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Compound sustained release injection containing newborn blood vessel inhibitor fumagillin

A slow-release injection and neovascularization technology, which is applied in the field of compound sustained-release preparations and its preparation, sustained-release injections and sustained-release implants, and can solve problems such as systemic toxicity and drug resistance limiting applications

Inactive Publication Date: 2008-07-23
JINAN KANGQUAN PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its obvious systemic toxicity and development of drug resistance greatly limit the application of this drug

Method used

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  • Compound sustained release injection containing newborn blood vessel inhibitor fumagillin
  • Compound sustained release injection containing newborn blood vessel inhibitor fumagillin
  • Compound sustained release injection containing newborn blood vessel inhibitor fumagillin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0111] 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 Hydroxycamptothecin and 10 mg marimastat were re-shaken and spray-dried to prepare injection microspheres containing 10% hydroxycamptothecin and 10% marimastat. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection with a viscosity of 220cp-460cp (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.

Embodiment 2

[0113] 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:

[0114] (1) 2-40% hydroxycamptothecin, mitozolomide, 4-carboxytemozolomide, docetaxel, oxaliplatin, heptaplatin, ifosfamide, lomustine, estramustine , formustine, samustine, etoposide, teniposide, vinblastine, anastrozole, fluorouracil, or mitomycin C; or

[0115] (2) 2-40% marimastat, SU5416, SU6668, fumagillin or TNP-470; or

[0116] (3) 2-40% hydroxycamptothecin, mitozolomide, 4-carboxytemozolomide, docetaxel, oxaliplatin, heptaplatin, ifosfamide, lomustine, estramustine , formustine, samustine, etoposide, teniposide, vinblastine, anastrozole, fluorouracil or mitomycin C with 2-40% marimastat, SU5416, SU6668, A combination of fumagillin or TNP-470.

Embodiment 3

[0118] 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, add 15 mg of fumagillin and 15 mg of lomustine, and re-shake Dry in vacuo to remove the organic solvent. Freezing and pulverizing the dried drug-containing solid composition to make micropowder containing 15% fumagillin and 15% lomustine, and then suspending in physiological saline containing 1.5% sodium carboxymethylcellulose to obtain the corresponding Suspension-type sustained-release injection with a viscosity of 300cp-400cp (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 invention relates to a compound sustained-released injection containing a neovascularization inhibitor, which comprises sustained-release microspheres and menstruum; wherein, the sustained-release microspheres are composed of sustained-release excipients, the neovascularization inhibitor selected from marimastat or fumagillin, etc. and a cytotoxic drug selected from hydroxyl campto thecine, mitozolomide, 4-carboxyl temozolomide, docetaxel, oxaliplatin, hetaplatin, ifosfamide, lomustine, estramustine, fotemustine, samustine, etoposide, teniposide, vinblastine, anastrozole, fluorouracil or mitomycin C. The menstruum is special menstruum containing a suspending agent. The sustained-release excipients are selected from polifeprosan, polylactic acid, decanedioic acid polymer, such as poly (erucic acid dipolyme-decanedioic acid) and poly (allomaleic acid-decanedioic acid), etc. and EVAc, etc; the suspending agent, the viscosity of which is 100cp-3000cp (between 25 DEG C and 30 DEG C), is selected from carboxymethylcellulose sodium, etc. The sustained-release microspheres can also be prepared to be a sustained-release implant. The sustained-release implant is injected or deposited to the interior of tumour or around the tumour, which can improve the treatment effect of non-operative treatments, such as radio-chemotherapy, etc.

Description

(1) Technical field [0001] The invention relates to a compound slow-release agent containing angiogenesis inhibitor and a preparation method thereof, belonging to the technical field of medicines. Specifically, the present invention provides a slow-release preparation of anticancer drugs containing angiogenesis inhibitors and / or cytotoxic drugs, mainly slow-release injections and slow-release implants. (2) Background technology [0002] Angiogenesis is necessary for the growth and metastasis of solid tumors. When the diameter of solid tumor is larger than 0.5cm, tumor cells depend on their own vascular system. Tumor cells can obtain nutrients and oxygen from the host through tumor blood vessels, and can continuously transport metastatic cells to the host through tumor blood vessels, and continue to grow and induce blood vessel formation in other parts of the body, leading to tumor metastasis. The emergence of new metastases is the main reason for treatment failure. Theref...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/336A61K31/7048A61K47/34A61P35/00A61K47/26A61K47/32A61K47/36A61K47/42
Inventor 田绍兰
Owner JINAN KANGQUAN PHARMA TECH
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