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Lipoic acid liquid preparation and preparation method thereof

A technology of liquid preparations and lipoic acid, which is applied in the field of medicine, can solve the problems of increasing the risk of adverse reactions and clinical medication, low content of lipoic acid injection, and unsatisfactory stability effects, etc., to achieve faster dissolution and environmental tolerance Good resistance, prevent degradation and deterioration

Active Publication Date: 2015-12-09
NANJING HERON PHARM CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, German EP0318891 disclosed a kind of lipoic acid injection in 1992, its prescription is to mix with tromethamine and arginine, the defective of this injection is that arginine consumption is very large, and mole fraction accounts for 30%, unit mole The amount of lipoic acid injection is relatively low, resulting in the need to increase the amount of clinical use, and the stability effect is not satisfactory
Chinese patent application CN200510025601 discloses a lipoic acid freeze-dried powder injection, which changes the injection into a freeze-dried powder injection, but makes the preparation process more complicated and increases the production cost
[0008] Lipoic acid in aqueous solution can generate free radicals under the catalysis of light and strong high temperature, and the free radicals connect with each other to form dimer impurities. The insoluble dimer impurities increase the risk of adverse reactions and clinical medication. Quality control of this dimer impurity is rarely reported in the literature

Method used

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  • Lipoic acid liquid preparation and preparation method thereof
  • Lipoic acid liquid preparation and preparation method thereof
  • Lipoic acid liquid preparation and preparation method thereof

Examples

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Effect test

Embodiment 1

[0033]Example 1 Each 0.3g / 10mL, 1000

[0034] Lipoic Acid 300g

[0035] Lysine 350g

[0036] Disodium hydrogen phosphate 25g

[0037] Phosphoric acid to adjust pH8.0~8.5

[0038] Make up to 10L the remaining amount of water for injection.

[0039] Preparation:

[0040] 1) Mix lipoic acid and lysine in a blender evenly, set aside;

[0041] 2) Fill the liquid mixing tank with nitrogen saturation for 10-20 minutes, then add 70% of the prescription water for injection, add disodium hydrogen phosphate and stir to dissolve, control the temperature at 35-40°C, and then inject nitrogen saturation, Control the residual oxygen to be less than 2%;

[0042] 3) Add the mixture of lipoic acid and lysine in step 1 under stirring, after it is completely dissolved, add 0.1mol / L phosphoric acid dropwise to adjust the pH value to 8.0-8.5, add medicinal activated carbon and stir for 15 minutes, decarburize, Make up the water for injection to the full amount;

[0043] 4) After fine filtrat...

Embodiment 2

[0044] Example 2 Each 0.3g / 10mL, 1000

[0045] Lipoic Acid 300g

[0046] Lysine 400g

[0047] Disodium hydrogen phosphate 25g

[0048] Phosphoric acid to adjust pH8.0~8.5

[0049] D-Sorbitol 30g

[0050] Make up to 10L the remaining amount of water for injection.

[0051] Preparation:

[0052] 1) Mix lipoic acid and lysine in a blender evenly, set aside;

[0053] 2) Fill the liquid mixing tank with nitrogen saturation for 10-20 minutes, then add 70% of the prescription amount of water for injection, add disodium hydrogen phosphate and D-sorbitol and stir to dissolve, control the temperature at 35-40°C, and then add Saturated with nitrogen, control the residual oxygen to less than 2%;

[0054] 3) Add the mixture of lipoic acid and lysine in step 1 under stirring, after it is completely dissolved, add 0.1mol / L phosphoric acid dropwise to adjust the pH value to 8.1-8.3, add medicinal activated carbon and stir for 15 minutes, decarburize, Make up the water for injection ...

Embodiment 3

[0056] Example 3 Each 0.3g / 10mL, 1000

[0057] D-lipoic acid 300g

[0058] Lysine 360g

[0059] Disodium hydrogen phosphate 24g

[0060] Phosphoric acid to adjust pH8.1~8.3

[0061] D-Sorbitol 30g

[0062] Make up to 10L the remaining amount of water for injection.

[0063] Preparation:

[0064] 1) Mix D-lipoic acid and lysine in a blender evenly, set aside;

[0065] 2) Fill the liquid mixing tank with nitrogen saturation for 10-20 minutes, then add 70% of the prescription amount of water for injection, add disodium hydrogen phosphate and D-sorbitol and stir to dissolve, control the temperature at 35-40°C, and then add Saturated with nitrogen, control the residual oxygen to less than 2%;

[0066] 3) Add the mixture of D-lipoic acid and lysine in step 1 under stirring, after it is completely dissolved, add 0.1mol / L phosphoric acid dropwise to adjust the pH value to 8.1-8.3, add medicinal activated carbon and stir for 15 minutes, remove Carbon, make up water for inject...

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Abstract

The invention discloses a lipoic acid liquid preparation and a preparation method thereof. The lipoic acid liquid preparation comprises main lipoic-acid ingredients, polymerization inhibitor lysine and a pH (potential of hydrogen) modifier. Though simple in component, the preparation can obviously improve stability of liquid medicine under high-temperature sterilization and high-light exposure, and generation of impurities of lipoic acid dimmers can be particularly greatly lowered. The effect of stabilizing the quality of the liquid medicine is further enhanced by adding an auxiliary stabilizer D-sorbitol. The preparation technology of injection is strictly controlled by performing entire nitrogen protection during liquid dosing, dissolution and potting and timely monitoring the oxygen volume of the liquid medicine, degradation of lipoic acid in water solution is effectively controlled, and the lipoic acid liquid preparation is ensured to be safe and effective in clinical application.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a liquid preparation of lipoic acid, in particular to an injection with stable quality and a preparation method thereof. Background technique [0002] Alphalipoic acid (alphalipoicacid) is a sulfur-containing octacarbonic acid, chemically named 1,2-dithiolane-3-pentanoic acid. It is an enzyme that exists in mitochondria, similar to vitamins, and can eliminate aging and disease-causing substances. free radicals. At present, lipoic acid is widely used in the treatment of diabetic neuropathy. In vitro tests show that this product can reduce lipid oxidation in nerve tissue, prevent protein glycosylation, and inhibit aldose reductase, thus preventing glucose or Galactose is converted into sorbitol, so lipoic acid can prevent diabetes, control blood sugar, and prevent neuropathy caused by high blood sugar. In recent years, a number of studies have found that lipoic acid has preventi...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/385A61K47/18A61K47/26A61K47/02A61K47/04A61P3/10A61P25/00A61P39/02
Inventor 晁阳包玉胜柏丹丹曹卫魏丹徐丽李晶晶
Owner NANJING HERON PHARM CO LTD
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