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Kidney target precursor medicine, said prepn., its preparing method and application

A prodrug and drug technology, applied in the field of pharmacy, can solve the problems of reducing inflammatory cells, metabolic disorders, pathogenic bacteria not easy to confine and phagocytosis, etc.

Inactive Publication Date: 2009-07-29
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its clinical application is often accompanied by many problems: first, metabolic disorders, which can cause metabolic disorders of sugar, fat, protein, water and electrolytes; second, greater damage to the digestive system, which can cause steroid ulcers, small intestinal bleeding and perforation and hormonal pancreatitis; third, glucocorticoids not only have no inhibitory and killing effect on pathogenic bacteria, but because of their anti-inflammatory response, they can reduce inflammatory cells and prevent fibroblasts from forming fibrous tissue, making pathogenic bacteria Not easy to confine and devour

Method used

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  • Kidney target precursor medicine, said prepn., its preparing method and application
  • Kidney target precursor medicine, said prepn., its preparing method and application
  • Kidney target precursor medicine, said prepn., its preparing method and application

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Embodiment 1

[0049] Accurately weigh 100 mg of triptolide, 200 mg of succinic anhydride, and 10 mg of dimethylaminopyridine, add 2 ml of anhydrous pyridine, and 1 ml of triethylamine, react overnight at room temperature, and monitor the reaction on a silica gel plate. After the reaction was completed, 50 ml of pure water was added, and the pH was adjusted to acidity with hydrochloric acid. 20ml of chloroform was extracted 3 times, the extracts were combined, concentrated in vacuo at room temperature, purified by silica gel column chromatography twice, the product was collected, concentrated in vacuo and dried to obtain 117.6 mg of off-white solid triptolide succinate with a yield of 91.5%. The structure of the product was tested by UV, MS, FTIR, 1 Confirmed by H-NMR. mp109~111°C; IR(KBr)3463(-COOH)cm 1 ; MS m / z 459(M-H) 1 ; 1 H-NMR (400MHz, CDCl 1 ): 5.06 (1H, s, -14CH), 4.67 (2H, s, 19-CH 2 ), 3.82 (1H, d, 11-CH), 3.50 (1H, d, 12-CH), 3.43 (1H, d, 7-CH), 2.75 (5H, m, CH 2 CH 2 , 5...

Embodiment 2

[0051] Accurately weigh 100 mg of lysozyme, dissolve in 5 mL of 0.1 mol / l borate buffer, dissolve 100 mg of EDC, 50 mg of HOBT and 100 mg of triptolide succinate in 0.5 ml of acetonitrile. Slowly add the acetonitrile solution dropwise into the borate buffer solution of lysozyme, stir at a moderate speed, and react at 0°C for 24 hours. The reaction solution was centrifuged for 10 minutes (2,000 rpm, 0°C) to remove insoluble matter, and unreacted triptolide succinate and small molecular impurities were removed by Sephadex G-25. The protein-containing effluent was collected and freeze-dried to obtain a white loose powder, which was sealed and stored at -20°C. The binding rate of lysozyme to triptolide succinate and the concentration of prodrug were determined by MS and HPLC. See the attached mass spectrum figure 1 , the binding ratio was found to be 1:1 to 1:7, and the binding ratio was 1:2.3 from the HPLC hydrolysis assay, which was consistent with the mass spectrometry result...

Embodiment 3

[0053] Accurately weigh 100mg of insulin, dissolve in 5mL of 0.1mol / L borate buffer, dissolve 100mg of EDC, 50mg of HOBT and 100mg of triptolide succinate in 0.5ml of acetonitrile. Slowly add the acetonitrile solution dropwise into the borate buffer solution of insulin, stir at a moderate speed, and react at 0°C for 24 hours. The reaction solution was centrifuged for 10 minutes (2,000 rpm, 0°C) to remove insoluble matter, and unreacted triptolide succinate and small molecular impurities were removed by Sephadex G-25. The protein-containing effluent was collected, the binding rate of insulin to triptolide succinate and the concentration of prodrug were determined, and freeze-dried to obtain a white loose powder, which was sealed and stored at -20°C.

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Abstract

A precursor medicine targetting to kidney is composed of the low-molecular protein chosen from lysozyme, insulin, cytochrome C and pepetide suppressing enzyme or its polypeptide fragment, and the extract of common threewingnut root or its derivative, or glucocorticoid. It can be used as the immune depressant for treating renal disease, or the medicines for treating the rejection reaction and nephritis.

Description

technical field [0001] The present invention relates to the field of pharmacy, and more specifically, the present invention relates to kidney-targeting prodrugs with high kidney-targeting efficiency, their preparation methods and the application of these drugs in diseases related to local immunosuppression of kidney diseases. Background technique [0002] Immunosuppressants are widely used in the treatment of autoimmune diseases and prevention of rejection. Common immunosuppressants include azathioprine, corticosteroids, cyclophosphamide and cyclosporine A, etc. These drugs are not completely effective, and their clinical application is often limited by their toxic and side effects. Indiscriminate suppression of the system, the use of an effective dose will increase the sensitivity of the patient to the infection of opportunistic invaders, therefore, the use of targeted drug delivery, local immunosuppression of the lesion organ can reduce the toxic side effects of immunosupp...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48A61K31/365A61K31/57A61K9/00A61K9/19A61P13/12A61K47/62
Inventor 张志荣龚涛孙逊郑强
Owner SICHUAN UNIV
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