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Formula for improving water-solubility of armillarisin and its preparation

A leucectin A, water-soluble technology, applied in antiviral agents, drug combinations, digestive system, etc., can solve the problems of coprecipitate aging, poor long-term storage stability, organic solvent allergies, etc., achieve stability improvement, in vitro Improvement of dissolution rate and improvement of water solubility

Inactive Publication Date: 2003-05-07
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These organic solvents will have adverse reactions to the human body, and some patients are allergic to organic solvents, which limits their clinical application
In addition, the Tween 80 in the prescription is hemolytic, and its application in intravenous injections has been limited or even banned at present.
In order to improve the water solubility of leucicillin A, some authors made polyvinylpyrrolidone (PVP) co-precipitates, but the co-precipitates made by using the optimal ratio (1:5) in the literature, the solubility in water is only 249.97ug / ml (Guo Jianlan et al. Improve the solubility of Leucectin A by co-precipitation method Pharmaceutical Bulletin 1986, 21 (5): 261, 263); At the same time, there is an "aging" problem in the coprecipitate, and the long-term storage stability is poor

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0008] Example 1: Preparation of leucectin A β-cyclodextrin inclusion complex (1mol: 1mol)

[0009] prescription:

[0010] Leucicillin A 2.34g (10mmol)

[0011] β-cyclodextrin 22.7g (20mmol)

[0012] Proper amount of ethanol

[0013] Appropriate amount of distilled water

[0014] Preparation Process:

[0015] Weigh the prescribed amount of β-cyclodextrin and leucectin A, put them in a beaker, add appropriate amount of ethanol and water, heat and stir to dissolve, cool to room temperature, and filter to obtain a solution. The obtained solution is vacuum-dried to obtain leucectin A β-cyclodextrin inclusion compound powder. The powder was subjected to X-diffraction examination, and the crystal diffraction peak of leucicillin A disappeared, while the X- In the diffraction pattern, obvious crystal diffraction peaks can be seen.

Embodiment 2

[0016] Example 2: Leucidin A 2-hydroxypropyl β-cyclodextrin inclusion complex (1mol: 2mol)

[0017] prescription:

[0018] Leucicillin A 2.34g (10mmol)

[0019] 2-Hydroxypropyl β-cyclodextrin 27.6g (20mmol)

[0020] Proper amount of ethanol

[0021] Appropriate amount of distilled water

[0022] Preparation Process:

[0023] Weigh the prescribed amount of 2-hydroxypropyl β-cyclodextrin and dissolve it with an appropriate amount (about 50ml) of distilled water; take another weighed prescribed amount of leucectin A, dissolve it in an appropriate amount of ethanol, and add the above-mentioned 2-hydroxypropyl β-cyclodextrin under stirring. β-cyclodextrin aqueous solution was filtered to obtain a solution. The resulting solution was freeze-dried to obtain a light yellow powder. The powder was subjected to X-diffraction inspection, and the crystal diffraction peak of leucicillin A disappeared, while leucicillin A and 2-hydroxypropyl β-cyclodextrin without cladding with 2-hydro...

Embodiment 3

[0024] Example 3: Weigh β-cyclodextrin and leucectin A according to the ratio of 3 mol: 1 mol, and place them in a beaker. The remaining operations are the same as in "Example 1", and the drying method is "spray drying". The X-ray diffractogram indicated the formation of clathrates.

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Abstract

A process for increasing the water solubility of leucocodin A features that the leucocidin A is mixed with beta-cyclodextrin or 2-hydroxypropyl beta-cyclo dextrin in the ratio of 1:(1-10) to obtain their inclusion compound "leucocidin A-beta cyclodextrin" or "leucocodin A-2 hydroxypropyl beta-cyclodextrin". Its advantages are high safety and high stability.

Description

Technical field: [0001] The present invention relates to the technical field of medicine, specifically, it utilizes β-cyclodextrin or 2-hydroxypropyl β-cyclodextrin to form an inclusion compound with leucidin A or adds β-cyclodextrin or 2-hydroxy Propyl β-cyclodextrin is used to improve the solubility of leucectin A in water to make efficient oral preparations or injections without organic solvents and Tween-80, which can improve curative effect and reduce side effects. Background technique: [0002] Leucicillin A can be extracted from Leucobacterium genus Pseudoarmillaria, or it can be synthesized artificially. Its properties are yellow or light yellow needle-like or crystalline powder. It has the effect of promoting bile secretion and has obvious effects on the 0ddis sphincter. Antispasmodic effect. In addition, it may still promote immune function and enhance the phagocytosis of phagocytes, it can also reduce the activity of serum transaminases, and it can still decompos...

Claims

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Application Information

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IPC IPC(8): A61K31/366A61P1/04A61P1/16A61P31/12
Inventor 邓意辉
Owner SHENYANG PHARMA UNIVERSITY
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