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Poorly soluble drug containing microsphere with improved bioavailabilty and method of preparing the same

Inactive Publication Date: 2012-03-29
SAMYANG BIOPHARMLS CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0010]The present invention provides a technology capable of remarkably increasing water solubility in order to increase bioavailability of a poorly soluble drug.

Problems solved by technology

However, since practical bioavailability of fenofibrate is still low and the use of a surfactant may induce toxicity to human body, there is still a demand for the improvement.

Method used

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  • Poorly soluble drug containing microsphere with improved bioavailabilty and method of preparing the same
  • Poorly soluble drug containing microsphere with improved bioavailabilty and method of preparing the same
  • Poorly soluble drug containing microsphere with improved bioavailabilty and method of preparing the same

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0053]10 g of HPMC (2910 series, ShinEtsu Chemical., hereinafter, the same) was mixed with 90 g of water and agitated to prepare a completely dissolved 10 % w / w solution. 2 g of fenofibrate was mixed with 200 g of ethanol and agitated to completely dissolve. The two solutions were mixed and agitated again to prepare a solution without precipitations. The weight ratio of fenofibrate and HPMC was 1:5 (weight of fenofibrate:weight of HPMC).

[0054]The solution was spray dried with a nozzle type spray drier (Mini spray dryer B-290, Buchi) at a injection temperature of 90° C. and injection amount of 3 mL / min, to obtain a fenofibrate containing microsphere of a relative spherical shape with an average particle size of 50 μm.

example 2

[0055]450 g of HPMC and 2550 g of water were mixed and agitated to prepare a completely dissolved 15 % w / w solution. 90 g of fenofibrate and 5500 g of ethanol were mixed and agitated to completely dissolve. The two solutions were mixed and agitated again to prepare a solution without precipitations. The weight ratio of fenofibrate and HPMC was 1:5.

[0056]The solution was spray dried with an atomizer type spray drier (DJE-003R, Donjin Spray Drying Technology), at a spray temperature of 110° C., injection amount of 45 mL / min, and atomizer speed of 3,500 rpm, to obtain a fenofibrate containing microsphere of a relatively spherical shape with a size of 50 μm.

experimental example 1

[0059]For the microspheres obtained in Example 1, Example 2 and Comparative Example 1, dissolution test was performed under the following conditions, and the results are shown in FIG. 1.

[0060]Dissolution test conditions are as follows.[0061]Test method: the second method of Korean Pharmacopoeia 9th Revision (Paddle method)[0062]Apparatus: LABFINE Dissolution tester (Model name DST-810, Wrap Fine Co. Ltd)[0063]dissolution solution: 500 mL water[0064]temperature: 37±0.5° C.[0065]paddle rotation speed: 100 rpm

[0066]The poorly soluble drug containing microspheres with uniform distribution (Examples 1 and 2) exhibited excellent dissolution compared to the crystalline poorly soluble drug (Comparative Example 1), in vitro dissolution test.

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Abstract

A poorly soluble drug containing microsphere with improved bioavailability, an oral formulation comprising the same, and a method of preparing the same are provided, wherein the poorly soluble drug containing microsphere is a solid dispersion wherein the poorly soluble drug is dispersed in the water-soluble polymer carrier in a noncrystalline form by spray drying, thus increasing bioavailability of the poorly soluble drug.

Description

TECHNICAL FIELD[0001]The present invention relates to a poorly soluble drug containing microsphere, a pharmaceutical composition comprising the same, and a method of preparing the same. More specifically, to a poorly soluble drug containing microsphere with improved bioavailability of the poorly soluble drug, an oral formulation comprising the same, and a method of preparing the same.BACKGROUND OF ART[0002]Since most of newly developed drugs are poorly soluble, it is required to improve the solubility or absorption.[0003]A method of increasing solubility of the existing poorly soluble drugs includes chemical modification and physical modification. The chemical modification includes salt addition, aqueous prodrug approach, and the like, and the physical modification includes modification of particle size or crystal form, formation of crystalline polymorph, formation of complex using a surfactant or cyclodextrin, drug dispersion using a dispersant, and the like. To increase solubility...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/519A61K31/343A61K31/216A61K31/55A61K31/593A61K31/4184A61K31/7048A61K31/522A61K31/52
CPCA61K9/1635A61K9/1694A61K31/522A61K9/1652A61K31/216A61K31/22A61K31/366A61K31/40A61K31/4178A61K31/4184A61K31/436A61K31/57A61P3/06A61K9/16A61K47/34A61K47/38
Inventor KIM, KYUNG-HEELEE, HYUN-KIHWANG, JUN- SEOKHWANG, SU-LONGPAI, CHAUL-MIN
Owner SAMYANG BIOPHARMLS CORP