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Preparation method of sustained-release microparticles, prepared sustained-release microparticles and application thereof

A technology of slow-release microparticles and microparticles, which is applied to medical preparations containing non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, and can solve problems such as denaturation, aggregation and precipitation of active substances, and unstable release.

Active Publication Date: 2021-01-22
AC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the process of volatilizing organic solvents to prepare solids is not conducive to temperature-sensitive active substances, which can easily cause their denaturation; if organic solvents are volatilized at lower temperatures, the active substances will aggregate and precipitate during solidification due to the slow volatilization of the solvent. The active substance in the final solid dispersion will also exist in a larger volume, such as block, ribbon, and filament, which will cause difficulties or waste in the subsequent preparation of fine particles, and will also lead to unstable release.

Method used

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  • Preparation method of sustained-release microparticles, prepared sustained-release microparticles and application thereof
  • Preparation method of sustained-release microparticles, prepared sustained-release microparticles and application thereof
  • Preparation method of sustained-release microparticles, prepared sustained-release microparticles and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0103] Example 1 Preparation of Glucagon / PLA Microparticles

[0104] (1) Preparation of solid dispersion

[0105] Dissolve 0.99g PLA (molecular weight 25kDa, terminal ester group) in about 5.50mL glacial acetic acid, then add 0.01g glucagon acetate, 0.05g xylitol and 0.05g zinc hydroxide, vortex to dissolve, then slowly Inject into stirred anhydrous diethyl ether (8°C) to produce a white precipitate, collect the white precipitate and extract about 5 times with anhydrous diethyl ether, dry the precipitate in a vacuum oven for 24 hours (10°C) to obtain a solid Dispersions.

[0106] (II) Preparation of microparticles

[0107] The solid dispersion obtained in step I was uniformly dispersed in about 5.50 g of dichloromethane to obtain an internal oil phase, and then the internal oil phase was injected into 200 mL of 0.05% (w / w) lecithin / peanut oil that had been pre-heated to about 10°C solution, and emulsified using a turbine homomixer to prepare S / O / O emulsion (running speed ...

Embodiment 2

[0108] Example 2 Preparation of Ziconotide / PLGA Microparticles

[0109] (1) Preparation of solid dispersion

[0110] Dissolve 0.97g PLGA (molecular weight 25KDa, monomer ratio 90 / 10, terminal ester group) in about 5.39mL acetonitrile, then add 0.03g ziconotide acetate, 0.05g xylitol and 0.03g zinc chloride, vortex Dissolved under low temperature, and then slowly injected into cyclohexane (6°C) under stirring to produce a white precipitate, which was collected and extracted about 5 times with cyclohexane, and dried in a vacuum oven for 24 hours after the precipitate was collected ( 10°C) to obtain a solid dispersion.

[0111] (II) Preparation of microparticles

[0112] The solid dispersion obtained in step I was uniformly dispersed in about 5.39 g of chloroform to obtain an internal oil phase, and then the internal oil phase was injected into 290 mL of a 0.1% (w / w) lecithin / liquid paraffin solution that had been pre-heated to about 8°C , and use a high-speed homogenizer to p...

Embodiment 3

[0113] Example 3 Preparation of Tecoctide / PLGA Microparticles

[0114] (1) Preparation of solid dispersion

[0115] Dissolve 0.95g PLGA (molecular weight 30kDa, monomer ratio 85 / 15, carboxyl-terminated) in a mixture of about 6.33mL glacial acetic acid and acetonitrile, then add 0.05g tecosetide acetate, vortex to dissolve, and then slowly Inject into stirred n-hexane (6°C) to produce a white precipitate. Collect the white precipitate and extract it with n-hexane for about 5 times. After collecting the precipitate, dry it in a vacuum oven for 24 hours (10°C) to obtain a solid dispersion .

[0116] (II) Preparation of microparticles

[0117] The solid dispersion obtained in step I was uniformly dispersed in about 6.33g of tetrachlorethylene to obtain an internal oil phase, and then the internal oil phase was injected into 480mL of 0.25% (w / w) lecithin / corn which had been pre-heated to about 6°C Oil solution, and use SPG membrane emulsifier to prepare S / O / O emulsion (membran...

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Abstract

The invention discloses a preparation method of sustained-release microparticles, which comprises the following steps: 1) preparing a solid dispersion of water-soluble medicine and a biodegradable and biocompatible poorly water-soluble polymer; 2) preparing the prepared solid dispersion Dissolve in organic solvent C to form a solid dispersion emulsion; 3) inject the obtained solid dispersion emulsion into an oil solution containing a surfactant to form a uniform emulsion; 4) solidify the particles in the emulsion by solvent volatilization or solvent extraction , collecting microparticles, washing and drying to obtain the sustained-release microparticles; the present invention also discloses the sustained-release microparticles prepared by the preparation method of the sustained-release microparticles and the application of the sustained-release microparticles in implantable sustained-release pharmaceutical compositions . The preparation method of the sustained-release microparticles of the present invention is at normal temperature or low temperature throughout the process, which is very beneficial for the preparation of polymer matrix compositions for high-temperature sensitive drugs; at the same time, the prepared sustained-release microparticles have an excellent sustained-release effect close to zero order, and the drug concentration is between Stable during sustained release.

Description

technical field [0001] The invention belongs to the field of water-soluble drugs, and in particular relates to a preparation method of sustained-release microparticles, the prepared sustained-release microparticles and the application of the sustained-release microparticles in implantable sustained-release pharmaceutical compositions. Background technique [0002] In recent years, a large number of biologically active substances such as oligopeptides, polypeptides and proteins have received a lot of attention as drug candidates, which play an important role in the treatment of serious conditions (cancer, anemia, multiple sclerosis, hepatitis, etc.). However, these macromolecular active ingredients are fragile because of their poor stability in the gastrointestinal tract (easily degraded by low pH or proteolysis), short circulating half-lives, and their poor permeability across the intestinal wall, leading to biological The availability is very low, making it difficult to adm...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K38/26A61K47/34A61K38/16A61K38/31A61K38/095A61K38/08A61K38/10A61K38/09A61K38/17A61K38/20
CPCA61K38/095A61K9/0002A61K9/1641A61K38/08A61K38/09A61K38/10A61K38/16A61K38/1703A61K38/20A61K38/26A61K38/31A61K38/17A61K47/34A61K9/16
Inventor 刘锋赖树挺郑阳曹付春连远发
Owner AC PHARMA CO LTD
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