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Naphthdianthrone compound and application of salt thereof in preparing developer of biliary tract and gall stones

A naphthodianthrone and compound technology, applied in preparations for in vivo tests, pharmaceutical formulations, etc., can solve the problem of non-specific affinity for gallstones, no gallstones, no biliary tract and gallstone imaging agents And other issues

Inactive Publication Date: 2012-07-04
JIANGSU PROVINCE INST OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are relevant patents on fluorescent biliary tract imaging agents in Europe, America, and Japan, such as: US7996068, WIPO Patent Application WO / 2004 / 090500. The fluorescent imaging agents used in these patents can only make positive imaging of the biliary tract, and do not have specificity. The ability to bind to gallstones cannot make positive fluorescent imaging of gallstones, so there is no fluorescent contrast agent that can be used to display gallstones, and there is no imaging agent that can simultaneously image the biliary tract and gallstones

Method used

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  • Naphthdianthrone compound and application of salt thereof in preparing developer of biliary tract and gall stones
  • Naphthdianthrone compound and application of salt thereof in preparing developer of biliary tract and gall stones
  • Naphthdianthrone compound and application of salt thereof in preparing developer of biliary tract and gall stones

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Experimental program
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Effect test

Embodiment 1

[0018] Reagents: SD rats were purchased from Shanghai Slack Experimental Animal Co., Ltd.; hypericin, pseudohypericin, trumpetin, hydroxyanthraquinone, nude pigment B, nude pigment D, heteronuclein D and chrysanthemum Purple was purchased from Beijing Xiantong Times Pharmaceutical Technology Development Co., Ltd.

[0019] Preparation preparation method: Weigh the above naphthodianthrone compounds and dissolve them in an appropriate amount of mixed solvent DMSO: PEG400: propylene glycol: normal saline (1:1:1:1), and configure them to be 0.1, 1.0, 5.0, and 20.0 mg respectively / ml solution.

[0020] Experimental method: 108 SD male rats were divided into 36 groups, including hypericin, protohypericin, pseudohypericin, trumpetin, hydroxyanthraquinone, nude pigment B, nude pigment D, iso 0.1, 1.0, 5.0, 20.0 mg / ml dosage groups of nude pigment D and ocher violet. Pentobarbital anesthetized, fixed, opened the abdomen to expose the bile duct, intravenous injection of different dose...

Embodiment 2

[0022] Prepare different concentration solutions of hypericin, pseudohypericin, trumpetin, hydroxyanthraquinone, nude pigment B, nude pigment D, isonuclein D and ocher violet, each concentration is 0.002, 0.02, 0.2 , 2mg / ml, human gallstones were taken, 6 human gallstones were put into solutions of different concentrations of each compound, and 6 pieces were put into blank bile, taken out after 24 hours, washed with bile and distilled water in turn, and placed under ultraviolet light at 365nm The fluorescence was observed, and the results showed that the gallstones in the bile solution of the above compound had red fluorescence, and the gallstones in the blank bile had no fluorescence.

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Abstract

The invention relates to a fluorescent developer, in particular to naphthdianthrone and salt thereof, which are injected intravenously or taken orally and displays the biliary tract and gall stones in operation. After being injected intravenously or taken orally, the developer is taken by hepatic cells, is discharged along with bile, is firmly combined with the gall stones and generates fluorescence under the excitation of certain wavelength light. The naphthdianthrone and salt thereof and developer provided by the invention are convenient for identifying the biliary tract structure, finding the intrahepatic and extrahepatic biliary duct stone and monitoring biliary tract damage and bile leakage in open surgery and peritoneoscope and choledochoscope surgeries.

Description

technical field [0001] The invention relates to the application of naphthodianthrone compounds and salts thereof in the preparation of biliary tract and gallstone imaging agents; Background technique [0002] The medical contrast agent is used to enter the biliary tract through a certain method and channel, so that the outline of the cholangiographic site and the lesion image can be clearly displayed. This method is cholangiography. In hepatobiliary surgery, intraoperative cholangiography can effectively detect biliary abnormalities, guide surgery, and avoid biliary damage. The data show that the rate of biliary tract injury caused by surgical operation errors is as high as 0.3% to 0.5%. During surgery, cholangiography can clearly display the entire biliary tract, detect the deformity and variation of the biliary tract in time, and effectively guide the surgery when the anatomical relationship is unclear. The doctor completed the operation safely, thus providing a reliable ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/00
Inventor 倪以成张健孙自平马琳孔铭蒋翠花李玥姚楠
Owner JIANGSU PROVINCE INST OF TRADITIONAL CHINESE MEDICINE
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