of weak interaction between crocetin and albumin. Also it can penetrate blood-brain barrier and reach CNS by passive transcellular diffusion; thus it can be effective in neurodegenerative disorders. The large portion of crocin is eliminated via feces.