Medicine A317491 nanometer particle and application and preparation thereof

A nanoparticle and drug technology, applied in the field of pharmaceutical preparations, can solve problems such as toxic side effects, short pain relief time, and inability to continuously relieve pain, and achieves avoiding side effects, good encapsulation and film formation, non-toxic encapsulation and formation. film effect

Inactive Publication Date: 2015-11-11
ZHANGJIAGANG INST OF IND TECH SOOCHOW UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, studies have shown that P2X3R is also involved in the formation of bone cancer pain. Using the specific inhibitor of P2X3R A317491 can significantly relieve pain, but the pain relief time is very short, that is, pain relief begins 0.5 hours after intrathecal injection of drug A317491. It lasts for about 2 hours, and the peak of the drug effect is 1 hour after the injection. After 3 hours, the drug effect basically disappears, and the pain cannot be relieved continuously. At the same time, if the injected dose is too large, there will be obvious side effects

Method used

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  • Medicine A317491 nanometer particle and application and preparation thereof
  • Medicine A317491 nanometer particle and application and preparation thereof
  • Medicine A317491 nanometer particle and application and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0084] Example 1: Preparation of diclofenac-modified dextran nanoparticles loaded with drug A317491

[0085] Under stirring conditions, 14.4 mg of dicyclohexylcarbodiimide (DCC) (0.07 mmol) and 20.7 mg of diclofenac (0.07 mmol) were added to 10 mL of dimethyl sulfoxide solvent, and the reaction was stirred at room temperature for 3 h; then 20mg of dextran (0.123mmol glucose unit) was added to the above reaction solution, and reacted at room temperature for 48h; the reaction solution was dialyzed for 24 hours, and freeze-dried to obtain diclofenac modified dextran; then, under stirring conditions, 20mg of the drug A317491 and 100 mg of diclofenac-modified dextran were dissolved in 20 mL of organic solvent dimethyl sulfoxide, and then added dropwise to 40 mL of hot water at 50°C in volume, and then the organic solvent was removed and freeze-dried to obtain the drug-loaded A317491-loaded diclofenac Modified dextran nanoparticles. It is determined that the drug loading amount of ...

Embodiment 2

[0086] Example 2: Preparation of diclofenac-modified dextran nanoparticles loaded with drug A317491

[0087]Under stirring conditions, 20.6mg of dicyclohexylcarbodiimide (DCC) (0.1mmol) and 29.6mg of diclofenac (0.1mmol) were added to 10mL of dimethyl sulfoxide solvent, and the reaction was stirred at room temperature for 3h; then 100mg dextran (0.617mmol glucose unit) was added to the above reaction solution, and reacted at room temperature for 48h; the reaction solution was dialyzed for 24 hours, and freeze-dried to obtain diclofenac modified dextran; then, under stirring conditions, 20mg of the drug A317491 and 100 mg of diclofenac-modified dextran were dissolved in 20 mL of organic solvent dimethyl sulfoxide, and then added dropwise to 40 mL of hot water at 50° C., after which the organic solvent was removed and freeze-dried to obtain the drug-loaded diclofenac A317491 Modified dextran nanoparticles. It is determined that the drug loading amount of 100 mg of nanoparticles...

Embodiment 3

[0088] Example 3: Preparation of diclofenac-modified dextran nanoparticles loaded with drug A317491

[0089] Under stirring conditions, 26.8mg of dicyclohexylcarbodiimide (DCC) (0.13mmol) and 38.5mg of diclofenac (0.13mmol) were added to 10mL of dimethyl sulfoxide solvent, and the reaction was stirred at room temperature for 3h; then 200mg of dextran (1.234mmol glucose unit) was added to the above reaction solution, and reacted at room temperature for 48h; the reaction solution was dialyzed for 24 hours, and freeze-dried to obtain diclofenac modified dextran; then, under stirring conditions, 20mg of the drug A317491 and 100 mg of diclofenac-modified dextran were dissolved in 20 mL of organic solvent dimethyl sulfoxide, and then added dropwise to 40 mL of hot water at 50° C., after which the organic solvent was removed and freeze-dried to obtain the drug-loaded diclofenac A317491 Modified dextran nanoparticles. It is determined that the drug loading amount of 100 mg of nanopar...

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Abstract

The invention relates to the technical field of medicine preparations, in particular to a medicine A317491 nanometer particle and an application and preparation thereof. The medicine A317491 nanometer particle comprises medicine A317491 and modified polysaccharide, wherein the modified polysaccharide is obtained by modifying diclofenac. With the diclofenac modified polysaccharide as the carrier, the medicine A317491 nanometer particle can slowly release the medicine A317491. With the diclofenac modified polysaccharide as the carrier, the half-life period of the medicine A317491 can be effectively prolonged, and meanwhile the diclofenac modified polysaccharide can slowly release diclofenac so that the effect of synergically, enduringly and slowly relieving bone cancer pains can be achieved.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to an A317491 drug nanoparticle and its application and preparation. Background technique [0002] Bone cancer pain is a kind of severe pain caused by primary or metastatic cancer. It is a typical representative of cancer pain and one of the most common symptoms when tumors metastasize to bone. The main clinical manifestations are: continuous and progressive pain, paroxysmal pain, and paroxysmal pain. According to reports, most patients with advanced cancer and metastatic cancer have cancer pain. At present, effective treatment measures are limited, and the cancer pain of most patients has not been effectively controlled, which seriously affects the quality of life of patients and increases the burden on families and society. [0003] There are many drugs to relieve the pain of bone cancer. In the early stage of the disease, paracetamol can be taken orally to r...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/48A61K31/196A61P29/00C08B37/00
Inventor 徐广银周友浪蒋国勤张弘弘胡淑芬刘春风
Owner ZHANGJIAGANG INST OF IND TECH SOOCHOW UNIV
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