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Glucan inclusion compound of water-insoluble small molecule drug and preparation method thereof

A water-insoluble and dextran technology, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, can solve problems such as low bioavailability and poor inclusion effect, and achieve Improve the solubility and solubilization, the preparation method is simple, and the effect of reducing stomach irritation

Inactive Publication Date: 2014-05-21
CHONGQING ACAD OF CHINESE MATERIA MEDICA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In view of this, the present invention provides a dextran inclusion compound of an insoluble water-soluble small molecule drug and a preparation method thereof to overcome the defects of poor inclusion effect and low bioavailability in the prior art, thereby providing a A formulation method to solve the low solubility, high toxicity and side effects, and low bioavailability of insoluble drugs and a new formulation for developing insoluble drugs

Method used

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  • Glucan inclusion compound of water-insoluble small molecule drug and preparation method thereof
  • Glucan inclusion compound of water-insoluble small molecule drug and preparation method thereof
  • Glucan inclusion compound of water-insoluble small molecule drug and preparation method thereof

Examples

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Comparison scheme
Effect test

Embodiment 1

[0036] Example 1 Preparation of chrysophanol-β-glucan inclusion compound

[0037] Add 1 g of chrysophanol to 3.0 mL of ethanol, add water to dilute to 10 mL, and obtain a clear chrysophanol solution. Under the condition of stirring and heating, completely dissolve the β-glucan, adjust the pH to 6.5, and add the chrysophanol solution to the dextran solution at 80°C, keep it for 30 minutes, and then evaporate the organic solution to obtain the aqueous solution. compound. After the synthesis reaction between chrysophanol and β-glucan, cool down, centrifuge at 14000r / min in a tube centrifuge to remove insoluble matter, ultrafilter with an ultrafiltration membrane with a molecular weight cut-off of 50000Dalton, and vacuum dry or spray dry at 60°C. Chrysophanol-β-glucan clathrate was obtained.

Embodiment 2

[0038] Example 2 Preparation of quercetin-β-glucan inclusion compound

[0039] Take 0.9g of quercetin, add 2mL of ethyl acetate, add water to dilute to 8mL, and stir for 10min to obtain a clear quercetin solution. Under the condition of stirring and heating, completely dissolve the β-glucan, adjust the pH to 5.5, and add the quercetin solution to the glucan solution at 90°C, keep it for 10 minutes, and then evaporate the organic solution to obtain the aqueous solution. clathrate. After the synthetic reaction between quercetin and β-glucan, cool down, centrifuge at 10,000r / min in a tube centrifuge, remove insoluble matter, ultrafilter with an ultrafiltration membrane with a molecular weight cut-off of 6000Dalton, freeze-dry or spray-dry to obtain quercetin Vein-β-glucan inclusion complex.

Embodiment 3

[0040] Example 3 Preparation of Coptisine-β-glucan Inclusion Compound

[0041] Take 0.9g coptisine, add 2mL dimethyl sulfoxide, add water to dilute to 8mL, stir for 10min to obtain a clear solution of coptisine. Under the condition of stirring and heating, completely dissolve the β-glucan, adjust the pH to 10, and the temperature is at 50°C, add coptisine solution to the dextran solution, and keep it for 100 minutes, after which the organic solution is evaporated to obtain an aqueous solution. compound. After the synthetic reaction of coptisine and β-glucan, cool down, centrifuge at 10,000r / min in a tube centrifuge to remove insoluble matter, ultrafilter with an ultrafiltration membrane with a molecular weight cut-off of 15,000Dalton, and freeze-dry or spray-dry to obtain coptisine- β-glucan inclusion complex.

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Abstract

The invention belongs to the technical field of a medicinal preparation, and provides a glucan inclusion compound of a water-insoluble small molecule drug and a preparation method thereof. The inclusion compound contains the water-insoluble small molecule drug and glucan, wherein the glucan is beta-glucan and / or beta-glucan derivative. The preparation method comprises the following steps: A, dissolving the water-insoluble small molecule drug into an organic solvent to obtain a drug solution; dissolving the beta-glucan and / or beta-glucan derivative into water to obtain a glucan solution; B, mixing the drug solution with the glucan solution under agitating and heating conditions, and volatilizing an organic solvent, so as to obtain an inclusion compound solution, wherein the inclusion compound is the glucan inclusion compound of the water-insoluble small molecule drug. By adopting the drug inclusion compound, the solubility (solubilizing), the encapsulation efficiency, the drug loading capacity and the bioavailability of the water-insoluble small molecule drug are improved, and the inclusion compound has sustained release action; the method for preparing the inclusion compound is easy to operate, and easy for large-scale production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to an inclusion compound of poorly water-soluble small-molecule drugs and a preparation method thereof. Background technique [0002] As we all know, many insoluble small molecule drugs have unfavorable factors such as bitter taste, irritating to the stomach, insoluble in water, unstable in physical and chemical properties, and easy to oxidize when exposed to light. and has lower bioavailability. Take chrysophanol as an example: chrysophanol, English name: Chrysophanol, abbreviated Chr, the structural formula is as follows: [0003] [0004] It is an anthraquinone active ingredient in rhubarb, Polygonum cuspidatum, Polygonum multiflorum, cassia seeds, etc. It has antibacterial, shortening blood coagulation time, exciting nerves, paralyzing muscles, relieving cough, diuretic, and anticancer effects. In recent years, studies have shown that chrysop...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K47/36A61K31/122A61K31/352A61K31/4375
Inventor 吴振陈岗师萱詹永谭红军陈航任昌琼
Owner CHONGQING ACAD OF CHINESE MATERIA MEDICA
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