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Nanometer emulsion oral liquid of andrographolide and its prepn process

A technology of andrographolide and oral emulsion, applied in the field of medicine, can solve the problems of reducing the pharmacological activity of andrographolide, large individual differences in drug absorption, and insoluble in water of andrographolide, etc. The effect of improved visual quality and high thermodynamic stability

Inactive Publication Date: 2007-03-21
NORTHWEST A & F UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Andrographolide is insoluble in water, and its dissolution rate in vitro is poor. At present, various andrographolide salt preparations are prepared by chemical structure modification. Most of them are solid preparations, and there are few liquid preparations.
These changes in chemical structure reduce the pharmacological activity of andrographolide and increase the toxic and side effects of the drug
Moreover, after oral administration of solid preparations, the absorption of drugs varies greatly among individuals, and the bioavailability fluctuates greatly, which affects the efficacy of the drug.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Use the oil selected by calculating the HLB value, surfactant, and co-surfactant to draw a pseudo-ternary phase diagram according to the rule of 9:1 to 1:9 to determine the optimal ratio. Accurately weigh 1.4g of Tween-80, 0.7g of Span-80, and 0.48g of ethanol (containing 0.012g of andrographolide), put them into a beaker, and mix them thoroughly by manual stirring at room temperature of 20°C. Then add 0.9 g of liquid paraffin to the mixture, mix it well, then slowly add distilled water to it, and stir manually while adding distilled water. At the beginning, the viscosity of the system is small, and as the amount of distilled water increases, the system will become viscous. When the system may appear liquid crystal or water-in-oil nanoemulsion, continue to drop and stir continuously. When the system suddenly becomes thinner, the light yellow transparent oil-in-water type andrographolide nanoemulsion oral liquid will be produced at this time. Its total weight is said to ...

Embodiment 2

[0052] Use the oil selected by calculating the HLB value, surfactant, and co-surfactant to draw a pseudo-ternary phase diagram according to the rule of 9:1 to 1:9 to determine the optimal ratio. Accurately weigh 4.5g of hydrogenated castor oil polyoxyethylene ether, 0.5g of olive oil, and 0.6g of ethanol (which contains 0.05g of andrographolide), put them into a beaker, and mix them thoroughly by manual stirring at room temperature of 25°C. Then slowly add distilled water to it, and stir manually while adding distilled water. At the beginning, the viscosity of the system is small. As the amount of distilled water increases, the system will become viscous. At this time, the system may appear liquid crystal or water-in-oil nanoemulsion. Continue Add dropwise and constantly stir, when the system suddenly becomes thinner, what obtains now is the colorless transparent oil-in-water type andrographolide nanoemulsion oral liquid, claiming that its total weight is 11.00g.

Embodiment 3

[0054] Use the oil selected by calculating the HLB value, surfactant, and co-surfactant to draw a pseudo-ternary phase diagram according to the rule of 9:1 to 1:9 to determine the optimal ratio. Accurately weigh 3.0 g of polyoxyethylene castor oil, 1.0 g of 1,3-butanediol (which contains 0.07 g of andrographolide), put it into a beaker, and under the room temperature condition of 24 ℃, manually stir it to fully mix it, and then Add 0.44g of isopropyl myristate to the mixture, mix it well, then slowly add distilled water to it, and stir manually while adding distilled water. At the beginning, the viscosity of the system is small. As the amount of distilled water increases, the system will become viscous At this time, the system may appear liquid crystal or water-in-oil nanoemulsion, continue to drop and stir continuously, when the system suddenly becomes thinner, what is produced at this time is colorless and transparent oil-in-water type andrographolide nanoemulsion oral liquid...

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PUM

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Abstract

The nanometer emulsion oral liquid of andrographolide consists of surfactant, oil, andrographolide and distilled water. Its preparation process includes the following steps:weighing surfactant with or without co-surfactant; calculating HLB value and selecting oil for reaching emulsifying HLB value near that of the surfactant phase; changing the ratio between the surfactant phase and the oil phase regularly to dissolve andrographolide in the surfactant; adding distilled water slowly at 20-25 deg.c to form clear and flowing O / W type stable nanometer emulsion oral liquid. The nanometer emulsion oral liquid has high dissolubility of andrographolide, raised bioavailability of andrographolide, less stimulation to gastrointestinal tract and raised patient's compliance, and may be also taken easily by children and persons with dysphagia.

Description

technical field [0001] The invention belongs to the field of medicine and relates to a new dosage form of an antibiotic drug, in particular to a transparent and stable oil-in-water type andrographolide nanoemulsion oral liquid and a preparation method thereof. Background technique [0002] Andrographolide is a diterpene lactone compound extracted from Andrographis paniculata. It is one of the main active ingredients of Andrographis paniculata. It has the functions of clearing heat and detoxification, cooling blood and reducing swelling. Modern pharmacological studies have shown that andrographolide has anti-inflammatory, antibacterial, antiviral, immune regulation, treatment of cardiovascular diseases, liver protection and choleretic effects. Due to its definite curative effect and no drug resistance, andrographolide is known as a natural antibiotic, and its clinical application is becoming more and more extensive. [0003] Andrographolide is insoluble in water, and its dis...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/365A61K47/44A61P31/04A61P31/12A61P11/00
Inventor 欧阳五庆吴旭锦
Owner NORTHWEST A & F UNIV
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