An angiogenesis inhibitor and synergist thereof co-carried sustained-releasing anticancer medicinal injection
A technology for sustained-release injections and vascular inhibitors, 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 enhanced tolerance to anti-cancer drugs. , treatment failure and other problems, to achieve the effect of convenient drug injection, lower costs, and fewer complications
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Embodiment 1
[0146] 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 Gefitinib and 7-hydroxyl-staurosporine, re-shake and spray-dry to prepare microspheres for injection containing 10% gefitinib and 10% 7-hydroxyl-staurosporine . 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 10-15 days, and the drug release time in mice subcutaneous is about 20-30 days.
Embodiment 2
[0148] 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:
[0149] (1) 1-40% of gefitinib, erlotinib, lapatinib, vatalanib, peritinib, carboxyaminotriazole, thalidomide, ranolamid, angiostatin, endostatin , endostatin, imatinib mesylate, semazinil, dasatinib, Avastin, canertinib, sorafenib, sunitinib, Teosta, or penito horse;
[0150] (2) 1-40% of 7-hydroxyl-staurosporine, 7-O-alkyl-staurosporine, β-methoxystaurosporine, alkyl phosphorylcholine, hexadecyl phosphate Choline, octadecyl-(1,1-dimethyl-4-piperidine) phosphate, 1-O-hexadecyl-2-O-methyl-rac-glyceryl-3-phosphocholine , 1-O-octadecyl-2-O-methyl-rac-propanetriyl-3-phosphocholine, 1-O-octadecyl-2-O-methyl-sn-propanetriyl-3 - Phosphocholine, inositol polyphosphate, cyclosporine A, tetradecylphosphorylcholine, hexacylphospho(N-N-N-trimethyl)hexanolamine, octadecylphosphor...
Embodiment 3
[0154] 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 erlotinib and 15 mg of 7-ethyl-10-hydroxycamptotheca Alkali, shake again and dry in vacuo to remove organic solvents. The dried drug-containing solid composition is frozen and pulverized to make a micropowder containing 15% erlotinib and 15% 7-ethyl-10-hydroxycamptothecin, and then suspended in a solution containing 1.5% sodium carboxymethylcellulose In physiological saline, the corresponding suspension-type sustained-release injection was prepared. 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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