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Chlorogenic acid composition and preparation method thereof

A technology of chlorogenic acid and composition, applied in the field of chlorogenic acid composition and preparation thereof, can solve the problems of limited clinical use of chlorogenic acid, inability to control pH value, poor stabilizer and the like

Active Publication Date: 2022-02-18
BEIJING COLLAB PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Prepared according to the existing patent CN103446064B, using sodium bisulfite as an antioxidant, mannitol as a proppant, and phosphate as a pH regulator, the stabilizer of the resulting preparation is poor
[0007] From the point of view of the prior art, due to the presence of strong acidic carboxylic acid structures in the chlorogenic acid structure and ester bonds that are prone to hydrolysis and loss of biological activity, in order to ensure the stability of chlorogenic acid and reduce irritation, the currently disclosed injection preparation technology only It can raise the pH to about 3.0, but cannot control the pH value to the range of 4.0-9.0, which is more tolerated by the human body
And preparation samples need to be stored and transported under dark and low temperature conditions, which greatly limits the clinical use of chlorogenic acid

Method used

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  • Chlorogenic acid composition and preparation method thereof
  • Chlorogenic acid composition and preparation method thereof
  • Chlorogenic acid composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0052] The freeze-dried powder composition includes chlorogenic acid and arginine, and the specific components are shown in the following table:

[0053]

[0054] Take 90% of the prescribed amount of water for injection, and cool to room temperature (25°C);

[0055] Add the raw and auxiliary materials in the prescription amount, stir well until they are completely dissolved, and replenish water to the full amount.

[0056] Sterilize by filtering through a 0.22μm filter membrane, fill 0.5ml / bottle into 2-3ml vials, and add freeze-dried stoppers.

[0057] Freeze-dry in a freeze dryer, pre-freeze at -40°C for 3 hours, vacuumize the system, raise the temperature to -20°C to start sublimation, and the sublimation drying time is about 8 hours; after most of the water is sublimated, increase the temperature of the plate layer and enter the second In the secondary drying stage, dry at 20°C for 6 hours; after the secondary drying, maintain a vacuum state and press the plug; the sys...

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Abstract

The present invention provides a new chlorogenic acid composition, which has the advantages of good stability at room temperature, high solubility, small reconstitution volume, and a pH value more tolerated by the human body, and is suitable for subcutaneous / intramuscular injection. medicine system. The preparation can better satisfy the safety during production, transportation and use, and provides a more effective drug delivery system composition for the clinical application of chlorogenic acid.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to a chlorogenic acid composition and a preparation method thereof. Background technique [0002] Chlorogenic acid (Chlorogenic acid), also known as coffee tannic acid or coffee tannic acid, is formed by condensation of caffeic acid and quinic acid (quinic acid, quinic acid). product of metabolism. The chemical name of chlorogenic acid is 5-O-caffeoylquinic acid (5-O-caffeoylquinic acid), molecular formula: C 16 h 18 o 9 , molecular weight: 354.31, and the structural formula is as follows. [0003] [0004] Chlorogenic acid is an important biologically active substance. The prior art discloses that it has various uses such as anti-oxidation, anti-aging, anti-musculoskeletal aging, anti-tumor, anti-inflammation, treatment of immune-related diseases, and protection of cardiovascular and cerebrovascular diseases. The oral bioavailability of chlorogenic a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K47/18A61K31/216A61P39/06A61P35/00A61P29/00A61P37/00A61P9/00
CPCA61K9/19A61K47/183A61K31/216A61P39/06A61P35/00A61P29/00A61P37/00A61P9/00
Inventor 陈先红邹德超沈璇邱敦有
Owner BEIJING COLLAB PHARMA
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