Slow-releasing injection contg anticarcinogen of Jixitabin
A technology of sustained-release injection and gemcitabine, which is applied in the field of compound anti-cancer drug sustained-release preparation, sustained-release injection and sustained-release implant, and can solve problems such as difference in sensitivity of chemotherapeutic drugs and failure of tolerance treatment.
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Embodiment 1
[0127] 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 Pemetrexed and 7-hydroxyl-staurosporine, re-shaken and spray-dried to prepare microspheres for injection containing 10% pemetrexed 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. The viscosity of the injection is 400cp-600cp (at 20°C-30°C).
Embodiment 2
[0129] 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:
[0130] (1) 1-40% Pemetrexed, Pemetrexed Disodium, Lumitrexed, Raltitrexed, Raltitrexed, Noratrexed, Carmofur, Dexrazoxane, Tega Fluorine, temozolomide, zalcitabine, emtricitabine, gallocitabine, ibacitabine, ancitabine, decitabine, flucitabine, enoxitabine, midazitabine, capecitabine Bine, gemcitabine, fludarabine, or cladribine;
[0131] (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...
Embodiment 3
[0134] 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 raltitrexed 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 was frozen and pulverized to make a micropowder containing 15% raltitrexed and 15% 7-ethyl-10-hydroxycamptothecin, and then suspended in 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. The viscosity of the injection is 480cp-620cp (at 20°C-30°C)
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