Preparation and application of human serum albumin-ruthenium inorganic drug complex

A human serum albumin, inorganic drug technology, applied in the field of anti-tumor drugs, to achieve the effect of improving targeting, high vascular permeability and retention rate, and reducing toxicity

Inactive Publication Date: 2015-11-18
GUANGXI NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, we have to face a reality: anti-tumor inorganic drugs are still a double-edged sword. While treating diseases, they will inevitably produce many side effects. Although NAMI-A and KP1019 in this paper have completed the first phase of clinical trials, they have Still have very toxic side effects

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  • Preparation and application of human serum albumin-ruthenium inorganic drug complex
  • Preparation and application of human serum albumin-ruthenium inorganic drug complex
  • Preparation and application of human serum albumin-ruthenium inorganic drug complex

Examples

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Effect test

Embodiment 1

[0024] Embodiment 1: the preparation of human serum albumin-NAMI-A ruthenium inorganic drug complex

[0025] NAMI-A was prepared according to the literature: 1g RuCl 3 Add to 30ml of ethanol, reflux for 3 hours to obtain a dark green solution, filter, concentrate to one-tenth of the initial volume, then add 1ml of concentrated hydrochloric acid and 2ml of DMSO, keep at 80°C for 15 minutes to obtain a bright orange solution. Cool the solution to room temperature, add 10ml of acetone to obtain orange-red crystals, add a few drops of diethyl ether to accelerate its crystallization, and collect by filtration. Wash with 20ml of cold acetone, then wash with 10ml of diethyl ether, and dry in vacuo to obtain 1.5g with a yield of 72%. Suspend 1.0 g of the above product in 20 ml of acetone, add 0.49 g of imidazole, stir for 4 hours, the color changes from orange to brick red, wash with 10 ml of acetone and 10 ml of ether, and dry the product at 60°C. Weigh the prepared NAMI-A drug, c...

Embodiment 2

[0026] Embodiment 2: the preparation of human serum albumin-Ru (ind) ruthenium inorganic drug complex

[0027] Ru(ind) was prepared according to literature: at 60-70°C, 0.2g, 1.7mmol of indazole was dissolved in 1ml of 2N HCl, 2ml of Ru(Ⅲ) solution was added to the hot solution, and a reddish-brown solid appeared immediately. Filtration, washing with ethanol and ether, and vacuum drying yielded 1.82 g of the product, with a yield of 50%. The prepared RIC drug was weighed and prepared into a 100mM solution with DMSO, and the human serum albumin (HSA) was prepared into a 1.5mM solution with secondary deionized water. The DMSO solution of RIC and the aqueous solution of HSA were mixed at a ratio of 1:1, and the content of DMSO was not more than 5%, and incubated at 4°C for 24 hours. Concentrate the mixture of HSA and ruthenium inorganic anticancer drugs, wash it repeatedly with deionized water twice to make the content of DMSO not more than 0.01%, and then concentrate to the req...

Embodiment 3

[0028] Embodiment 3: Preparation of human serum albumin-KP1019 ruthenium inorganic drug complex

[0029] KP1019 was prepared according to the literature: at 70°C, indazole (0.6g; 5.1mmol) was dissolved in 8ml of 12N HCl, 2ml of Ru(Ⅲ) solution was added to the hot solution, stirred at 80-90°C for 15 minutes, and immediately appeared An ocher-colored substance appeared, continued stirring to remove HCl residues, filtered, washed with ethanol and ether, and dried in vacuo to obtain 0.296 g of the product, with a yield of 87%. The prepared NAMI-A drug was weighed and made into a 400mM solution with DMSO, and human serum albumin (HSA) was made into a 1.5mM solution with secondary deionized water. The prepared KP1019 drug was weighed and made into a 100mM solution with DMSO, and human serum albumin (HSA) was made into a 1.5mM solution with secondary deionized water. Mix the DMSO solution of KP1019 and the HSA aqueous solution at a ratio of 1:1, the content of DMSO should not exceed...

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Abstract

The invention discloses a preparation and application of a human serum albumin-ruthenium inorganic drug complex. After incubating the ruthenium inorganic drug with human serum albumin, concentrating the mixture, and washing it repeatedly with deionized water twice Wash until the content of DMSO is less than 0.01%, concentrate to obtain the human serum albumin-ruthenium inorganic drug complex, and then make the complex into injections, tablets, pills, capsules, suspensions or emulsions for the treatment of breast cancer , stomach, lung, colon or liver disease. The complex of the present invention has high blood vessel permeability and retention rate, and the drug is selectively accumulated in tumor cells without any influence on normal cells, and the targeting property of the ruthenium inorganic drug is obviously improved, and the toxicity is greatly reduced.

Description

technical field [0001] The invention relates to antitumor drugs, in particular to the preparation and application of human serum albumin-ruthenium inorganic drug complexes. Background technique [0002] In recent years, ruthenium complexes have been extensively studied as new anticancer drugs. Due to the unique physical and chemical properties of ruthenium complexes, it is generally believed internationally that ruthenium complexes are low-toxic, easy to absorb and excreted quickly in the body. At present, hundreds of ruthenium complexes have been synthesized, and NAMI-A and KP1019 have completed Phase I clinical trials and are entering Phase II clinical trials. However, we have to face a reality: anti-tumor inorganic drugs are still a double-edged sword. While treating diseases, they will inevitably produce many side effects. Although NAMI-A and KP1019 in this paper have completed the first phase of clinical trials, they have Still have great toxic and side effects. Obvi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48A61K31/555A61P35/00
Inventor 杨峰张耀梁宏李梅
Owner GUANGXI NORMAL UNIV
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