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Method for preparing andrographolide solid dispersion

A technology of andrographolide and solid dispersion, which is applied in the direction of medical preparations containing active ingredients, pharmaceutical formulas, organic active ingredients, etc., and can solve the problem of poor thermal stability of polyethylene glycol-based solid dispersions and difficulty in regrinding , drug dissolution rate decline and other issues, to achieve the effect of being suitable for large-scale production, reducing the loss of pharmacological activity, and low temperature in the preparation process

Inactive Publication Date: 2009-05-20
TIANJIN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] The polyethylene glycol matrix solid dispersion prepared by the melting method has a certain loss of pharmacological activity in the preparation process for heat-sensitive drugs such as andrographolide (easy to inactivate above 80°C), and the polyethylene glycol matrix solid dispersion In addition, the thermal stability of andrographolide-polyethylene glycol matrix solid dispersion is relatively soft, so it is not easy to grind again, and the prepared polyethylene glycol matrix solid dispersion powder is also easy to aggregate into agglomerates. Ethylene glycol matrix solid dispersion tends to form a drug-rich surface layer when polyethylene glycol dissolves, which hinders further erosion of the matrix, resulting in a decrease in the dissolution rate of the drug

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  • Method for preparing andrographolide solid dispersion
  • Method for preparing andrographolide solid dispersion

Examples

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Embodiment 1

[0022] A preparation method of a solid dispersion of andrographolide, comprising the following steps:

[0023] (1) 5g andrographolide, 35g polyvinylpyrrolidone k30, 7.5g Tween 80 are dissolved in 250ml absolute ethanol;

[0024] (2) The mixture obtained in step (1) was heated in a water bath at 45° C. to vacuumize to obtain a viscous substance, which was dried to a constant weight and pulverized to obtain a solid dispersion powder of andrographolide.

[0025] Andrographolide (Andro) bulk drug (over 80 mesh), PVPk30, Tween 80, the physical mixture of bulk drug and carrier and the X-ray diffraction curve of Andro solid dispersion are as shown in Figure 1. It can be seen from curve 5 in Figure 1 that the Andro API has a very strong crystal diffraction peak at 17°-18°. However, the diffraction pattern (curve 2) of the carrier PVPk30 has only two very weak diffuse peaks, indicating that the carrier PVPk30 exists in a microcrystalline or amorphous state. In addition, because the d...

Embodiment 2

[0028] Three andrographolide solid dispersions with different PVPk30 contents were prepared.

[0029] The first part: take 5gAndro, 7.5g Tween 80 and 25g PVPk30;

[0030] The second part: take 5gAndro, 7.5g Tween 80 and 35g PVPk30;

[0031] The third part: Take 5g Andro, 7.5g Tween 80 and 45g PVPk30, dissolve the above three parts in three parts of 250ml absolute ethanol respectively, heat the obtained three parts in a water bath at 45°C, and vacuumize most of the free Evaporate the water and ethanol to obtain a viscous substance, pour it into a watch glass, put it in a drying oven, and dry it for several days, then crush the dried solid dispersion and grind it to 80 meshes to obtain three Andro solid dispersions with different PVPk30 contents. body powder. Their release curves with Andro bulk drug and PEG carrier Andro preparation (Andro dropping pills) in simulated gastric juice (pH=1 hydrochloric acid: dehydrated alcohol=65:35) are as follows: image 3 . Depend on ima...

Embodiment 3

[0033]5gAndro, 45g PVPk30, 5g Tween 80 were dissolved in 250ml absolute ethanol, and the resulting mixture was spray-dried at 60°C to directly obtain white Andro solid dispersion powder, which was dissolved in simulated gastric juice (pH=1 hydrochloric acid: absolute ethanol =65:35) the cumulative dissolution rate reached 100% in 5 minutes.

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Abstract

The invention discloses a method for preparing a solid dispersion of andrographolidume. The method comprises the following steps: (1) mixing the andrographolidume, kollidon k30 and tween 80 according to the weight ratio of 1 to 5-9 to 0.5-1.5 to obtain a mixture 1, and adding the mixture to absolute ethanol to completely dissolve the mixture 1 to obtain a mixture 2; and (2) heating and vacuumizing the mixture 2 obtained from the step (1) in a water bath at a temperature of between 40 and 70 DEG C to obtain a sticky substance, drying the sticky substance until constant weight, and crushing the dried substance to obtain solid dispersion powder of the andrographolidume. The preparation process at low temperature reduces loss of pharmacological activity of the andrographolidume, and improves the dispersion degree of the andrographolidume in a solid dispersion carrier, thereby further improving dissolution of a medicine; and the prepared solid dispersion has high hardness and good thermal stability, and can be further conveniently prepared into dispersing tablets, capsules and other formulations.

Description

technical field [0001] The invention relates to a preparation method of andrographolide solid dispersion, which belongs to the improvement of the dosage form of oral andrographolide preparations. Background technique [0002] Andrographolide (Andro) is a diterpene lactone compound extracted from the plant Andrographis paniculata of the Acanthaceae family, and is one of the main active ingredients of the traditional Chinese medicine Andrographis paniculata. Modern pharmacological studies have shown that andrographolide has the functions of clearing heat and detoxification, cooling blood and reducing swelling, anti-inflammatory and antibacterial, anti-virus and anti-tumor, and is known as an anti-inflammatory drug in traditional Chinese medicine. [0003] Andrographolide is insoluble in water and other aqueous media, so the dissolution rate of the drug in the body is low, making the bioavailability also low. Solid dispersion technology is one of the effective methods to impro...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/365A61P29/00A61P31/00A61P35/00
Inventor 王康赵彤何志敏
Owner TIANJIN UNIV
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