Gel injection of sustained-released topology enzyme inhibitor and preparation method thereof

A technology of sustained-release gel injection and topozyme inhibitor, which is applied in the field of sustained-release gel injection and can solve the problems of ineffective removal of tumor cells, inability to effectively control postoperative recurrence, tissue trauma, and the like

Inactive Publication Date: 2009-01-07
济南基福医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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 dissemination
In addition, organic solvents or high heat processes of

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0073] Put 4, 2, 1 and 0.5g amphiphilic block copolymer (PLGA-PEG-PLGA) into the four containers of A, B, C, and D respectively, and then transfer to the four containers of A, B, C and D respectively. Add 6, 8, 9 and 9.5 milliliters of water for injection to the container to prepare 40%, 20%, 10% and 5% hydrogels;

[0074] 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; The molar ratio is 6:1;

[0075] The preparation of microspheres is prepared by double emulsion method or O / W method. The auxiliary material in sustained-release microspheres is polylactic acid / glycolic acid copolymer. Among them, the blending ratio of lactic acid (LA) and glycolic acid (GA) can be 75 / 25(W / W), the molecular weight of the copolymer of lactic acid and glycolic acid (PLGA) can be 15000-38000, and the weight ratio of copolymer to camptothecin is 9:1.

Embodiment 2

[0077] The gelation temperatures of the four hydrogels in Example 1 were measured, and the results showed that the gelation temperatures of 40% and 20% hydrogels were 32°C (40%) and 36°C (20%), respectively, and 10 The gelation temperature of the% and 5% hydrogels was not measured at 10°C-38°C.

Embodiment 3

[0079] Put 4, 2, 1 and 0.5g amphiphilic block copolymer (PLGA-PEG-PLGA) into the four containers of A, B, C, and D respectively, and then transfer to the four containers of A, B, C and D respectively. Add 6, 8, 9 and 9.5 milliliters of water for injection to the container to prepare 40%, 20%, 10% and 5% hydrogels;

[0080] 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; The molar ratio is 4:1;

[0081] The preparation of microspheres is prepared by double emulsion method or O / W method. The auxiliary material in sustained-release microspheres is polylactic acid / glycolic acid copolymer. Among them, the blending ratio of lactic acid (LA) and glycolic acid (GA) can be 75 / 25(W / W), the molecular weight of the copolymer of lactic acid and glycolic acid (PLGA) can be 25,000-35,000, and the weight ratio of the copolymer to hydroxycamptothecin is 6:4.

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Abstract

The invention relates to a slow-release topoismerase inhibitor gel injection which contains an anticancer-effective amount of topoismerase inhibitor microspheres (or microsphere and topoismerase inhibitor micropowder), an amphiphilic block polymer composed of polyethylene glycol and polyester, a solvent and a certain amount of slow-release regulator. The amphiphilic block polymer aqueous solution is liquid at the room temperature and turns into a semisolid or solid biodegradable water-insoluble gel in vivo in warm-blooded animals, so that the topoismerase inhibitor encapsulated therein is sustainedly and locally released around the tumor and the microspheres can further control the slow release for a plurality of weeks to a plurality of months. After the intratumoral injection or peritumoral injection or post-operative intracavitary injection or arterial embolization, the slow-release topoismerase inhibitor gel injection can significantly reduce the general drug reaction and selectively enhance the curative effect of non-operative treatment such as chemotherapy and radiotherapy, and is used for the treatment of tumors of different stages. The topoismerase inhibitor is selected from camptothecin, topoteean, etoposide, teniposide, esorubicin, pirarubicin and valrubicin.

Description

(1) Technical field [0001] The invention relates to a sustained-release gel injection containing a topozyme inhibitor, which belongs to the technical field of medicines. Part or all of the topozyme inhibitor in the gel sustained-release injection is present in the sustained-release microspheres. The dual sustained release of the gel and the microspheres can prolong the release time of the topoenzyme inhibitor contained in the local tumor. Several weeks to several months. (2) Background technology [0002] There are many ways to treat solid tumors and many related studies have been reported. However, the survival conditions of most patients have not been significantly improved in the past few decades. Among various treatments, chemotherapy is still one of the commonly used options. Although conventional chemotherapy has been used for a long time, its therapeutic effect on solid tumors is uncertain. The fundamental problem is that traditional chemotherapy cannot achieve effective d...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K45/06A61K47/34A61P35/00
Inventor 张伟毛海婷
Owner 济南基福医药科技有限公司
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