A product of the invention is a variety of hydroxycamptothecin derivative referred to as bipiperidine hydroxycamptothecin {chemical name: (+)-(4S)-4-ethyl-4-hydroxy-9 [ (4-piperidyl
piperidine) carbonyl]-1H-pyrano [ 3 ', 4 ', 6 ', 7 '] butoprizine [1, 2-b]
quinoline-3, 14-( 4H, 12H ) dione and (0-10)
hydrate thereof}. The derivative is a broad-spectrum
antineoplastic drug, and has curative effects on
primary liver cancer, gastric
cancer,
head and neck adenoid epithelial cancer,
leukemia, colon
cancer,
bladder cancer and other malignant tumors. The ipiperidine hydroxycamptothecin, salts thereof and (0-10)
hydrate of the salts are prodrugs for hydroxycamptothecin and converted into closed hydroxycamptothecin
in vivo, so as to overcome defects of open loop, poor effect and
instability of a hydroxycamptothecin preparation (injection, lyophilized injection and oral preparation); and the derivative has good water
solubility and is suitable for preparation of various types of preparations. The bipiperidine hydroxycamptothecin can be added with different salts to be prepared into different water-soluble compounds and hydrates thereof, is beneficial to preparation of various preparations, and has stable quality and
curative effect obvious better than that of hydroxycamptothecin and preparation thereof. The bipiperidine hydroxycamptothecin, salts thereof, (0-10)
hydrate of the salts and preparations thereof are in forms of tablet,
capsule, particulate agent, oral liquid, injection, infusion solutions and lyophilized injection.