The invention discloses a method for preparing nanometer magnetic microspheres and an anticancer oral preparation prepared by utilizing the method. The method comprises the process steps of: a, material preparation, in which a 
carrier material, a framework material, a 
drug and a 
solvent are prepared; b, the preparation; c, the stability and 
drying; and d, the crushing and preparation and so on. The method takes beta-
cyclodextrin as the framework material and includes the 
carrier material (a nanometer magnetic 
biomaterial) and 
drug combination and so on. The 
drug-loaded nanometer magnetic microspheres can quickly reach appointed focus target positions, penetrate target 
cell membranes to enter cells, realize the trans-
membrane transport of target macromolecules, achieve the effects of 
targeted release and slow / 
controlled release, improve the 
drug concentration in target cells, and inhibit the 
gene expression and amplification of the target cells to ensure that the target cells are degenerated to necrotize or apoptosize; at the same time, the microspheres strengthen the killing activity of T cells and NK cells and the phagotrophic ability of macrophages to the target cells, improve the 
immunity of organisms, and achieve the effects of multiple treatment and multi-
drug resistance reverse.