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An anti-cancer drug slow release injection and an application thereof

A technology for sustained-release injections and sustained-release microparticles, which can be used in anti-tumor drugs, drug combinations, pharmaceutical formulations, etc., and can solve problems such as treatment failure and enhanced tolerance.

Inactive Publication Date: 2009-03-04
山东同科供应链股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The latter often leads to increased resistance of tumor cells to anticancer drugs, with consequent treatment failure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] Put 90 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 25,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 10 mg of O6-benzylguanine, re-shake, and vacuum dry to remove organic matter. solvent. Freezing and pulverizing the dried drug-containing solid composition to make a micropowder containing 10% by weight of O6-benzylguanine, and then suspending in physiological saline containing 1.5% sodium carboxymethylcellulose to obtain the corresponding suspension sustained-release injections. The drug release time of the slow-release injection in physiological saline in vitro is 10-15 days, and the drug release time in mouse subcutaneous is 20-30 days.

Embodiment 2

[0079] The method step of being processed into sustained-release injection is the same as that of Example 1, but the difference is that the contained anticancer active ingredients and their weight percentages are: 20% benzylguanine, O6-benzylguanine, O6-butyl Guanine, O6-methylguanine, O6-alkylguanine, O6-benzyluric acid or O4-benzylfolate.

Embodiment 3

[0081] Put 80mg of polyphenylpropane (p-carboxyphenylpropane: sebacic acid weight ratio is 30:70) copolymer into the container, add 100ml of dichloromethane, dissolve and mix well, then add 20mg of 7-hydroxyl-star As for the staurosporine, the microspheres for injection containing 20% ​​by weight of 7-hydroxyl-staurosporine were prepared by spray-drying after re-shaking. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The drug release time of the slow-release injection in physiological saline in vitro is 10-15 days, and the drug release time in mouse subcutaneous is 20-30 days.

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PUM

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Abstract

Disclosed is an anticancer medicinal injection and its use, which comprises slow release microspheres and dissolvent, the slow release microballoons comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being conventional dissolvent or specific dissolvent containing suspension adjuvant. The anticancer active constituents include anti-metabolism anti-cancer drugs, phosphoinositide-3-kinase inhibitor, DNA restoration enzyme inhibitor or CENUs, the suspending agent is selected from sodium carboxymethylcellulose and mannitol. The injection can lower down the whole body toxicity reaction of the anti-cancer medicament, selectively increase the tumor local medicinal concentration, and improve the treatment effect of the non-operative treatment methods such as chemotherapy, medicament and radiation.

Description

(1) Technical field [0001] The invention relates to an anticancer drug sustained-release injection and a preparation method thereof, belonging to the technical field of sustained-release drugs. (2) Background technology [0002] Cancer treatment mainly includes surgery, radiotherapy and chemotherapy. Among them, the effect of chemotherapy is more obvious, and has been widely used in many malignant tumors. However, further studies have found that blood vessels, connective tissue, matrix proteins, fibrinoproteins, and collagen in the tumor stroma not only provide scaffolds and essential nutrients for the growth of tumor cells, but also affect the effect of chemotherapy drugs on tumor cells. Permeation and diffusion in the surrounding and tumor tissue, see Netti et al. "The influence of the condition of the extracellular matrix on the movement of drugs in solid tumors" "Cancer Research" 2000 60 pp. 2497-503 (Netti PA, CancerRes.2000, 60(9):2497-503). Due to the excessive exp...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K45/00A61K9/10A61P35/00
Inventor 孔庆忠孙娟张楠宋邦强
Owner 山东同科供应链股份有限公司
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