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

Method for preparing microspheres with hydrophilic oil in ethanol, oil in hydrophilic oil, solid in oil

An oil-in-oil and ethanol technology, which is applied in the direction of pharmaceutical formulations, medical preparations of non-active ingredients, non-effective ingredients of polymer compounds, etc., can solve the problems of incomplete release and inability to overcome the encapsulation rate, and achieve redispersibility good effect

Inactive Publication Date: 2013-04-17
SHANGHAI JIAOTONG UNIV
View PDF2 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But still can not overcome the low encapsulation efficiency, there are shortcoming of sudden release and incomplete release

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
  • Method for preparing microspheres with hydrophilic oil in ethanol, oil in hydrophilic oil, solid in oil

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0037] Preparation of the oil phase (O): the controlled-release or slow-release material is dissolved in an organic solvent to prepare a concentration of 1-50% by weight to form the oil phase (O).

[0038] The preparation of hydrophilic oil phase (hO): formula 1: use surfactant and sodium chloride etc. salt mixed aqueous solution, their weight percentage concentration is respectively 1-10% and 0-10%, accounts for the weight percentage of hydrophilic oil phase 0-40%; ethanol, ethylene glycol, propylene glycol or normal temperature liquid polyethylene glycol is 60-100%; or formula 2: mixed aqueous solution with salts such as surfactant and sodium chloride, and their weight percentage concentrations are respectively 1-10% and 0-10%, accounting for 0-40% by weight of the hydrophilic oil phase; use 0-50% by weight of glycerin and 50-100% of ethanol, ethylene glycol, propylene glycol or normal temperature liquid The polyethylene glycol solution accounts for 60-100% of the hydrophili...

Embodiment 1

[0051] Preparation of polylactic acid-polyglycolic acid (PLGA) microspheres loaded with small molecule drug particles

[0052] (1) According to the small molecule drug particles 0.4mg, 2mg, 1.5mg, 1mg or 0mg (the particle size is 0.2-1μm, 1-5μm, 2-6μm, 2-10μm or 0μm respectively) and the weight percentage concentration is 2 %, 10%, 15%, 20% or 30% PLGA in dichloromethane solution weight ratio of 1:20, 1:30, 1:30, 1:45 or 1:4 equal proportion stirring, vortex or ultrasonic 0.5- Form a uniform suspension in 5 minutes, i.e. a solid in oil (S / O) emulsion (preparing the corresponding drug particles accounts for the percentage of microsphere components: 50%, 40%, 25%, 10% or 0% ;PLGA is 50%, 60%, 75%, 90% or 100%);

[0053] (2) Step (1) is added dropwise to the hydrophilic oil phase (hO) by the emulsion: [The preparation of the hydrophilic oil phase (hO): formula 1: use polyvinyl alcohol (PVA) surfactant and sodium chloride salt Mixed aqueous solution, their weight percentage conc...

Embodiment 2

[0058] Preparation of polylactic acid-polyglycolic acid (PLGA) microspheres loaded with biomacromolecular drug particles

[0059] (1) According to the concentration of 0.4mg, 2mg, 1.5mg, 1mg or 0mg of biomacromolecular drug particles (the particle size is 0.2-1μm, 1-5μm, 2-6μm, 2-10μm or 0μm respectively) and the weight percentage concentration is The weight ratio of 2%, 10%, 15%, 20% or 30% PLGA in dichloromethane solution is 1:20, 1:30, 1:30, 1:45 or 1:4. Stir, vortex or sonicate 0.5 -5 minutes to form a uniform suspension i.e. solid-in-oil (S / O) emulsion (preparing the corresponding drug particles accounts for the percentage of microsphere components are respectively: 50%, 40%, 25%, 10% or 0 %; 50%, 60%, 75%, 90% or 100% for PLGA);

[0060] (2) Step (1) is added dropwise to the hydrophilic oil phase (hO) by the emulsion: [The preparation of the hydrophilic oil phase (hO): formula 1: use polyvinyl alcohol (PVA) surfactant and sodium chloride salt Mixed aqueous solution, th...

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 diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
Login to View More

Abstract

The invention relates to a method for preparing microspheres with solid-in-oil-in-hydrophilic oil-in-ethanol, belonging to the field of the pharmaceutical technology and comprising the following steps: (1) adding and stirring or swirling medicament particles to the organic solution, i.e. the oil phase of sustained-release or controlled-release material; (2) adding mixed suspension to another hydrophilic organic solution, i.e. hydrophilic oil phase and stirring the mixed suspension to the hydrophilic organic solution, i.e. the hydrophilic oil phase for 0.1-5 min to form spheres of 1-500 Mum; (3) transferring the mixed suspension containing the microspheres to ethanol and solidifying the mixed suspension for 1-4h; (4) and drying and freezing the sample to obtain the dry microspheres. The diameter of the microspheres can be controlled and adjusted from 1 Mum to 500 Mum according to the need; the microspheres can not cause pollution to the environment; the surfaces of the microspheres aresmooth and round; the microspheres are consistent without being adhered; the frozen-dried powder of the microspheres is white, fine and loose, can not collapse, can not be adhered and has good dispersity. The method can be used for preparing various sustained-release or controlled-release microspheres of various medicament or preparing the adjuvant of vaccines.

Description

technical field [0001] The invention relates to a preparation method in the field of pharmaceutical technology, in particular to a method for preparing hydrophilic oil-in-ethanol-oil-in-oil-oil-in-oil solid (S / O / hO / E) microspheres. Background technique [0002] In the pharmaceutical industry, from drug discovery to clinical application, the last link is drug preparation. Some of the drugs need long-term administration to be cured; others need targeted and other local administration. To achieve these goals, raw materials must be prepared into corresponding dosage forms. For example, drugs that require long-term administration but have a short half-life in the body should be prepared as sustained-release dosage forms; for the treatment of some tumors, some drugs need to be targeted to the disease, such as embolization microsphere preparations that target tumor blood vessels; Since recombinant technology has been used in the expression and production of therapeutic proteins f...

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 Patents(China)
IPC IPC(8): A61K9/16A61K47/10A61K47/14A61K47/16A61K47/32A61K47/34A61K47/36A61K47/42
Inventor 金拓袁伟恩吴飞任甜甜胡振华
Owner SHANGHAI JIAOTONG UNIV
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