Preparation method of levocarnitine composition for injection and liposome injection thereof

Abstract

The invention relates to a preparation method of levocarnitine composition for injection and liposome injection thereof. The preparation method comprises the following steps: using sodium dihydrogen phosphate and sodium hydroxide with a volume ratio of 10:1-12:1 solution, preparing an acid-base buffer solution, wherein the molar concentration of the acid-base buffer solution is between 0.010-0.012mol / L; fructose diphosphate sodium and levocarnitine injection are added to the acid-base buffer solution, wherein the fructose diphosphate The mass ratio of sodium phosphate to levocarnitine is between 0.8:1-1.1:1, and the mass concentration of levocarnitine is between 18-22g / L; add a needle with a mass concentration of 0.1g / L and stir well with activated carbon, Stirring and adsorption for 30 minutes; ultrasonic filtration of activated carbon; vacuum freeze-drying to obtain the finished levocarnitine composition. The levocarnitine composition for injection prepared by the invention has a stable microstructure of the finished product, good resolubility, good safety, and better drug properties than existing drugs.

Description

technical field [0001] The invention relates to the technical field of chemical drug preparations, in particular to a preparation method of a levocarnitine composition for injection and a liposome injection thereof. Background technique [0002] L-carnitine is a natural substance in the body needed in mammalian energy metabolism, and its main function is to promote lipid metabolism. During hypoxia and ischemia, fatty acyl-CoA accumulates, long-chain fatty acyl-carnitine in mitochondria also accumulates, and free carnitine decreases due to massive consumption. Ischemia and hypoxia lead to a decrease in ATP levels, an increase in the permeability of cell membranes and subcellular membranes, and the accumulation of fatty acyl-CoA can cause changes in membrane structure, disintegration of membrane phases, and cell death. In addition, during hypoxia, the anaerobic glycolysis of sugar is the main method, and the accumulation of fatty acids leads to acidosis, ion disturbance, and ...

AI Technical Summary

Problems solved by technology

[0003] 1. The traditional preparation process is to adjust the pH with hydrochloric acid after preparing the semi-finished solution, which will easily lead to uneven pH of the solution system, thus affecting the efficacy of the drug

[0004] 2. The levocarnitine produced in the traditional preparation process is prone to discoloration in clinical use, causing consumers to have a crisis of confidence in the product

[0005] 3. The temperature setting in the freeze-drying process of the traditional preparation process is too rough, without considering the physical properties of the product itself, resulting in the collapse of the product’s skeleton and freeze-dried microstructure, which affects production efficiency and resolubilization performance

[0006] In summary, the existing levocarnitine preparation process needs to be improved urgently