Self-assembly precursor liposome containing camptothecine medicine, and its preparing method

Abstract

A self-assembling precursor liposome containing the camptothecine medicines contains camptothecine medicines (0.01-5 Wt %), phosphate (1-50), dispersing medium (10-90), polyethanediol (0.1-30) and disperser (1-40). It has high stability and low cost. Its preparing process is also disclosed.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a self-assembled proliposome containing camptothecin drugs, and also relates to a preparation method of the self-assembled proliposome. Background technique [0002] In view of the unique anti-cancer mechanism of camptothecin and its derivatives (specifically blocking the synthesis of Top I enzymes), since 1985, especially after entering the 1990s, countries such as the United States, Japan, Canada and the United Kingdom have actively invested a lot of The research and development of camptothecin has made camptothecin the second most important woody anti-cancer medicinal plant after paclitaxel, and has become a worldwide hot research topic. [0003] Since camptothecin and its derivatives are mostly difficult to dissolve in water, the currently existing domestic marketed varieties utilize alkaline solution to open their lactone rings to form carboxylate salts to prepare in...

AI Technical Summary

Problems solved by technology

[0006] 1. The preparation process is complicated, prone to bacterial contamination, poor reproducibility, difficult to industrialized large-scale production, and high manufacturing cost

[0007] 2. Poor preparation quality stability

[0009] (2) During storage of drug-containing liposome liquid preparations, there are objectively: the phenomenon of drug diffusion (or leakage) from liposomes to the liquid medium, resulting in reduced or unstable drug encapsulation efficiency; (or aggregation) tendency, also causes the important factor that liposome particle size becomes larger or unstable

[0010] (3) During the dissolution and dispersion process of drug-containing liposome solid (lyophilized) preparations before use, liposome aggregation or particle size increase due to incomplete local dissolution and uneven dispersion of liposome nanoparticles; Or liposome rupture, drug leakage, resulting in decreased encapsulation efficiency of drug-containing liposomes

In view of the fact that in the process of preparing solid proliposomes, the process of removing organic solvents is the main technical bottleneck to realize industrialization, and the hydration process of solid proliposomes will also objectively have a slow hydration rate and incomplete local dissolution , uneven dispersion and other problems, resulting in the main quality indicators such as drug encapsulation rate and average particle size are difficult to effectively control, and it is difficult to meet the requirements of clinical use

In the existing published patents, research literature and reports on the preparation of liposomes and proliposomes, no preparation technology directly using liquid self-assembled proliposomes has been found.

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