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Slow released compound anticancer injection containing bendamustine

A technology of sustained-release injection and bendamustine, which is applied in the field of compound anticancer drug sustained-release preparation, sustained-release injection and sustained-release implant, and can solve the problems of complicated surgical operation, large trauma, decreased immunity, etc. , to achieve the effect of increasing drug concentration, reducing drug concentration and reducing complications

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 Qet 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

[0119] 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 bendamustine 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% bendamustine 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

[0121] As described in Example 1, the difference is that the anticancer active ingredient and weight percentage are one of the following:

[0122] (a) 2-40% bendamustine and 2-40% bleomycin, daunorubicin, diethoxyacetamicin, nocardin, nocardioerythrin, norcardiac Carbamycin, nogamycin, mitomycin, polymyxin E, pirinomycin, dirithromycin, antramycin, pelomycin, puromycin, spamycin , Anthramycin, Caminomycin, Puromycin, Azurubicin, Aclarubicin-B, Idarubicin, Serpentin, Clarithromycin, Adazol Hydrochloride, Adidas Zol, doxorubicin, epirubicin, valrubicin, pirarubicin, loxantrone, loxoxantrone, mitoxantrone, pyroxantrone, tiloxantrone, or clozocin a combination of; or

[0123] (b) 2-40% bendamustine with 2-40% pemetrexed, pemetrexed disodium, lumitrexed, carmofur, tegafur, temozolomide, zalcitabine , Emtricitabine, Galloitabine, Ibacitabine, Ancitabine, Decitabine, Flucitabine, Enoxitabine, Mizocitabine, Capecitabine, Gemcitabine, Fludarabine , raltitrexed, raltitrexed, dexrazo...

Embodiment 3

[0126] 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 of doxorubicin were re-shaken and spray-dried to prepare microspheres for injection containing 10% bendamustine 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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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 and its copolymer, polifeprosan, EVAc, etc or their composition. The .suspending agent has viscosity of 80-3000 cp. The slow released microsphere may be also prepared into slow released implanting agent. The present invention can inhibit the growth of tumor 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 sustained-release injection, which belongs to the technical field of medicines. Specifically, the present invention provides a sustained-release compound anticancer drug containing bendamustine and its synergist, mainly sustained-release injections and sustained-release implants. (2) Background technology [0002] As a new chemotherapeutic drug, bendamustine has been widely used in the treatment of childhood acute myeloid leukemia (ALL), lymphoma, adult leukemia, breast cancer and ovarian cancer and other malignant tumors, and the effect is relatively obvious. However, its obvious systemic toxicity greatly limits the application of this drug. [0003] In addition, 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 periphery o...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K45/00A61K31/4184A61K31/704A61K31/7076A61K47/34A61K47/38A61P35/00A61K47/26
Inventor 孔庆伦
Owner JINAN SHUAIHUA PHARMA TECH
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