Novel idarubicin hydrochloride compound

A technology of idarubicin hydrochloride and its compound, which is applied in the field of medicine to achieve the effects of controllability, reduction of manufacturing costs and costs, and ease of preparation

Inactive Publication Date: 2020-02-28
刘力
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, so far, there are no published literature reports at home and abroad that are easier to prepare or have better stability than the novel idarubicin hydrochloride compounds of the present invention, such as idarubicin hydrochloride ω-type crystal compounds, that is, different molecular formulas or structural forms Novel compound of idarubicin hydrochloride and its preparation method and use

Method used

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  • Novel idarubicin hydrochloride compound
  • Novel idarubicin hydrochloride compound
  • Novel idarubicin hydrochloride compound

Examples

Experimental program
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Embodiment 1

[0128] The preparation of embodiment 1 idarubicin hydrochloride 1.25 hydrate (ω type compound)

[0129] Add 5 g of idarubicin and 10 ml of methanol into a 250 ml three-necked flask, stir, and protect with nitrogen, add an appropriate amount of dichloromethane, heat up to 30-40 ° C, stir to dissolve, add 4M ethanol hydrochloric acid solution at room temperature to adjust the solution The pH value is about 3.0, stir for 20 minutes, evaporate part of the solvent under reduced pressure, then add 20ml of absolute ethanol, place at 0°C, wait until the precipitate is fully separated, filter with suction, wash with a small amount of ethanol, and filter with suction, the obtained solid is diluted in an oven for 40 Blow dry at about ℃ for 3 hours, and obtain about 4.2 g of orange-red crystals; Identification: ①Take about 10 mg of this crystal, add 0.5 ml of nitric acid to dissolve, add 0.5 ml of water, burn with flame for 2 minutes, let cool, add dropwise silver nitrate for test Liquid,...

Embodiment 2

[0130] The preparation of embodiment 2 idarubicin hydrochloride 1.25 hydrate (ω type compound)

[0131]Add 8g of idarubicin hydrochloride anhydrous to a 250ml three-necked flask, add an appropriate amount of methanol, protect with nitrogen, stir, heat up to about 50-63°C, stir until completely dissolved, add 60ml of acetonitrile, cool to below 5°C and place , when the precipitate is fully separated, filter with suction, wash with a small amount of ethanol twice, and filter with suction, put the obtained solid in a flask, add appropriate amount of methanol and water (95:5), heat and stir to dissolve, add acetonitrile and ethanol (1:1) 150ml Carry out recrystallization, place it below 5°C until the crystals are fully separated, filter with suction, wash the solid with a small amount of ethanol, filter with suction, dilute the obtained solid in an oven at 35°C for about 3 hours, and dry at about 50°C for 1 hour to obtain Orange-red crystalline solid 5.2g; Identification: ①Take 10...

Embodiment 3

[0132] Embodiment 3 Preparation of idarubicin hydrochloride crystalline hydrate freeze-dried powder injection (prescription: 1000 bottles)

[0133] Prescription: idarubicin hydrochloride crystalline hydrate (prepared by the method of embodiment 1 or embodiment 2, the main ingredient weight is calculated in idarubicin hydrochloride) 10g, sorbitol 40g, disodium EDTA 0.05g, lactic acid of about 1M and Disodium hydrogen phosphate solution, appropriate amount, appropriate amount of water for injection;

[0134] Take the prescribed amount of idarubicin hydrochloride crystalline hydrate, sorbitol, and disodium EDTA in the liquid preparation tank, add about 1000ml of water for injection, stir to dissolve, and adjust the pH to 4.5 with about 1M lactic acid and disodium hydrogen phosphate solution ~5.5, add activated carbon 0.01% (W / V) and stir for 30 minutes, filter with 0.22 micron microporous membrane, pack according to the weight of main drug 10mg / bottle, freeze at -45~-30℃ for abou...

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Abstract

Disclosed is a novel idarubicin hydrochloride omega-type compound. The novel idarubicin hydrochloride omega-type compound has low hygroscopicity and high storage stability, is beneficial to drug quality control and the like, and is applicable to preparation of drugs for treating or preventing acute leukemia, advanced breast cancer, diffuse large B cell lymphoma of central nervous systems, non-Hodgkin's lymphoma, myelodysplastic syndrome, lung cancer, melanoma, soft tissue sarcoma, multiple myeloma, liver cancer, colorectal cancer, kidney cancer, prostate cancer, endometrial cancer, testiculartumor, ovarian cancer, head and neck cancer, and the like.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to provide anti-tumor drug idarubicin hydrochloride with better stability, a compound with a new molecular formula and a new molecular structure and a pharmaceutical composition thereof. Background technique [0002] Idarubicin hydrochloride (Idarubicin hydrochloride, CAS Registry Number: 57852-57-0, molecular formula C 26 h 27 NO 9 HCl, M=533.97), idarubicin is a 4-demethoxy-anthracycline analogue of daunorubicin, a DNA intercalator that acts on topoisomerase II and can inhibit Nucleic acid synthesis. The compound has high lipophilicity, and compared with doxorubicin and daunorubicin, the uptake of the drug by cells is increased, but its cytotoxicity is stronger than that of daunorubicin and doxorubicin, and it has a broader anti-inflammatory effect. Tumor spectrum, intravenous or oral administration is more effective against murine leukemia and lymphoma. [0003] In vitro ex...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/252C07H1/06A61K31/704A61P35/02A61P35/00
CPCA61P35/00A61P35/02C07B2200/13C07H1/06C07H15/252
Inventor 刘力
Owner 刘力
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