Repaglinide/metformin composition

A technology of metformin hydrochloride and its composition, which is applied in the field of medicine and can solve the problems of high tablet hardness, inconsistent onset time, and high treatment costs for patients

Active Publication Date: 2013-08-21
HANGZHOU ZHUYANGXIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0016] The disadvantage of the above-mentioned double-layer sustained-release tablets or compressed small tablets separately is that their preparation requires too much equipment and is difficult to industrialized production. Even if the products are put on the market, patients will need to pay high treatment costs; The preparation process will lead to excessive hardness of the tablet, which will affect the release of the drug, and it will be difficult to release the drug from the connecting surface of the upper and lower double-layer tablets
Moreover, because repaglinide is almost insoluble in water, the drug's in vitro dissolution rate is poor, resulting in low bioavailability.
[0017] In the compound tablet containing repaglinide and metformin, the weights of the two active ingredients differ greatly, so special consideration needs to be given to the uniformity of low-dose repaglinide, that is, the content uniformity; Glinide has poor solubility and metformin has very good solubility. There is a big difference between the two in the dissolution performance of the tablet, which may cause the onset time of the two drugs to be inconsistent after the tablet is taken.

Method used

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  • Repaglinide/metformin composition
  • Repaglinide/metformin composition
  • Repaglinide/metformin composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] Embodiment 1: preparation pharmaceutical composition

[0080] formula:

[0081]

[0082] In the above table, the amount of arginine is 1.95 mole times that of repaglinide (both are expressed in mole times when calculating the relative amounts of the two below).

[0083] Preparation method:

[0084] (a) Grinding each material to a pharmaceutically acceptable particle size (particle size less than 80 mesh);

[0085] (b) Preparation of granule I: Repaglinide, alkaline agent, solubilizer, and binder are dissolved in an appropriate amount of water to make a 2 / 4 saturated solution, and the solution is sprayed (retrofitted syringe at the outlet, solution can be ejected from it when extruded outwards) into the filler, fully mixed evenly, dried to a particle with moisture lower than 2%, and then the dried particle is ground into a fine powder with a particle size of less than 80 mesh to obtain particle I (this process The repaglinide yield of medium granule I is 96.7%); ...

Embodiment 2

[0090] Supplementary Example 2: Referring to the formula and method of the above-mentioned Example 1, the difference is that the amount of colloidal silicon dioxide is adjusted, which are 0, 1, 2.5, 5, 7.5, 12.5, 15, 20, 30, and 50 times by weight, the plain tablets obtained are respectively recorded as Ex121, Ex122, Ex123, Ex124, Ex125, Ex126, Ex127, Ex128, Ex129 and Ex130, and are sealed and packed in aluminum-plastic composite film bags respectively.

Embodiment 3

[0091] Supplementary Example 3: Referring to the formula and method of the above-mentioned Example 1, the difference is that arginine is replaced by meglumine, and the amounts are 0.5, 1.0, 2.0, 5.0, 10.0 mole times of repaglinide respectively , The plain sheets obtained are recorded as Ex131, Ex132, Ex133, Ex134, Ex135 respectively, and are sealed and packed in aluminum-plastic composite film bags respectively.

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Abstract

The invention relates to a repaglinide / metformin composition, particularly a pharmaceutical composition which comprises the following components in parts by weight: 500 parts of metformin hydrochloride, 0.5-5 parts of repaglinide and 10-200 parts of medicinal auxiliary materials. The medicinal auxiliary materials include, but are not limited to filler, disintegrant, binding agent, alkali and lubricant. The invention also relates to a method for preparing the pharmaceutical composition. The pharmaceutical composition provided by the invention has favorable pharmaceutical properties.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a tablet pharmaceutical composition with repaglinide and metformin as active ingredients and a preparation method thereof. Background technique [0002] Repaglinide (English name 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: C27H36N2O4, molecular weight: 452.59, and its structural formula is as follows: [0003] [0004] Repaglinide is a benzoic acid derivative, a non-sulfonylurea insulin secretagogue, a new type of oral hypoglycemic drug that acts rapidly, and specifically binds to the 36KDA protein on the ATP-dependent potassium ion channel outside the islet D cell membrane , to close the potassium channel, depolarize the D cell, open the calcium channel, and promote the influx of calcium ions to promote insulin secretion. [0005] Metformin (Metformin), i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/451A61K9/20A61K9/48A61K9/28A61K47/16A61P3/10A61K31/155
Inventor 沈如杰李阅东唐建飞何海珍姚成娥赵福斌刘玉艳刘秋敏马雯霞
Owner HANGZHOU ZHUYANGXIN PHARMA
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