Taxane derivative TM-2 micellar injection, preparation method thereof and application thereof

A technology of TM-2 and taxanes, applied in the field of medicine, can solve the problems of complex preparation process of lipid microsphere injection, unstable preparation, high drug concentration, etc., so as to avoid severe allergic reactions and peripheral neuropathy, Good stability and high drug loading effect

Inactive Publication Date: 2019-01-11
沈阳东星医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But there are following problems in CN104323990: 1, TM-2 lipid microsphere injection can't realize higher drug concentration, is generally 1~2mg / ml, if increase drug concentration, then preparation is unstable, and problems such as oil-water separation can occur
2. The preparation process of lipid microsphere injection is relatively complicated and the cost is relatively high
3. Lipid microsphere injection will use a large amount of phospholipids, which itself contains a small amount of lysophospholipids. Lysophospholipids will also be produced during the preparation and placement process, which may cause hemolysis
4. Long-term storage of lipid microsphere injection may cause stability problems such as oil-water layering

Method used

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  • Taxane derivative TM-2 micellar injection, preparation method thereof and application thereof
  • Taxane derivative TM-2 micellar injection, preparation method thereof and application thereof
  • Taxane derivative TM-2 micellar injection, preparation method thereof and application thereof

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Embodiment 1

[0038] This embodiment provides a taxane derivative TM-2 micellar injection, which includes the following components: mPEG-PLA, TM-2, lyoprotectant, water for injection; wherein mPEG-PLA, TM- 2. The composition of the freeze-drying protective agent according to the mass percentage is: mPEG-PLA 10.8%, TM-2 2.7%, and the freeze-drying protective agent 86.5%. The mPEG-PLA is a block copolymer of polyethylene glycol monomethyl ether and polylactic acid, wherein the molar ratio between the polyethylene glycol monomethyl ether and the polylactic acid is 1:1; The molecular weight of glycol monomethyl ether is 2000, the molecular weight of the polylactic acid is 2000, and the molecular weight of the mPEG-PLA is 4000.

[0039] The lyoprotectant is used in combination with PEG4000 and sucrose, and the weight ratio of the two is 1:1.

[0040] The preparation method of the taxane derivative TM-2 micellar injection comprises the following steps:

[0041] (1) According to the above-mentione...

Embodiment 2

[0047] This embodiment provides a taxane derivative TM-2 micellar injection, which includes the following components: mPEG-PLA, TM-2, lyoprotectant, water for injection; wherein mPEG-PLA, TM- 2. The composition of the freeze-drying protective agent according to the mass percentage is: mPEG-PLA 15.1%, TM-2 3.1%, and the freeze-drying protective agent 81.8%. The mPEG-PLA is a block copolymer of polyethylene glycol monomethyl ether and polylactic acid, wherein the molar ratio between the polyethylene glycol monomethyl ether and the polylactic acid is 1:1; The molecular weight of glycol monomethyl ether is 4000, the molecular weight of the polylactic acid is 5000, and the molecular weight of the mPEG-PLA is 9000.

[0048] The freeze-drying protectant is a combination of poloxamer 188, sucrose and hydroxyethyl starch, and the weight ratio of the three is 1:1:1.

[0049] The preparation method of the taxane derivative TM-2 micellar injection comprises the following steps:

[0050]...

Embodiment 3

[0056] This embodiment provides a taxane derivative TM-2 micellar injection, which includes the following components: mPEG-PLA, TM-2, lyoprotectant, water for injection; wherein mPEG-PLA, TM- 2. The composition of the freeze-drying protective agent according to the mass percentage is: mPEG-PLA 50%, TM-2 10.5%, and the freeze-drying protective agent 39.5%. The mPEG-PLA is a block copolymer of polyethylene glycol monomethyl ether and polylactic acid, wherein the molar ratio of the polyethylene glycol monomethyl ether to the polylactic acid is 1:1.25; The molecular weight of glycol monomethyl ether is 2000, the molecular weight of the polylactic acid is 2500, and the molecular weight of the mPEG-PLA is 4500.

[0057] The lyoprotectant is HAS.

[0058] The preparation method of the taxane derivative TM-2 micellar injection comprises the following steps:

[0059] (1) According to the above-mentioned mass percentage ingredients, first mix mPEG-PLA and TM-2 with dichloromethane to ...

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Abstract

The invention provides a taxane derivative TM-2 micellar injection, a preparation method thereof and an application thereof. The injection comprises the following ingredients: mPEG-PLA, TM-2, lyophilize that protective agent and injecting water. The preparation method comprises that follow steps: after ingredients are mixed, uniformly mixing mPEG-PLA and TM-2 with an organic solvent; removing organic solvent; adding preheated injection water to make the carrier material hydrate and self-assemble, then passing through a 0.22 mu m filter membrane to remove the unencapsulated drug; adding lyophilized protective agent, then passing through a 0.45 mu m filter membrane to filter coarsely, and then passing through a 0.22 mu m filter membrane to filter finely; and at last, obtaining the drug-loaded micellar lyophilize powder, and obtaining the taxane derivative TM-2 micellar injection by diluting the drug-loaded micellar lyophilized powder with water for injection to a desired concentration. The invention can effectively reduce the toxic and side effects of the traditional preparation of taxanes, has the advantages of high drug loading amount, good stability, targeting and sustained-release effect, and improves the pharmaceutical effect, etc.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a taxane derivative TM-2 micellar injection and a preparation method and application thereof. Background technique [0002] Cancer has been threatening human health since ancient times, and medical workers have never stopped researching anti-tumor cell drugs. Nowadays, the treatment of tumor cells is to kill tumor cells and prevent the proliferation of tumor cells. However, large doses of anti-tumor drugs with low drug loading will kill normal cells and have extremely toxic side effects. The unstable factors generated during the storage of medicines are also challenges that the pharmaceutical industry and medical workers are currently facing. [0003] Taxanes are anti-tumor active ingredients isolated from plants, and a series of derivatives synthesized by structural modification of the obtained active ingredient compounds. Taxane drugs mainly include paclitaxel, d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/34A61K31/337A61P35/00
CPCA61K9/0019A61K9/1075A61K31/337A61K47/34A61P35/00
Inventor 唐星黄浩尹湉刘懿王俏
Owner 沈阳东星医药科技有限公司
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