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Preparation method of slow-released microgranules, prepared slow-released microgranules and application thereof

A technology for slow-release microparticles and microparticles, which can be applied to medical preparations without active ingredients, medical preparations containing active ingredients, pharmaceutical formulas, etc., and can solve the problems of unstable release, waste, disadvantage, etc.

Active Publication Date: 2016-08-24
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 slow-released microgranules, prepared slow-released microgranules and application thereof
  • Preparation method of slow-released microgranules, prepared slow-released microgranules and application thereof
  • Preparation method of slow-released microgranules, prepared slow-released microgranules 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 slow-released microgranules. The preparation method of the slow-released microgranules includes the following steps: (1) preparing solid dispersion of biodegradable and biocompatible water-insoluble polymer and water-soluble drug; (2) dissolving the prepared solid dispersion in an organic solvent C to form solid dispersion emulsion; (3) injecting the obtained solid dispersion emulsion in an oil solution which contains a surfactant to form uniform emulsion; and (4) solidifying microgranules in the emulsion by solvent volatilization or solvent extraction, collecting the microgranules, and washing and drying to obtain the slow-released microgranules. The invention further discloses slow-released microgranules prepared by the preparation method and an application of the slow-released microgranules in an implantable slow-released pharmaceutical composition. By the preparation method of the slow-released microgranules, the temperature is normal or low in the whole process, and the preparation method is quite beneficial to preparation of a compound of a polymer matrix by high-temperature-sensitive drug; and meanwhile, the prepared slow-released microgranules have excellent slow-released effect close to zero level, and the concentration of the drug is stable in a slow release period.

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 Applications(China)
IPC IPC(8): A61K9/16A61K38/26A61K47/34A61K38/16A61K38/31A61K38/11A61K38/08A61K38/10A61K38/09A61K38/17A61K38/20
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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