A kind of phospholipid compound of hydrophilic drug, its pharmaceutical composition and application

Abstract

The invention discloses a phospholipid compound of hydrophilic drugs as well as a pharmaceutical composition and application of the phospholipid compound. The pharmaceutical composition of the phospholipid compound of the hydrophilic drugs or a combined pharmaceutical composition of the phospholipid compound of the hydrophilic drugs and a pharmacologically acceptable carrier; and the pharmaceutical composition is in the form of a liquid preparation, a solid preparation, a semisolid preparation, a capsule, granules, a gel or an injection. The pharmaceutical composition is in the form of liposome nanoparticles prepared from the phospholipid compound of the hydrophilic drugs or the phospholipid compound of the hydrophilic drugs and adjuvants, and the pharmaceutical composition is 10-1000nm in grain size. The phospholipid compound of the hydrophilic drugs and the liposome nanoparticles thereof can serve as a liquid preparation, a solid preparation, a semisolid preparation, a sterilized preparation and a sterile preparation; and the phospholipid compound of the hydrophilic drugs and the liposome nanoparticles thereof are low in toxicity, and are applicable to the efficient treatment of various tumors and the like.

Description

technical field

[0001] The invention relates to a phospholipid compound of a hydrophilic drug with anti-tumor effects, its pharmaceutical composition and application, and relates to the technical field of medicine. Background technique

[0002] Hydrophilic drugs can be formulated into solutions orally or administered by injection. However, due to their excellent hydrophilicity and poor lipophilicity, these drugs often cannot or are difficult to pass through the cell membrane and enter cells by passive diffusion, resulting in limited drug efficacy. Some or even most of the drug is excreted as the original drug.

[0003] Nucleoside anti-metabolite anticancer drugs are water-soluble analogues of deoxycytidine. Due to their excellent water solubility and poor lipophilicity, they cannot pass through the cell membrane and enter cells by passive diffusion. Gemcitabine (2'-deoxy-2', 2'-difluorocytidine) is a pyrimidine nucleoside analogue developed by Eli Lilly and Company. Gemcit...

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