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

Method for preparing shell-core double-layer microspheres

A microsphere and double-layer technology, which is applied in the field of preparation of shell-core double-layer microspheres, can solve the problems of incomplete release and inability to overcome the encapsulation rate, so as to avoid the influence of the effect, the particles are regular and non-adhesive, and the redispersibility good effect

Inactive Publication Date: 2012-09-05
SHANGHAI JIAO TONG UNIV
View PDF0 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

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0029] Oil phase-1(O 1 ) preparation: PSA and PLA according to the weight ratio of 1:1, 1:2, 1:3, 1:4, 1:5, 1:6, 6:1, 5:1, 4:1, 3: 1, or 2: 1 mixed and dissolved in an organic solvent to prepare a concentration of 1-50% (w / w), forming an oil phase-1 (O 1 ).

[0030] 2. Preparation of blank shell-core microspheres

[0031] Oil phase-1(O 1 ) is added to an aqueous surfactant solution with a concentration of 1-10% (w / w) by weight of sodium chloride and a concentration of 1-10% (w / w) by weight and stirred, sonicated or vortexed for 0.1-5 minutes to form O / W, then transfer to 100-1000ml sodium chloride solution with a concentration of 1-10% (w / w) by weight to solidify for 1-4 hours, collect the microspheres by centrifugation and lyophilize or volatilize to remove the organic solvent to obtain dried microspheres .

[0032] 2. Preparation of drug-loaded microspheres

[0033] 1. To prepare drug granules, for small molecule drugs, it can be conventional milling, precipitation, p...

Embodiment 1

[0041] Preparation of PLA / PSA Shell-Core Microspheres Loaded with Small Molecule Drug Particles

[0042] (1) According to the weight ratio of hydrophilic small molecule drug particles and PLA in dichloromethane, acetonitrile or ethyl acetate solution is 1:1, 1:2, 1:3, 1:4, 1:5, 1:6 , 1:7, 1:8, 1:9, 1:10 in equal proportions, vortex or ultrasonic for 1-5 minutes to form a uniform suspension, then add the organic solution of PSA to the above suspension, and then stir , vortex or ultrasonic for 1-5 minutes to form a uniform suspension, that is, solid in oil (S / O 1 ) emulsion; or according to the weight ratio of hydrophobic drug molecule particles and PLA in dichloromethane, acetonitrile or ethyl acetate solution is 1: 1, 1: 2, 1: 3, 1: 4, 1: 5, 1: 6 , 1:7, 1:8, 1:9, 1:10 in equal proportions, vortex or ultrasonic for 1-5 minutes to form a uniform suspension, then add the organic solution of PLGA to the above suspension, and then stir , vortex or ultrasonic for 1-5 minutes to fo...

Embodiment 2

[0047] Preparation of PLA / PSA Shell-Core Microspheres Loaded with Biomacromolecule Drug Particles

[0048] (1) According to the weight ratio of dichloromethane, acetonitrile, ethyl acetate or their mixed solutions of biomacromolecule drug particles and PLA, it is 1:1, 1:2, 1:3, 1:4, 1:5, 1 : 6, 1: 7, 1: 8, 1: 9, 1: 10 in equal proportions, vortex or ultrasonic for 1-5 minutes to form a uniform suspension, then add the organic solution of PSA to the above suspension, Then stir, vortex or ultrasonic for 1-5 minutes to form a uniform suspension, that is, solid in oil or solid in oil (S / O 1 ) lotion;

[0049] (2) The emulsion obtained in step (1) is added dropwise to an aqueous surfactant solution of 1-10% (w / w) sodium chloride and 1-10% (w / w) by weight and stirred, vortexed or ultrasonically 0.1-5 minutes to form double emulsion;

[0050] (3) Add the double emulsion of step (2) to the 1000ml sodium chloride solution that is 1-10% (w / w) by weight and solidify for 1-4 hours;

...

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
Login to View More

Abstract

The invention relates to a method for preparing a preparation in the technical field of pharmacy, in particular to a method for preparing shell-core double-layer microspheres. The method comprises the following steps: dispersing medicament particles into organic solution consisting of PLA and PSA and stirring or eddying to uniformly disperse a mixture to form a suspension; adding the suspension into an external oil phase, stirring or eddying again to form the microspheres, transferring the microspheres into a big water phase and solidifying the microspheres for 1 to 4 hours; and centrifugallycollecting, freeze-drying and storing the microspheres. The microspheres prepared by the method have smooth and round surfaces and are uniform and non-adhesive; the particle sizes of the microspherescan be regulated and controlled to between 1 and 500 mu m; and freeze-dried powder of the microspheres is white, fine, loose, fall-proof and non-adhesive and has excellent dispersibility. The method can be used for preparing various medicament slow release microspheres or controlled-release microspheres and adjuvants of vaccines.

Description

technical field [0001] The invention relates to a method for preparing preparations in the field of pharmaceutical technology, in particular to a method for preparing shell-core double-layer 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 or controlled-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 etc.; Gene recombination technology has been used in the expression and production of therapeutic proteins ...

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): A61K9/19A61K47/34A61K47/32A61K45/00
Inventor 金拓袁伟恩吴飞任甜甜洪晓芸
Owner SHANGHAI JIAO TONG 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