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Compound preparation having anti-tumor action

An anti-tumor effect and compound preparation technology, applied in the field of anti-tumor drugs, can solve the problems of affecting bioavailability, inconsistent release, and oral absorption differences.

Inactive Publication Date: 2012-05-02
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The dissolution of tablets and sustained-release capsules on the market is carried out with hydrochloric acid (9→1000) according to the Pharmacopoeia. Since dipyridamole is dissolved in acidic medium, but when it is transported from the stomach to the intestine, the intestinal juice The pH is alkaline, dipyridamole will be precipitated, and the precipitated dipyridamole will be affected by many factors such as food and preparation excipients, resulting in great differences in oral absorption
Especially for the 1, 3, and 7-hour release of dipyridamole sustained-release capsules, the dissolution medium is also an acidic medium. It is well known that the general capsule stays in the stomach for 2 hours, and then enters the intestinal tract. The release under acidic conditions is inconsistent, which may affect its bioavailability
The inventors found in the research that dipyridamole is not uniformly dispersed when it is dissolved in acid and precipitated in alkali, and there are phenomena such as aggregation, that is, the particle size of dipyridamole may be very large when it is precipitated, thereby causing Affect the absorption of drugs through the mucosa. Therefore, the blood concentration of the current oral preparations fluctuates greatly, and it is difficult for ordinary preparations to maintain a relatively stable and effective concentration for inhibiting platelet aggregation.

Method used

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  • Compound preparation having anti-tumor action
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  • Compound preparation having anti-tumor action

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0084] Recipe: Dipyridamole is 1mg, 5mg, 50mg, 100mg, 200mg, 400mg, 800mg or 1600mg, Ubenimex is 1mg, 10mg, 50mg, 100mg, 200mg, 400mg, 800mg, 1600mg or 3200mg Methasone is 0.1 mg, 1 mg, 10 mg, 20 mg, 40 mg, 80 mg or 160 mg respectively, and the three drugs are stirred and mixed to obtain drug mixtures in different proportions.

Embodiment 2

[0085] Embodiment 2: the in vitro cytotoxicity experiment of medicine

[0086] 1. Materials and methods:

[0087] 1.1 Drugs and reagents: dipyridamole: standard product, purchased from China National Institute for the Control of Pharmaceutical and Biological Products; Ubenimex: raw material drug, Zhejiang Prokangyu Pharmaceutical Co., Ltd.; dexamethasone: standard product, purchased from China Pharmaceutical Biological Products Co., Ltd. Product Testing Institute;

[0088] 1.2 Experimental cells: liver cancer BEL-7402 cells, purchased from the Cell Center of the Institute of Basic Medical Sciences, Chinese Academy of Medical Sciences

[0089] 1.3 Drug tested: the drug mixture of Example 1

[0090] 1.4 Experimental method: detection by colony formation method. BEL-7402 cells in the logarithmic growth phase were taken, and 50 cells / 0.2ml per well were added to a 96-well plate, and cultured for 24 hours. Add different concentrations of samples to be tested, set three parallel...

Embodiment 3

[0095] Example 3: Research on anti-tumor activity of drugs in vivo - inhibition of tumor growth in mice

[0096] 1 Materials and methods:

[0097] 1.1 Drugs and reagents: dipyridamole: standard product, purchased from China National Institute for the Control of Pharmaceutical and Biological Products; Ubenimex: raw material drug, Zhejiang Prokangyu Pharmaceutical Co., Ltd.; dexamethasone: standard product, purchased from China Pharmaceutical Biological Products Co., Ltd. Product Testing Institute; Dipyridamole Tablets: Shanxi Bao Pharmaceutical Group Co., Ltd.; Dexamethasone Acetate Tablets: Tianjin Lisheng Pharmaceutical Co., Ltd.; Ubenimex (Baishixin) Capsules: Zhejiang Puluo Produced by Kangyu Pharmaceutical Co., Ltd.; mouse liver cancer H 22 The cells were passaged in Kunming mice in the form of ascites.

[0098] 1.2 Animals: Kunming mice (cleaning class II) are female, 6-8 weeks old, weighing 18-22 g, provided by the Experimental Animal Center of the Academy of Military ...

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Abstract

The invention provides a compound preparation having an anti-tumor action. The compound preparation comprises therapeutically effective amounts of ingredient A, ingredient B, ingredient C and a pharmaceutically acceptable carrier; or mixture of the ingredient A, the ingredient B and the ingredient C; or a capsule taking the mixture of the ingredient B and the ingredient C as restricted substances; the ingredient A is enteric coating particles of dipyridamole and is formed by dipyridamole enteric particles and coating layers for packing the dipyridamole enteric particles; the ingredient B is ubenimex adhesion particles taking insoluble cellulose and biological adhesive materials as carriers; and the ingredient C is dexamethasone with a particle size of 100-200 nm. The compound preparation having the anti-tumor action formed by the three compositions can reach the peak value in blood at a higher speed, and can remain longer effective concentration time respectively, so that the requirement of clinical application can be met.

Description

technical field [0001] The invention relates to an antitumor drug, in particular to a compound preparation with dipyridamole, ubenimex and dexamethasone as active ingredients. Background technique [0002] Malignant tumor is a common disease that seriously threatens human health. In today's world, there is an urgent need for anti-tumor drugs. According to the data in 2007, there were 12 million newly diagnosed cancer patients in the world, and 7.6 million people died of cancer. According to the data of the top ten disease mortality and cause of death of urban and rural residents in my country in 2007, the cause of death of malignant tumors in my country's urban and rural areas is 28.5% and 24.8%, respectively, ranking first in the cause of death. WHO data It shows that cancer is the main cause of death, and cancer patients will continue to increase. Cancer as the cause of death accounted for 13.8% in 2008, 15.2% in 2015, and 17.6% in 2030. [0003] In clinical cancer trea...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/573A61K31/519A61K31/198A61P35/00
Inventor 侯惠民吴岱卫贺芬刘秀均甄永苏余岚裘渊黄冲马鸿飞吴朝倩
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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