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Pharmaceutical combination with repaglinide and metformin as active components and preparation method thereof

A technology of metformin and active ingredients, applied in the field of medicine, can solve the problems of difficult industrial production, affecting drug release, low bioavailability, etc., and achieve the effect of convenient recycling, convenient separation and purification

Inactive Publication Date: 2011-10-19
HAINAN JINRUI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] The disadvantage of the above-mentioned double-layer sustained-release tablets or respectively compressed small tablets is that their preparation requires too much equipment and is difficult for industrial production, and the preparation process of the double-layer sustained-release tablets will cause the tablet hardness to be too large, which will affect drug release. The connection surface is difficult to release the drug
Moreover, because repaglinide is almost insoluble in water, the drug's in vitro dissolution rate is poor, resulting in low bioavailability.

Method used

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  • Pharmaceutical combination with repaglinide and metformin as active components and preparation method thereof
  • Pharmaceutical combination with repaglinide and metformin as active components and preparation method thereof
  • Pharmaceutical combination with repaglinide and metformin as active components and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0084] [Example 1] Preparation of repaglinide crystals

[0085] 1) dissolving the repaglinide powder in ethanol to form a repaglinide solution as a dispersed phase;

[0086] 2) dissolving sodium 2-ethylhexyl succinate sulfonate in isooctane to form a solution of sodium 2-ethylhexyl succinate sulfonate as a dispersion medium;

[0087] 3) Under the ultrasonic field, use a micro-injector to add the dispersed phase solution into the dispersion medium, continue ultrasonication, and centrifuge to separate repaglinide superpowder, remove the supernatant and add isooctane to wash and centrifuge to remove Sodium 2-ethylhexyl succinate sulfonate adsorbed on the surface of repaglinide, vacuum-dried to obtain repaglinide crystals.

[0088] The particle diameter of the prepared repaglinide crystal is 1 μm, and the X-ray powder diffraction pattern obtained by using Cu-Kα ray measurement (see figure 1 ) at 2θ of 4.8°, 13.6°, 14.9°, 15.2°, 16.0°, 19.1°, 21.2° and 24.1°.

Embodiment 2

[0089] [Example 2] Preparation of repaglinide crystals

[0090] 1) dissolving the repaglinide powder in ethanol to form a repaglinide solution as a dispersed phase;

[0091] 2) Dissolve sodium 2-ethylhexyl succinate sulfonate in isooctane to make 0.05mol L -1 2-ethylhexyl succinate sodium sulfonate solution as a dispersion medium;

[0092] 3) Under an ultrasonic field with a power of 0.1KW, add the dispersed phase solution into the dispersion medium with a micro-injector, continue ultrasonication for 1 minute, and -1 Repaglinide superpowder was separated by high-speed centrifugation under certain conditions, and the supernatant was removed, washed and centrifuged twice with isooctane to remove sodium 2-ethylhexyl succinate sulfonate adsorbed on the surface of repaglinide, Vacuum drying for 8 hours, that is repaglinide crystals.

[0093] The obtained repaglinide crystals had a particle size of 5 μm, and the X-ray powder diffraction pattern measured by Cu-Kα rays was consiste...

Embodiment 3

[0094] [Example 3] Preparation of repaglinide crystals

[0095] 1) dissolving the repaglinide powder in ethanol to form a repaglinide solution as a dispersed phase;

[0096] 2) Dissolve sodium 2-ethylhexyl succinate sulfonate in isooctane to make 0.3mol L -1 2-ethylhexyl succinate sodium sulfonate solution as a dispersion medium;

[0097] 3) Under an ultrasonic field with a power of 0.3KW, add the dispersed phase solution into the dispersion medium with a micro-injector, continue ultrasonication for 3 minutes, and -1 Repaglinide superpowder was separated by high-speed centrifugation under certain conditions, and the supernatant was removed and washed with isooctane and centrifuged 4 times to remove sodium 2-ethylhexyl succinate sulfonate adsorbed on the surface of repaglinide. After vacuum drying for 12 hours, repaglinide crystals were obtained.

[0098] The obtained repaglinide crystals had a particle size of 3 μm, and the X-ray powder diffraction pattern measured by Cu-Kα...

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Abstract

The invention relates to a pharmaceutical combination with repaglinide and metformin as active components and a preparation method thereof. The pharmaceutical combination comprises 0.1-10 weight portions of repaglinide and 100-1500 weight portions of metformin as active components and pharmaceutic adjuvants, wherein, the pharmaceutic adjuvants comprise filler, disintegrating agent, adhesive, flavoring agent, lubricant and swelling accessory, and the repaglinide is repaglinide crystal. The invention adopts the repaglinide crystal with small particle size, metformin and pharmaceutic adjuvants to prepare the pharmaceutical combination, so as to realize the purpose of simultaneous release. Since the particle size of the repaglinide used in the invention is small, the dissolvability is improved, so that the dissolution is improved and the bioavailability is increased.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a pharmaceutical composition with repaglinide and metformin as active ingredients and a preparation method thereof. Background technique [0002] Repaglinide, its chemical name is: S(+)-2-ethoxy-4-{2-[(3-methyl-1-(2-(1-piperidinyl)phenyl)butyl )amino]-2-oxoethyl}benzoic acid. Molecular formula: C 27 h 36 N 2 o 4 , molecular weight: 452.59, its structural formula is as follows: [0003] [0004] Repaglinide is a benzoic acid derivative, a non-sulfonylurea insulin secretagogue, a rapid-acting new oral hypoglycemic drug that specifically binds to the 36KDA protein on the ATP-dependent potassium ion channel outside the islet β cell membrane , to close potassium channels, depolarize β cells, open calcium channels, influx calcium ions, and promote insulin secretion. [0005] Metformin, chemical name: 1,1-dimethylbiguanide, a commonly used drug for the treatment o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/451A61K31/155A61K9/30C07D295/135A61P3/10
Inventor 马鹰军钟正明
Owner HAINAN JINRUI PHARMA CO LTD
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