The invention discloses a kind of method of utilizing the functionalization self-assembled film to regulate the medicinal advantage crystal formation of tolbutamide comprise the steps: silylating reagent NH is immersed in the substrate through the clean surface oxidation2(CH2) nSi[O (CH2) mCH3]3Or NH2(CH2) nSiCl3Organic solvent solution in soak take out clean place again the dichloromethane solution of acyl chlorides after the drying adding triethylamine is that catalysts soaks and takes out and cleans and dries up and makes the functionalization self-assembled film; The functionalization self-assembled film is put into the container of the alcoholic solvent solution that is contained with oversaturated tolbutamide C1-C3 and the crystallization of tolbutamide is carried out in cooling namely obtains the medicinal advantage crystal formation of tolbutamide.Method of the present invention has realized the immobilized and assembling of the success of different structure function self-assembled film at substrate surface and then on the surface of this modified has successfully guided the growth of advantage crystal formation of the high biological activity of Remedies for diabetes tolbutamide.

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