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Anti-cancer pellet and colonic targeting agent

A technology of colon targeting and micropills, which is applied in the direction of antineoplastic drugs, pharmaceutical formulations, bulk delivery, etc. It can solve the problems of low level of preparations, obvious adverse reactions, poor quality controllability, and poor stability, so as to improve compliance , Improve anti-tumor activity, improve the effect of drug activity

Active Publication Date: 2013-07-10
广州鲁比生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are not many traditional Chinese medicine preparations that can be clinically used to treat CC. Among the 5017 preparations contained in the "New National Chinese Patent Medicine", only Aidi Injection, Compound Mylabris Capsules, Kangaiping Pills, Xiaoaiping Tablets and Syrup, Zhemu Several Chinese patent medicines such as syrup have the effect of treating CC, and there are the following common problems: ①The drugs are all water, alcohol crude extracts or medicinal powders, the preparation level is low, and the quality controllability and stability are poor; ②Intravenous infusion or Taken orally, the drug cannot target cancer tissue, and the systemic or gastrointestinal adverse reactions are obvious; ③Widely used in the treatment of lung cancer, liver cancer, lymphoma, etc., lack of targeted treatment for CC
[0006] At present, OCTDS has developed a variety of colon-targeted drug delivery systems based on different principles, including the pH-dependent type prepared from pH-sensitive materials based on the gradually increasing pH value of the gastrointestinal tract; the time-lag type based on the constant transit time of the small intestine ; Based on the unique enzyme system produced by colonic bacteria, the enzyme-triggered type prepared from enzyme-degradable materials; in addition, there are studies on various drug release systems such as pressure-dependent type, organic acid-induced type, and pulse type.

Method used

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  • Anti-cancer pellet and colonic targeting agent
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  • Anti-cancer pellet and colonic targeting agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] The preparation of embodiment 1 micropill of the present invention

[0035] (1) Raw material formula

[0036] Emodin: Sophoridine: Matrine=1:20:25;

[0037] (2) Take a total of 50g of the above formula raw materials and 50g of microcrystalline cellulose passed through a 100-mesh sieve, mix well, moisten with 50% ethanol in an appropriate amount, prepare a soft material, pass through a 20-mesh sieve, and put it in a centrifugal coating granulator, At 30°C, the rotating speed is 35 rev / min, the wind speed is 8cfm, the pellets are rounded for 4 minutes, taken out and dried at 50°C to obtain the pellets of the present invention.

Embodiment 2

[0038] Embodiment 2 Preparation of colon targeting agent of the present invention

[0039](1) Take 10g of EudragitⅢ, add about 100ml of ethanol, soak and swell for 12 hours, stir to fully disperse and dissolve evenly. Dissolve 2g of diethyl phthalate in 100ml of ethanol, then add 1g of micropowdered silica gel, and homogenize at high speed for 20 minutes. Add the suspension of plasticizer and micropowder silica gel into the Eudragit III solution, stir to disperse evenly, and obtain the coating liquid, and keep stirring during the coating process.

[0040] (2) Take the pellets prepared in Example 1, put them in a centrifugal coating granulator, adjust the parameters as wind speed 8cfm, speed 35 rpm, wind temperature 30°C, peristaltic pump 1-2, spray pressure 0.25MPa Spray the above-mentioned coating solution for coating to increase the weight of the pellets by 30%.

Embodiment 3

[0041] Embodiment 3 Micropill preparation technology research of the present invention

[0042] According to the properties and dosage of the material, it is planned to use a centrifugal coating granulator to prepare vegetarian pills first, and then coat a layer of colon-targeting coating to prepare the colon-targeting pellets of the present invention.

[0043] In the early stage, the starch blank pellet core was used as the mother core, and the method of spraying wetting agent and powder to increase the layer size and spheroidization was investigated. The results found that the following problems existed: ①The drug powder was very viscous, and it was easy to stick to the pills during the process of adding powder and spheronizing, and a large amount of excipients needed to be added, resulting in a large amount of finished product, which was difficult to meet the needs of preparing capsules; ②The combination of powder and wetting agent Proportion coordination control is difficu...

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Abstract

The invention provides an anti-cancer pellet. The anti-cancer pellet is a preparation which is prepared from the following materials and the auxiliary material in parts by weight: 1 part of material medicines including rheum emodin, sophoridine and sophocarpidine in a ratio of (20-100):(250-2000):(500-2500) and 0.5-2 parts of auxiliary material including diluents. The invention further provides an anti-cancer colonic targeting agent and a preparation method of each preparation. According to the anti-cancer pharmaceutical composition, rheum emodin, sophoridine and sophocarpidine are selected from a plurality of anti-tumor natural medicines and reasonably combined, so that a synergistic interaction effect is brought into play, anti-tumor activity of single medicine is remarkably improved; meanwhile, the dispensed medicines are prepared into the colonic targeting agent and each medicine generates effects to colonic infection focuses, so that not only pesticide effect activity can be improved, but also side effects of digestive systems including a stomach, small intestines and the like can be reduced, and therefore, novel medicine choices are provided for treating the colorectal cancer.

Description

technical field [0001] The invention relates to an anticancer pellet and a colon targeting agent. Background technique [0002] Cancer, also known as malignant tumor (Malignant neoplasm), is a disease caused by the abnormal mechanism of controlling cell growth and proliferation. In addition to growing out of control, cancer cells can also locally invade the surrounding normal tissues and even transfer to other parts of the body through the internal circulatory system or lymphatic system. Common cancers include gastric cancer, colon cancer, liver cancer, nasopharyngeal cancer, lung cancer, and intracranial tumors. Among them, colon cancer (CC) refers to malignant tumors that occur in the cecum, ascending colon, transverse colon, descending colon, and sigmoid colon. In recent years, with the improvement of living standards and changes in living habits, the incidence of colon cancer in my country is also on the rise, ranking second only to gastric cancer among digestive tract...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4375A61K9/16A61P35/00A61K31/122
Inventor 赵斌王琼刘敬熊文明李拥军谢兴亮王建国谢彩玲邓仙梅
Owner 广州鲁比生物科技有限公司
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