Compound sustained-released injection containing neonatal blood vessel restraining agent
A sustained-release injection and neovascularization technology, which is applied in the field of sustained-release injections, sustained-release implants, compound sustained-release preparations and their preparation, and can solve problems such as systemic toxicity and drug resistance limiting application
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Embodiment 1
[0111] 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 Hydroxycamptothecin and 10 mg marimastat were re-shaken and spray-dried to prepare injection microspheres containing 10% hydroxycamptothecin 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
[0113] 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:
[0114] (1) 2-40% hydroxycamptothecin, mitozolomide, 4-carboxytemozolomide, docetaxel, oxaliplatin, heptaplatin, ifosfamide, lomustine, estramustine , formustine, samustine, etoposide, teniposide, vinblastine, anastrozole, fluorouracil, or mitomycin C; or
[0115] (2) 2-40% marimastat, SU5416, SU6668, fumagillin or TNP-470; or
[0116] (3) 2-40% hydroxycamptothecin, mitozolomide, 4-carboxytemozolomide, docetaxel, oxaliplatin, heptaplatin, ifosfamide, lomustine, estramustine , formustine, samustine, etoposide, teniposide, vinblastine, anastrozole, fluorouracil or mitomycin C with 2-40% marimastat, SU5416, SU6668, A combination of fumagillin or TNP-470.
Embodiment 3
[0118] 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, add 15 mg of fumagillin and 15 mg of lomustine, and re-shake 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% lomustine, and then suspending in physiological saline containing 1.5% sodium carboxymethylcellulose to obtain 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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