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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 sustained-release injections and sustained-release implants, compound anti-cancer drug sustained-release preparations, and compound anti-cancer drug sustained-release injections, and can solve treatment failure, anti-cancer drug resistance Receptivity enhancement and other issues

Inactive Publication Date: 2008-09-03
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

[0145] 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

[0147] 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:

[0148] (1) 1-40% clorabine and 1-40% 7-hydroxyl-staurosporine, 7-O-alkyl-staurosporine, β-methoxystaurosporine, alkane A combination of phosphocholine or hexadecylphosphorylcholine;

[0149] (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

[0150] (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

[0153] 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

A slow release anticancer injection carrying clofarabine and a synergist thereof comprises slow release microspheres and a solvent, wherein the slow release microspheres comprise effective anticancer ingredients and slow release adjuvants, and the solvent is a special solvent containing a suspending agent. The effective anticancer ingredients comprise clofarabine and a clofarabine synergist selected from phosphoinositol-3-kinase inhibitor, pyrimidine analogues and / or DNA repairase inhibitor; the slow release adjuvants comprise biocompatible polymers such as polylactic acid (PLA) and copolymer thereof, polylactic acid-polyethylene glycol (PEG)-COOH copolymers, fatty acid dimmer-sebacic acid copolymers, polys(erucic acid dimmer-sebacic acid), polys(fumaric acid-sebacic acid), polifeprosan, polylactic acid and EVAc; the suspending agent has viscosity of 100-3,000cp (at 20-30 DEG C) and is selected from sodium carboxymethyl cellulose, etc. The effective anticancer ingredients and the slow release microspheres can also be made into slow release implant, and the slow release injection and implant can be injected into tumor or around tumor to effectively inhibit tumor growth and remarkably strengthen the effect of non-surgery treatments as chemotherapy or the like.

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.1998 Oct; 69(2):76-82). [0003] Local placement of chemoth...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/08A61K31/7076A61K45/06A61K47/30A61P35/00
Inventor 孔庆新
Owner JINAN KANGQUAN PHARMA TECH
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