Self assembled precusor liposome containing hard soluble medicine and its preparation method

Abstract

A self-assembled precursor liposome of medicine difficult to dissolve is proportionally prepared from medicine difficult to dissolve, phosphatide, polyethylene glycol and dispersing medium through mixing, dispersing, press filtering by millipore film, and pouring it in a container full of N2.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a self-assembled proliposome containing insoluble drugs, and also relates to a preparation method of the self-assembled proliposome. Background technique [0002] Liposomes (liposomes, also known as lipid globules) are bilayer microvesicles that resemble biological membrane structures. In 1971, British Rymen et al began to use liposomes as drug carriers. [0003] Liposome is a nanoscale particle containing phospholipid components, which can be used as a carrier for insoluble and water-soluble drugs, and is a new type of pharmaceutical preparation. After the drug-containing liposome is administered intravenously, it is mainly swallowed by the reticuloendothelial system, so that the drug is mainly accumulated in tissues and organs such as the liver, spleen, lung and bone marrow, and the distribution of the encapsulated drug in the body is changed, thereby improving the the...

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 average 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 average particle size becomes larger 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, which makes it difficult to effectively control the main quality indicators such as drug encapsulation rate and average particle size

[0014] 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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