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A technology of topozyme inhibitor and sustained-release injection, which is applied in the fields of sustained-release gel injection, temperature-controlled sustained-release injection, and sustained-release gel preparation, and can solve the problem of tumor cell seeding or dissemination, tissue trauma, and ineffective tumor cells. Clearing etc.
Inactive Publication Date: 2008-07-30
SHANDONG LANJIN PHARMA +1
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Problems solved by technology
Therefore, in most cases, the final sustained-release formulations are mostly solid shapes (eg, microspheres, tablets, or rods), which require a more complicated implantation process and are prone to tissue trauma and even tumor cell seeding or disse
Method used
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Embodiment 1
[0047] Put 4, 2, 1 and 0.5g of amphiphilic block copolymers (PLGA-PEG-PLGA) into four containers of A, B, C and D respectively, and then pour them into four containers of A, B, C and D respectively Add 6, 8, 9 and 9.5 milliliters of water for injection into the container to prepare 40%, 20%, 10% and 5% hydrogels.
[0048] The molecular weight of polyethylene glycol in the amphiphilic block copolymer is 800-1200, accounting for 20% of the weight of the amphiphilic block copolymer; in the glycolide-lactide copolymer, the ratio of glycolide and lactide The molar ratio is 6:1.
Embodiment 2
[0050] Measure the gelation temperature of four kinds of hydrogels in embodiment 1, the result shows that the gelation temperature of 40% and 20% hydrogel is respectively 28 ℃ (40%) and 35 ℃ (20%), and 10 The gelation temperatures of the % and 5% hydrogels were not determined at 10°C-38°C.
Embodiment 3
[0052] Put 4, 2, 1 and 0.5g of amphiphilic block copolymers (PLGA-PEG-PLGA) into four containers of A, B, C and D respectively, and then pour them into four containers of A, B, C and D respectively Add 6, 8, 9 and 9.5 milliliters of water for injection into the container to prepare 40%, 20%, 10% and 5% hydrogels.
[0053] The molecular weight of polyethylene glycol in the amphiphilic block copolymer is 1200-1600, accounting for 15% of the weight of the amphiphilic block copolymer; in the glycolide-lactide copolymer, the ratio of glycolide and lactide The molar ratio is 4:1.
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Abstract
A temperature control sustained release injection comprising topoisomerase inhibitor is composed of the topoisomerase inhibitor with an effective anti-cancer amount, an amphiphilic block copolymer, menstruum, and medicine release regulator with a fixed amount; wherein, the amphiphilic block copolymer consists of polyethylene glycol and polyester and an aqueous liquid of the amphiphilic block copolymer under a room temperature can change into a semi-solid or solid gel which can be absorbed by biodegradation and insoluble in water in a body of a hot blood animal; thereby being able to slowly release the Polyphosphate 3-Kinase inhibitor comprised in partial knub for a plurality of weeks to a plurality of months; an anti-cancer sustained release injection, being injected in the knub or in the surroundings of the knub or being arranged in a knub cavity after operation, can remarkably reduce the general reaction of the medicine, selectively enhance the curing effects of non operative treatments like chemotherapy and radiotherapy, and is used for curing the knub of different stages. The topoisomerase inhibitor is selected from self-hydroxy camptothecin, lartotecan, topotecan, irinotecan, etoposide, teniposid, podophyllotoxin, amrubicin, doxorubicin, esorubicin, pirarubicin and valrubicin.
Description
(1) Technical field [0001] The invention relates to a temperature-controlled slow-release injection containing a topoase inhibitor, which belongs to the technical field of medicines. Specifically, the invention relates to a slow-release gel preparation capable of stably releasing topoase inhibitors locally in solid tumors, mainly a slow-release gel injection. The slow-release gel preparation is an aqueous solution at room temperature, In animals, it can become a semi-solid or solid gel, so that the included topoase inhibitor can be slowly released locally in the tumor, from several days to several weeks. (2) Background technology [0002] Local application of chemotherapeutic drugs, especially local sustained release, has become the current research direction and focus of solid tumor chemotherapy. However, the current biodegradable sustained and controlled release preparations mostly use solid polymers such as polyglycolic acid, polylactic acid or their copolymers as sustai...
Claims
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