Cabazitaxel composition for injection and preparation method thereof

A technology of cabazitaxel and composition, which is applied in the field of cabazitaxel composition for injection and its preparation, can solve the problems such as the inability to improve the solubility of cabazitaxel, and achieves a cabazitaxel with long reconstitution stability time, convenient clinical use and high solubility. Effect

Active Publication Date: 2018-05-25
BIKA BIOTECH GUANGZHOU CO LTD
View PDF9 Cites 9 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Based on the commercially available formulation JEVTANA Inspired by the formula containing polysorbate and ethanol and the patented formula of CA2900508A1 (US20150325321A1) containing a high ratio (greater than 1:30) of cyclodextrin, an obvious result is to continue to increase the ratio of cyclodextrin and / or increase the formula The amount of ethanol in the polysorbate can meet the preparation formula of replacing polysorbate, but the result of this attempt of the inventor is that neither improving the content of cyclodextrin nor increasing the amount of ethanol can improve the solubility of cabazitaxel to meet the requirements of clinical drug use. needs

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Cabazitaxel composition for injection and preparation method thereof
  • Cabazitaxel composition for injection and preparation method thereof
  • Cabazitaxel composition for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041]

[0042]

[0043] Weigh the SBE-β-CD of the recipe quantity, add the PEG300 and water of the recipe quantity, stir and dissolve at 23~25 ℃, add the PVPK12 and citric acid of the recipe quantity, add the sodium bisulfite and cabazita of the recipe quantity after stirring and dissolving Continue to stir for 2 h after stirring to dissolve the solution to make the solution uniform. Take samples to measure the pH value and content. After passing the test, filter them with a 0.2 μm polytetrafluoroethylene (PTFE) membrane, sub-pack vials, fill with nitrogen, press stoppers, roll caps, and label them.

Embodiment 2

[0045]

[0046] Weigh the prescribed amount of SBE-β-CD, add the prescribed amount of PEG300 and water, stir and dissolve at 22 to 25°C, add the prescribed amount of PVPK12 and citric acid, add the prescribed amount of cabazitaxel after stirring and dissolving, and stir and dissolve. Continue stirring for 2h to make the solution homogeneous. Take samples to measure the pH value and content. After passing the test, filter them with a 0.2 μm polytetrafluoroethylene (PTFE) membrane, sub-pack vials, fill with nitrogen, press stoppers, roll caps, and label them.

Embodiment 3

[0048]

[0049]

[0050] Weigh the prescribed amount of SBE-β-CD, add the prescribed amount of PEG300 and water, stir and dissolve at 18 to 20 ° C, add the prescribed amount of PVPK12 and citric acid, add the prescribed amount of cabazitaxel after stirring and dissolving, and stir and dissolve. Continue stirring for 100 min to make the solution homogeneous. Take samples to measure the pH value and content. After passing the test, filter them with a 0.2 μm polytetrafluoroethylene (PTFE) membrane, sub-pack vials, fill with nitrogen, press stoppers, roll caps, and label them.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The invention relates to a cabazitaxel composition for injection. The cabazitaxel composition comprises, by weight, 1 part of cabazitaxel, 1-100 parts of cyclodextrin, 10-200 parts of cosolvent, 1-60parts of povidone (PVP) and 0.02-0.1 part of additive. The composition does not contain polysorbate and alcohol and is low in histamine release; using of antihistamine, corticosteroid and H2 antagonist are not needed before administration; the composition is a single small bottle ready to use, and the composition does not need to be diluted in two steps. The composition has the advantages of highcabazitaxel solubility, high stability, long redissolving stable time and convenience for clinical use. The composition does not contain polysorbate and alcohol, so that side effects like allergy, irritation and addiction are lowered. In addition, the invention further relates to preparation method of the cabazitaxel composition.

Description

Field of Invention [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a cabazitaxel composition for injection and a preparation method thereof. technical background [0002] Cabazitaxel is a white or off-white powder, almost insoluble in water, soluble in ethanol, and unstable under alkaline conditions. The chemical name is (1S,2S,3R,4S,7R,9S,10S,12R,15S)-4-acetoxy-15-{[(2R,3S)-3-{[(tert-butoxy)carbonyl Amino]}-2-hydroxy-3-phenylpropionyl]oxy}-1-hydroxy-9,12-dimethoxy-10,14,17,17-tetramethyl-11-oxo-6 -oxatetracycline [11.3.1.0 3；10 .0 4；7 ] Heptadec-13-en-2-ylbenzoate. Molecular formula C 45 H 57 N 14 , the molecular weight is 835.93, and the structural formula is as follows: [0003] [0004] Cabazitaxel is a new generation of taxane antitumor drugs, which can be prepared by semi-synthesis of the precursors extracted from Taxus chinensis. Cabazitaxel binds to tubulin to promote its assembly into microtubules, and...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/32A61K47/10A61K47/12A61K47/02A61K9/08A61K9/19A61K31/337A61P35/00A61P35/04
CPCA61K47/02A61K47/10A61K47/12A61K47/32A61K9/0019A61K9/08A61K9/19A61K31/337A61K47/6951A61P35/00A61P35/04C08B37/0015A61K47/40C08L5/16C08L71/02C08L39/06C08K5/205
Inventor 童克勤成金兰
Owner BIKA BIOTECH GUANGZHOU CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap