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Slow released anticancer medicine injection containing bendamustine and its synergist

A technology for carrying bendamustine and sustained-release injections, which is applied in the fields of sustained-release injections and sustained-release implants, compound anti-cancer drug sustained-release injections, and compound anti-cancer drug sustained-release preparations, and can solve the problem of anticancer drug resistance. Receptivity enhancement, treatment failure, etc.

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

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 Bendamustine and 7-hydroxyl-staurosporine, re-shaken and spray-dried to prepare injection containing 10% bendamustine and 10% 7-hydroxyl-staurosporine Microspheres. 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 14-20 days, and the drug release time in mice subcutaneous is about 30-40 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) 2-40% bendamustine and 1-40% 7-hydroxyl-staurosporine, 7-O-alkyl-staurosporine, β-methoxystaurosporine , a combination of alkylphosphorylcholine or hexadecylphosphorylcholine;

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

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

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 bendamustine and 15 mg of 7-ethyl-10-hydroxyl The resin was shaken again and dried under vacuum to remove the organic solvent. Freezing and pulverizing the dried drug-containing solid composition to make micropowder containing 15% bendamustine and 15% 7-ethyl-10-hydroxycamptothecin, and then suspending in 1.5% sodium carboxymethylcellulose The corresponding suspension-type sustained-release injection was prepared in normal saline. 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

The slow released compound anticancer injection containing bendamustine and its synergist 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 phosphoinositide 3-kinase inhibitor, pyrimidine analog and DNA repairase inhibitor. The slow releasing supplementary material is polylactic acid and its copolymer, polifeprosan, EVAc or other biocompatible polymer. The .suspending agent is carboxymethyl cellulose, etc. and has viscosity of 100-3000 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 and enhance the curative effect of chemotherapy, radiotherapy and other non-operative treatment.

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 sustained-release compound anticancer drug containing bendamustine and its synergist, mainly sustained-release injections and sustained-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 pl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K45/00A61K31/4184A61K47/34A61K47/38A61P35/00A61K47/32A61K47/36A61K47/42
Inventor 孙中先
Owner JINAN SHUAIHUA PHARMA TECH
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