Preparation method of levocarnitine composition for injection and liposome injection thereof

A composition and technology for injection, which is applied in the preparation of levocarnitine composition for injection and in the field of liposome injection, which can solve the problem of easy discoloration of levocarnitine, influence on drug efficacy, rough temperature setting in freeze-drying process, etc. problem, to achieve the effect of stable microstructure, good safety and good resolubility of the finished product

Active Publication Date: 2022-01-28
HAINAN GENERAL & KANGLI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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

Method used

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Effect test

preparation example Construction

[0037] Because in the existing preparation process, after mixing levocarnitine and freeze-dried proppant in the solution, and then adjusting the pH of the mixed solution system, there are many defects in this method: 1. Adding hydrochloric acid dropwise will easily lead to uneven distribution of pH in the solution system, resulting in low product quality; 2. After mixing levocarnitine and freeze-dried proppant, the solution will be in a colloidal state, which is not easy to stir, and the acid-base adjustment control process consumes Labor cost and time cost; 3. The pH of the solution during the acid-base adjustment process changes drastically, and the semi-finished product is easily degraded in this environment.

[0038] The method of the present invention to solve this problem is: prepare the buffer in advance, and then dissolve levocarnitine and freeze-dried proppant in the buffer. The inventor has verified through a large number of comparative experiments: the concentration ...

Embodiment 1

[0065] Step S1: using sodium dihydrogen phosphate and sodium hydroxide solution with a volume ratio of 10:1 to prepare an acid-base buffer solution, wherein the molar concentration of the acid-base buffer solution is 0.010 mol / L;

[0066] Step S2: Add fructose diphosphate sodium and levocarnitine injection into the acid-base buffer solution, wherein the mass ratio of fructose diphosphate sodium to levocarnitine is 1.0:1, and the mass concentration of levocarnitine is 18 / L, control the system temperature of the mixed solution between 55-65 degrees Celsius, and the pH between 5.9-6.2;

[0067] Step S3: Add activated carbon for needles with a mass concentration of 0.1 g / L, stir evenly, and stir for adsorption for 30 minutes;

[0068] Step S4: Ultrasonic filtration of activated carbon;

[0069] Step S5: Take a small amount of semi-finished products to be vacuum freeze-dried, and determine the eutectic point by monitoring the freeze-drying curve; and determine the eutectic point ...

Embodiment 2

[0076] Embodiment 2: same as embodiment 1, the only difference is that the molar concentration of the acid-base buffer solution is 0.012 mol / L.

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PUM

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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 ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K9/127A61K47/02A61K47/26A61K31/205A61P3/00A61P3/06A61P9/10A61P9/06A61P9/04
CPCA61K9/19A61K9/0019A61K9/127A61K47/02A61K47/26A61K31/205A61P3/00A61P3/06A61P9/10A61P9/06A61P9/04
Inventor 杨杰吴玉章钟海雄林小雪符永红王静
Owner HAINAN GENERAL & KANGLI PHARMA
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