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Thermostatic sustained release injection containing taxane and preparing method thereof

A technology for sustained-release injections and taxanes, which is applied in the fields of temperature-controlled sustained-release injections, sustained-release gel injections, and sustained-release gel preparations, and can solve problems such as ineffective coverage, complex implantation process, and inability to effectively remove tumor cells, etc. question

Inactive Publication Date: 2008-07-30
SHANDONG LANJIN PHARMA +1
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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 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

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] 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.

[0047] 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

[0049] 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

[0051] 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.

[0052] 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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PUM

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Abstract

A temperature controlled and sow-released injection consists of taxane with anti-cancer effective quantity, amphiphilic block copolymer, menstruum and a certain quantity of medicine release regulating agent; wherein, the amphiphilic block copolymer consists of polyethylene glycol and polyester and the mixture with the menstruum belonging to organic solvent has temperature-sensitive gelation property; the mixture is flow liquid in the environment with the temperature under somatic temperature and can automatically converted into water insoluble gelatin which can not flow, be biodegraded and absorbed in the body of a warm blood animal, can slowly release the taxane in part of a tumor and can maintain the effective medicine concentration for a plurality of weeks and even mouths. The viscocity of the temperature controlled and sow-released injection is 10 to 3000 cp(5 to 30 DEG C), the temperature of the gelation is 35 to 37 DEG C. the anti-cancer slowly-release gelation injection carries on intra-tumor injection or is put into tumor cavity to cure tumors at different stages. The invention has the advantages of small side effect and obvious curing effect. The taxane is chosen from taxol, docetaxel, 2- hydroxide radical paclitaxel, 10-dehanoyl paclitaxel or 7-epi-taxol, etc.

Description

(1) Technical field [0001] The invention relates to a taxane-containing temperature-controlled slow-release injection, which belongs to the technical field of medicines. Specifically, the invention relates to a slow-release gel preparation capable of stably releasing taxanes locally in solid tumors, mainly a slow-release gel injection. The slow-release gel preparation is an aqueous solution at room temperature and can It can become a semi-solid or solid gel in the body, so it can slowly release the contained taxane 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 sustained release carriers. Due to the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/337A61K9/00A61K47/34A61K47/36A61K47/38A61K47/42A61P35/00A61K47/26
Inventor 孔庆忠刘玉燕
Owner SHANDONG LANJIN PHARMA