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
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Embodiment 1
[0106] 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 Violet tetrazolium and 10 mg marimastat were re-shaken and spray-dried to prepare microspheres for injection containing 10% violet tetrazolium 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
[0108] 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:
[0109] (a) 2-40% of marimastat, SU5416, SU6668, fumagillin or TNP-470 and 2-40% of tetrazole violet, p-iodonitrotetrazole violet or nitrotetrazole violet combination;
[0110] (b) 2-40% of gefitinib, erlotinib, lapatinib, vatalanib, peritinib, carboxyaminotriazole, thalidomide, ranolamid, angiostatin, endostatin , endostatin, imatinib mesylate, semazinil, dasatinib, Avastin, canertinib, sorafenib, sunitinib, Teosta, or penito Combinations of horses with 2-40% of violet tetrazolium, p-iodonitro violet tetrazolium or nitro violet tetrazolium.
Embodiment 3
[0112] Put 70mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 65,000 into a container, add 100ml of dichloromethane, dissolve and mix well, then add 15mg of fumagillin and 15mg of p-iodonitrotetrazolium violet, Shake again and 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% p-iodonitrotetrazolium violet, and then suspending in physiological saline containing 1.5% sodium carboxymethylcellulose , to prepare 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
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