Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Temsirolimus albumin nano-composition as well as lyophilized preparation, preparation method and application thereof

A nanotechnology of temsirolimus and albumin, which is applied in the field of temsirolimus albumin nanocomposition and its freeze-dried preparation, to achieve the effect of increasing stability, safety and excellent stability

Active Publication Date: 2018-02-23
SICHUAN KELUN PHARMA RES INST CO LTD
View PDF7 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The technical solution of the present invention creatively uses a water-miscible organic solvent to prepare an organic phase, and prepares stable nanoparticles with a particle size of less than 200nm, which solves the problem of using water-immiscible organic solvents such as chloroform / dichloromethane in the prior art. Solvent Technical Defects

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
  • Temsirolimus albumin nano-composition as well as lyophilized preparation, preparation method and application thereof
  • Temsirolimus albumin nano-composition as well as lyophilized preparation, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] Dissolve 300mg of temsirolimus in 30ml of ethanol to form an organic phase, use 1000ml of 15mg / ml human serum albumin aqueous solution as the water phase, mix the water phase with the organic phase, and place in a high-speed shear After shearing at a speed of 10000rpm, it was transferred to a high-pressure homogenizer, homogenized under a pressure of 35000psi, and circulated 5 times to prepare particles of the composition, with an average particle size of 124.3nm and a pH of 6.7, passed through a 0.22μm Sterilize by filtration with a sterile filter head and freeze-dry for 60 hours. After freeze-drying was completed, physiological saline was used as the reconstitution medium, and the measured zeta potential was -5.7mv.

Embodiment 2

[0067] 300mg of temsirolimus was dissolved in 15ml of ethanol to form an organic phase, 100ml of human serum albumin (6mg / ml) was used as the water phase, the water phase was mixed with the organic phase, placed in a high-speed shearing machine to After shearing at a speed of 7000rpm, it was transferred to a high-pressure homogenizer, and homogenized under a pressure of 30,000psi for 5 cycles. The prepared composition was determined to have an average particle size of 139.4nm, a pH of 6.5, and a pass of 0.22 Filter and sterilize with a μm sterile filter head, and freeze-dry for 60 hours. After freeze-drying, using water as the reconstitution medium, the measured zeta potential was -23.6mv.

Embodiment 3

[0069] 300mg of temsirolimus was dissolved in 10ml of ethanol to form an organic phase, 20ml of human serum albumin (20mg / ml) was used as the water phase, the water phase was mixed with the organic phase, placed in a high-speed shearing machine to After shearing at a speed of 15000rpm, it was transferred to a high-pressure homogenizer, and homogenized under a pressure of 40000psi for 6 cycles. The prepared composition was measured to have an average particle size of 185.7nm, a pH of 7.0, and a particle size of 0.22μm Sterilize by filtration with a sterile filter head and freeze-dry for 60*h. After freeze-drying was completed, physiological saline was used as the reconstitution medium, and the measured zeta potential was -7.5mv.

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

PropertyMeasurementUnit
particle sizeaaaaaaaaaa
particle diameteraaaaaaaaaa
particle sizeaaaaaaaaaa
Login to View More

Abstract

The invention belongs to the field of preparation of medicines, and particularly relates to a stable temsirolimus albumin nano-composition as well as a lyophilized preparation, a preparation method and application thereof. By adopting the temsirolimus albumin nano-composition disclosed by the invention, the technical defect that organic solvents such as chloroform / dichloromethane are not dissolvedwith water are required to use in the prior art is overcome. The temsirolimus albumin nano-composition is characterized in that temsirolimus or a derivative of the temsirolimus is dissolved by adopting an organic solvent mutually dissolved with the water, albumin is dispersed by adopting water-based medium, and temsirolimus is mixed with the albumin to prepare nano-suspension liquid, so that thenano-composition of which pH is 6.0 to 7.5 and the average particle size is not greater than 200nm is obtained. The nano-composition has nano-particles with excellent stability, so that the stabilityand the security of the medicine are improved; meanwhile, when the lyophilized preparation is prepared by adopting the nano-composition, even if a lyophilization protector and a protein stabilizationagent are not needed, the qualified lyophilized preparation also can be prepared. After the lyophilized preparation is prepared, zeta electrical potential of the lyophilized preparation after dispersion of the water-based medium is -2 to -40mv.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a stable temsirolimus albumin nano composition and its freeze-dried preparation, preparation method and application. Background technique [0002] Temsirolimus (English name, Temsirolimus) is 4,2-bis-hydroxymethyl propionate of rapamycin, and its structural formula is as follows: [0003] [0004] The compound was disclosed in US Patent No. 5,362,718A for the first time, and studies have shown that temsirolimus has an inhibitory effect on the growth of tumor cells in various tissues. In 2007, the U.S. FDA approved the marketing of the two-bottle preparation developed by Wyeth for advanced renal cell carcinoma, and the European Union approved it for the first-line treatment of advanced renal cell carcinoma with at least three or more prognostic risk factors. [0005] Because temsirolimus has poor water solubility and is a non-electrolyte, it is difficult ...

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): A61K9/14A61K9/19A61K31/436A61K47/10A61K47/42A61P35/00A61P37/02A61P29/00A61P31/10A61P43/00
CPCA61K9/145A61K9/146A61K9/19A61K31/436
Inventor 苏正兴杨立开赵栋单凤英王利春王晶翼
Owner SICHUAN KELUN PHARMA RES INST CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com