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Preparation method for insoluble spherical medical granules

A technology of insoluble drugs and spherical particles, which is applied in the direction of pharmaceutical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc.

Active Publication Date: 2012-09-19
QILU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no report on the preparation of microsphere particles containing only drugs without other excipients by emulsification solvent evaporation method

Method used

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  • Preparation method for insoluble spherical medical granules
  • Preparation method for insoluble spherical medical granules
  • Preparation method for insoluble spherical medical granules

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Embodiment 1: the preparation of spherical particle of the present invention and its suspension

[0065] Add 4 g of paclitaxel to 100 ml of dichloromethane, and use a 250W ultrasonic cleaning machine (JCX-250G, Jining City, Shandong Province Ultrasonic Electronic Instrument Factory) to set the power at 100%, set the temperature at 37 ° C, and ultrasonically for 30 min. Dissolves active ingredient. The solution was sterile filtered through a 0.22 μm filter, and the resulting solution was the dispersed phase. Under aseptic conditions, take 2500ml of sterile glycerol for injection as the continuous phase.

[0066] In a 5L stainless steel reactor, a peristaltic pump was used to add the dispersed phase into the continuous phase, and at the same time, a high-shear homogeneous emulsifier (L4RT type, Silverson Company) was used to emulsify at 600 rpm for 3 min to form an emulsion. Under low-speed stirring with mechanical stirring in the reaction kettle, an oil-free chemical d...

Embodiment 2

[0070] Embodiment 2: the preparation of spherical particle of the present invention and suspension thereof

[0071] Add 4 g of paclitaxel into 100 ml of dichloromethane, and dissolve the active ingredient by ultrasonication at 37° C. for 30 min. The solution was sterile filtered through a 0.22 μm filter, and the resulting solution was the dispersed phase. Under aseptic conditions, take 3000ml of sterile glycerol for injection as the continuous phase.

[0072] The two solutions were respectively pressed into a static mixer (RZ-04667-14 Static mixer, Cole Parmer Company) with a peristaltic pump to mix and emulsify. The formed emulsion enters a heatable stirring tank, heats the solution to 35°C under stirring, and keeps stirring for 60 minutes to remove the solvent in the dispersed phase. Under stirring, the solution was transferred to a washing tank filled with 10L water for injection for washing, and the washing liquid was pressed into a collection tube with a 0.45 μm mixed c...

Embodiment 3

[0075] Embodiment 3: the preparation of spherical particle of the present invention and suspension thereof

[0076] Add 4 g of paclitaxel to 100 ml of dichloromethane, and use a 250W ultrasonic cleaning machine (JCX-250G, Jining City, Shandong Province Ultrasonic Electronic Instrument Factory) to set the power at 100%, set the temperature at 37 ° C, and ultrasonically for 30 min. Dissolves active ingredient. The solution was sterile filtered through a 0.22 μm filter, and the resulting solution was the dispersed phase. Take 25g of polyvinyl alcohol and dissolve it in 142g of water for injection. After the solution is sterilized and filtered with a 0.22μm filter membrane, 2333ml of sterile glycerin for injection is added, and stirred to form a continuous phase.

[0077] In a 5L stainless steel reactor, a peristaltic pump was used to add the dispersed phase into the continuous phase, and at the same time, a high-shear homogeneous emulsifier (L4RT type, Silverson Company) was use...

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Abstract

The invention relates to a preparation method for insoluble spherical medical granules. The preparation method comprises the following steps: (1) dissolving insoluble medicines into a lipophilic solvent to prepare into a dispersed phase; (2) adding the dispersed phase prepared in the step (1) into a continuous phase which is immiscible from the dispersed phase so as to form an emulsion, wherein the continuous phase consists of 60-100% of non-water solvent, 0-20% of emulsifier and 0-20% of water; (3) removing the lipophilic solvent from the dispersed phase to obtain a suspension in which the insoluble fine medical granules are in the continuous phase; (4) cleaning to remove the continuous phase; and (5) collecting and drying the obtained spherical granules, wherein the prepared spherical granules are 2-50 microns in average grain size.

Description

technical field [0001] The present invention relates to a method for preparing insoluble drugs into spherical or nearly spherical particles, and also relates to the spherical particles obtained by the method of the present invention, pharmaceutical preparations containing the spherical particles and the use of the spherical particles in preparing medicines. Background technique [0002] About 40% of commercially available drugs are insoluble drugs, and the proportion of drugs under research is as high as 70-90%. For some drugs with strong activity and poor solubility, it usually requires more effort to develop them into ordinary injections or oral preparations. [0003] For many insoluble drugs or insoluble salts or esters of water-soluble drugs, it is an excellent choice to develop them into sterile preparations to achieve long-acting sustained release or local targeting. When the drug is slowly dissolved and transported into the blood, it can ensure that the drug enters t...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K45/00A61K47/10A61K47/32A61K47/34A61K47/38A61K47/44
Inventor 王晶翼蒋朝军杨清敏董广金张明会
Owner QILU PHARMA
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