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Slow-release particle and a production method therefor

A microparticle and controlled-release layer technology, applied in the field of controlled-release microparticles and its preparation, can solve the problems of difficult drug release control, no controlled-release microparticles, long coating time, etc., and achieve excellent dissolution properties

Inactive Publication Date: 2011-11-16
AMOREPACIFIC CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this patent relates to controlled release microparticles without a drug-containing matrix
The disadvantage of the disclosed controlled-release microparticles is that it is difficult to control the release of the drug, a large amount of coating material is required to achieve the controlled release of the microparticles, and a long coating time is required

Method used

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  • Slow-release particle and a production method therefor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Tamsulosin hydrochloride (3.33 g) was ground well and mixed with microcrystalline cellulose powder (Vivapur PH101, 496.67 g). Then, a spherical matrix containing tamsulosin hydrochloride was prepared while spraying water (500 g) with a rotary fluidized bed apparatus (GPCG-1, Glatt, Germany).

[0042] Among the particles prepared, only those with a particle diameter of 150-250 μm (60-100 mesh) were selected.

Embodiment 2

[0044] Spherical matrices were prepared in the same manner as in Example 1, except that the spray contained a dispersion of Eudragit L30D-55 (88.90 g; solids 26.67 g (solids content = 30%), water 62.23 g) and water (437.77 g) body. Only particles with a particle size of 150-250 μm (60-100 mesh) are selected.

Embodiment 3

[0046] Tamsulosin hydrochloride (3.33 g) was ground well and mixed with microcrystalline cellulose (346.67 g), calcium hydrogen phosphate (100 g) and lactose (50 g). Then, spherical substrates were prepared while spraying a dispersion comprising Eudragit L30D-55 (88.90 g; solids 26.67 g (solid content = 30%), water 62.23 g) and water (437.77 g).

[0047] Among the particles prepared, only those with a particle diameter of 150-250 μm (60-100 mesh) were selected.

[0048] Preparation of controlled release microparticles

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Abstract

The present invention relates to a slow-release particle comprising: a matrix having a pharmacologically active component; and a slow-release layer having a substance which forms a slow-release stratum on the matrix. The slow-release particle of the present invention not only allows control of the dual release of drugs of an effective kind but can also exhibit outstanding elution characteristics even when a small amount of coating substance is used.

Description

technical field [0001] The present disclosure relates to controlled release microparticles comprising a matrix comprising a pharmacologically active component and methods for their preparation. Background technique [0002] Many pharmacologically active substances, including drugs and prodrugs, are prepared as orally available formulations that allow controlled release (also known as slow or sustained release). [0003] When a drug such as tamsulosin hydrochloride is administered in controlled release tablet form, due to its uneven rate of passage through the pyloric sphincter, increased blood levels and resulting concentration-dependent side effects often occur. Attempts have therefore been made to prepare tablets with small particle sizes, which disintegrate rapidly in the oral cavity. [0004] For example, Korean Patent No. 0530546 discloses a composition for tablets comprising drug-containing controlled-release microparticles of 350 μm or less, excipients, and a binder....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/48
CPCA61K9/5042A61K9/5026A61K9/5047A61P1/04A61P11/06A61P11/08A61P11/14A61P13/08A61P17/02A61P23/02A61P25/00A61P25/08A61P25/24A61P3/06A61P9/04A61P9/06A61P9/12A61P3/10A61K47/50A61K9/16
Inventor 申光炫金栽宽全宰逸洪德基裵埈浩
Owner AMOREPACIFIC CORP
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