Abstract: OBJECTIVE To study the preparation of NL-101-hydroxypropyl betacyclodextrin inclusion complex. METHODS The NL-101-hydroxypropylbetadex inclusion complex was prepared by freeze drying method and was optimized with inclusion ratio as index by orthogonal experiment. RESULTS The optimized conditions were 100 r·min^-1 of stirring speed, 10℃ of stirring temperature, 30 min of stirring time, 1:10 of ratio of NL-101:hydroxypropyl betacyclodextrin confirmed by X-ray diffraction method and infrared spectroscopy. CONCLUSION NL-101-hydroxypropylbetadex inclusion complex can be effectively prepared with freeze drying method. And the inclusion with greater than 95% of the inclusion ratio is prepared. The solubility of NL-101 is increased when the durg was included by hydroxypropyl betacyclodextrin.