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Method for preparing hydrophobic medicament nuclear shell granule-type solid dispersion by static electricity spraying method

A technology of solid dispersion and hydrophobic drugs, which is applied in the direction of making drugs into special physical or ingestible devices, pharmaceutical formulas, medical preparations of non-active ingredients, etc., and can solve the problems that limit the wide application of solid dispersions Wide particle size distribution, poor stability of solid dispersion and other problems, to achieve the effect of controlled drug release, high affinity and good dispersibility

Inactive Publication Date: 2013-05-15
杨晔
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The main problems faced by the existing solid dispersion preparation technology are: (1) The stability of the prepared solid dispersion is not good, and the drug agglomeration phenomenon is serious; (2) Steps such as crushing and sieving are often required, and the process is complicated and there are many influencing factors , the resulting solid dispersion has a wide particle size distribution; (3) Some non-degradable materials, such as surfactants, are often added during the preparation process; (4) The residual organic solvent is relatively high, which is difficult to effectively remove, etc.
These problems limit the further widespread application of solid dispersions

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] The active ingredient neogambogic acid of the anti-tumor plant medicine and the fat-soluble polymer material polylactic acid are dissolved in chloroform to form a homogeneous solution. The water-soluble / water-dispersible polymer material chitosan is dissolved / dispersed in water to form a homogeneous aqueous phase solution. Slowly drop the mixed solution of chlordiazepoxide and cellulose acetate into the aqueous phase solution of sodium starch glycolate, mix well to form an oil-in-water emulsion, and then spray, collect, and dry the emulsion by high-voltage electrostatic spraying to obtain The core-shell particle solid dispersion loaded with hydrophobic drugs is neogambogic acid-polylactic acid / chitosan.

Embodiment 2

[0022] This embodiment is the same as Embodiment 1, except that the hydrophobic drug in step A is the antipsychotic drug haloperidol, and the fat-soluble polymer material is polypropylene resin; the water-soluble / The water-dispersible polymer material is sodium carboxymethyl cellulose, and the obtained solid dispersion of hydrophobic drug core-shell particles is haloperidol-polypropylene resin / sodium carboxymethyl cellulose.

Embodiment 3

[0024] This example is the same as Example 1, except that the hydrophobic drug in step A is lovastatin, a lipid-regulating drug, and the fat-soluble polymer material is polyisobutylene; the water solubility / dispersibility in step B is high The molecular material is gelatin, and the obtained hydrophobic drug core-shell particle type solid dispersion is lovastatin-polyisobutene / gelatin.

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PUM

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Abstract

The invention discloses a method for preparing a hydrophobic medicament nuclear shell structure micro / nano granule-type solid dispersion by a high-voltage static electricity spraying method, relating to the pharmaceutics and biomedical field. The method comprises the following steps of: dissolving hydrophobic medicaments and fat soluble high polymer materials together into an organic solvent, and emulsifying and dispersing the mixture into an aqueous solution containing water soluble high polymer material; then placing oil-in-water emulsion into a trace propeller, and carrying out electrostatic spraying under the effect of high-voltage electrostatic field, thereby obtaining the hydrophobic medicament nuclear shell structure micro / nano granule-type solid dispersion finally. According to the preparation method, the operation is simple, the cost is low, environmental protection is realized and industrial production is facilitated. The particle size of the prepared hydrophobic medicament nuclear shell structure micro / nano granule-type solid dispersion is controllable, and the solid dispersion has tissue and organ targeting; and the granules of the nuclear shell structure is beneficial to prolonging the medicament action time.

Description

technical field [0001] The invention relates to the fields of pharmacy and biomedicine, in particular to a method for preparing hydrophobic drug core-shell particle solid dispersion by electrostatic spraying. Background technique [0002] Solid dispersion refers to the highly dispersed drug in a solid carrier to form a dispersion system in solid form, which is mainly used to accelerate and increase the dissolution of insoluble drugs and improve their bioavailability. At present, the commonly used techniques for preparing drug-loaded micro / nanoparticles include melting method, solvent method, solvent-melting method, grinding method, solvent spray drying method, freeze drying method and so on. The main problems faced by the existing solid dispersion preparation technology are: (1) The stability of the prepared solid dispersion is not good, and the drug agglomeration phenomenon is serious; (2) Steps such as crushing and sieving are often required, and the process is complicated...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/30A61J3/02
Inventor 杨晔尹登科
Owner 杨晔
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