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Application of natural polysaccharides in increasing solubility of indissolvable drugs

A technology of insoluble drugs and natural polysaccharides, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc. It can solve problems such as toxic side effects, high cost, and complicated process, and achieve low toxicity , easy to obtain, and simple to operate

Pending Publication Date: 2020-12-29
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0019] The object of the present invention is to overcome at least one deficiency such as toxic and side effects, complicated process, high cost, etc.

Method used

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  • Application of natural polysaccharides in increasing solubility of indissolvable drugs
  • Application of natural polysaccharides in increasing solubility of indissolvable drugs
  • Application of natural polysaccharides in increasing solubility of indissolvable drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] Embodiment 1 natural polysaccharide increases the solubility of rhein

[0084] Accurately weigh 2mg of rhein reference substance, add 2mg / mL pullulan, hyaluronic acid (1800KDa), hyaluronic acid (90KDa), hyaluronic acid (10KDa), hyaluronic acid (4KDa), xanthan Glue, locust bean gum, chondroitin sulfate, and heparin sodium polysaccharide solution were each 4 mL, mixed, heated in a water bath at 75°C for 30 min, vortexed for 30 s, left at room temperature for 20 min, and then centrifuged at 4000 rpm for 10 min, and the supernatant was obtained. Solubilized rhein solution. In addition, accurately weigh 2 mg of rhein reference substance, add 4 mL of ultrapure water, mix well, and operate according to the law. Measure the concentration of rhein in the sample by high performance liquid chromatography, calculate the solubility of rhein without adding natural polysaccharide (adding ultrapure water) and adding natural polysaccharide, the results are as shown in table 1: after ad...

Embodiment 2

[0088] Embodiment 2 natural polysaccharide increases the solubility of baicalin

[0089] Accurately weigh 2mg baicalin reference substance, add 2mg / mL pullulan, hyaluronic acid (1800KDa), hyaluronic acid (90KDa), hyaluronic acid (10KDa), hyaluronic acid (4KDa), xanthan gum 4 mL each of locust bean gum, chondroitin sulfate, and sodium heparin polysaccharide solution, mix well, and shake at a constant temperature of 100 rpm for 26 h at room temperature, then centrifuge at 4000 rpm for 10 min, and take the supernatant to obtain a baicalin solution solubilized by natural polysaccharides. In addition, accurately weigh 2 mg of baicalin reference substance, add 4 mL of ultrapure water, mix well, and operate according to the law. Measure the concentration of baicalin in the sample by high performance liquid chromatography, calculate the solubility of baicalin without adding natural polysaccharide (adding ultrapure water) and adding natural polysaccharide, the results are shown in Tabl...

Embodiment 3

[0092] Embodiment 3 natural polysaccharide increases the solubility of hydroxycamptothecin

[0093] Accurately weigh 2mg of hydroxycamptothecin, add 2mg / mL pullulan, hyaluronic acid (1800KDa), hyaluronic acid (90KDa), hyaluronic acid (10KDa), hyaluronic acid (4KDa), xanthan gum 4 mL each of locust bean gum, chondroitin sulfate, and heparin sodium polysaccharide solution, mixed evenly, heated in a water bath at 75°C for 30 min, vortexed for 30 s, left at room temperature for 20 min, and then centrifuged at 4000 rpm for 10 min. Soluble hydroxycamptothecin solution. In addition, accurately weigh 2 mg of hydroxycamptothecin, add 4 mL of ultrapure water, mix well, measure the concentration of hydroxycamptothecin in the sample by high performance liquid chromatography, and calculate the concentration of hydroxycamptothecin without adding natural polysaccharide (adding ultrapure water) and adding natural polysaccharide The solubility of hydroxycamptothecin, the results are shown in ...

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Abstract

The invention discloses an application of natural polysaccharides in increasing the solubility of indissolvable drugs. The indissolvable drugs are at least one of anthraquinone compounds, flavonoid compounds and alkaloids. The natural polysaccharides are at least one of Pulullan, hyaluronic acid, xanthan gum, locust bean gum, chondroitin sulfate and heparin sodium. According to the invention, a natural polysaccharide solution and the indissolvable drugs are uniformly mixed, heated or oscillated, so that the purpose of increasing the solubility of the indissolvable drugs can be achieved, and hyaluronic acids with different molecular weights have different solubilizing effects. The natural polysaccharide solubilizing method is simple to operate, and structural modification does not need to be performed, so that the use of organic reagents is avoided; and the natural polysaccharides are wide in source and easy to obtain, so that the preparation cost can be reduced. Meanwhile, all the natural polysaccharides are clear in structure, low in toxicity, good in biocompatibility, degradable and environmentally friendly, and have development prospects of serving as functional auxiliary materials with the solubilizing effect.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to the application of natural polysaccharides in increasing the solubility of poorly soluble medicines. Background technique [0002] Traditional Chinese medicine is an important part of Chinese medicine research in my country. Many active active ingredients or active monomers are extracted and separated from traditional Chinese medicine, which have good curative effect on corresponding diseases. However, the water solubility of many active ingredients of Chinese medicine is poor, resulting in oral Poor post bioavailability affects the performance and application of clinical curative effect, and limits the development of traditional Chinese medicine preparations. For example, rhein, baicalin and hydroxycamptothecin are all insoluble drugs. [0003] Rhein (1,8-dihydroxy-3-carboxyanthraquinone) is an anthraquinone component extracted and isolated from legumes and Polygon...

Claims

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Application Information

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IPC IPC(8): A61K47/36A61K31/192A61K31/7048A61K31/4745
CPCA61K47/36A61K31/192A61K31/7048A61K31/4745
Inventor 胡巧红
Owner GUANGDONG PHARMA UNIV
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