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SLGT2 inhibitor granule 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: 2015-03-04
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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  • SLGT2 inhibitor granule and preparation method thereof
  • SLGT2 inhibitor granule and preparation method thereof
  • SLGT2 inhibitor granule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] The preparation of embodiment 1 canagliflozin granules

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

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

[0038] Step (3): Add solution A to solution B, stir to make it evenly dispersed, and use it 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 spray-drying temperature is controlled to be 100° C.; collect the spray-dried materials, Pass through a 60-mesh sieve to obtain canagliflozin granules.

Embodiment 2

[0040] The preparation of embodiment 2 canagliflozin granules

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

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

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

Embodiment 3

[0045] The preparation of embodiment 3 canagliflozin granules

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

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

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

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

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Abstract

The invention discloses an SLGT2 inhibitor granule and a preparation method thereof. The SLGT2 inhibitor granule comprises an SLGT2 inhibitor, a crystal inhibitor and a filler, of which the mass ratio is 10: (0.5-10): (0.5-20), preferably 10:(1-5):(1-15). The SLGT2 inhibitor is any one component selected from the group consisting of Invokana, Dapagliflozin and Empagliflozin. An organic solution containing the SLGT2 inhibitor, the crystal inhibitor and the filler is formed and is spray-dried to be prepared into the granule. The granule has good mobility, strong compressibility and less dust, and can be further prepared into preparations such as tablets, capsules and granules, and the problems that the dissolution and the bioavailability are low due to the poor water solubility of the SLGT2 inhibitor are solved.

Description

technical field [0001] The invention relates to SLGT2 inhibitor particles and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] SLGT2 inhibitors (sodium-glucose co-transporter 2 inhibitors, sodium-glucose co-transporter 2 inhibitors) are a kind of inhibitor that can specifically inhibit the glomerular proximal tubules, reabsorb filtered glucose, and make excess glucose from urine Drugs that directly lower blood sugar. Clinical studies have shown that SGLT2 inhibitors have good drug efficacy, safety and tolerance, can effectively lower blood sugar, increase the excretion of glucose in urine, and become a new method for the treatment of hyperglycemia in type 2 diabetes (Hu Li, Zhou Zhaoyuan.Research progress of SGLT2 inhibitor drugs[J].Medical Review.2011,17(24):3782-3785). The clinically used drug has Canagliflozin (Canagliflozin, trade name: ) and Dapagliflozin (trade name: ), in addition, drugs such as E...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/381A61K31/351A61K47/32A61K47/34A61K47/38A61K47/26A61P3/10
Inventor 翟光喜汪洋杨小叶
Owner SHANDONG UNIV
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