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Multiphase-stable albumin conjunction type cabazitaxel

A technology of albumin-binding type and cabazitaxel, which is applied in the direction of drug combination, medical preparations containing active ingredients, non-active ingredients of polymer compounds, etc. It can solve problems such as many influencing factors, difficulty in scale-up production, stability research, etc. , to achieve the effects of fewer process influencing factors, strict temperature control, and improved stability

Inactive Publication Date: 2015-04-08
SHENZHEN NEPTUNUS PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Methods such as high-pressure homogenization are not easy to achieve scale-up production, and the preparation process is complicated and there are many influencing factors
Chinese patent [Publication No. CN 102784109A] discloses a taxane drug albumin nanoparticle preparation for injection and its preparation method. The post-treatment uses a rotary evaporation method. To study its stability

Method used

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  • Multiphase-stable albumin conjunction type cabazitaxel
  • Multiphase-stable albumin conjunction type cabazitaxel
  • Multiphase-stable albumin conjunction type cabazitaxel

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Ratio of components in heterogeneously stable albumin-bound cabazitaxel (mg)

[0031]

[0032]

[0033] Preparation:

[0034] (1) Dissolving cabazitaxel, phospholipid and citric acid in an appropriate amount of chloroform / dichloromethane as the oil phase;

[0035] (2) Dissolving the prescription amount of albumin, phospholipids and mannitol in an appropriate amount of deionized water as the water phase;

[0036] (3) Add the oil phase prepared in (1) dropwise to (2), and grind it using a temperature-controllable planetary ball mill (ball milling speed 38Hz, ball milling temperature 4°C, ball milling time 1.5 hours), take out, pour After lyophilization, a heterogeneous and stable albumin-bound cabazitaxel was obtained. The particle size was measured using a laser particle size analyzer, and the result was 321 nm.

Embodiment 2

[0038] Ratio of components in heterogeneously stable albumin-bound cabazitaxel (mg)

[0039]

[0040] Preparation:

[0041] (1) Dissolving cabazitaxel, PEG-PLGA and citric acid in an appropriate amount of chloroform / dichloromethane as the oil phase;

[0042] (2) dissolving the prescribed amount of albumin, PEG-PLGA, and mannitol in an appropriate amount of deionized water as the water phase;

[0043] (3) Add the oil phase prepared in (1) dropwise to (2), grind it with a temperature-controllable planetary ball mill, take it out, fill it, and freeze-dry it to obtain a multiphase stable albumin-binding type Cabernet. The particle size was measured using a laser particle size analyzer, and the result was 386 nm.

Embodiment 3

[0045] Ratio of components in heterogeneously stable albumin-bound cabazitaxel (mg)

[0046]

[0047] Preparation:

[0048] (1) Dissolving cabazitaxel, PEG-PLGA and citric acid in an appropriate amount of chloroform / dichloromethane as the oil phase;

[0049] (2) dissolving the prescribed amount of albumin, PEG-PLGA, and mannitol in an appropriate amount of deionized water as the water phase;

[0050] (3) Add the oil phase prepared in (1) dropwise to (2), grind it with a temperature-controllable planetary ball mill, take it out, fill it, and freeze-dry it to obtain a multiphase stable albumin-binding type Cabernet. The particle size was measured using a laser particle size analyzer, and the result was 263 nm.

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Abstract

The invention belongs to the field of pharmaceutical preparations and discloses multiphase-stable albumin conjunction type cabazitaxel prepared by virtue of a novel albumin nanoparticle preparation technique. The prescription of a preparation comprises cabazitaxel, albumin, a stabilizer, a protective agent and a pH regulating agent. The preparation is prepared by virtue of the novel albumin nanoparticle preparation technique, and albumin conjunction type cabazitaxel is preferably prepared by virtue of high shearing force of a temperature-controllable planetary ball mill. According to the method, raw materials are crushed during the preparation, so that the particle size is reduced, and the solubility of drugs is increased.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a prescription and a preparation method of an albumin-bound freeze-dried preparation of a heterogeneously stable insoluble drug. Background technique [0002] Cabazitaxel is a new member of the taxane family. Its anti-cancer mechanism and characteristics are similar to those of docetaxel, and it belongs to anti-microtubule drugs. Cabazitaxel binds to tubulin, promotes its assembly into microtubules, and at the same time prevents the disassembly of these assembled microtubules, stabilizes the microtubules, and then inhibits cell mitosis and interphase cell function. Compared with other paclitaxel drugs on the market, the drug has a lower affinity with the drug-expelling pump mediated by P-glycoprotein, and the probability of drug resistance is lower, so it can be used to treat multidrug-resistant tumors. This drug crosses the blood-brain barrier. In combination with pred...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/337A61K47/42A61P35/00
Inventor 田野王志国崔婧王丽丽杨经安肖琰李晓彤
Owner SHENZHEN NEPTUNUS PHARM CO LTD
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