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Anti-cancer pharmaceutical composition

A technology of anticancer drugs and compositions, applied in drug combinations, antineoplastic drugs, drug delivery, etc., can solve problems such as point mutations, imatinib resistance, and decreased affinity of imatinib, and achieve low toxicity , Improve drug resistance and improve compliance

Active Publication Date: 2012-04-04
SHANDONG NEWTIME PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Taking imatinib mesylate as an example, long-term high-dose imatinib mesylate will lead to point mutations in the BCR-ABL protein kinase domain, resulting in a decrease in the affinity of imatinib to it, resulting in the formation of imatinib Resistance to tinib

Method used

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1 pharmaceutical composition microemulsion preparation of the present invention

[0024] Arctigenin 10g

[0025] Gefitinib 0.05g

[0026] soybean oil 35g

[0027] Polyoxyethylene-23-lauryl ether 60g

[0028] 1,2-propanediol 30g

[0029] Preparation process: Weigh the prescription amount of soybean oil, polyoxyethylene-23-lauryl ether, and 1,2-propylene glycol, mix and stir evenly, then add arctigenin and gefitinib to dissolve, and ultrasonic treatment can also be used to accelerate the dissolution , to obtain a clarified concentrate, which is the arctigenin and gefitinib microemulsion concentrate. The particle size was measured by a laser particle size analyzer, and the average particle size was 15nm.

Embodiment 2

[0030] Embodiment 2 pharmaceutical composition microemulsion preparation of the present invention

[0031] Arctigenin 0.1g

[0032] Gefitinib 5g

[0033] Hydrogenated Coco Glycerides 5g

[0034] Lauroyl PEG-32-Glyceride 20g

[0035] 1,2-propanediol 5g

[0036] Polyethylene glycol 3350 20g

[0037] Preparation process: Weigh the prescription amount of hydrogenated cocoglyceride, lauroyl polyethylene glycol-32-glyceride, 1,2-propylene glycol, polyethylene glycol 3350, mix and stir evenly, then add arctigenin, gemfi The dissolving of tini can also be accelerated by ultrasonic treatment to obtain a clear concentrated solution, which is arctigenin and gefitinib microemulsion concentrate. The particle size was measured by a laser particle size analyzer, and the average particle size was 40nm.

Embodiment 3

[0038] Embodiment 3 pharmaceutical composition microemulsion preparation of the present invention

[0039] Arctigenin 10g

[0040] Gefitinib 5g

[0041] Safflower oil 35g

[0042] Polyoxyethylene-23-lauryl ether 60g

[0043] 1,2-propanediol 30g

[0044] The preparation process is the same as in Example 2. The particle size was measured by a laser particle size analyzer, and the average particle size was 36nm.

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Abstract

The invention relates to an anti-cancer pharmaceutical composition comprising arctigenin and a tyrosine kinase inhibitor. Compared to single-component medicines, the pharmaceutical composition provided by the invention has synergic anti-cancer activity in the aspect of non-small-cell lung carcinoma inhibiting. The invention also provides a micro emulsion preparation of the pharmaceutical composition.

Description

technical field [0001] The invention relates to an anticancer pharmaceutical composition, in particular to a pharmaceutical composition containing arctigenin and a tyrosine kinase inhibitor. Background technique [0002] Non-small cell lung cancer is the most common pathological type of lung cancer, accounting for about 85% of lung cancers. Non-small cell lung cancer includes several types such as squamous cell carcinoma, adenocarcinoma and large cell carcinoma. The cancer cells of non-small cell carcinoma grow slowly, the degree of malignancy is relatively low, and the diffusion and metastasis occur later. The clinical treatment of non-small cell lung cancer mainly includes surgical treatment, radiotherapy, chemotherapy, traditional Chinese medicine treatment and new treatment methods represented by molecular targeted therapy, but the sensitivity of non-small cell lung cancer to chemotherapy and radiotherapy is poor. Effective treatment is an urgent problem in the current ...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K31/365A61K31/505A61K31/5377A61K31/517A61P35/00A61P11/00
CPCA61K9/0019A61K31/365A61K36/28A61K47/10A61K9/107A61K45/06A61P11/00A61P35/00A61P35/02A61P35/04A61K2300/00
Inventor 赵志全
Owner SHANDONG NEWTIME PHARMA
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