Disclosed herein are methods and formulation for enhancing oral availability of CPT-11 during cancer therapy while at the same time, reducing its gastrointestinal (GI) toxicity; thus the methods and formulations as disclosed herein may augment the efficacy of cancer therapy.此處揭示的方法與組合物可用以改善CPT-11於癌症治療的口服可用率,並同時降低CPT-11誘發之腸胃道毒性;因此,此處所揭示的方法和配方可以提升癌症治療的效果。