Anethol trithione and phospholipid compound and preparation method thereof

A kind of technology of anetis phospholipid and compound, which is applied in the field of anetis phospholipid compound and its preparation, can solve the problems of not seeing, reducing drugs, not seeing anetis phospholipid compound, etc., so as to improve the effect and reduce the Metabolism, the effect of improving the bioavailability of absorption in the body

Inactive Publication Date: 2010-01-06
成都国嘉联合制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, which drugs can be complexed with phospholipids is difficult to predict for those skilled in the art
[0010] After literature search, there is no report about the preparation of phospholipid complex
In addition, there is no report on the use of phospholipid complex preparation technology to reduce the metabolism of drugs in the digestive tract and thereby increase the drug dose in liver tissue

Method used

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  • Anethol trithione and phospholipid compound and preparation method thereof
  • Anethol trithione and phospholipid compound and preparation method thereof
  • Anethol trithione and phospholipid compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The preparation of embodiment 1 anetellithion phospholipid complex

[0029] Weigh acetone, lecithin or phosphatidylcholine or phosphatidylethanolamine or phosphatidylserine or hydrogenated lecithin in a beaker with a molar ratio of 1:0.1~30, add 20ml~60ml of acetone or chloroform or tetrahydrofuran or ethanol or Ethyl acetate is placed on a magnetic stirrer, the water bath is kept at a constant temperature of 30-60°C, and reacted for 0.5-6 hours, then the reaction solvent is removed by rotary evaporation, and the product is obtained by vacuum drying.

[0030] The preparation of the oral preparation of embodiment 1 anethrose

[0031] 1. Anetis trisulfide enteric-coated capsules

[0032] Weigh 0.27g of anetis trisulfide crude drug and 0.88g of soybean lecithin into a beaker, add 20ml of acetone, place on a magnetic stirrer at 35-45°C and stir with nitrogen for 1-3 hours, remove the solvent of the reactant by rotary evaporation, and dry , to obtain the phospholipid compl...

Embodiment 2

[0045] Example 2 Preparation and formulation optimization test of the anetellithion phospholipid complex of the present invention

[0046] Utilizing the property that anethole trithion is almost insoluble in petroleum ether, but phospholipids and phospholipid complexes are soluble in petroleum ether, an injection method was used to prepare anetis trithion phospholipid complex. Through single factor investigation, the recombination rate of phospholipid complex is used as the evaluation index, and the formula ratio of anetetitie and phospholipid is optimized.

[0047] The test method is as follows:

[0048] (1) Preparation of anetellitthione phospholipid complex:

[0049] Take the prescribed amount of anetis trisulfide and soybean lecithin (E200, Jiaji, Germany), dissolve in 20ml of acetone, stir in a water bath at 35-45°C to dissolve until clear, react for 1-3 hours, and dry in a vacuum oven , to obtain a yellow semi-viscous solid, which is the anetis phospholipid complex. Di...

Embodiment 3

[0059] The test of parameter selection in the preparation method of embodiment 3 anetellithion phospholipid complex

[0060] 1. Preparation of Anetellithion Phospholipid Complex

[0061] 1.1 Screening of the types of solvents

[0062] The anetthio-phospholipid complex was prepared by solvent method.

[0063] Weigh equimolar amounts of anetisone and phospholipid, add methanol, absolute ethanol, acetone, ether, chloroform, dichloromethane, benzene, ethyl acetate and tetrahydrofuran 20ml, seal, put in a constant temperature shaking bath at 37°C, shake After 24 hours, the dissolution reached equilibrium, and the solubility properties of anetellitsulfione powder and phospholipids in different solvents were investigated. The results are shown in Table 1.

[0064] Table 1 Solubility properties of anetthio and phospholipids in different solvents

[0065] sample

Methanol

Absolute ethanol

Acetone

Ether

Chloroform

Anetellithion

partially dissolv...

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PUM

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Abstract

The invention relates to a peroral anethol trithione preparation and a preparation method thereof, belonging to the field of pharmaceutical preparations, The preparation method comprises the following steps: dissolving anethol trithione and phospholipid in a compound mode to one or a plurality of fatty acid triglycerides to prepare soft capsules and / or palletizing the phospholipid compound and suitable pharmaceutical excipient to further prepare enteric-coated capsules. Compared with preparations sold in markets, animal experiment results show that the prepared new preparation of the phospholipid compound obviously improves the peroral bioavailability of the anethol trithione and the pharmaceutical concentration in the target tissue liver and predicts favorable liver protection efficacy and cholagogic efficacy.

Description

technical field [0001] The present invention relates to a kind of phospholipid complex of anetellithion and its preparation method, which belongs to the field of medicaments. Background technique [0002] With the continuous improvement of people's living standards, in recent years, the number of patients with fatty liver over the age of 40 has increased significantly. According to relevant statistics, at present, the incidence of fatty liver in adults in my country is about 10%, and fatty liver has become a common and frequently-occurring disease in clinical practice. The incidence rate has become the second common liver disease after viral hepatitis, and it is expected to become the first common liver disease in the next 10 to 20 years. Fatty liver has become the common concern of multiple disciplines such as digestion, endocrinology, nutrition, and cardiovascular. focus. [0003] Anetthio, also known as bilivitamin, anethole trithione, and 3-p-methoxyphenyl trithione, f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K47/24A61K31/385A61K9/48A61K9/20A61P1/16A61K47/55
Inventor 江云张大永孙毅毅梁恒兴陈文文李垚黄蕾蕾
Owner 成都国嘉联合制药有限公司
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