Novel anticancer sustained-release injection
A technology of sustained-release injections and sustained-release excipients, applied in the field of medicine, can solve the problems of many complications, poor curative effect, and difficult operation.
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Embodiment 1
[0115] Put 80mg polyphenylene propane (p-CPP: sebacic acid (SA) 20:80) copolymer into a container, add 100ml methylene chloride, dissolve and mix well, then add 10mg Actinomycin D and 10 mg of formustine were re-shaken and spray-dried to prepare microspheres for injection containing 10% actinomycin D and 10% formustine. 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
[0117] 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:
[0118] (1) 2-40% formustine or bendamustine and 2-40% melphalan, 4H-peroxycyclophosphamide, vinorelbine, tamoxifen, methotrexate, doxorubicin , the combination of epirubicin or actinomycin D;
[0119] (2) 2-40% tamustine or carmustine and 2-40% melphalan, 4H-peroxycyclophosphamide, vinorelbine, tamoxifen, methotrexate, doxorubicin, A combination of epirubicin or actinomycin D;
[0120] (3) 2-40% nimustine or lomustine and 2-40% melphalan, 4H-cyclophosphamide peroxide, vinorelbine, tamoxifen, methotrexate, doxorubicin, a combination of epirubicin or actinomycin D; or
[0121] (4) 2-40% semustine or ramustine and 2-40% melphalan, 4H-peroxycyclophosphamide, vinorelbine, tamoxifen, methotrexate, doxorubicin, A combination of epirubicin or actinomycin D.
[0122] The su...
Embodiment 3
[0124] 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 carmustine and 15 mg of melphalan, re-shake and vacuum Dry to remove organic solvent. The dried drug-containing solid composition was frozen and pulverized to make micropowder containing 15% carmustine and 15% melphalan, and then suspended in physiological saline containing 1.5% carboxymethylcellulose sodium 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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