Indirubin phosphatide compound and its preparation method

A technology of indirubin phospholipid and compound, which is applied in the field of indirubin phospholipid compound and its industrializable preparation, can solve the problems of poor water-solubility and fat-solubility, incomplete oral absorption, large gastrointestinal irritation, etc. Improve absorption, enhance pharmacological action and curative effect, and improve bioavailability

Inactive Publication Date: 2005-07-06
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Indirubin has a definite curative effect, but its water-solubility and fat-solubility are relatively poor, and its effect is slow when administered orally, and its oral absorption is incomplete, and 40%-50% of the drug is excreted with excretion, and it has no effect on human body. Gastrointestinal irritation is large. After taking the medicine, patients are prone to gastrointestinal discomfort and vomiting. Some patients may cause gastrointestinal symptoms such as abdominal pain, diarrhea, and even blood in the stool. In clinical application, in order to improve its oral bioavailability and reduce the dosage, it is necessary to further Improves Indirubin Oral Absorption

Method used

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  • Indirubin phosphatide compound and its preparation method
  • Indirubin phosphatide compound and its preparation method
  • Indirubin phosphatide compound and its preparation method

Examples

Experimental program
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Effect test

Embodiment 1

[0019] Example 1: Take 5 mg of indirubin, dissolve it in 25 ml of ethyl acetate to obtain a purple-red clear liquid, add soybean lecithin (Shanghai Taiwei Pharmaceutical Co., Ltd., injection grade, batch number 040108, containing 75-80% of phospholipid) 45 mg (Indirubin 5mg: phospholipid 45mg is equivalent to a molar ratio of 1:3), stirred until the solution became clear, heated at 80°C while shaking and reacted for 2 hours, removed the reaction solvent under reduced pressure, and dried in a conventional low-temperature vacuum to obtain a purple-red semi-solid compound things. Get phospholipids, indirubin and indirubin phospholipid complex for DSC analysis (attached Figure 1-3 ), the result is that indirubin has a phase transition point at 353.0°C, and the phase transition point of the compound is increased, and the phase transition point of indirubin is no longer visible at 353.0°C, which proves the formation of "indirubin phospholipid complex" .

[0020] The solubility of...

Embodiment 2

[0021] Example 2: Weigh 10 mg of indirubin, dissolve it in 50 ml of tetrahydrofuran to obtain a purple-red clear liquid, add 90 mg of soybean lecithin, stir until the solution is clear, shake and react for 2 hours while heating at 30 ° C, remove the reaction solvent under reduced pressure, and vacuum at low temperature After drying, a purple-red semi-solid compound was obtained.

Embodiment 3

[0022]Example 3: Weigh 10 mg of indirubin, dissolve it in 50 ml of hot acetone to obtain a purple-red clear liquid, add 90 mg of egg yolk phospholipid, stir until the solution is clear, and shake the reaction for 3 hours while heating at 60°C to keep warm, remove the reaction solvent under reduced pressure, and lower the temperature After vacuum drying, a purple-red semisolid compound was obtained.

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Abstract

Disclosed is an indirubin phosphatide compound and process for preparation, wherein the compound consists of indirubin and phosphatide by the mol ratio of 1 : 1-15, the indirubin phosphatide compound has good stability, stronger lipophilicity and superior property in medicament absorption degree, speed of action, and effect duration, it can be prepared into various oral dosages.

Description

technical field [0001] The invention relates to an indirubin phospholipid complex and an industrialized preparation method thereof, including a pharmaceutical composition containing the indirubin phospholipid complex and a preparation method thereof. Background technique [0002] Indirubin is a bisindole compound extracted from the traditional Chinese medicine Qingdai, the chemical composition is 2,2'-biindole-3,3'-dione, and the molecular formula is C 16 h 10 N 2 o 2 , molecular weight 262.26, purple-red crystal, insoluble in water, in CHCl 3 It is soluble in many organic solvents, but the solubility is very small, mp353.0℃, UV290nm. Indirubin is the anti-tumor active ingredient of Qingdai, which can inhibit the DNA synthesis and protein translation process of chronic myelogenous leukemia cells and transplanted tumor cells to inhibit protein biosynthesis, thereby inhibiting the normal growth of cancer cells, and has no effect on bone marrow. Obvious inhibitory effect. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K9/16A61K9/20A61K9/48A61K31/404A61K47/24A61P35/00
Inventor 吴正红周静平其能徐蓓
Owner CHINA PHARM UNIV
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