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An anticancer sustained release injection carrying clorfarabine and its synergist

A technology for sustained-release injections and anti-cancer drugs, which is applied in the fields of compound anti-cancer drug sustained-release injections, compound anti-cancer drug sustained-release preparations, sustained-release injections and sustained-release implants, and can solve the problem of enhanced tolerance to anti-cancer drugs. , treatment failure, etc.

Inactive Publication Date: 2006-12-13
JINAN KANGQUAN PHARMA TECH
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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

[0135] 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 Clorabine and 7-hydroxyl-staurosporine, re-shake and spray-dry to prepare microspheres for injection containing 10% clorabine and 10% 7-hydroxyl-staurosporine. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. 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

[0137] 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:

[0138] (1) 1-40% clorabine and 1-40% 7-hydroxyl-staurosporine, 7-O-alkyl-staurosporine, β-methoxystaurosporine, alkane A combination of phosphocholine or hexadecylphosphorylcholine;

[0139] (2) 1-40% clorabine and 1-40% O4-benzyl folic acid, 2,4,5-triamino-6-benzyloxypyrimidine, 2,4-diamino-6-benzyloxy Base-5-nitrosopyrimidine, 2,4-diamino-6-benzyloxy-5-bromopyrimidine, 2-amino-4-benzyloxy-5-nitropyrimidine, 2-amino-4- A combination of benzyloxy-6-methyl-5-nitropyrimidine, 2,4-diamino-6-benzyloxy-s-triazine or 2-amino-O4-benzylpteridine; or

[0140] (3) 1-40% clorabine and 1-40% imidazopiperazine, imidazopyridine, wortmannin, benzopyran, 6-aryl-2-morphol-4-yl-pyridine Fyran-4-yl, 2-(4-morpholinyl)-8-phenylchromone, 7-ethyl-10-hydroxycamptothecin, 3-cyano-6-hydrazono...

Embodiment 3

[0143] 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, then add 15 mg of clorabine and 15 mg of 7-ethyl-10-hydroxycamptothecin , shake again and dry in vacuo to remove the organic solvent. The dried drug-containing solid composition is frozen and pulverized to make micropowder containing 15% clorabine and 15% 7-ethyl-10-hydroxycamptothecin, and then suspended in a physiological solution containing 1.5% sodium carboxymethylcellulose. In saline, the corresponding suspension-type sustained-release injection was prepared. The drug release time of the slow-release injection in physiological saline in vitro is 20-35 days, and the drug release time in mice subcutaneous is about 35-50 days.

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Abstract

Disclosed is an anticancer slow release injection carrying both clofarabine and its synergistic agent, which comprises slow release micro-balloons and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being specific dissolvent containing suspension adjuvant. The anticancer effective ingredients include clofarabine and its synergistic agents selected from phosphoinositide-3-enzyme inhibitor, pyrimidine analog and / or DNA restoring enzyme inhibitor, the slow release auxiliary materials are selected from polylactic acid and copolymer, polyethylene glycol, PLA-COOH copolymer, di-aliphatic acid and sebacylic acid copolymer, poly(erucic aciddipolymer-sebacylic acid), poly(fumaric acid-sebacylic acid), Polifeprosan, poly(lactic acid) and EVAc, the viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C), and is selected from sodium carboxymethylcellulose.

Description

(1) Technical field [0001] The invention relates to a sustained-release injection of a compound anticancer drug, belonging 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] Currently, chemotherapy is still the main treatment for cancer. However, traditional chemotherapy is not selective, and it is difficult to form an effective drug concentration or therapeutic dose locally in the tumor. The effect is poor and the toxicity is high. Simply increasing the drug or radiation dose 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.1998Oct; 69 (2): 76-82). [0003] Local placement of chemot...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K45/00A61K31/7076A61K47/34A61P35/00
Inventor 孔庆新
Owner JINAN KANGQUAN PHARMA TECH
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