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A kind of liquid preparation of lipoic acid 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: 2018-04-13
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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  • A kind of liquid preparation of lipoic acid and preparation method thereof
  • A kind of liquid preparation of lipoic acid and preparation method thereof
  • A kind of liquid preparation of lipoic acid and preparation method thereof

Examples

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Comparison scheme
Effect test

Embodiment 1

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

[0034] Alpha Lipoic Acid 300g

[0035] Lysine 350g

[0036] Disodium hydrogen phosphate 25g

[0037] Phosphoric acid to adjust pH 8.0 to 8.5

[0038] The balance of water for injection is made up to 10L.

[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 filt...

Embodiment 2

[0044] Example 2 0.3g / 10mL per tube, 1000 tubes

[0045] Alpha Lipoic Acid 300g

[0046] Lysine 400g

[0047] Disodium hydrogen phosphate 25g

[0048] Phosphoric acid to adjust pH 8.0 to 8.5

[0049] D-Sorbitol 30g

[0050] The balance of water for injection is made up to 10L.

[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 fo...

Embodiment 3

[0056] Example 3 0.3g / 10mL per tube, 1000 tubes

[0057] R-lipoic acid 300g

[0058] Lysine 360g

[0059] Disodium hydrogen phosphate 24g

[0060] Phosphoric acid to adjust pH 8.1~8.3

[0061] D-Sorbitol 30g

[0062] The balance of water for injection is made up to 10L.

[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 inj...

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Abstract

The invention discloses a lipoic acid liquid preparation and a preparation method thereof. The preparation comprises lipoic acid as a main ingredient, a polymerization inhibitor lysine, and a pH regulator. The composition of the preparation is simple, but it can significantly improve the stability of the liquid medicine under high-temperature sterilization and strong light irradiation, and in particular can greatly reduce the generation of lipoic acid dimer impurities. By adding the auxiliary stabilizer D-sorbitol, the effect of stabilizing the quality of the medicinal solution is further enhanced. The invention strictly controls the preparation process of the injection, fills the liquid with nitrogen for protection in the whole process of liquid preparation, dissolution and potting, timely monitors the residual oxygen of the liquid, effectively controls the degradation of lipoic acid in the aqueous solution, and ensures the safety of clinical use. Safe and effective.

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] Alpha lipoic acid (alpha lipoic acid) is sulfur-containing octacarbonic acid, the chemical name is 1,2-dithiolane-3-pentanoic acid, it is an enzyme existing in mitochondria, similar to vitamins, it can eliminate accelerated aging and disease 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 preventive and ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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