Marimastat sustained-release implant for treating solid tumor
A marimastat and slow-release implant technology, applied in the field of medicine, can solve the problems of failure to prolong the survival period of patients, decline in quality of life, systemic toxicity and side effects that limit clinical application, etc.
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Embodiment 1
[0075] Put the weighed (95 mg) sustained-release excipient (polylactic acid (PLA) with a molecular weight of 15000-25000) into a container, add a certain amount of organic solvent to dissolve and mix (subject to full dissolution), then add 5 mg of horse Immediately shake the mixture and dry it in vacuum to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain a slow-release implant containing 5% marimastat. The release time of the slow-release implant in physiological saline in vitro is 25-36 days, and the release time in mouse subcutaneous is 26-35 days.
Embodiment 2
[0077] Sustained-release implants were made according to the method described in Example 1, but the anti-cancer active ingredients contained were one of the following:
[0078] (A) 1% marimastat and 99% polylactic acid;
[0079] (B) 5% marimastat and 95% polylactic acid;
[0080] (C) 10% marimastat and 90% polylactic acid;
[0081] (D) 15% marimastat and 85% polylactic acid;
[0082] (E) 20% marimastat and 80% polylactic acid.
Embodiment 3
[0084] Put the weighed (97mg) sustained-release excipient (PLGA with a molecular weight of 15000-25000, 50:50) into the container, add a certain amount of organic solvent to dissolve and mix well (subject to complete dissolution), then add 3mg of Malima Sestat, re-shake, and then vacuum-dry to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain a sustained-release implant containing 3% marimastat. The release time of the sustained-release implant in physiological saline in vitro is 20-28 days, and the release time in mice subcutaneous is 24-28 days.
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