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

A new blood vessel and violet technology, applied in the preparation of sustained-release preparations, sustained-release injections and sustained-release implants, can solve problems such as systemic toxicity and drug resistance limiting applications

Inactive Publication Date: 2007-03-14

SHANDONG LANJIN PHARMA

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AI-Extracted Technical Summary

Problems solved by technology

However, its obvious systemic toxicity and development of ...

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 acid copolymer, 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 agent can 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.

Application Domain

Solution deliveryPharmaceutical non-active ingredients +3

Technology Topic

Sodium carboxymethylcelluloseDepressant +27

Examples

Experimental program(21)

Example Embodiment

[0105] Example 1.

[0106] 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.

Example Embodiment

[0107] Example 2.

[0108] 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:

[0109] (a) 2-40% of marimastat, SU5416, SU6668, fumagillin or TNP-470 and 2-40% of tetrazolium violet, p-iodonitrotetrazole violet or nitrotetrazolium violet combination;

[0110] (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.

Example Embodiment

[0111] Example 3.

[0112] 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 again 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.

PUM

Property	Measurement	Unit
Viscosity	220.0 ~ 460.0	cp
Viscosity	100.0 ~ 200.0	cp
Viscosity	560.0 ~ 640.0	cp

Description & Claims & Application Information

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