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Trelagliptin succinate rapid-release pellet preparation and preparation method thereof

A technology of troxagliptin succinate and micropills, which is applied in pill delivery, microcapsules, and pharmaceutical formulations, and can solve the problems of inability to take oral administration, short half-life of the drug, and poor compliance of injections

Inactive Publication Date: 2017-05-10
FOSHAN TENGRUI MEDICINE TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The technical problem to be solved in the present invention is the short drug half-life in the development of trexagliptin succinate medicine, problems such as poor compliance of clinical application injection (cannot be administered orally)

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1 Formulation 1

[0030] Troxagliptin succinate 5000mg Microcrystalline cellulose blank pellet core4000g 0.3% acetic acid solution200ml Hypromellose (HPMC)300g talcum powder50g water5500g

[0031] Preparation:

[0032] (1) Preparation of the drug solution: weigh 5000 mg of troxagliptin succinate according to the formula, add 200 mL of 0.3% acetic acid solution to dissolve, and then dissolve in an aqueous solution containing 100 g of hypromellose (HPMC) to prepare 1500 g Medicine solution.

[0033] (2) Spraying medicine at the bottom of the fluidized bed: Place 4000g of microcrystalline cellulose blank pellets in the fluidized bed, start the fluidized bed, and set the fluidized bed medicine parameters: fan air volume 150m3·h-1, liquid supply The pump speed is 5r·min-1, the material temperature is controlled at 30-40℃, the atomization pressure is 0.16MPa, and the medicine is applied in the fluidized state. After the medicine is completed, fluidized and dried for...

Embodiment 2

[0036] Example 2 Formulation 2

[0037] Troxagliptin succinate1g Sucrose blank pellet core4000g 0.1% citric acid solution300ml Povidone (PVP)8g Acrylic200g water5000g

[0038] Preparation:

[0039] (1) Preparation of the drug solution: Weigh 1g of troxagliptin succinate according to the formula, add 300mL of 0.1% citric acid solution to dissolve it, and then dissolve it in an aqueous solution containing 8g of povidone (PVP) to prepare 1500g. Medicine solution.

[0040] (2) Spraying medicine at the bottom of the fluidized bed: Put 4000g of sucrose blank pellet cores in the fluidized bed, start the fluidized bed, and set the fluidized bed medicine parameters: fan air volume 150m3·h-1, liquid supply pump speed 5r ·Min-1, the material temperature is controlled at 30~40℃, the atomization pressure is 0.16MPa, and the medicine is applied in a fluidized state. After the application is completed, fluidized and dried for 15 minutes.

[0041] (3) Fluidized bed coating-protective film la...

Embodiment 3

[0042] Example 3 Formulation 3

[0043] Troxagliptin succinate1g Sucrose blank pellet core4000g 0.6% hydrochloric acid solution700ml syrup70g Acrylic200g water4500g

[0044] Preparation:

[0045] (1) Preparation of the drug solution: Weigh 1 g of troxagliptin succinate according to the formula, add 700 mL of 0.6% hydrochloric acid solution to dissolve, and then dissolve it in an aqueous solution containing 70 g of syrup to prepare 1500 g of drug solution.

[0046] (2) Spraying medicine at the bottom of the fluidized bed: Put 4000g of sucrose blank pellet cores in the fluidized bed, start the fluidized bed, and set the fluidized bed medicine parameters: fan air volume 150m3·h-1, liquid supply pump speed 5r ·Min-1, the material temperature is controlled at 30~40℃, the atomization pressure is 0.16MPa, and the medicine is applied in a fluidized state. After the application is completed, fluidized and dried for 15 minutes.

[0047] (3) Fluidized bed coating-protective film layer: w...

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PUM

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Abstract

The invention discloses a trelagliptin succinate rapid-release pellet preparation and a preparation method thereof, and relates to the field of pharmaceutic preparation technologies and application. The rapid-release pellet preparation is administrated orally; a core pellet is taken as a carrier, and a trelagliptin succinate aqueous solution containing a co-solvent and a bonding agent is taken as an administration solution. The trelagliptin succinate rapid-release pellet preparation has the characteristics of high administration rate, high content uniformity, rapid release, quick response of the analgesic activity and the like. Meanwhile, the rapid-release pellet preparation has high clinical use compliance, high security and the like.

Description

Technical field [0001] The invention relates to the field of pharmaceutical preparation technology and application, in particular to a troxagliptin succinate quick-release pellet preparation, a preparation method and application thereof. Background technique [0002] Trelagliptin (Trelagliptin succinate), developed by Takeda and Furiex, was launched on March 7, 2015 under the trade name: Zafatek. Troxagliptin is an ultra-long-acting dipeptidyl peptidase IV (DPP-4) inhibitor, which controls blood glucose levels by selectively and persistently inhibiting DPP-4. It is taken once a week, compared with similar DPP on the market. -4 inhibitors need to be taken orally once a day. The advantages of Zafatek's medication will undoubtedly provide patients with diabetes with a more convenient treatment option, which is expected to greatly improve the convenience and compliance of patients. [0003] Troxagliptin is a once-weekly dipeptidyl peptidase IV (DPP-4) inhibitor that can trigger incret...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K9/16A61K9/20A61K31/513A61K47/38A61K47/32A61P3/10
CPCA61K9/5078A61K9/1676A61K9/1688A61K9/2081A61K9/5089A61K31/513
Inventor 王雪峰
Owner FOSHAN TENGRUI MEDICINE TECH CO LTD
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