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