Temperature controlled sustained-release injection containing steroids anti-cancer drugs
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A technology of slow-release injections and slow-release gel injections, which is applied in the fields of slow-release gel injections, slow-release gel preparations, and temperature-controlled slow-release injections. Problems with planting or spreading
Inactive Publication Date: 2008-10-01
SHANDONG LANJIN PHARMA +1
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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 dissemination
In addition, organic solvents or high-heat processes often lead to the degradation and denaturation of many anti-cancer active ingredients, and solid implants cannot effectively cover the irregular tumor cavity after tumor resection. relapse
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Embodiment 1
[0048] 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.
[0049] 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
[0051] 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
[0053] 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.
[0054] 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
The invention relates to a temperature-controlled sustained-release injection containing a hormone anti-cancer drug, which comprises the anti-cancer drug, an amphiphilic block copolymer, a solvent and a certain amount of drug release regulator, wherein, the mixture of the amphiphilic block copolymer and a solvent without organic solvent has the temperature-sensitive gelatinization feature, which is flowable liquid in the environment that is lower than the body temperature and can be automatically converted to the water-insoluble gel that can not flow and be biodegradable for absorption in an endotherm, and the water-insoluble gel can allow the contained hormone anti-cancer drug to have the local sustained release in a tumor and maintain the effective drug concentration for a plurality of weeks to a plurality of months; the viscosity of the temperature-controlled sustained-release injection is 10cp to 3000cp ( at 5 DEG C to 30 DEG C ), and the gelatinization temperature is 35 DEG C to 37 DEG C. The sustained-release injection can be injected in the tumor or the tumor periphery or be arranged in the postoperative tumor cavity, thus significantly reducing the systemic reaction of the drug, selectively strengthening the treatment effects of chemotherapy, radiotherapy and other non-surgical therapies, and being used for the treatment of the tumors in different stages. The anti-cancer drug can be triptorelin, goserelin, leuprorelin, anastrozole, idoxifene, tamoxifen and other hormone anti-cancer drugs.
Description
(1) Technical field [0001] The invention relates to a temperature-controlled slow-release injection containing hormone anticancer drugs, belonging to the technical field of medicines. Specifically, the invention relates to a slow-release gel preparation capable of stably releasing hormonal anticancer drugs locally in solid tumors, mainly a slow-release gel injection. The slow-release gel preparation is an aqueous solution at room temperature, The body of a warm-blooded animal can become a semi-solid or solid gel, so that the contained hormone anticancer drugs can be slowly released in the local 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 a...
Claims
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