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Carfentanyl (CFTN) is a derivative of fentanyl with significant analgesic effects but poor water solvent.The 2,6-di-O-methyl-beta-Cyclodextrin package and its nasal spray carrying CFTN were prepared by ultrasound to increase the solubility of CFTN.The package was significantly higher in hydrochloric acid and phosphate buffer than in free CFTN.The in vivo test of the CFTN-DM-β-CD package (250 g / kg) was performed with intravenous, intramuscular, oral and nasal administration in rats.Results The CFTN-DM-β-CD package was absorbed faster, cmax and higher bioavailability by nasal administration compared with intramuscular injection and oral administration.Therefore, the CFTN-DM-β-CD package nasal spray is a relatively safe, rapid-onset, and effective dosage form.