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Preparation method of sustained-release microparticles

A technology for slow-release microparticles and microparticles, which can be applied to medical preparations without active ingredients, medical preparations containing active ingredients, and pharmaceutical formulations, etc., and can solve the problems of difficulty, disadvantage, and denaturation in the preparation of microparticles.

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
Comparison scheme
Effect test

Embodiment 1

[0096] Example 1: Preparation of Glucagon / PLA Microparticles

[0097] (1) Preparation of solid dispersion

[0098] Dissolve 0.99g PLA (molecular weight 25kDa, terminal ester group) in about 5.50mL glacial acetic acid, then add 0.01g sermorelin acetate, 0.05g xylitol and 0.05g zinc hydroxide, vortex to dissolve, and 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.

[0099] (II) Preparation of microparticles

[0100] Uniformly disperse the solid dispersion obtained in step 1 in about 5.50 g of dichloromethane to obtain an internal oil phase, and then inject the internal oil phase into 210 mL of 0.1% (w / w) polyvinyl alcohol aqueous solution that has been pre-heated to about 6°C and emulsifying with a wheel-type homomixer to prepare S / O / W emulsion (running speed ...

Embodiment 2

[0101] Embodiment 2: Preparation of Ziconotide / PLGA microparticles

[0102] (1) Preparation of solid dispersion

[0103]Dissolve 0.97g PLGA (molecular weight 25kDa, monomer ratio 90 / 10, terminal ester group) in about 5.39mL glacial acetic acid, then add 0.03g ziconotide acetate, 0.05g xylitol and 0.03g zinc chloride, vortex Spin down to dissolve, and then slowly inject into anhydrous ether (6°C) under stirring, resulting in a white precipitate, collect the white precipitate and extract it with anhydrous ether for about 5 times, collect the precipitate and dry it in a vacuum oven for 24 hours (10°C) to obtain a solid dispersion.

[0104] (II) Preparation of microparticles

[0105] Uniformly disperse the solid dispersion obtained in step 1 in about 5.39 g of dichloromethane to obtain an internal oil phase, and then inject the internal oil phase into 290 mL of 0.5% (w / w) polyvinyl alcohol aqueous solution that has been pre-heated to about 4°C , and use a high-speed homogenizer...

Embodiment 3

[0106] Example 3: Preparation of Tecoctide / PLGA Microparticles

[0107] (1) Preparation of solid dispersion

[0108] Dissolve 0.95g PLGA (molecular weight 30kDa, monomer ratio 85 / 15, carboxyl-terminated) in about 6.33mL glacial acetic acid / acetonitrile mixture, then add 0.05g tecosetide acetate, vortex to dissolve, and then slowly inject In cyclohexane (6°C) under stirring, a white precipitate is produced. Collect the white precipitate and extract it with cyclohexane for about 5 times. After collecting the precipitate, dry it in a vacuum oven for 24 hours (10°C) to obtain a solid dispersion body.

[0109] (II) Preparation of microparticles

[0110] The solid dispersion obtained in step 1 was uniformly dispersed in about 6.33 g of chloroform to obtain the internal oil phase, and then the internal oil phase was injected into 480 mL of 1% (w / w) hypromellose aqueous solution that had been pre-heated to about 4 °C , and use SPG membrane emulsifier to prepare S / O / W emulsion (memb...

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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): A61K9/16A61K47/34A61K38/26A61K38/17A61K38/35A61K38/31A61K38/11A61K38/08A61K38/09A61K38/20
CPCA61K38/095A61K9/0002A61K9/1641A61K9/1647A61K38/08A61K38/09A61K38/17A61K38/20A61K38/26A61K38/31A61K38/35A61K47/34A61K9/16A61K9/1635A61K38/12A61K9/1682
Inventor 刘锋赖树挺郑阳曹付春连远发
Owner AC PHARMA CO LTD
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