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A pharmaceutical composition for targeted tumor therapy and its preparation method

A composition and drug technology, applied in the field of pharmaceutical compositions containing antitumor antibiotic-dipeptide derivatives and its preparation, can solve the problem of not having salt formation, antitumor antibiotic-dipeptide derivative compounds not having water solubility, etc. question

Inactive Publication Date: 2011-12-28
重庆寰瑞生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

If the free amino group of the antitumor antibiotic drug molecule is blocked due to the derivatization reaction, there is no possibility of salt formation, resulting in the embarrassment that the obtained antitumor antibiotic-dipeptide derivative compound does not have water solubility. Currently known research Literature and patent literature all do not relate to the pharmaceutical preparation of this class novel compound to solve the problem

Method used

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  • A pharmaceutical composition for targeted tumor therapy and its preparation method
  • A pharmaceutical composition for targeted tumor therapy and its preparation method
  • A pharmaceutical composition for targeted tumor therapy and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Embodiment 1: Synthesis and characterization of carproyl epirubicin

[0056] Epirubicin (Epi) is selected as a representative of anti-tumor antibiotics for illustration. With reference to the synthetic thinking disclosed in Chinese patent (00807538.7), take Epi as the starting compound to carry out the synthesis of benzyl-glycyl-prolyl-eprubicin compound (hereinafter referred to as glycoprolyl-eprubicin, abbreviated formula Synthesized for Z-GP-Epi), and characterized and analyzed the structure of the synthesized new compound.

[0057] 1. The synthesis reaction steps of Z-GP-Epi are as follows:

[0058] (1) Synthesis of Benzyl-Glycyl-Proline (Z-Gly-Pro-OH)

[0059]

[0060] Put 2.10 g of solid benzyl-glycine (Z-Gly-OH) in a 100 mL round bottom flask, add 25 mL of acetone to dissolve the solid, and add 1.27 g (1.2 eq) of N-hydroxysuccinimide (HOSu). 2. Dissolve 10g of N,N-dicyclohexylcarbodiimide (DCC) in 10mL of acetone, add it slowly through the dropping funnel, ...

Embodiment 2

[0071] Example 2: Preparation, Analysis and Stability Investigation of Lyproyl Epirubicin Freeze-dried Powder for Injection

[0072] 1. Preparation of Z-GP-Epi freeze-dried powder for injection

[0073] Prepare raw materials and excipients according to the following formulation prescription (1), mix well, and fully dissolve to obtain an organic solvent phase solution sample; meanwhile prepare an aqueous phase solution sample according to formulation prescription (2).

[0074] Prescription (1)

[0075]

[0076] Prescription (2)

[0077]

[0078] Slowly add the aqueous phase solution sample to the organic solution phase sample under stirring conditions, stir at room temperature for 30 minutes, intermittently sonicate for 30 minutes, filter through 0.220 μm sterile filter, and dispense it into 15ml transparent vials. 10.0ml.

[0079] The subpackaged samples were put into the freeze dryer, and the pre-freezing temperature was set at -45°C, and the pre-freezing time was 20...

Embodiment 3

[0084] Example 3: Cytotoxicity investigation of epirubicin freeze-dried powder against tumor cells

[0085] In this experiment, the tumor cell line 4T1 with negative expression of FAP α was used as a cell model to investigate the cytotoxicity of Epi and Z-GP-Epi on tumor cells, so as to understand the cytotoxicity of Epi modified by Z-GP.

[0086] 1. Main material

[0087] Epirubicin injection (Zhejiang Hisun Pharmaceutical); Z-GP-Epi freeze-dried powder for injection; mouse breast cancer cell line 4T1 (purchased from Shanghai Cell Bank, Chinese Academy of Sciences); CCK-8 kit (specification 200 time / box, purchased from Biyuntian Company); MTT (specification 200mg / bottle, purchased from Sigma)

[0088] Microplate reader (type 680), produced by Bio-Rad; CO 2 Incubator (2323-2), manufactured by SHEL-LAB Company; Inverted Biological Microscope (TS-100), manufactured by Nikon Company.

[0089] 2. Test method

[0090] 4T1 cells were routinely cultured and passaged in RPMI-1640 ...

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Abstract

The patent of the present invention relates to a pharmaceutical composition containing antitumor antibiotic-dipeptide derivatives that can be used for targeted tumor therapy and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. The pharmaceutical composition is an injection composed of antitumor antibiotic-dipeptide derivatives, phospholipids, stabilizers, organic solvents, antioxidants, surfactants, and pH regulators. Dry powder needle. The pharmaceutical composition greatly increases the solubility and stability of the antitumor antibiotic-dipeptide derivatives with targeted antitumor effects in aqueous solution, and can be effectively used for malignant epithelial tumors (such as breast cancer, ovarian cancer, Targeted therapy for lung cancer, colon cancer, pancreatic cancer, skin melanoma) and other solid tumors.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a pharmaceutical composition containing antitumor antibiotic-dipeptide derivatives for targeted tumor therapy and a preparation method thereof Background technique [0002] In the current clinical treatment of tumors, antitumor antibiotics have played a great role, especially antitumor antibiotics with anthracycline structure, and many varieties have developed into first-line drugs for clinical treatment of tumors, such as daunorubicin ( Daunorubicin), Doxorubicin, Epirubicin, Pirarubicin, etc. The anti-tumor mechanism of anti-tumor antibiotics with anthracycline structure is directly embedded between DNA double helix molecules, interferes with the transcription process, and prevents the formation of mRNA to exert anti-tumor effects. However, while the above-mentioned antitumor antibiotics with anthracycline structure exert a significant antitumor effect, the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/05A61K38/14A61K38/08A61K9/08A61P35/00A61K31/704A61K31/407
Inventor 杜军蔡绍晖王建
Owner 重庆寰瑞生物技术有限公司
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