Fruithy Holdings Limited

Yihua Wang

Xiao Wang

Shanchun Zhang

Jiashi Peng

Kaisheng Cheng

Bin Yang

Shu Gao

Hongzhang Sun

Xiaorong Lu

Min Xu

The present disclosure relates to the field of pharmaceutical chemistry, and particularly to a compound represented by Formula (I), a preparation method and medical use thereof. In the compound represented by Formula (I), a lactulosyl group is connected to a heteroatom of genin (G) via a glycosidic bond, wherein the genin (G) is a group formed by removing one hydrogen atom from a heteroatom of an active pharmaceutical molecule, and '' indicates that the lactulosyl group is connected to the heteroatom of the genin (G) via an &#x3b1;-glycosidic bond or a &#x3b2;-glycosidic bond. Pharmacokinetic experiments prove that the lactuloside compound according to the present disclosure can pass through the gastrointestinal tract of a mammal without being absorbed significantly by the gastrointestinal tract and hydrolyzed significantly by endogenous enzymes of a mammal host. Therefore, the lactuloside compound can arrive at the colon site of the mammal, and release an active drug in the colon under the action of colon flora. The lactuloside compound has a function of colon-localized drug release, and can be used for preventing or treating an intestinal disease. 

Lactuloside compounds and preparation and use thereof

The present invention provides a complex of formula (I) or a solvate thereof (wherein n is 1 to 4), a pharmaceutical composition, and use of the pharmaceutical composition in the prevention or treatment of surgical pain, intraoperative pain and postsurgical pain. The technical solution according to the present invention provides a medicament which can be produced by a simple production process and can stably release a local anesthetic in body for a long period. The medicament can be released for at least three days or more, which can prolong the analgesic effect on the postsurgical pain, can be used conveniently by the physician and the patient, and has a good treatment compliance. 

Insoluble complex or solvate thereof, pharmaceutical composition and use thereof

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Hefei, China

Yihua Wang