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A composition containing polydatin and its application

A technology of polydatin and composition, which is applied in the field of polydatin-containing compositions, can solve problems such as limited solubility, difficulty in reaching the drug concentration in conventional aqueous solutions, and no further explanation on the feasible preparation method of the solution, and achieve low toxicity, good water solubility, Response to the effect of a narrow temperature range

Active Publication Date: 2022-03-22
HUNAN NUSTREETCARAX
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Chinese patent application CN1709269A points out: in the research literature of polydatin basic pharmacology, in human experiment research, adopt intravenous route to give polydatin more, test sample adopts water or physiological saline to prepare polydatin solution of 2-5mg / mL concentration more, but literature There is no further explanation on the feasible preparation method of the solution; according to literature calculations, the clinical effective dose of polydatin (for adults) should be above 112mg / time, and under the specifications of 1-20mL conventional injections, the concentration of polydatin in clinical injections should not be lower than 5.6mg / mL; the solubility of polydatin in pure water or normal saline solution is limited, and its conventional aqueous solution is difficult to reach the drug concentration described in the literature: at room temperature, the saturation concentration of polydatin in water and normal saline is lower than 0.5 mg / mL, much lower than the above-mentioned 2-5mg / mL administration concentration
It can be seen that ethanol and / or propylene glycol are used as organic solvents in this patent to increase the solubility of polydatin, and the formed composition contains a large amount of organic solvents, which limits the application of polydatin to a certain extent, and can only be injected with water or physiologically. Saline can be used in human body only after being diluted to a certain extent

Method used

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  • A composition containing polydatin and its application
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  • A composition containing polydatin and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Composite hydrogels are made through the following steps:

[0029] Step 1, add 30wt% sodium hydroxide aqueous solution in chitosan, after stirring at 300r / min for 45min, the mixture is placed in a freezer, frozen at -23°C for 20h, then the frozen mixture is taken out, and placed in Thaw in the oven, then put the thawed mixture back into the three-necked flask, add isopropanol, stir at 300r / min for 30min, then add the isopropanol solution of chloroacetic acid drop by drop to keep the temperature of the reaction system below 8°C , after the dropwise addition, continue to react for 20h, then filter the reaction mixture, wash the filter cake with deionized water, centrifuge, take the filter cake, then fully dialyze with deionized water, freeze-dry the dialyzate, and obtain carboxymethyl Base chitosan, wherein, the amount ratio of chitosan, 30% sodium hydroxide aqueous solution, isopropanol, chloroacetic acid isopropanol solution is 1g: 4mL: 10mL: 4g, and in the isopropanol ...

Embodiment 2

[0032] Composite hydrogel is made through the following steps: with reference to each step in embodiment 1; In step one, the consumption ratio of the isopropanol solution of chitosan, 30% sodium hydroxide aqueous solution, isopropanol, chloroacetic acid is 1g: 6mL: 15mL: 5g, and the mass fraction of chloroacetic acid in the isopropanol solution of chloroacetic acid is 45%; in step 2, silk fibroin, poloxamer, deionized water, p-toluenesulfonic acid, carboxymethyl shell The dosage ratio of the polysan aqueous solution is 12mg: 100mg: 10mL: 2.5mL: 60mg, and the mass fraction of the carboxymethyl chitosan aqueous solution is 40%, and the poloxamer is P407.

Embodiment 3

[0041] A composition containing polydatin, each raw material is weighed according to the formula in Table 1:

[0042] Table 1

[0043] raw material Dosage The ethanol solution of polydatin (mass concentration is 60%) 0.5g Composite hydrogel is prepared for embodiment 1 2g normal saline 10mL Sodium carbonate-sodium bicarbonate buffer solution Adjust the pH of the solution to 8.0

[0044] Preparation method: Use physiological saline as a solvent, immerse the composite hydrogel in the solvent, add polydatin ethanol solution, add sodium carbonate-sodium bicarbonate buffer solution, stir at 200r / min for 20min at 37°C, and then place in Stand at constant temperature in a fume hood for 12 hours, remove absolute ethanol, and obtain a polydatin composition.

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Abstract

The invention discloses a composition containing polydatin and its application, which belongs to the technical field of polydatin application and aims to solve the technical problem of the limited solubility of polydatin in pure water or physiological saline solution. And this kind of polydatin-containing composition adopts composite hydrogel as loading agent, improves the solubility of polydatin in aqueous solution or saline solution, and makes it meet the needs of clinical medicine of polydatin; and the composite hydrogel utilizes Poloxamer has the property of reverse reversible thermal gelation, and the introduction of silk fibroin and carboxymethyl chitosan utilizes the carboxyl group on carboxymethyl chitosan to combine with the amino group on silk fibroin and poloxamer The hydroxyl group on the hydrogel reacts to form an interpenetrating network in the composite gel system, which improves the mechanical strength of the composite hydrogel, and there are hydrophilic segments of silk fibroin and poloxamer in the entire gel system, making the gel ‑Sol transition temperature tends to body temperature, suitable for human administration.

Description

technical field [0001] The invention belongs to the technical field of polydatin application, and in particular relates to a composition containing polydatin and its application. Background technique [0002] Polydatin, namely 3,4', 5-trihydroxystilbene-3-β-D-glucoside (C20H22O8) as a medicinal ingredient can be found in literature and patent reports. Circulation, hypolipidemic, anti-tumor and other pharmacological activities. [0003] Chinese patent application CN1709269A points out: in the research literature of polydatin basic pharmacology, in human experiment research, adopt intravenous route to give polydatin more, test sample adopts water or physiological saline to prepare polydatin solution of 2-5mg / mL concentration more, but literature There is no further explanation on the feasible preparation method of the solution; according to literature calculations, the clinical effective dose of polydatin (for adults) should be above 112mg / time, and under the specifications o...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/06A61K9/70A61K31/7034A61K47/26A61K47/36A61K47/42A61K47/20A61P17/02A61P17/16
CPCA61K31/7034A61K9/06A61K47/36A61K47/42A61K47/26A61K9/0019A61K9/0014A61K9/7015A61P17/02A61P17/16A61K47/20
Inventor 张建张宝堂谭家忠尹振华王会文
Owner HUNAN NUSTREETCARAX
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