Disclosed are 6-deoxy-6-thioether-amino acid cyclodextrin derivatives, obtained from condensation of amino acid derivatives with halo-cyclodextrin in the presence of a base. The 6-deoxy-6-thioether-amino acid cyclodextrin derivatives include 6-deoxysulfinyl-6- thioether-amino acid cyclodextrin derivative and 6-deoxysulfonyl-6-thioether-amino acid cyclodextrin derivative. The compounds disclosed in the present invention can be used to reverse neuromuscular relaxation in patients and animals induced by muscular relaxants, with a rapid reversing and antagonist effect on muscular relaxation induced by muscular relaxants, applicable in the preparation of medicaments with an antagonist effect on muscular relaxation, and are characterized by low production cost and able to reserve and antagonize a wide range of muscular relaxants, thus effectively broaden the scope of clinical use. Most importantly, the compounds disclosed in the present invention have a safe dosage at least two times higher than that of known compounds. The general formula (I) of the present invention is: (I)
