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

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: 2010-06-09
SHANGHAI JIAO TONG UNIV
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  • 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

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

Examples

Experimental program
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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...

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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

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Application Information

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Patent Type & Authority Applications(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 JIAO TONG UNIV
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