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High molecular antineoplastic cisplatin medicine and preparation method thereof

An anti-tumor drug and polymer technology, applied in the field of medicine, can solve the problems of high toxicity and side effects, fast metabolism, etc.

Inactive Publication Date: 2005-11-23
AMOSI TIANJIN TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the drug has disadvantages such as large toxic and side effects, fast metabolism in the body, and easy to be quickly cleared, which limits the further improvement of the therapeutic index of cisplatin.
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Method used

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  • High molecular antineoplastic cisplatin medicine and preparation method thereof
  • High molecular antineoplastic cisplatin medicine and preparation method thereof
  • High molecular antineoplastic cisplatin medicine and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] RPEG 2 Synthetic method of CO-B-C (taking monomethoxypolyethylene glycol (mPEG) molecular weight 2000 as an example)

[0046] 1. Dissolve 10 g of mPEG (Mn=2000, 5 mmol) in about 150 mL of toluene, and evaporate most of the toluene under normal pressure under nitrogen protection to remove trace moisture contained in mPEG. After cooling to room temperature, about 200 mL of anhydrous THF was added thereto, heated to a slight boil until mPEG was completely dissolved. Subsequently, 0.2 mol / L sodium naphthalene solution was added dropwise to the mPEG solution until the solution was gray-green. 5.24 mL of ethyl chloroacetate (6.03 g, 50 mmol) was diluted with 50 mL of THF and added to the reaction solution, and stirred at room temperature for 4 h. The reaction solution was concentrated and then precipitated with anhydrous ether. The obtained crude product was added to 300 mL of 0.1 mol / L NaOH solution and stirred at 50°C for 12 hours. Then use 1mol / L HCl to adjust pH=3, use...

Embodiment 2

[0057] Preparation of RPEGCO-B-C-Pt (taking mPEG molecular weight 4000 as an example)

[0058] Weigh 10g of mPEG (Mn=4000, 2.5mmol), prepare the mPEG-CH with carboxyl group in the same way as in Example 1 2 COOH, linked with diethyl aminomalonate, hydrolyzed, and finally synthesized mPEG-CH 2 CO-Lysine-Pt. The yield was 81%, and the molar content of cisplatin in the final product was 85.2%.

Embodiment 3

[0060] RPEG 2 Synthetic method of CO-B-C (taking monomethoxypolyethylene glycol (mPEG) molecular weight 80000 as an example)

[0061] 16g mPEG (Mn=80000, 0.2mmol) was used in the same way as in Example 1 to obtain mPEG-CH 2 CO-Lysine-Pt 4.5g, total yield 28%. The molar content of cisplatin in the final product was 80.4%.

[0062] According to the steps of the above examples, the present invention synthesized polymer drugs with three molecular weights for in vitro cytotoxicity experiments. Three kinds of dual-arm mPEG (abbreviation: DImPEG) cisplatin conjugates with carrier molecular weights of 4000, 6000 and 9400 were synthesized: DImPEG-4000-Pt, DImPEG-6000-Pt, DImPEG-9400-Pt and three linear mPEG cisplatin Conjugates: mPEG-4000-Pt, mPEG-6000-Pt, mPEG-9400-Pt. The molar content of cisplatin in the above various medicines is listed in the following table 1:

[0063] Table.1 Molar content of platinum in macromolecule drugs

[0064] drug

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Abstract

According the invention , double-arm RPEG2Y is used as the carrying agent, the coupling to the antineoplastic cisplatin is utilized to obtain a macromolecular antineoplastic medicament, pharmaceutical experiment has shown that, cisplatin medicament by using double-arm PEG as the carrying agent has higher curative effect compared with cisplatin using line type PEG as the carrying agent.

Description

technical field [0001] The invention relates to a medicine, in particular to a polymer anti-tumor cisplatin drug with double-armed polyethylene glycol as a carrier and a preparation method thereof, that is, a double-armed RPEG 2 Y- (abbreviation: double-armed polyethylene glycol) is used as a carrier, and the small molecule anti-tumor drug cisplatin is modified through a functional group reaction. Background technique [0002] Since B.Rosenberg and V.Camp reported for the first time in 1969 that cis-dichlorodiammine platinum (referred to as cisplatin) has broad-spectrum anticancer activity, the application and research of cisplatin in cancer treatment have developed rapidly. , has become an anti-tumor drug commonly used clinically in various countries. However, the drug has disadvantages such as large toxic and side effects, fast metabolism in the body, and easy to be quickly cleared, which limits the further improvement of the therapeutic index of cisplatin. Therefore, re...

Claims

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Application Information

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IPC IPC(8): A61K47/60
Inventor 黄骏廉
Owner AMOSI TIANJIN TECH DEV
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