Preparation and application of phospholipid complex as EV71 and CAV16 virus inhibitor

A CAV16, phospholipid complex technology, applied in the direction of antiviral agents, drug delivery, medical preparations of non-active ingredients, etc., can solve the problems of clinical application and dosage form development restrictions, restrictions on oral absorption rate, etc., to improve in vivo absorption capacity , Easy to prepare, fast absorption effect

Inactive Publication Date: 2018-04-03
TIANJIN INT JOINT ACADEMY OF BIOTECH & MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, TJAB-1099 is a water-insoluble compound, and its water solubility limits its oral absorption rate, which greatly limits its clinical application and dosage form development

Method used

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  • Preparation and application of phospholipid complex as EV71 and CAV16 virus inhibitor
  • Preparation and application of phospholipid complex as EV71 and CAV16 virus inhibitor
  • Preparation and application of phospholipid complex as EV71 and CAV16 virus inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1: Preparation of EV71 virus and CAV16 virus inhibitor (TJAB-1099) phospholipid complex

[0025] Weigh 0.10 g of TJAB-1099 raw material, 0.36 g of egg yolk lecithin, add 5 mL of chloroform, and react at 40°C for 3 hours until clarification. The chloroform was volatilized by rotary evaporation under reduced pressure to dryness, and vacuum-dried for 24 hours to obtain 0.46 g of phospholipid complex. It was sealed and packaged, and stored in a refrigerator at 4°C.

Embodiment 2

[0026] Embodiment 2: Preparation of EV71 virus and CAV16 virus inhibitor (TJAB-1099) phospholipid complex

[0027] Weigh 0.10 g of TJAB-1099 raw material, 0.36 g of egg yolk lecithin, add 5 mL of dichloromethane, and react at 40°C for 0.5 hours until clarification. Dichloromethane was volatilized by rotary evaporation under reduced pressure to dryness, and vacuum-dried for 24 hours to obtain 0.46 g of phospholipid complex, which was sealed and packaged, and stored in a refrigerator at 4°C.

Embodiment 3

[0028] Embodiment 3: the preparation of EV71 virus and CAV16 virus inhibitor (TJAB-1099) phospholipid complex

[0029] Weigh 0.10 g of TJAB-1099 raw material, 0.36 g of egg yolk lecithin, add 5 mL of cyclohexane, and react at 60°C for 3 hours until clarification. Dichloromethane was volatilized by rotary evaporation under reduced pressure to dryness, and vacuum-dried for 24 hours to obtain 0.46 g of phospholipid complex, which was sealed and packaged, and stored in a refrigerator at 4°C. The formation of the complex was confirmed by thermal analysis and nuclear magnetic resonance, as shown in Figure 1A to Figure 2B shown.

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Abstract

The invention provides a preparation method and an application of a phospholipid complex as an EV71 and CAV16 virus inhibitor. The method for preparing the phospholipid complex as the EV71 and CAV16 virus inhibitor TJAB-1099 comprises the following steps: mixing the TJAB-1099 with phospholipid, and adding an organic solvent; conducting refluxing and stirring at a temperature of 30-60 DEG C for 0.5-3h, so that a reaction solution is obtained; conducting reduced pressure evaporation on the reaction solution at a temperature of 30-60 DEG C, and removing an organic solvent; and implementing drying, so that the TJAB-1099 phospholipid complex is obtained. With the application of the complex formed by the TJAB-1099 and the phospholipid, the hydrophilic performance and the lipophilic performance of drugs can be effectively improved, and the phospholipid is excellent in biological affinity. An in-vivo absorption capacity is improved, and bioavailability is enhanced.

Description

technical field [0001] The present invention relates to a drug compound, more specifically, relates to a preparation method and application of a phospholipid compound as an inhibitor of EV71 virus and CAV16 virus and its oral preparation. Background technique [0002] Human hand-foot-mouth disease (HFMD) is a common acute infectious disease and is distributed all over the world. The incubation period of hand, foot and mouth disease is 2-10 days, with an average of 3-5 days, and the course of disease is generally 7-10 days. Fever symptoms appear at the onset of the disease, scattered herpes appear on the oral mucosa, maculopapules and herpes appear on the hands, feet and buttocks, and there may be inflammatory flushes around the herpes, and there is less fluid in the pustules. Accompanied by cough, runny nose, loss of appetite and other symptoms. In a small number of cases, especially in children with EV71 infection, meningitis, encephalitis, encephalomyelitis, neurogenic, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4439A61K9/00A61K47/24A61P31/14
CPCA61K47/24A61K9/0053A61K31/4439
Inventor 饶子和杨诚郭宇马海秋蔡岩李爽汪颖左臣强张玉普李玉彩
Owner TIANJIN INT JOINT ACADEMY OF BIOTECH & MEDICINE
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