Anti-cancer drug slow release injection and uses thereof

A technology of slow-release injections and anticancer drugs, which is applied in the field of medicine and can solve problems such as increased tolerance and treatment failure

Inactive Publication Date: 2007-03-07
孔庆忠
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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

[0067] 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, add 10 mg of oxaliplatin, re-shake, and vacuum dry to remove the organic solvent. Freezing and pulverizing the dried drug-containing solid composition to make a micropowder containing 10% oxaliplatin, and then suspending it in physiological saline containing 1.5% sodium carboxymethylcellulose to prepare the corresponding suspension 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.

Embodiment 2

[0069] The method step of being processed into sustained-release injection is the same as in Example 1, but the difference is that the contained anticancer active ingredients are:

[0070] Cisplatin, Carboplatin, Heptaplatin, Denaplatin, Enloplatin, Epithioplatin, Cispiroplatin, Dexomaplatin, Oxaliplatin, Isoproplatin, Lobaplatin, Miplatin, Nedaplatin, Omaplatin , Siplatin, spiroplatin or zeniplatin.

Embodiment 3

[0072] Put 80mg of polyphenylpropane (p-carboxyphenylpropane: sebacic acid weight ratio is 20:80) copolymer into a container, add 100ml of dichloromethane, dissolve and mix well, add 20mg of 5-fluorouracil, and shake again Afterwards, injectable microspheres containing 20% ​​5-fluorouracil were prepared by spray-drying method. 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 microballoons including anticancer active constituents and slow release auxiliary materials and dissolvent, the anticancer active constituents being platinum-group compounds, anti-metabolism, anti-cancer drugs, anticancer antibiotics or topoisomerase inhibitor, the slow release auxiliary materials are selected from polylactic acid, polyglycolic acid and glycolic acid copolymer, which can slowly release the anti-cancer medicament onto tumor partially during the degradation and absorption process, thus the whole body toxicity reaction is reduced appreciably , and the effective medicinal concentration can be sustained to the tumor partially. 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 slow-release injection and application thereof, belonging to the technical field of medicines. (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. Infiltration and diffusion in the surrounding and tumor tissues (see Netti et al. "The influence of the status of the extracellular matrix on the delivery of drugs in solid tumors" "Cancer Research" 60 pp. 2497-503 (2000) (Netti PA, Cancer Res .2000, 60(9): 2497-503). Due to the excessive expansive hyperplasia of so...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61P35/00
Inventor 孔庆忠孙娟陈颖孙中厚
Owner 孔庆忠
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