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A kind of slgt2 inhibitor particle and preparation method thereof

A technology of inhibitors and granules, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of low dissolution rate of tablets, uneven mixing, and difficulty in crushing, etc. Achieve the effects of improving drug release, increasing dispersion state, and improving solubility

Inactive Publication Date: 2017-12-08
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Studies have found that before making SLGT2 inhibitors into preparations, if the raw materials are micronized to reduce the particle size, but due to the low melting point of the drug (for example, canagliflozin is 98-100°C, and dapagliflozin is 75-80°C), It is easy to produce "sticky phenomenon", and it is difficult to carry out subsequent crushing; if the particle size of the drug can be controlled within a small range, such as D 90 ≤50μm, but due to the large specific surface area of ​​the drug, the drug density is small, and it is easy to float. When using 4-8% hydroxypropyl cellulose aqueous solution for wet granulation, it is easy to produce uneven mixing. Long-term granulation can produce a large amount of Heat, causing the drug to aggregate into balls and increase the particle size, resulting in low dissolution of the prepared tablets or large differences between tablets
[0009] The experiment also found that after the SLGT2 inhibitor is prepared into an amorphous form, the amorphous form has poor stability and a low melting point (such as dapagliflozin at 49.5-62.6°C), and it is easy to convert into a stable crystal form, which is difficult to store for a long time

Method used

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  • A kind of slgt2 inhibitor particle and preparation method thereof
  • A kind of slgt2 inhibitor particle and preparation method thereof
  • A kind of slgt2 inhibitor particle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1 Preparation of canagliflozin granules

[0036] Step (1): Take 100 g of canagliflozin, add 1500 g of ethanol, stir to dissolve or disperse uniformly, and use it as solution A for use.

[0037] Step (2): Take 25 g of povidone (K30) and 20 g of lactose, add 500 g of purified water, stir to dissolve, and use it as solution B.

[0038] Step (3): Add solution A to solution B, stir to make it evenly dispersed, as solution C.

[0039] Step (4): Solution C is spray dried in a spray dryer (Model: SD-1500, Shanhai Wodi Automation Equipment Co., Ltd., the same below), and the temperature of spray drying is controlled to 100°C; the spray dried materials are collected, Pass through a 60-mesh sieve to obtain canagliflozin particles.

Embodiment 2

[0040] Example 2 Preparation of canagliflozin granules

[0041] Step (1): Take 100 g of canagliflozin, add 700 g of acetone, stir to dissolve or disperse uniformly, and use it as solution A for use.

[0042] Step (2): Take 80 g of polyvinyl alcohol-polyethylene glycol graft copolymer and 180 g of mannitol, add 1500 g of 10% acetone aqueous solution (w / w), stir to dissolve, and use it as solution B.

[0043] Step (3): Add solution A to solution B, stir to make it evenly dispersed, as solution C.

[0044] Step (4): Solution C is spray-dried in a spray dryer, and the temperature of spray-drying is controlled to 115°C; the spray-dried materials are collected and passed through a 60-mesh sieve to obtain canagliflozin particles.

Embodiment 3

[0045] Example 3 Preparation of canagliflozin granules

[0046] Step (1): Take 100 g of canagliflozin, add 1500 g of ethanol-isopropanol solution (2:8, w / w), stir to dissolve or disperse uniformly, and use it as solution A for use.

[0047] Step (2): Take 50 g of hydroxypropyl cellulose (ELF) and 100 g of xylitol, add 800 g of aqueous solution, stir to dissolve, and use it as solution B.

[0048] Step (3): Add solution A to solution B, stir to make it evenly dispersed, as solution C.

[0049] Step (4): Solution C is spray-dried in a spray dryer, and the temperature of spray-drying is controlled to be 105°C; the spray-dried materials are collected and passed through a 60-mesh sieve to obtain canagliflozin particles.

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Abstract

The invention discloses a SLGT2 inhibitor granule and a preparation method thereof. The SLGT2 inhibitor granule is composed of an SLGT2 inhibitor, a crystal inhibitor and a filler, and the mass ratio of the SLGT2 inhibitor, the crystal inhibitor and the filler is 10 :0.5~10:0.5~20, preferably 10:1~5:1~15, the SLGT2 inhibitor is selected from any one of canagliflozin, dapagliflozin and empagliflozin. The granules are prepared by forming an organic solution containing SLGT2 inhibitors, crystal inhibitors and fillers, and spray drying. The granules have good fluidity, strong compressibility and less dust, and can be further prepared into tablets, capsules, granules and other preparations, which solve the problem of low dissolution and bioavailability of SLGT2 inhibitors caused by poor water solubility.

Description

Technical field [0001] The invention relates to SLGT2 inhibitor particles and a preparation method thereof, and belongs to the field of pharmaceutical preparations. Background technique [0002] SLGT2 inhibitor (sodium-glucose co-transporter 2inhibitors) is a kind of inhibitor that can specifically inhibit the proximal tubules of the glomerulus, reabsorb the filtered glucose, and make excess glucose from the urine It is a drug that directly lowers blood sugar. Clinical studies have shown that SGLT2 inhibitors have good efficacy, safety and tolerance, can effectively reduce blood sugar, increase the excretion of glucose in urine, and become a new method for the treatment of type 2 diabetes hyperglycemia (Hu Li,Zhou Zhaoyuan.Research progress of SGLT2 inhibitor drugs[J].Medical Review.2011,17(24):3782-3785). The drugs used clinically are Johnson & Johnson's Canagliflozin (Canagliflozin, trade name: ) And Bristol-Myers Squibb (abbreviation: BMS)'s Dapagliflozin (trade name: ), i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/381A61K31/351A61K47/32A61K47/38A61K47/26A61P3/10
Inventor 翟光喜汪洋杨小叶
Owner SHANDONG UNIV
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