Cisplatin complex and preparation method thereof

A complex, cisplatin technology, applied in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. It can avoid the sudden release of cisplatin, promote the release and improve the stability.

Active Publication Date: 2013-01-09
CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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  • Abstract
  • Description
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Problems solved by technology

For example, the micelles (NC-6004) prepared by Kataoka et al. using polyethylene glycol-b-polyglutamic acid complexed with cisplatin have entered the second phase of clinical research, but the micelles obtained are cross-linked between polyamino acid side chains. Formed, the lyophilized powder of the complex obtained by this method will be difficult to redissolve
Stenzel et a

Method used

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  • Cisplatin complex and preparation method thereof
  • Cisplatin complex and preparation method thereof
  • Cisplatin complex and preparation method thereof

Examples

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Example Embodiment

[0068] The present invention also provides a method for preparing a cisplatin complex, comprising the following steps: a complex reaction occurs between cisplatin and a polymer having the structure of formula (I) in an aqueous medium to generate a cisplatin complex;

[0069]

[0070] In formula (I), R 1 Independently selected from C2-C10 straight-chain alkyl, C3-C10 branched-chain alkyl, phenyl or R'-CO-, R' is independently selected from C2-C10 straight-chain alkyl, C3-C10 branched alkyl or phenyl, R 1 It is preferably C3-C8 straight-chain alkyl, C4-C8 branched-chain alkyl, and phenyl, more preferably C6 alkyl;

[0071] R 2 independently selected from H atom, C1-C20 alkyl group or substituted C1-C20 alkyl group, preferably H atom, C1-C10 alkyl group or substituted C1-C10 alkyl group, the substituted alkyl group The substituent is selected from one or more of ketal, acetal, hydroxyl, aldehyde group, amino group, sulfhydryl group and sugar residue;

[0072] R 3 independ...

Example Embodiment

[0095] Example 1

[0096] Add 10 g of γ-benzyl-L-glutamic acid to 100 ml of anhydrous tetrahydrofuran under the condition of dry inert gas, fully react under the action of 6.5 g of triphosgene, and then add petroleum ether for sedimentation to obtain a solid, heavy. After crystallization and drying, 7.85g of γ-benzyl-L-glutamic acid-N-carboxylic acid anhydride (BLG-NCA) monomer was finally obtained; under the condition of inert gas, the dimethylformamide (DMF) of n-hexylamine was The solution was added to the DMF solution of BLG-NCA. The ratio of n-hexylamine to γ-benzyl-L-glutamic acid-N-carboxylic acid anhydride (BLG-NCA) was 1:160. After the reaction, ether was added for sedimentation and filtered. The solid was obtained, and after drying, a glutamic acid copolymer with a benzyl protecting group with a degree of polymerization of 160 was obtained; after deprotection, a glutamic acid copolymer with a structure of the formula (II) with a degree of polymerization of 160 was ob...

Example Embodiment

[0099] Example 2

[0100] Add 10 g of γ-benzyl-L-glutamic acid to 100 ml of anhydrous tetrahydrofuran under the condition of dry inert gas, fully react under the action of 6.5 g of triphosgene, and then add petroleum ether for sedimentation to obtain a solid, heavy. After crystallization and drying, 7.34g of γ-benzyl-L-glutamic acid-N-carboxylic acid anhydride (BLG-NCA) monomer was finally obtained; under the condition of inert gas, the dimethylformamide (DMF) solution of n-hexylamine was Added to the DMF solution of BLG-NCA, the ratio of n-hexylamine to γ-benzyl-L-glutamic acid-N-carboxylic acid anhydride (BLG-NCA) was 1:160. After the reaction, ether was added for sedimentation and filtered to obtain Solid, after drying, a glutamic acid copolymer with a benzyl protective group with a degree of polymerization of 160 is obtained; after deprotection, a glutamic acid copolymer with a degree of polymerization of 160 in the structure of formula (II) is obtained, denoted as P(Glu) ...

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Abstract

The invention provides a cisplatin complex which is formed by complexing cisplatin with polymer with a structure as a formula (I), and further provides a preparation method of the cisplatin complex. The cisplatin and the polymer with the structure as the formula (I) are in complex reaction in aqueous media to generate the cisplatin complex. The cisplatin complex has fine biocompatibility and is degradable, and polyethylene glycol is grafted on a side chain of the polymer, so that the prepared cisplatin complex has fine dissolvability. When the cisplatin complex is dissolved in the aqueous media, the cisplatin is protected by a hydrophilic polyethylene glycol chain segment and a hydrophobic amino acid chain segment, and accordingly sudden release of cisplatin caused by influences of a blood circulation system after intravenous injection can be effectively avoided, and stability of the cisplatin complex is improved. In addition, carboxyl contained in the cisplatin complex has pH sensitivity and deprotonation tendency in a low-pH environment, medicine release is facilitated, and medicine curative effect can be improved.

Description

technical field [0001] The invention relates to the field of polymer medicine, in particular to a cisplatin complex and a preparation method thereof. Background technique [0002] Cisplatinum (cis-diamminedichloroplatinum, referred to as CDDP) is a metal complex with anticancer activity, which was first discovered by B. Rosenborg et al. in 1965. Cisplatin has the characteristics of broad anticancer spectrum, strong effect, synergistic effect with many antitumor drugs, and no cross-resistance. Therefore, cisplatin is one of the most commonly used drugs in combination chemotherapy. At present, cisplatin has a good effect on the treatment of reproductive system tumors, malignant lymphoma, head and neck cancer, bladder cancer, and lung cancer. Oral administration of cisplatin is ineffective, and the clinical application method is mostly in the form of intravenous infusion. After intravenous injection, cisplatin disappears rapidly in the plasma and quickly distributes throughout...

Claims

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Application Information

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IPC IPC(8): C08G81/00C08G69/48A61K47/48A61K33/24A61P35/00A61K33/243
CPCC08G69/10A61K47/48C08G69/40A61K47/48246C08L77/04A61K47/48215A61K33/24C08G81/00A61K47/60A61K47/64A61K47/645A61P35/00A61K33/243
Inventor 汤朝晖于海洋宋万通李明强庄秀丽陈学思
Owner CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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