Antimetabolites and potentiating agent thereof carried by anticancer sustained-release injection

A slow-release injection, anti-metabolism technology, used in anti-tumor drugs, drug combinations, drug delivery, etc., can solve problems such as differences in chemotherapeutic drug sensitivity and tolerance treatment failures

Inactive Publication Date: 2008-11-05
SHANDONG LANJIN PHARMA +1
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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

[0141] 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

[0143] 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:

[0144] (a) 5-20% cisplatin, carboplatin, omaplatin, dexomaplatin, heptaplatin, lobaplatin, nedaplatin or oxaliplatin;

[0145] (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

[0146] (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

[0149] 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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Abstract

The invention disclose an anticancer slow-release injection of sync-loaded anti-metabolites and synergists thereof, which comprises slow-release microspheres and menstruum, wherein, the slow-release microspheres comprise anticancer active ingredient and slow-release auxiliary material, and the menstruum is a special menstruum containing a suspending agent. The anticancer active ingredient is an anti-metabolite selected from Zalcitabine, emtricitabine, Galocitabine, ibacitabine, ancitabine, Decitabine, flurocitabine, enocitabine, imidazoletabine, capecitabine, Gemcitabine, Fludarabine or Cladribine and / or the synergist of the anti-metabolite selected from hormone anticancerogen and / or platinum compounds; the slow-release auxiliary material is selected from one or the combination of bi-fatty acids and sebacic acid copolymer, poly-(erucic acid dimer-sebacic acid), poly-( fumaric acid-sebacic acid), polifeprosan, polylactic acid copolymer and EVAc; the suspending agent is selected from carboxymethyl cellulose, etc. and the viscosity of the suspending agent ranges from 80cp to 3000cp (at the temperature of 20 DEG C to 30 DEG C). The slow-release microspheres can be produced to be a slow-release implant to be injected or placed in a tumour or the periphery of the tumour, and are independently used or used with non-operative treatment such as radiotherapy, chemotherapy or microwave, 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): A61K45/06A61K9/00A61K9/10A61K9/08A61K47/34A61P35/00
Inventor 孔庆忠孙娟俞建江孔令栋
Owner SHANDONG LANJIN PHARMA
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