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Anticancer slow release agent loading both newborn blood vessel and tetrazole violet

A technology for violet and sustained-release injections, which is applied in the field of sustained-release injections and sustained-release implants, and the preparation of sustained-release preparations, which can solve the problems of systemic toxicity and drug resistance that limit the application.

Inactive Publication Date: 2010-03-24
SHANDONG LANJIN PHARMA
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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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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0112] Put 80mg of polyphenylpropanine (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) 20:80) copolymer into the container, add 100ml of dichloromethane, dissolve and mix well, add 10mg Tetrazolium violet and 10mg marimastat were shaken again and spray-dried to prepare injection microspheres containing 10% tetrazolium violet and 10% marimastat. Then the microspheres were suspended 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 release time of the sustained-release injection in physiological saline in vitro is 10-15 days, and the release time under the skin of mice is about 20-30 days.

Embodiment 2

[0114] The method steps for processing into a sustained-release injection are the same as in Example 1, but the difference is that the anti-cancer active ingredients and their weight percentages are:

[0115] (a) 2-40% of marimastat, SU5416, SU6668, fumagillin or TNP-470 and 2-40% of tetrazolium violet, p-iodonitrotetrazole violet or nitrotetrazolium violet combination;

[0116] (b) 2-40% Gefitinib, Erlotinib, Lapatinib, Votaranib, Peritinib, Carboxyaminotriazole, Thalidomide, Ranolamide, Angiostatin, Endostatin , Endostatin, imatinib mesylate, simasini, dasatinib, avastin, canatinib, sorafenib, sunitinib, teosta, or panito A combination of horse and 2-40% tetrazolium violet, p-iodonitrotetrazolium violet or nitrotetrazolium violet.

Embodiment 3

[0118] Put 70mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 65000 into the container, add 100ml of dichloromethane, dissolve and mix well, add 15mg of fumagillin and 15mg of p-iodonitrotetrazolium violet, Shake well and vacuum dry to remove organic solvents. The dried medicinal solid composition was freeze-pulverized into a micropowder containing 15% fumagillin and 15% p-iodonitrotetrazolium violet, and then suspended in physiological saline containing 1.5% sodium carboxymethyl cellulose , Prepared the corresponding suspension type sustained-release injection, the viscosity is 300cp-400cp (20℃-30℃). The release time of the sustained-release injection in physiological saline in vitro is 10-15 days, and the release time under the skin of mice is about 20-30 days.

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PUM

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Abstract

Disclosed is an anticancer slow release injection carrying both anti-angiogenesis agent and tetrazole Ionone, which comprises slow release micro-balloons and dissolvent, the slow release micro-balloons include anticancer active constituents, slow release auxiliary materials and specific dissolvent containing suspension agent. The anti-angiogenesis agent is selected from Marimastat, Fumagillin, gefinitib, erlotinib, lapatinib, pelinib, Thalidomide, Ranolazine, endostatin, imatinib, Avastin, sorafenib, sunitinib, the slow release auxiliary materials are selected from Polifeprosan, sebacylic acidcopolymer, EVAc, polylactic acid and their mixture of copolymer, the viscosity of the suspension adjuvant is 100-3000cp (at 25-30 deg C), and is selected from sodium carboxymethylcellulose. The agentcan also be prepared into implanting agent for injection or placement in or around tumor with the effects of selectively increasing local concentration, lowering general reaction of the drugs, suppressing growth of tumor cells and blood vessel, and improving the treatment effect of the non-operative treatment methods such as chemotherapy.

Description

(1) Technical field [0001] The invention relates to a sustained-release agent carrying both neovascularization inhibitor and tetrazolium violet and its preparation method, which belongs to the technical field of medicine. Specifically, the present invention provides a sustained-release anti-cancer drug containing a neovascularization inhibitor and / or violet tetrazolium, mainly a sustained-release injection and a sustained-release implant. (2) Background technology [0002] Angiogenesis is necessary for the growth and metastasis of solid tumors. When the diameter of a solid tumor is greater than 0.5 cm, the tumor cells depend on their own vascular system. Tumor cells can obtain nutrients and oxygen from the host through tumor blood vessels, and they can continuously deliver 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...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61K31/41A61K45/06A61K47/34A61P35/00A61K47/32
Inventor 孔庆忠孙娟俞建江
Owner SHANDONG LANJIN PHARMA
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