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Slow released compound anticancer prepn containing bendamustine

A technology of bendamustine and sustained-release agent, which can be applied to medical preparations containing active ingredients, anti-tumor drugs, pharmaceutical formulations, etc., can solve the problems of accelerated tumor spread and metastasis, large trauma, and restrictions.

Inactive Publication Date: 2007-01-03
JINAN SHUAIHUA PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

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 conventional chemotherapy to form an effective drug concentration in the tumor. See Kong Qingzhong "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), simply increasing the dosage is limited by systemic reactions
Local application of drugs may solve the problem of drug concentration to some extent (Chinese patent), however, surgical operations such as drug implantation are more complicated and traumatic, and in addition to easily leading to various complications such as bleeding, infection, and decreased immunity, It can also cause or accelerate the spread and metastasis of tumors
In addition, the preparation and expensive costs before and after the operation often affect its effective implementation.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0112] Put 80 mg of polylactic acid (PLGA) with a peak molecular weight of 35,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 10 mg of bendamustine and 10 mg of methotrexate, re-shake and remove by vacuum drying Organic solvents. The dried solid composition is shaped immediately, subpackaged and then sterilized by radiation to obtain the anti-cancer slow release containing 10% bendamustine and 10% methotrexate. All are percentages by weight. The drug release time of the anti-solid tumor pharmaceutical composition in physiological saline in vitro is 15-25 days, and the drug release time in mouse subcutaneous is 25-50 days.

Embodiment 2

[0114] As described in Example 1, the difference is that the anticancer active ingredient and weight percentage are one of the following:

[0115] (1) A combination of 1-40% bendamustine and 1-40% doxorubicin, epirubicin, mitomycin C, actinomycin D or dactinomycin; or

[0116] (2) 1-40% of bendamustine and 1-40% of fluorouridine, deoxyfluorouridine, 5-deoxyfluorouridine, propylthiouracil, fluorouracil, butyl fluorouracil, bisfluridine , 5-fluoropyrimidinol, sodium sulfcaptopurine, mercaptopurine, mercaptopurine, 6-mercaptopurine, 6-aminopurine hydrochloride, glycinethiopurine, thioguanine, methotrexate, flumethhotrexate Methotrexate, dioxetrexate, 10-ethyldeazaminopterate, methotrexate, folic acid, 5,10-dideazatetrahydrofolate, calcium levofolinate, calcium folinate, carmofur, Tegafur, Youfudine, Tegafur Uracil, 8-Azaguanine, Uracil, Thimethouracil, Topotecan, Topotecan Hydrochloride, Cytarabine, Cyclocytidine, Hydroxyurea, A combination of hydroxyguanidines.

[0117] The s...

Embodiment 3

[0119]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 benzene Damustine and 10 mg fluorouracil were re-shaken and spray-dried to prepare microspheres for injection containing 10% bendamustine and 10% fluorouracil. 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 15-25 days, and the drug release time in mice subcutaneous is about 30-40 days.

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Abstract

The slow released compound anticancer injection containing bendamustine 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 the composition of bendamustine and bendamustine synergist selected from antitumor antibiotic and antimetabolite. The slow releasing supplementary material is polylactic acid / glycolic acid copolymer, polyethylene glycol / polylactic acid, EVAc, etc. 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. The present invention can inhibit the growth of tumor effectively and enhance the curative effect of chemotherapy, radiotherapy and other non-operative treatment.

Description

(1) Technical field [0001] The invention relates to a compound anticancer slow-release agent containing bendamustine, which belongs to the technical field of medicines. Specifically, it is a slow-release preparation against solid tumors, including slow-release injections and slow-release implants. (2) Background technology [0002] As a new chemotherapeutic drug, bendamustine has been widely used in the treatment of various malignant tumors such as leukemia, lymphoma, breast cancer, and ovarian cancer, and the effect is relatively obvious. However, its obvious systemic toxicity greatly limits the application of this drug. [0003] Not only that, blood vessels, connective tissue, matrix proteins, fibrin, 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 the surrounding tumor and tumor tissue. Penetration and diffusion within (see Netti et al. "The influence o...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K45/00A61K31/4184A61K31/7076A61K47/34A61K47/38A61P35/00A61K47/26A61K47/36A61K47/42
Inventor 孙宪君
Owner JINAN SHUAIHUA PHARMA TECH
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