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Compound anti-cancer slow-release injected containing blood vessel inhibitor

A technology of vascular inhibitors and sustained-release injections, which is applied in the field of compound anti-cancer sustained-release injections, and can solve problems such as increased tolerance of anti-cancer drugs and treatment failure

Inactive Publication Date: 2006-10-25
SHANDONG LANJIN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Not only that, the blood vessels in the tumor stroma are not sensitive to conventional chemotherapy drugs, which often leads to the enhancement of tumor cell resistance to anticancer drugs, and the result is treatment failure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0130] Put 80 mg of polylactic acid (PLGA) with a peak molecular weight of 25,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 10 mg of imatinib and 10 mg of gemcitabine, re-shake, and then vacuum-dry to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and then sterilized by radiation to obtain the slow-release anticancer drug containing 10% imatinib and 10% gemcitabine. All are percentages by weight. The drug release time of the anti-solid tumor pharmaceutical composition in physiological saline in vitro is 14-21 days, and the drug release time in mouse subcutaneous is 25-45 days.

Embodiment 2

[0132] As described in Example 1, the difference is that the anticancer active ingredient and weight percentage are one of the following:

[0133] (1) 1-50% of gefitinib, erlotinib, lapatinib, vatalanib, peritinib, carboxyaminotriazole, thalidomide, ranolamid, angiostatin, endostatin , endostatin, imatinib mesylate, semazinil, dasatinib, Avastin, canertinib, sorafenib, sunitinib, Teosta, or penito horse;

[0134] (2) 1-50% pemetrexed, pemetrexed disodium, lumitrexed, carmofur, tegafur, temozolomide, zalcitabine, emtricitabine, galocitabine, Ibacitabine, Ancitabine, Decitabine, Flucitabine, Enoxitabine, Mizotabine, Capecitabine, Gemcitabine, Fludarabine, Raltitrexed, Raltitrexed, Dexrazoxane, cladribine, or noratrexed; or

[0135] (3) 1-50% of gefitinib, erlotinib, lapatinib, vatalanib, peritinib, carboxyaminotriazole, thalidomide, ranolamid, angiostatin, endostatin , endostatin, imatinib mesylate, semazinil, dasatinib, Avastin, canertinib, sorafenib, sunitinib, Teosta, or ...

Embodiment 3

[0138] Put 80mg of polyphenylpropane (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) at 20:80) copolymer into a container, add 100ml of dichloromethane, dissolve and mix well, then add 10mg of Lotinib and 10 mg doxorubicin were re-shaken and spray-dried to prepare microspheres for injection containing 10% erlotinib and 10% doxorubicin. 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.

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PUM

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Abstract

The present invention relates to a compound anticarcinogen slow-released injection containing vasoinhibitor and its synergist. It is composed of slow-released microsphere and solvent. The slow-released microsphere includes anticancer effective component and slow-released auxiliary material, the solvent is general solvent or special solvent containing suspension adjuvant. The anticancer effective component is combination of vasoinhibitor and vasoinhibitor synergist of antitumor antibiotic or antimetabolite medicine, the slow-released auxiliary material is one selected from racemic polylactic acid and its copolymer, monomethyl polyethylene glycol and polylactic acid copolymer, polyethylene glycol and polylactic acid copolymer, carboxyl terminated polylactic acid and glycollic acid copolymer and ethylene-vinylacetate, etc. or their combination. The viscosity of suspension adjuvant is 100 cp-3000 cp, said suspension adjuvant is selected from sodium cellulose glycollate. The slow-released microsphere also can be made into slow-released implant preparation. Said invention also provides its application method for curing various tumors and cancers.

Description

(1) Technical field [0001] The invention relates to a compound anticancer sustained-release injection, which belongs to the technical field of medicines. (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 carmustine in the treatment of rat brain tumors" "Journal of Surgical Oncology" 69 pages 76-82 (1998) (Kong Q et al., J Surg Oncol.1998 Oct; 69(2):76-82). [0003] Local placement of antitumor d...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K45/08A61K47/34A61K47/42A61P35/00
Inventor 孔庆忠、刘恩祥、张婕
Owner SHANDONG LANJIN PHARMA
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