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Preparation method of sustained-release microparticles

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: 2016-09-28
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
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  • Preparation method of sustained-release microparticles

Examples

Experimental program
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Effect test

Embodiment 1

[0096] Embodiment 1: Preparation of albiglutide / PLGA microparticles

[0097] (1) Preparation of solid dispersion

[0098] 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.

[0099] (II) Preparation of microparticles

[0100] 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 1% (w / w) polyvinyl alcohol aqueous solution that had been pre-heated to about 4°C , and use a high-speed homogenizer to prepare S / O / W emulsion (rotor speed a...

Embodiment 2

[0101] Example 2: Preparation of dulaglutide / PLGA microparticles

[0102] (1) Preparation of solid dispersion

[0103]Dissolve 0.95g PLGA (molecular weight 30kDa, monomer ratio 50 / 50, carboxyl-terminated) in about 7.92mL glacial acetic acid, then add 0.05g dulaglutide 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.

[0104] (II) Preparation of microparticles

[0105] The solid dispersion obtained in step I was uniformly dispersed in about 7.92 g of dichloromethane to obtain an internal oil phase, and then the internal oil phase was injected into 420 mL of 1.5% (w / w) polyvinyl alcohol aqueous solution that had been pre-heated to about 4°C , and use a high-speed homogenizer to prepare S / O / W emulsion (rotor speed abo...

Embodiment 3

[0106] Example 3: Preparation of follicle stimulating hormone / PLA microparticles

[0107] (1) Preparation of solid dispersion

[0108] Dissolve 0.97g of PLA (molecular weight 20kDa, terminal ester group) in about 5.39mL of glacial acetic acid / acetonitrile mixture, then add 0.03g of follicle-stimulating hormone acetate, 0.05g of xylitol and 0.03g of zinc chloride, and dissolve under vortex , and then slowly inject cyclohexane (8°C) under stirring to produce a white precipitate, collect the white precipitate and take it about 5 times with cyclohexane, dry the precipitate in a vacuum oven for 24 hours (10°C), to obtain a solid dispersion.

[0109] (II) Preparation of microparticles

[0110] 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 400 mL of a 0.5% (w / w) hypromellose aqueous solution that had been pre-heated to about 6°C and emulsifying with a ...

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Abstract

The invention provides sustained-release microparticles. According to the invention, a preparation method of the sustained-release microparticles is conducted at normal temperature or low temperature in a whole course, which is quite conducive to high-temperature sensitive drugs, in particular compositions which polymer matrixes prepared from protein, nucleic acid and peptide drugs. Compared with public technologies, the preparation method disclosed by the invention can keep bioactivity of active substances to the greatest extent in the entire technological process; meanwhile, the prepared sustained-release microparticles have an excellent sustained-release effect close to a zero level, and drug concentration is kept stable in a sustained-release period, so that shortcomings of microparticles, which are prepared by a conventional S / O / W (solid-in-oil-in-water) process which needs to prepare the drug microparticles in advance, that drug release fails to occur in an early stage while rapid drug release happens in a late stage are overcome; and moreover, the sustained-release microparticles are relatively high in drug loading ratio and drug entrapment efficiency.

Description

technical field [0001] The invention relates to a method for encapsulating water-soluble medicines, especially protein, nucleic acid and peptide medicines, in biodegradable and biocompatible polymers, so as to obtain sustained-release microparticles capable of continuously releasing medicines. Background technique [0002] In recent years, a large number of biologically active substances such as oligopeptides, polypeptides and proteins have gained 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 administer orally. Injection or parenteral adm...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/34A61K38/24A61K38/26A61K38/35A61K38/16A61K38/22A61K38/11A61K38/20A61K31/7125A61K38/095
CPCA61K38/095A61K9/0002A61K9/1641A61K9/1647A61K31/7125A61K38/16A61K38/20A61K38/22A61K38/24A61K38/26A61K38/35A61K2300/00A61K47/34A61K9/16A61K9/1635A61K38/29A61K9/1682
Inventor 刘锋赖树挺郑阳曹付春连远发
Owner AC PHARMA CO LTD
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