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Slow released anticancer injection with both antimetabolite and its synergist

A slow-release injection and anti-metabolism technology, which can be used in anti-tumor drugs, drug combinations, medical preparations with non-active ingredients, etc.

Inactive Publication Date: 2006-11-08
DASEN BIOLOGICAL PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the sensitivity of tumor cells to chemotherapeutic drugs varies greatly
Many tumor cells are not sensitive to drugs, and some tumor cells are sensitive in the early stage of chemotherapy, but quickly tolerate it
Especially when anticancer drugs, such as antimetabolites, are used alone, increased tolerance often leads to treatment failure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0134]Put 80mg polyphenylene propane (p-CPP: sebacic acid (SA) 20:80) copolymer into a container, add 100ml dichloromethane, dissolve and mix well, then add 10mg heptane Platinum and leuprolide, after re-shaking, microspheres for injection containing 10% heptaplatin and 10% leuprolide 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 with a viscosity of 20cp-300cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 10-15 days, and the drug release time in mice subcutaneous is about 20-30 days.

Embodiment 2

[0136] 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 and their weight percentages are:

[0137] (a) 5-20% cisplatin, carboplatin, omaplatin, dexomaplatin, heptaplatin, lobaplatin, nedaplatin or oxaliplatin;

[0138] (b) 5-30% triptorelin, goserelin, leuprolide, anastrozole, edoxifene, milprexifen, tamoxifen, 4-monohydroxytamoxifen , comoxifen, raloxifene, steroid estrogen, anticancer stenol, 4-hydroxytamoxifen, flutamide, aminoglutethimide, pirumide, megestrol, formazan hydroxyprogesterone, clomiphene, toremifene, letrozole, anastrozole, exemestane, or bicalutamide; or

[0139] (c) 5-20% cisplatin, carboplatin, omaplatin, dextro-omaplatin, heptaplatin, lobaplatin, nedaplatin or oxaliplatin and 5-30% triptorelin, goserelin , Leuprolide, Anastrozole, Edoxifene, Miprexifen, Tamoxifen, 4-Monohydroxytamoxifen, Comoxifen, Raloxifene, Steroid Antiestrogens, Anti...

Embodiment 3

[0142] Put 70 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 15 mg of lobaplatin and 15 mg of pemetrexed, re-shake and dry in vacuo Remove organic solvents. The dried drug-containing solid composition was frozen and pulverized to make micropowder containing 10% lobaplatin and 10% pemetrexed, and then suspended in physiological saline containing 1.5% carboxymethylcellulose sodium to prepare the corresponding mixed Suspension-type sustained-release injection with a viscosity of 220cp-340cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 10-15 days, and the drug release time in mice subcutaneous is about 20-30 days.

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PUM

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Abstract

The slow released anticancer injection consists of slow released microsphere and solvent. The slow released microsphere includes effective anticancer component and slow releasing supplementary material, and the solvent is special solvent containing suspending agent. The effective anticancer component is antimetabolite Zalcitabine, Emtricitabine, etc and / or antimetabolite synergist selected from hormone anticarcinogen and / or platinum compound. The slow releasing supplementary material is selected from difatty acid-sebacic acid copolymer, poly (erucic acid dipolymer-sebacic acid), poly(fumaric acid-sebacic acid), etc or their composition. The suspending agent is carboxymethyl cellulose, etc. and has viscosity of 80-3000 cp at 20-30 deg.c. The slow released microsphere may be also prepared into slow released implanting agent for use alone or together with chemotherapeutic medicine, radiotherapeutic medicine, etc.

Description

(1) Technical field [0001] The invention relates to an anti-cancer slow-release injection containing anti-metabolism drugs and their synergists, belonging to the technical field of medicines. Specifically, the present invention provides a slow-release injection or slow-release implant loaded with an anti-metabolite drug and / or its synergist. (2) Background technology [0002] Cancer treatment mainly includes surgery, radiotherapy and chemotherapy. Among them, surgical treatment cannot remove scattered tumor cells, so it often recurs or causes tumor cells to spread and metastasize due to surgical stimulation; radiotherapy and traditional chemotherapy are not selective, and it is difficult to form an effective drug concentration or therapeutic dose in the local tumor, resulting in poor efficacy and high toxicity. Simply increasing the dose of drugs or radiation is limited by systemic toxicity. See Kong Qingzhong et al. "Intratumoral placement of cisplatin plus systemic carmu...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/519A61K45/00A61K47/32A61K47/34A61K47/36A61K47/38A61K47/42A61P35/00
Inventor 孔庆忠孙娟俞建江孔令栋
Owner DASEN BIOLOGICAL PHARMA CO LTD
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