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Sustained-release microgranules, method for preparing same and application of sustained-release microgranules

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

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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  • Sustained-release microgranules, method for preparing same and application of sustained-release microgranules
  • Sustained-release microgranules, method for preparing same and application of sustained-release microgranules
  • Sustained-release microgranules, method for preparing same and application of sustained-release microgranules

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0104] Example 1 Preparation of albiglutide / PLGA microparticles

[0105] (1) Preparation of solid dispersion

[0106] Dissolve 0.90g PLGA (molecular weight 25kDa, monomer ratio 65 / 35, carboxyl-terminated) in about 6.00mL glacial acetic acid, then add 0.10g albiglutide acetate, dissolve under vortex, and then slowly pour into a stirring In water ether (6°C), a white precipitate was produced, collected the white precipitate and extracted about 5 times with anhydrous ether, dried in a vacuum oven for 24 hours (10°C) after collecting the precipitate, to obtain a solid dispersion.

[0107] (II) Preparation of microparticles

[0108] The solid dispersion obtained in step I was uniformly dispersed in about 6.00 g of dichloromethane to obtain an internal oil phase, and then the internal oil phase was injected into 230 mL of 0.05% (w / w) lecithin / peanut oil that had been pre-warmed to about 4°C solution, and use a high-speed homogenizer to prepare S / O / O emulsion (rotor speed about 3...

Embodiment 2

[0109] Example 2 Preparation of dulaglutide / PLGA microparticles

[0110](1) Preparation of solid dispersion

[0111] Dissolve 0.95g PLGA (molecular weight 30kDa, monomer ratio 50 / 50, carboxyl-terminated) in about 7.92mL acetonitrile, then add 0.05g dulaglutide acetate, dissolve under vortex, and then slowly pour into the cyclohexane under stirring In alkanes (6°C), a white precipitate was produced, which was collected and extracted about 5 times with cyclohexane. After the collected precipitate was dried in a vacuum oven for 24 hours (10°C), a solid dispersion was obtained.

[0112] (II) Preparation of microparticles

[0113] The solid dispersion obtained in step I was uniformly dispersed in about 7.92 g of chloroform to obtain an internal oil phase, and then the internal oil phase was injected into 420 mL of a 0.1% (w / w) lecithin / liquid paraffin solution that had been pre-warmed to about 5°C , and use a high-speed homogenizer to prepare S / O / O emulsion (rotor speed about 3...

Embodiment 3

[0114] Example 3 Preparation of follicle stimulating hormone / PLA microparticles

[0115] (1) Preparation of solid dispersion

[0116] Dissolve 0.97g PLA (molecular weight 20kDa, terminal ester group) in about 5.39mL dimethyl sulfoxide, then add 0.03g follicle-stimulating hormone acetate, 0.05g xylitol and 0.03g zinc chloride, dissolve under vortex, Then it is slowly injected into n-hexane (8°C) under stirring to produce a white precipitate, which is collected and extracted about 5 times with n-hexane, and dried in a vacuum oven for 24 hours (10°C) after the precipitate is collected to obtain Solid dispersion.

[0117] (II) Preparation of microparticles

[0118] The solid dispersion obtained in step I was uniformly dispersed in a mixed solution of about 5.39 g of dichloromethane and chloroform to obtain an internal oil phase, and then the internal oil phase was injected into 410 mL of 0.25% (w / w ) lecithin / soybean oil solution, and emulsified using a turbine homomixer to p...

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Abstract

The invention discloses a method for preparing sustained-release microgranules. The method includes steps of 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 into oil solution with surfactants to form uniform emulsion; 4), curing microgranules in the emulsion by means of solvent evaporation or solvent extraction, and collecting, washing and drying the microgranules to obtain the sustained-release microgranules. The invention further discloses the sustained-release microgranules prepared by the aid of the method and application of the sustained-release microgranules to implantable sustained-release pharmaceutical compositions. The method, the sustained-release microgranules and the application have the advantages that full procedures for preparing the sustained-release microgranules by the aid of the method are carried out at the normal temperature or the low temperatures, and accordingly the method is quite favorable for preparing polymer matrix compositions from high-temperature-sensitive drugs; excellent similarly zero-level sustained-release effects can be realized by the prepared sustained-release microgranules, and the drugs are stable in concentration in sustained-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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IPC IPC(8): A61K9/16A61K47/34A61K31/7088A61K38/16A61K38/20A61K38/22A61K38/24A61K38/26A61K38/29A61K38/35
CPCA61K9/0002A61K9/0024A61K9/1647A61K31/7088A61K38/16A61K38/20A61K38/22A61K38/24A61K38/26A61K38/29A61K38/35A61K9/16A61K47/34
Inventor 刘锋赖树挺郑阳曹付春连远发
Owner AC PHARMA CO LTD
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