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A solid dispersion of amorphous empagliflozin and a preparing method thereof

A technology of solid dispersion and empagliflozin, which is applied in the direction of medical preparations of non-active ingredients, pharmaceutical formulas, non-active ingredients of polymer compounds, etc., which can solve the difficulties in the development of pharmaceutical formulations and the inability to obtain easily separated solids , the total amount of excipients, etc., to achieve the effect of fast dispersion and dissolution, which is conducive to absorption and increased dissolution

Inactive Publication Date: 2017-06-23
CHANGZHOU FANGNAN MEDICINE TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Pharmaceutical preparations must use a variety of pharmaceutical excipients, and the total amount of excipients is also limited. For example, when a single excipient is used in a large amount, it will also bring certain difficulties to the development of pharmaceutical formulations.
In addition, for the separation of solid dispersions that only add one polymer excipient, no easy-to-separate solids can be obtained.

Method used

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  • A solid dispersion of amorphous empagliflozin and a preparing method thereof
  • A solid dispersion of amorphous empagliflozin and a preparing method thereof
  • A solid dispersion of amorphous empagliflozin and a preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Add empagliflozin (50 mg), hydroxypropyl cellulose SSL (50 mg) and povidone K30 (50 mg) into methanol (800 microliters), heat to 60 ° C and stir to dissolve, and remove by vacuum evaporation solvent to obtain a white powdery solid, i.e. a solid dispersion of amorphous empagliflozin, hydroxypropyl cellulose SSL and povidone K30. The X-ray powder diffraction pattern of this solid dispersion is as follows figure 1 As shown, there is no characteristic peak of the empagliflozin crystal form in the X-ray powder diffraction pattern after deducting the background peak of the pharmaceutical excipient.

Embodiment 2

[0055] Dissolve empagliflozin (50 mg), polyacrylic acid resin Eudragit L100 (50 mg) and polyethylene glycol 4000 (200 mg) in ethanol (600 μl) and water (600 μl) at -40 °C Stir and mix evenly under vacuum, remove the solvent by vacuum evaporation, and obtain a white powdery solid, that is, a solid dispersion of amorphous empagliflozin, polyacrylic acid resin Eudragit L100 and polyethylene glycol 4000. In the X-ray powder diffraction pattern of the solid dispersion, there is no characteristic peak of the crystal form of empagliflozin after deducting the background peak of the pharmaceutical excipient.

Embodiment 3

[0057] Add empagliflozin (2 g), dextrin (2 g) and polyethylene glycol 8000 (10 g) into water (300 ml), heat to 60°C and stir to dissolve. The above solution was dried with JISL micro-spray dryer LSD-48, the inlet temperature was maintained at 60°C and the outlet temperature was 50°C, and the outlet material was collected to obtain a white powdery solid, which was further vacuum-dried to obtain amorphous empagliflozin, dextrin and poly Solid dispersion of ethylene glycol 8000. In the X-ray powder diffraction pattern of the solid dispersion, there is no characteristic peak of the crystal form of empagliflozin after deducting the background peak of the pharmaceutical excipient.

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Abstract

A solid dispersion of amorphous empagliflozin and a preparing method thereof are provided. The solid dispersion includes empagliflozin and two or more than two medicinal auxiliary materials, and the weight ratio of the empagliflozin to all the medicinal auxiliary materials is 1:0.1-100. The empagliflozin in the solid dispersion is amorphous. An X-ray amorphous powder diffraction spectrum of the solid dispersion does not has a characteristic peak of empagliflozin crystals after deducting background peaks of the medicinal auxiliary materials. The solid dispersion has good stability and dispersibility, and the dissolution rate of the empagliflozin is increased, thus increasing bioavailability of a medicine preparation and medicine absorption by a human body. Under accelerated testing conditions, good physical stability and chemical stability can be maintained. The method has characteristics of simple operation, convenient separation, a low cost, good reappearance and easy implementation and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a solid dispersion of amorphous empagliflozin and a preparation method thereof. The present invention also relates to a pharmaceutical composition, which comprises solid dispersion of empagliflozin in amorphous form and at least one pharmaceutically acceptable auxiliary material for treating diabetes. Background technique [0002] Empagliflozin (Emagliflozin), trade name Jardiance, chemical name is: (1S)-1,5-Anhydro-1-C- [4-Chloro-3-[[4-[[(3S)-tetrahydro-3-furyl]oxy]phenyl]methyl]phenyl]-D-glucitol , its structure is shown in formula (I): [0003] [0004] Formula I [0005] Empagliflozin is a drug for the treatment of type II diabetes jointly developed by Boehringer Ingelheim of Germany and Eli Lilly and Company of the United States. Empagliflozin was approved for marketing in the European Union on May 22, 2014, and was approved for marketing by the US FDA on...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/351A61K47/38A61K47/32A61K47/10A61K47/36A61K47/40A61K47/42A61P3/10
CPCA61K9/146A61K31/351
Inventor 张席妮熊志刚周涛胡涛
Owner CHANGZHOU FANGNAN MEDICINE TECH CO LTD
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