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Compound anticancer sustained-release injection containing clofarabine

A slow-release injection and compound technology, applied in the field of compound anti-cancer drug slow-release, slow-release injection and slow-release implants, can solve the problem of local formation of effective drug concentration in difficult tumors, accelerate tumor spread and metastasis, and effectively affect cost. implementation and other issues to achieve the effect of facilitating drug injection, reducing complications and reducing costs

Inactive Publication Date: 2009-01-28
JINAN KANGQUAN 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.1998Oct; 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

[0124] 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 clorabine 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 anticancer slow-release product containing 10% clorabine 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

[0126] As described in Example 1, the difference is that the anticancer active ingredient and weight percentage are one of the following:

[0127] (a) 2-40% clorabine and 2-40% bleomycin, daunorubicin, diethoxyacetamicin, nocardin, nocardioerythrin, nocardia-type Mycin, Nogamycin, Mitomycin, Polymyxin E, Pilimycin, Dirithromycin, Antramycin, Pelomycin, Puromycin, Spamycin, Anthracene Caminomycin, Caminomycin, Puromycin, Alarubicin, Aclarubicin-B, Idarubicin, Serpentin, Clarithromycin, Adazol Hydrochloride, Adazol, Combinations of doxorubicin, epirubicin, valrubicin, pirarubicin, loxantrone, loxoxantrone, mitoxantrone, pyroxantrone, tiloxantrone, or clozocin ;or

[0128] (b) 2-40% clorabine and 2-40% pemetrexed, pemetrexed disodium, lumitrexed, carmofur, tegafur, temozolomide, zalcitabine, Tritabine, gallocitabine, ibacitabine, ancitabine, decitabine, flucitabine, enoxitabine, midazitabine, capecitabine, gemcitabine, fludarabine, radium A combination of tetrozan, raltitrexe...

Embodiment 3

[0131] Put 80mg polyphenylene propane (p-CPP: sebacic acid (SA) at 20:80) copolymer into a container, add 100ml dichloromethane, dissolve and mix well, then add 10mg Rorabine and 10 mg doxorubicin were re-shaken and spray-dried to prepare microspheres for injection containing 10% clorabine 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 invention discloses a clofarabine compound anticancer slow-release injection which is an anticancer slow-release injection and consists of slow-release microspheres and solvent; wherein, the slow-release microspheres comprise anticancer effective ingredients and slow-release auxiliary materials; the solvent is a special solvent containing a suspending agent; the anticancer effective ingredients are combination of the clofarabine and a clofarabine synergist which is selected from antitumor antibiotics and / or antimetabolic drugs; the slow-release auxiliary materials are selected from one or combination of copolymer of racemic polyactic acid and copolymer thereof, copolymer of monomethyl polyethylene glycol or polyethylene glycol or carboxyl-terminated polyactic acid and polyactic acid, copolymer of bi-fatty acid and sebacic acid, poly-(erucic acid dimmer-sebacic acid), poly-(fumaric acid-sebacic acid), polifeprosan and EVAc; the suspending agent has 80cp-3000cp of viscosity; the slow-release microspheres also can be made into a slow-release implant, is injected or placed in tumor or around the tumor, and release drugs for about 40 days; the slow-release injection and the slow-implant can be applied separately so as to suppress the tumor growth or is applied with the non-operative treatment of chemoradiotherapy, and the like, in a combining way, so as to enhance the curative effect thereof significantly.

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 slow-release compound anticancer drug containing clorabine and its synergist, mainly slow-release injections and slow-release implants. (2) Background technology [0002] Clofarabine, as a new class of chemotherapy drugs, has been widely used in the treatment of childhood acute myeloid leukemia (ALL), relapsed or resistant acute myeloid leukemia (AML), adult leukemia and solid tumors and other malignancies. Tumors, and the effect is more 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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/08A61K31/7076A61P35/00
Inventor 孙忠厚
Owner JINAN KANGQUAN PHARMA TECH
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