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Method for preparing slow-release drug particles facilitating release control

A slow-release, drug-based technology, applied in drug delivery, pharmaceutical formulations, microcapsules, etc., to achieve excellent results in drug loading

Inactive Publication Date: 2020-03-31
DAEWOONG PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the problem that arises when volatilization starts from around the boiling point of a volatile solvent remains

Method used

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  • Method for preparing slow-release drug particles facilitating release control
  • Method for preparing slow-release drug particles facilitating release control
  • Method for preparing slow-release drug particles facilitating release control

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0047] Preparation Example 1: Preparation of Oil-in-Water Emulsion Containing Donepezil

[0048] Polyvinyl alcohol (PVA, 90% hydrolyzed, Mw=20000-30000) was dissolved in sterilized water to prepare a 0.5% w / v aqueous solution of polyvinyl alcohol.

[0049] On the other hand, donepezil, dichloromethane, and polylactic acid (ResomerTM R 203H, Poly(D, L-lactide), Mw 18000-24000) were put into a beaker and completely dissolved by stirring to prepare a polymer / drug solution.

[0050] The polymer / drug solution was put into the above polyvinyl alcohol aqueous solution and stirred to form an oil-in-water (O / W) emulsion.

[0051] The resulting oil-in-water (O / W) emulsion was re-stirred once in aqueous polyvinyl alcohol solution to minimize drug content loss. At this time, the number of recirculation is not limited to one.

preparation example 2

[0052] Preparation Example 2: Preparation of Microparticles Containing Donepezil

[0053] Donepezil-containing microparticles were formed from the oil-in-water emulsion of Preparation Example 1 above by a solvent evaporation method. At this time, the microparticles of Comparative Examples 1 to 3 and Example 1 can be formed according to the setting of temperature conditions for solvent evaporation. The formed microparticles were centrifuged at 1500 rpm for 5 minutes, and the obtained microparticles were lyophilized overnight and sieved with a 100-mesh (180-80um, 125um) sieve.

[0054] Table 1

[0055] Preparation of Microparticles of Comparative Examples 1 to 3 and Example 1 According to Setting of Temperature Conditions for Solvent Evaporation

[0056]

[0057] The specific method of temperature adjustment in this preparation example is as follows.

[0058]1) A circulator for temperature adjustment is attached to the reactor in the form of a water jacket made of stainles...

Embodiment 2 to Embodiment 5

[0061] Example 2 to Example 5: Preparation of microparticles containing donepezil

[0062] In addition to mixing polylactic acid-glycolic acid RG752H (polylactic acid: polyglutamic acid = 75:25) or polylactic acid-glycolic acid RG502H (polylactic acid: polyglutamic acid = 50:50) to replace polylactic acid by 10-25% Except for the polymer alone, one-month drug-releasing fine particles were prepared in the same manner as the preparation method of the fine particles of Example 1 according to the composition of Table 2 below.

[0063] The composition of table 2 embodiment 1 to embodiment 5

[0064]

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Abstract

The present invention relates to a method for preparing slow-release drug particles facilitating release control. Although the preparation method according to the present invention is a simple methodof controlling the evaporation temperature of a solvent in a conventional particle preparation process, the initial release amount can be easily controlled as shown in the following example. In addition, the drug loading rate is very good since an additional separate process is not required, and the stability of a heat-susceptible drug is not threatened since high temperature control is not required.

Description

technical field [0001] The invention relates to a method for preparing sustained-release drug microparticles which are easy to control release. Background technique [0002] In order to sustain the release of drugs, the technology of loading drugs on biodegradable polymer particles has been developed. However, drugs developed into microparticle systems have a problem of often higher initial drug release. [0003] The preparation of microparticles is performed by solvent evaporation, spray drying, coacervation, etc., among which solvent evaporation is the most commonly used. [0004] The solvent evaporation method means, for example, a method of forming microparticles by evaporating a solvent therefrom after preparing an oil-in-water (O / W) or water-in-oil-in-water (W / O / W) emulsion. The most common method of evaporating the solvent is the method of removing the solvent by raising the temperature to around the boiling point of the solvent. However, if volatilization starts f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/34A61K31/445A61K9/00
CPCA61K31/445A61K9/5026A61K9/5089A61K9/5031A61K9/146A61K47/34A61K9/0019A61K9/107A61K9/1682
Inventor 裵秉灿朴圣勋李太镐
Owner DAEWOONG PHARM CO LTD