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

Preparation method of everolimus solid dispersion

A solid dispersion, everolimus technology, applied in antitumor drugs, powder delivery, drug combination and other directions, can solve the problems of difficult material handling, low drying efficiency, etc., to improve drying efficiency, avoid oxidative degradation, and surface crispy Effect

Inactive Publication Date: 2017-01-04
CHANGZHOU LANLING PHARMA +1
View PDF4 Cites 7 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The purpose of the present invention is to solve the problems in the prior art that the air direct contact type is easy to cause the oxidative degradation of everolimus and the air non-direct contact type has low drying efficiency and difficult material handling, and provides a method that can effectively avoid everolimus Preparation method of everolimus solid dispersion with high drying efficiency and simple material handling after drying

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
  • Preparation method of everolimus solid dispersion
  • Preparation method of everolimus solid dispersion

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1）

[0025] The preparation method of the everolimus solid dispersion of the present embodiment has the following steps:

[0026] ① Mix 1 g of everolimus, 8.98 g of hydroxypropyl methylcellulose (E3 PREMIUM LV1 from Dow) and 0.02 g of 2,6-di-tert-butyl-4-methylphenol and add to 100 mL of ethanol and 100 mL of acetone, and stir to mix the materials evenly.

[0027] ② Spread the material obtained in step ① evenly on the flat rotating sample tray of the microwave vacuum dryer, turn on the vacuum pump, control the vacuum degree to be ≤-0.085MPa, pre-equilibrate for 2 minutes, set the microwave power to 518W, turn on the microwave function, and wait for the material After the temperature rose to 40°C, microwave vacuum drying was completed.

[0028] Discharge, and then lay the material flat in a vacuum drying oven at 50°C and a vacuum degree of ≤-0.085MPa, and continue to remove the organic solvent for 24h.

[0029] Discharge and pulverize to obtain solid dispersion powder.

Embodiment 2）

[0031] The preparation method of the everolimus solid dispersion of the present embodiment has the following steps:

[0032] ①Mix 10g of everolimus and 30g of hydroxypropyl methylcellulose (E3 PHARM from Ashland), add 1000mL of ethanol, and stir to mix the materials evenly.

[0033] ② Spread the material obtained in step ① evenly in the sample tray of the three-dimensional rotating support of the microwave vacuum dryer, turn on the vacuum pump, control the vacuum degree to be ≤-0.090MPa, pre-equilibrate for 10 minutes, set the microwave power to 550W, turn on the microwave function, wait for After the temperature of the material rose to 50°C, microwave vacuum drying was completed.

[0034] Discharge and pulverize to obtain solid dispersion powder.

Embodiment 3）

[0036] The preparation method of the everolimus solid dispersion of the present embodiment has the following steps:

[0037] ① Mix 1 g of everolimus, 20 g of hydroxypropyl methylcellulose (630 from Shin-Etsu), 3.9 g of lactose monohydrate and 0.1 g of dl-α-tocopherol acetate, then add 300 mL of methanol and 200 mL of methanol of acetone, and stir to mix the materials evenly.

[0038] ② The material obtained in step ① is evenly spread on the material belt of the belt-type continuous production microwave vacuum continuous dryer through the feeding device, and the vacuum degree is controlled to be ≤-0.080MPa, and the conveying speed and microwave power are adjusted. The material device collects the material.

[0039] Discharge and pulverize to obtain solid dispersion powder.

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
viscosityaaaaaaaaaa
viscosityaaaaaaaaaa
Login to View More

Abstract

The invention discloses a preparation method of everolimus solid dispersion. The preparation method particularly comprises the following steps that 1, everolimus, hydroxypropyl methyl cellulose and organic solvent are stirred and mixed to be uniform; 2, the organic solvent in the materials which are stirred to be uniform in the step 1 is removed through a microwave vacuum drying method, and then the everolimus solid dispersion is obtained, wherein the vacuum degree of microwave vacuum drying is lower than or equal to 0.080 MPa, and the drying temperature is lower than or equal to 55 DEG C. According to the method, the organic solvent in the preparation process of the everolimus solid dispersion is removed by adopting the microwave vacuum drying method which is conventionally applied to agricultural product and food processing, oxidative degradation of everolimus can be effectively avoided, the drying efficiency can be greatly improved, the dried materials are loose in surface, and the next processing step is easy to operate.

Description

Technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and specifically relates to a preparation method of everolimus solid dispersion. Background technology [0002] Everolimus is an orally effective rapamycin derivative developed by Novartis in Switzerland. It belongs to a new generation of macrolide immunosuppressants and anti-tumor drugs. [0003] Everolimus is a poorly soluble and low-stability drug. Its solubility in water, 0.1mol / L hydrochloric acid solution, and buffers with different pH (pH=2.0~10.0) is less than 0.1mg / mL. In addition, everolimus is a heat-sensitive drug, which is prone to oxidative degradation when exposed to air at high temperatures. It usually needs to be stored in a light-proof and sealed container at -20°C under the protection of antioxidants. [0004] In order to improve the drug dissolution rate and oral bioavailability, one of the commonly used methods in this field is to use the solvent evaporat...

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): A61K9/14A61K31/436A61K47/38A61P37/06A61P35/00
CPCA61K31/436A61K9/146
Inventor 柴旭煜刘玉华陈中亚尹文娟李金樊榕
Owner CHANGZHOU LANLING PHARMA
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