6-deoxy-6-thioether-amino acid cyclodextrin derivative is obtained bycondensing an amino acid derivative with halogenated cyclodextrin in presenceofalkali. The 6-deoxy-6-thioether-amino acid cyclodextrin derivative includes6-deoxysulfinyl-6-thioether-amino acid cyclodextrin derivative and 6-deoxysulfonyl-6-thioether-amino acid cyclodextrin derivative. Compounds provided are forreversingneuromuscular relaxation in patients and animals induced by muscularrelaxants. Thecompounds are able to rapidly reverse and antagonize muscular relaxationinduced bymuscular relaxants and can be administrated in preparing a drug having anantagonisteffect on muscular relaxation. The compounds have low production cost and areableto reverse and antagonize a wide rage of muscular relaxations, thuseffectivelybroaden scope of clinical use. More importantly, the compounds have a safedose atleast doubled compared to prior arts. The compounds have a general formula(I).