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Albumin composition highly-carrying cabazitaxel medicine, preparation and preparation method thereof

A cabazitaxel, albumin technology, applied in the direction of drug combination, inactive components of polymer compounds, pharmaceutical formulations, etc., can solve the problem of increasing the amount of albumin injected into the human body, reducing the targeting of nanoparticles, and reducing the targeting of nanoparticles. and other problems, to achieve the effect of being conducive to industrial application, solving toxic and side effects, and being easy to sterilize and filter.

Active Publication Date: 2016-07-06
SICHUAN KELUN PHARMA RES INST CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

CN102458112A discloses a taxane drug albumin nanoparticle composition, but its entrapment efficiency is not high, less than about 25% of the albumin in the composition is entrapped in the form of nanoparticles, most of the albumin and drugs are in the form of non-nanoparticles form, which greatly reduces nanoparticle targeting, so Abraxane products prepared using this technology do not show very good tissue targeting in tissue distribution
CN103393632A also discloses a cabazitaxel albumin composition, but the drug loading of the composition is lower than 12.5%, which greatly increases the amount of albumin injected into the human body, and correspondingly brings certain side effects of albumin use, including chills, fever, facial flushing, Rash, nausea and vomiting
[0005] New technologies for the preparation of albumin nanoparticles have been gradually developed. The high-pressure homogenization method of patent CN1515244A and the protein folding denaturation and renaturation method of patent CN102048695A can effectively prepare cabazitaxel albumin nanoparticles. Protein-bound non-nanoparticle form exists, greatly reducing nanoparticle targeting

Method used

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  • Albumin composition highly-carrying cabazitaxel medicine, preparation and preparation method thereof
  • Albumin composition highly-carrying cabazitaxel medicine, preparation and preparation method thereof
  • Albumin composition highly-carrying cabazitaxel medicine, preparation and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040]Add 300mg of cabazitaxel to a 50ml bottle, add 20ml of ethanol and chloroform mixed solvent (ethanol: chloroform volume ratio = 1:1), dissolve it and homogenize it under high-speed shear at 20,000 revolutions per minute (rpm). Disperse in 750ml, 1mg / ml albumin aqueous solution. Then transfer to a homogenizer, emulsify at 15,000 pounds per square inch (psi), and the resulting system is transferred to an ultrafiltration concentration device (PALL, 100KD membrane bag), and ultrafiltered to 50ml. The average particle diameter of the produced cabazitaxel composition particles is 180nm (MalvernNano-ZS90, see figure 1 ), the Zeta potential is -15.3mv, and the pH is 6.95. Sterilize by filtering through a 0.22 μm sterile filter head, and freeze-dry for 48 hours. Through HPLC analysis and detection, the drug loading capacity of the cabazitaxel albumin composition was calculated to be 25.4%, and the encapsulation efficiency was 93.2%.

Embodiment 2

[0042] Add 200mg of cabazitaxel to a 50ml bottle, add 15ml of ethanol and chloroform mixed solvent (ethanol: chloroform volume ratio = 1:4), ultrasonically dissolve it and put it under high-speed shear at 30,000 revolutions per minute (rpm) Evenly dispersed in 50ml of saline containing 15mg / ml albumin. Then transfer to a homogenizer, emulsify at 20,000 pounds per square inch (psi), and the resulting system is transferred to an ultrafiltration concentration device (PALL, 100KD membrane bag), and ultrafiltered to 25ml. The average particle size of the produced cabazitaxel composition particles is 153nm (MalvernNano-ZS90), and the Zeta potential is -20.8mv (see Figure 4 ), the pH is 7.03. Sterilize by filtering through a 0.22 μm sterile filter head, and freeze-dry for 48 hours. Through HPLC analysis and detection, the calculated drug loading capacity of the cabazitaxel albumin composition is 18.2%, and the encapsulation efficiency is 95.7%.

Embodiment 3

[0044] Add 150 mg of cabazitaxel to a 50 ml bottle, add 10 ml of acetone and chloroform mixed solvent (acetone: chloroform volume ratio = 1:5), ultrasonically dissolve it and put it under high-speed shear at 40,000 revolutions per minute (rpm) Evenly dispersed in 15ml of 5% glucose solution containing 50mg / ml albumin. Then transfer to a homogenizer, emulsify at 25,000 pounds per square inch (psi), and the resulting system is transferred to an ultrafiltration concentration device (PALL, 100KD membrane bag), and ultrafiltered to 8ml. The resulting cabazitaxel composition particles had an average particle size of 138 nm (MalvernNano-ZS90), a Zeta potential of -32.4 mv, and a pH of 7.03. Sterilize by filtering through a 0.22 μm sterile filter head, and freeze-dry for 48 hours. According to HPLC analysis and detection calculation, the drug loading capacity of the cabazitaxel albumin composition is 13.4%, and the encapsulation efficiency is 98.5%.

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Abstract

The invention provides an albumin composition highly loaded with cabazitaxel and its preparation and preparation method. In the albumin composition highly loaded with cabazitaxel drug of the present invention, the carrier albumin in the form of albumin nanoparticles and non-nanoparticles encapsulates the drug loading of cabazitaxel up to 13% to 25% (weight), and The carrier albumin in the form of nanoparticles accounts for more than 50% by weight of the total albumin carriers. The composition of the present invention is convenient for clinical use, greatly reduces the amount of albumin as an auxiliary material, and more efficiently entraps drugs, delivers them to lesions, and plays a role.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations. More specifically, the present invention relates to an albumin composition highly loaded with cabazitaxel and its formulation and preparation method. Background technique [0002] Cabazitaxel was developed by Sanofi-aventis, and the FDA approved its injection (trade name Jevtana) in 2010. Indicated in combination with prednisone for the treatment of patients with metastatic prostate cancer who have previously been hormone-refractory to docetaxel-containing regimens. Jevtana belongs to the taxane class of antineoplastic drugs, and it has an antitumor effect by interfering with the microtubule network necessary for cell mitosis and interphase cell functions. It can combine with free tubulin, promote the assembly of tubulin into stable microtubules, and inhibit its depolymerization, resulting in the loss of normal function of microtubule bundles and the fixation of microtubules, thereby ...

Claims

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Application Information

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IPC IPC(8): A61K47/42A61K31/337A61K9/51A61K9/19A61P35/00
Inventor 苏正兴赵栋杨立开单凤英王利春胡思玉王晶翼
Owner SICHUAN KELUN PHARMA RES INST CO LTD
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