Sustained-release injection containing nitrosourea drugs
A technology of sustained-release injection and nitrosourea, which is applied in the field of medicine and can solve problems such as treatment failure and enhanced tolerance
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Embodiment 1
[0113] Put 80, 80 and 80 mg of p(BHET-EOP / TC) (BHET-EOP: TC is 80:20) copolymers into three containers of A, B and C respectively, and then add 100 ml of dichloromethane to each , after dissolving and mixing, add 20mg carmustine, 20mg camptothecin, 10mg carmustine and 10mg camptothecin respectively, shake up again and prepare 20% carmustine, 20% camptothecin with spray drying method Injection microspheres of thecine, and 10% carmustine and 10% camptothecin. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The release time of the sustained-release injection in physiological saline in vitro is 60-70 days, and the release time in mouse subcutaneous is more than 65 days.
Embodiment 2
[0115] The method step of being processed into sustained-release injection is the same as that of Example 1, but the difference is that the adjuvant used is p(BHET-EOP / TC) of 50:50, containing anticancer active ingredients and their weight percentages: 5-40% Combination of carmustine or nimustine with 1-20% camptothecin or hydroxycamptothecin.
Embodiment 3
[0117] Put 70 mg of p(LAEG-EOP) with a peak molecular weight of 10,000-25,000 into three containers of A, B, and C, respectively, and then add 100 ml of dichloromethane to each, dissolve and mix well, and pour into the three containers respectively Add 30mg carmustine, 30mg camptothecin, 25mg carmustine and 5mg camptothecin, re-shake and prepare 30% carmustine, 30% camptothecin, 25% carmustine by spray drying method Injectable microspheres of statin and 5% camptothecin. The dried microspheres are suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to prepare the corresponding suspension-type sustained-release injection. The drug release time of the sustained release injection in physiological saline in vitro is 65-70 days, and the drug release time in mice subcutaneous is about 70 days.
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