Method of preparing porous polymer microspheres by high voltage electrostatic anti-solvent process

A high-voltage electrostatic and porous microsphere technology, which is applied in the preparation of microspheres, pharmaceutical formulations, microcapsule preparations, etc., can solve the problems of non-porous, impermeable, and hollow surfaces of microspheres

Active Publication Date: 2013-02-27
HUAQIAO UNIVERSITY
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Problems solved by technology

[0005] There are very few reports on the preparation of porous microspheres by the high-voltage electrostatic antisolvent method. Based on the reports that have been seen, the inventors have concluded th

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  • Method of preparing porous polymer microspheres by high voltage electrostatic anti-solvent process
  • Method of preparing porous polymer microspheres by high voltage electrostatic anti-solvent process
  • Method of preparing porous polymer microspheres by high voltage electrostatic anti-solvent process

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Embodiment 1

[0019] The amount of ammonium bicarbonate added was changed, and polylactic acid porous microspheres were prepared by high-voltage electrostatic antisolvent method, as shown in Table 1. figure 1 The preparation procedure is as follows: 150 mg PLLA and 150 mg pluronic F127 (PF127) were dissolved in 5 mL dichloromethane as the oil phase (O). Freshly prepare 0.5 mL of ammonium bicarbonate (AB) aqueous solution of different concentrations as the water phase (W), and mix the two with a cell disruptor for ultrasonic emulsification for 1 min (power 200W, ultrasound 1s, interval 1s) to form a water-in-oil emulsion. The prepared water-in-oil emulsion is immediately loaded into a syringe, electrosprayed into an anhydrous ethanol solution through a high-pressure microcapsule forming device and a syringe pump, and is precipitated and solidified due to an anti-solvent process. The process parameters are: voltage 10kV, advancing speed 50mm / h, 26G needle (inner diameter 0.24mm), receiving di...

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Abstract

The present invention discloses a method of preparing porous polymer microspheres by high voltage electrostatic anti-solvent process. Under the effect of high voltage electrostatic force, water-in-oil emulsion is discharged from an injection needle and is added dropwise to an anti-solvent. The organic solvent in the water-in-oil emulsion and the anti-solvent are miscible with each other, so that the polymer droplets takes the water emulsion droplets as nucleus and are cured and precipitated on surfaces of the nucleus, and the polymer microsphere structure containing pore-foaming agent water emulsion droplets is formed. The gas generated by ammonium hydrogen carbonate decomposition inside the microspheres because of emulsification opens holes on the surfaces of the polylactic acid microspheres to generate the porous structural microspheres. The present invention can be used for preparing drug carriers for inhaled pulmonary drug delivery. The experimental results show that: porous microspheres having a large geometric particle size can be prepared under ideal process parameters; the degree of sphericity is good, the surface is rough, the surface has a large number of pores of different sizes, and the interior is filled with through-hole structure; and increasing the input amount of ammonium hydrogen carbonate, the geometric particle size of the product can be significantly improved and the aerodynamic diameter can be reduced.

Description

technical field [0001] The invention relates to a novel method for preparing a drug carrier, that is, a method for preparing a drug carrier by treating an emulsion with a high-voltage electrostatic antisolvent method. Specifically, the composition of the solution was changed in the conventional high-voltage electrostatic system, and the aqueous phase dissolved in the porogen was added to the single organic solution, so that the rapidly precipitated microspheres had more porous properties for pulmonary drug delivery. surface morphology. Background technique [0002] Porous microspheres refer to microspheres with low density and hollow / porous structure formed from solid microspheres by appropriate methods. Appropriate methods include adding auxiliary materials such as porogens, and additional steps such as supercritical treatment. In terms of pharmaceutical carriers, with large geometric particle size, low density, and irregular surface morphology, it has good aerodynamic pro...

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Application Information

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IPC IPC(8): B01J13/02A61K47/34A61K47/02
Inventor 王士斌杨月梅陈爱政刘源岗
Owner HUAQIAO UNIVERSITY
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