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Preparation method of targeting antineoplastic medicine nitidine chloride complexes, product thereof and injection containing the product

A technique for chlorinated syringamine and antitumor drugs, which is applied to the preparation of targeted antitumor drug chloramphenicol complexes, and the field of preparation of water-soluble compounds, and can solve the problems of large toxic side effects, poor water solubility and the like

Inactive Publication Date: 2012-08-22
刘华钢 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved by the present invention is to provide a targeted antineoplastic drug with high solubility and low toxic and side effects in view of the poor water solubility and relatively large toxic and side effects of the antitumor drug Echidine chloride in the prior art Preparation method and product of chlorinated acanthine compound, and injection containing the product

Method used

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  • Preparation method of targeting antineoplastic medicine nitidine chloride complexes, product thereof and injection containing the product
  • Preparation method of targeting antineoplastic medicine nitidine chloride complexes, product thereof and injection containing the product
  • Preparation method of targeting antineoplastic medicine nitidine chloride complexes, product thereof and injection containing the product

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] 1: Preparation of the targeted antineoplastic drug Echidine chloride complex.

[0059] (1) Pretreatment of chlorinated dimethicone:

[0060] Under the protection of nitrogen, accurately weigh the dihedral chloride and add it to an appropriate amount of concentrated hydroiodic acid, so that the concentration of the dihedral chloride is 0.001mol / L, heat up to 50°C while stirring; cool to 50°C after reacting for 6 hours At room temperature, adjust the pH of the mixed solution to about 10 with ammonia water, repeatedly extract the mixed solution three times with dichloromethane, evaporate the solvent in the water phase to dryness, dissolve the residue with methanol, add hydrochloric acid to adjust the pH to 2.5, and precipitate needle-shaped crystals after standing , which is the dihedral chloride crystal in which the methoxy group at the C-8 and / or C-9 position is replaced by a hydroxyl group.

[0061] Accurately weigh the needle-like crystals and malonic acid (1:1 molar ...

Embodiment 2

[0072] 1: Preparation of the targeted antineoplastic drug Echidine chloride complex.

[0073] Repeat the preparation method of Example 1 targeted antineoplastic chlorinated chlorinated compound, the difference is, with distearoylglycerol phosphatidylethanolamine-polyethylene glycol amine (DSPE-PEG-NH 2 , 10kDa) instead of biotin polyethylene glycol amine (Biotin-PEG-NH 2 , molecular weight is 5kDa), with 4-arm polyethylene glycol amino group (4-Arm-PEG-NH 2 , 5kDa) to replace the six-arm polyethylene glycol amino group (6-Arm-PEG-NH 2 , 10kDa).

[0074] 2: Preparation of the targeted antineoplastic drug Ephedrine Chloride Complex Injection.

[0075] Take 16.3g of polyether F-68 and dissolve it in 800mL of water for injection to obtain a 2% aqueous solution of polyether F-68 for subsequent use; accurately weigh 2.0g of the targeted antineoplastic drug chlorine Put the water-soluble compound of limpet base and single-walled carbon nanotubes in a 500mL volumetric flask, prepa...

Embodiment 3

[0079] 1: Preparation of the targeted antineoplastic drug Echidine chloride complex.

[0080] Repeat the preparation method of the targeted antineoplastic drug Echinacea chloride complex in Example 1, the difference is that adipic acid is used instead of malonic acid.

[0081] Two: Preparation of the targeted antineoplastic drug Echidine chloride complex powder injection.

[0082] Take the water-soluble complex (0.1%) of the targeted antineoplastic drug dihedral chloride and single-walled carbon nanotubes (0.1%), egg yolk lecithin (50%), cholesterol (20%) and polyether F-68 (5%) was dissolved in an appropriate amount of ethyl acetate, and the solvent was recovered under reduced pressure at 40°C with a rotary evaporator, and a lipid film was formed on the bottle wall; then an appropriate amount of aqueous solution with a pH of 6.5 was added to dissolve the lipid Membrane elution is dispersed in the aqueous solution, and the liposome solution of gained is supersonicated 30min u...

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Abstract

The invention discloses a method for preparing target antineoplastic drug chlorinated nitidine compound, products thereof and an injection containing the products. The method for preparing the target antineoplastic drug chlorinated nitidine compound comprises the steps of pre-treating the chlorinated nitidine to acquire carboxylic acid-modified chlorinated nitidine, then using amphiphilic polymers to implement non-covalent functionalized modification on the outer wall of a single-wall carbon nano tube that is cut to be 20-500 nm long, and coupling the carboxylic acid-modified chlorinated nitidine with the single-wall carbon nano tube after the non-covalent functionalized modification by means of esterification and amidation reactions to acquire the compound. The preparation method of the compound is simple, the solubility of the resulting products can reach 5.0mg / mL, and the antineoplastic target is strong, thus favorably settling the problems of low solubility and strong toxicity of the chlorinated nitidine; in addition the invention can be applied clinically as a substitute for the chlorinated nitidine and provides a new water-soluble compound for the clinical trial of the chlorinated nitidine.

Description

Technical field: [0001] The present invention relates to a preparation method of a targeted antineoplastic drug chlorinated chlorinated chlorinated compound, in particular to a method for preparing a water-soluble compound of a chlorinated chlorinated compound with single-walled carbon nanotubes; The targeted antineoplastic compound of acanthine chloride prepared by the method and the injection containing the product as an active ingredient. Background technique: [0002] Nitidine chloride (1, English name nitidine chloride), the structure shown in the following formula 1, is a benzophenanthridine alkaloid, yellow or light yellow green needle-like crystals. In 1980, Huang Zhixun et al. (Acta Chemicals, 1980, 38 (6): 535.) isolated Zanthoxylumnitidum (Roxb.) DC root dry powder and obtained Zanthoxylumnitidum chloride and other 5 Alkaloids, and through animal experiments, it was found that dianthine chloride can prolong the life of Ehrlich ascites cancer mice, the inhibition ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4741A61K47/48A61P35/00A61K9/08A61K9/14A61K47/69
Inventor 刘华钢赖泽锋
Owner 刘华钢
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