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Solidified andrographolide solution for oral administration, and preparation method of solidified andrographolide solution

A solidification technology of andrographolide, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of changing the pharmacokinetic characteristics, tissue distribution characteristics, and crystallization of the main drug. Or crystallization coarsening, irritating gastrointestinal mucosa, etc., to achieve the effect of simple and easy preparation method, improved stability and good fluidity

Active Publication Date: 2021-12-07
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these methods have their own defects. For example, some inclusion materials may change the pharmacokinetics and tissue distribution characteristics of the main drug to varying degrees, which may lead to safety and effectiveness issues; micronization makes the surface free energy increase, which accelerates the tendency of drug spontaneous aggregation and reduces the effect of micronization; after the solid dispersion is placed for a period of time, there will be aging phenomena such as drug dissolution rate reduction, crystallization or crystallization coarsening; emulsification technology is used more emulsifiers, which are expensive, irritating to the gastrointestinal mucosa, or chronically toxic to the whole body

Method used

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  • Solidified andrographolide solution for oral administration, and preparation method of solidified andrographolide solution
  • Solidified andrographolide solution for oral administration, and preparation method of solidified andrographolide solution
  • Solidified andrographolide solution for oral administration, and preparation method of solidified andrographolide solution

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-9

[0041] Solubility Determination of Andrographolide in Different Solvents

[0042] Add andrographolide to PEG 200, PEG 400, PEG 600, Transcutol P, 1,2-propanediol, absolute ethanol, NMP, dimethyl sulfoxide, and dimethylformamide respectively, and grind in a mortar for 15 minutes , divided into two EP tubes, respectively placed in 25°C and 50°C collector-type constant temperature heating magnetic stirrers for 24h, centrifuged at 2000rpm for 10min, took 5 drops of the supernatant and weighed them accurately, and diluted them with methanol properly. Amount of 10 μL was injected into a high-performance liquid chromatograph for determination, the peak area was recorded, and the solubility of andrographolide in different solvents was calculated. The details are shown in Table 1.

[0043] The solubility of table 1 andrographolide in different solvents

[0044]

[0045]

[0046] From the above results, it can be seen that absolute ethanol has a low boiling point and has volatil...

Embodiment 10-15

[0048] Different proportions of F127 solidified andrographolide solution

[0049] prescription

[0050] Andrographolide 0.1g

[0051] NMP 400 μL

[0052] F127 0.1~0.6g

[0053] Weigh 0.1 g of andrographolide, add 400 μL of NMP to dissolve it ultrasonically, then add different masses of F127, heat and stir at 65°C until it melts, stop heating and continue stirring until it cools and solidifies to obtain a solidified solution of andrographolide containing F127.

[0054] Table 3 Adding different proportions of F127 solidified andrographolide solution at room temperature

[0055] F127 added amount State of the obtained andrographolide solidified solution at room temperature Example 10 0.1g It is in a liquid state at room temperature, and does not meet the requirement of being a solid solution at room temperature. Example 11 0.2g It is in a liquid state at room temperature, and does not meet the requirement of being a solid solution at room temperat...

Embodiment 16-21

[0057] Different proportions of Compritol 888ATO solidified andrographolide solution

[0058] Prescription Andrographolide 0.1g

[0059] NMP 400 μL

[0060] Compritol 888ATO 0.1~0.6g

[0061] Weigh 0.1 g of andrographolide, add 400 μL of NMP to dissolve it ultrasonically, then add different masses of Compritol 888ATO, heat and stir at 65°C until it melts, stop heating and continue stirring until it cools and solidifies to obtain a solidified andrographolide solution containing Compritol 888ATO.

[0062] Table 4 Add different proportions of Compritol 888ATO to solidify andrographolide solution at room temperature

[0063]

[0064] Table 5 solidified andrographolide solution in vitro release results under non-sink conditions

[0065]

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Abstract

The invention relates to a solidified andrographolide solution for oral administration and a preparation method of the solidified andrographolide solution, and belongs to the technical field of pharmaceutical preparations. Andrographolide is dissolved in a proper organic solvent, a nonionic surfactant, a solid or semi-solid carrier material and a crystallization inhibitor are added, and the medicine-containing solid powder capable of remarkably improving the dissolution rate of the andrographolide is prepared after treatment of a porous adsorption material. According to the solidified andrographolide solution, the porous material is adopted to adsorb and solidify the liquid or semi-solid state transfer system, and the solidified solution can improve the stability of the medicine and improve the dissolution speed, the dissolution rate and the oral bioavailability of the medicine.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a solidized andrographolide solution for oral administration and a preparation method thereof. Background technique [0002] At present, improving the dissolution rate and bioavailability of poorly soluble drugs is a difficult problem in the field of pharmaceutical preparation research and pharmaceutical production. [0003] Andrographolide (An) is the main active ingredient of the traditional Chinese medicine Andrographis paniculata, belonging to diterpene lactone compounds, and its molecular formula is C 20 h 30 NO 5 , with a relative molecular mass of 350.44 and a melting point of 230-231°C. It is easily soluble in acetone, methanol, and ethanol, slightly soluble in chloroform and ether, and hardly soluble in water. [0004] Andrographolide is poorly soluble in water, resulting in slow drug absorption in the body, low bioavailability, and extremely bitter ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/365A61K47/10A61K47/14A61K47/26A61K47/36A61P31/04
CPCA61K31/365A61K9/146A61K9/145A61K9/0053A61K47/26A61K47/10A61K47/14A61K47/36A61P31/04Y02A50/30
Inventor 徐晖陈慧琳刘孟珂陈璐璐王绍宁
Owner SHENYANG PHARMA UNIVERSITY
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