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Loaded vascular inhibitor and cellulotoxic drug anticancer slow-release injection

A technology for sustained-release injections and vascular inhibitors, which can be used in drug combinations, antineoplastic drugs, and pharmaceutical formulations, and can solve problems such as difficult operation, poor curative effect, and many complications

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

However, solid sustained-release implants (Chinese Patent No. ZL96115937.5; ZL97107076.8) and existing sustained-release microspheres for the treatment of brain tumors (ZL00809160.9) or U.S. Patent (US5,651,986) all have inadequacies. Easy operation, poor curative effect, many complications, etc.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0118]Put 80mg of polyphenylpropane (p-CPP: 20:80 of sebacic acid (SA)) copolymer into a container, add 100ml of dichloromethane, dissolve and mix well, then add 10mg Hydroxycamptothecin and 10 mg gefitinib were re-shaken and spray-dried to prepare injection microspheres containing 10% hydroxycamptothecin and 10% gefitinib. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection with a viscosity of 220cp-460cp (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

[0120] 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:

[0121] (1) 2-40% hydroxycamptothecin, mitozolomide, 4-carboxytemozolomide, docetaxel, oxaliplatin, heptaplatin, ifosfamide, lomustine, estramustine , formustine, samustine, etoposide, teniposide, vinblastine, anastrozole, tamoxifen, fluorouracil, or mitomycin C;

[0122] (2) 2-40% of gefitinib, erlotinib, lapatinib, vatalanib, peritinib, carboxyaminotriazole, thalidomide, ranolamid, angiostatin, endostatin , endostatin, imatinib mesylate, semazinil, dasatinib, Avastin, canertinib, sorafenib, sunitinib, Teosta, or penito horse; or

[0123] (3) 2-40% hydroxycamptothecin, mitozolomide, 4-carboxytemozolomide, docetaxel, oxaliplatin, heptaplatin, ifosfamide, lomustine, estramustine , formustine, samustine, etoposide, teniposide, vinblastine, anastrozole, tamoxifen, fluoro...

Embodiment 3

[0126] Put 70 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 65,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 15 mg of erlotinib and 15 mg of lomustine, and re-shake Dry in vacuo to remove the organic solvent. The dried drug-containing solid composition was frozen and pulverized to make a micropowder containing 15% erlotinib and 15% lomustine, and then suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to obtain the corresponding Suspension-type sustained-release injection with a viscosity of 300cp-400cp (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 present invention relates to an anticancer slow-released injection containing vasoinhibitor. It is formed from slow-released microsphere and solvent. The slow-released microsphere includes anticancer effective component and slow-released auxiliary material, the solvent is special solvent containing suspension adjuvant. The anticancer effective component is vasoinhibitor selected from gemfitine, elotine, pelitine, thalidomide, vascular inhibine, endothelium inhibine, smasni, awasdine, kanatine or panitoma, etc. and / or cytotoxin medicine selected from antimitotic medicine, anticancer antibiotic and / or antimetabolite medicine. The slow-released auxiliary material is selected from polylactic acid and its copolymer, monomethyl polyethylene glycol / polylactic acid copolymer, polyethylene glycol / polylactic acid copolymer. sebacic acid and its copolymer and EVAc, etc. The suspension adjuvant is selected from carboxymethyl cellulose sodium, etc. and its viscosity is 10 cp-3000 cp (20 deg.C-30 deg.C). The slow-released microsphere also can be made into slow-released, implant preparation.

Description

(1) Technical field [0001] The invention relates to an anti-cancer slow-release injection containing vascular inhibitors and cytotoxic drugs and a preparation method thereof, belonging to the technical field of medicines. Specifically, the present invention provides a slow-release preparation of anticancer drugs containing angiostatinants and / or cytotoxic drugs, mainly slow-release injections and slow-release implants. (2) Background technology [0002] As one of the conventional treatment methods for cancer, chemotherapy drugs have been widely used in the treatment of various malignant tumors, and the effect is relatively obvious. However, its obvious systemic toxicity greatly limits the application of this drug. [0003] Due to the excessive expansion and hyperplasia of solid tumors, the interstitial pressure, tissue elastic pressure, fluid pressure and interstitial viscosity are all higher than those of the surrounding normal tissues. Therefore, it is difficult for conve...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K45/00A61K47/06A61K47/34A61P35/00
Inventor 孔庆忠刘恩祥张婕
Owner SHANDONG LANJIN PHARMA
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