Sustained-release microspheres and preparation method thereof

A slow-release microsphere and slow-release technology, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of incomplete release and inability to overcome the encapsulation rate, and achieve Good uniformity, regular particles without adhesion, and good redispersibility

Inactive Publication Date: 2011-09-14
SHENZHEN SCIPROGEN BIO PHARMA +2
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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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  • Sustained-release microspheres and preparation method thereof
  • Sustained-release microspheres and preparation method thereof
  • Sustained-release microspheres and preparation method thereof

Examples

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preparation example Construction

[0025] The present invention addresses the problems of low encapsulation rate, incomplete release, severe burst release, and easy environmental pollution in the current preparation method of sustained-release microspheres, and provides a method for preparing sustained-release microspheres. A new preparation process is adopted: the preparation technology of hydrophilic oil-in-water-hydrophilic oil-in-oil-solid-in-oil (S / O / hO / W), which specifically includes the following steps:

[0026] A. Add the embedded solid components to the organic solution of the slow-release or controlled-release material, that is, the oil phase, and mix to form a suspension;

[0027] B. Add the suspension of step A to the hydrophilic organic solution that does not dissolve the sustained or controlled release material of step A, that is, the hydrophilic oil phase, and stir to form microspheres;

[0028] C. Disperse the microspheres formed in step B into the water phase and solidify to obtain the sustained-relea...

Embodiment 1

[0039] Preparation of blank microspheres:

[0040] (1) Preparation of oil phase (O) and hydrophilic oil phase (hO)

[0041] Oil phase (O): The controlled-release or sustained-release material is dissolved in an organic solvent to prepare a concentration of 1-50% by weight to form the oil phase (O).

[0042] Hydrophilic oil phase (hO): Formulation 1: Use surfactants and sodium chloride and other salts to mix the aqueous solution, their weight percentage concentrations are respectively 1-10% and 0-10%, and the weight percentage of the hydrophilic oil phase is 0 -40%; ethanol, ethylene glycol, propylene glycol or normal temperature liquid polyethylene glycol is 60-100%; or formula 2: use surfactant and sodium chloride and other salts to mix the aqueous solution, and their weight percentage concentration is 1- 10% and 0-10%, the weight percentage of the hydrophilic oil phase is 0-40%; the weight percentage is 0-50% glycerol and 50-100% ethanol, ethylene glycol, propylene glycol or norma...

Embodiment 2

[0048] Preparation of polylactic acid-polyglycolic acid (PLGA) microspheres containing erythropoietin dextran particles:

[0049] (1) Mix 10 mg of erythropoietin dextran particles (EPO) (with a particle size of 1-5 μm) and 100 mg of a dichloromethane solution of PLGA with a concentration of 20% by weight, stir, vortex or ultrasonic 0.5- 5 minutes to form a uniform suspension, that is, a solid-in-oil (S / O) emulsion;

[0050] (2) Add the emulsion obtained in step (1) dropwise to the hydrophilic oil phase (hO): [Preparation of the hydrophilic oil phase (hO): mix the aqueous solution with polyvinyl alcohol (PVA) surfactant and sodium chloride salt Account for 10% (5% by weight of polyvinyl alcohol, 5% by weight of sodium chloride salt); 90% by weight of ethylene glycol] and stir, vortex or ultrasonic for 0.5-5 minutes to form double emulsion;

[0051] (3) Add the double emulsion of step (2) dropwise to the water phase (W) [preparation of the water phase (W): 5% sodium chloride aqueous s...

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Abstract

The invention discloses a preparation method of sustained-release microspheres and hemopoietin sustained-release microspheres prepared thereby. The preparation method adopts a hydrophilic-oil-in-water, oil-in-hydrophilic-oil and solid-in-oil technique, which comprises the following steps: A, adding coated solid particles in organic solution of a sustained/controlled-release material, and uniformly mixing to form mixed suspension; B, adding the mixed suspension obtained by the step A into hydrophilic organic solution which does not dissolve the sustained/controlled-release material used in the step A, and stirring to form microspheres; and C, dispersing the microspheres formed by the step B into a water phase for solidification. The preparation method can effectively overcome the drawbacks of low coating rate, serious sudden release, incomplete release and the like. The hemopoietin sustained-release microspheres and hemopoietin sustained-release microspheres have smooth surface and are round, the particles are regular and not adhered, and the freeze-dried powder of the hemopoietin is white, fine, loose and free from collapse and adhesion and has high redispersibility. The hemopoietin sustained-release microspheres can be used for treating various related diseases to be treated for a long time with hemopoietin.

Description

Technical field [0001] The invention relates to the field of drug sustained-release microspheres, in particular to a method for preparing sustained-release microspheres, and erythropoietin sustained-release microspheres prepared by the method. Background technique [0002] From drug discovery to clinical application in the pharmaceutical industry, the last link is pharmaceutical preparations. Some of them require long-term administration to cure; some require local administration such as targeting. To achieve these goals, APIs 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 into sustained-release dosage forms; for the treatment of some tumors, some drugs are required to target the disease, such as embolic microsphere preparations that target tumor blood vessels; Recombinant technology has been used in the expression and production of therapeutic proteins for more...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/34A61K47/38A61K38/19A61P7/06
Inventor 袁伟恩金拓吴飞张向荣张涤平盛光阳胡振华
Owner SHENZHEN SCIPROGEN BIO PHARMA
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