The invention provides a 9-nitrocamptothecin (NC)-cyclodextrin inclusion compound aiming at the technical problems of poor solubility and low bioavailability of 9-nitrocamptothecin in the prior art. The 9-NC-cyclodextrin inclusion compound comprises an active ingredient 9-NC of which the molecular mole ratio is 1:(30-200), an inclusion agent beta-CD or a derivant thereof. A concrete preparation method comprises the following steps: dropwise adding a 9-NC-acetone saturated solution to a CD solution; magnetically stirring at 25-60 DEG C until acetone completely volatilizes; taking supernate to carry out freeze drying after centrifuging the obtained suspension, so as to obtain 9-NC-CD inclusion compound powder. Meanwhile, the invention provides a pharmaceutical composition containing the 9-NC-CD inclusion compound and a pharmaceutically acceptable excipient. Compared with a 9-NC free drug, the solubility of the inclusion compound provided by the invention is increased by over 300 times; meanwhile, the inclusion compound displays higher lactone stability and in-vitro slow-release effect. An X-ray diffraction analysis method and a thermal analysis method indicate that 9-NC in the inclusion compound is completely included, and the reliability of the technology is further verified. Therefore, the inclusion compound can be developed into a liquid preparation, also can improve in vivo absorption of a 9-NC solid preparation, and the bioavailability is improved.