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Preparation method of glimepiride tablets

A technology of urea tablets and povidone, which is applied in the field of medicine and can solve problems such as low bioavailability, harsh conditions, and instability

Inactive Publication Date: 2016-07-20
CHONGQING CONQUER PHARML
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] Our company has applied for a patent authorization announcement number of CN102488667B, announcing a glimepiride tablet and its preparation method. The products prepared according to this prescription process cannot meet the requirements of the new standard. At the same time, the particle size of the drug in this patent is controlled below 2 μm. The conditions are relatively harsh, requiring high-performance jet mill performance, as well as a large amount of energy and manpower consumption
[0006] In the prior art, the invention patent with the patent number CN102512388B provides a glimepiride orally disintegrating tablet, which is prepared by inclusion technology, and glimepiride is clathrated with polypropylene resin S100 to prepare Tablets disintegrate quickly but dissolve poorly
[0007] The invention patent with the patent number CN102600106A relates to glimepiride nanoparticle capsules and its preparation method, which can effectively solve the problems of poor water solubility, short half-life, instability, low bioavailability and poor effect of targeted therapy of glimepiride. The technical solution is: by weight ratio: 1 part of glimepiride, 1 to 30 parts of surfactant, and 3 to 60 parts of lyoprotectant; The mixture of meurea and the above-mentioned surfactant is dissolved in an organic solvent to prepare an initial suspension, and a suspension with an average particle size of 300±60nm is obtained by using a high-pressure homogenization method or an emulsification diffusion method; the nano-suspension After the liquid is freeze-dried and sieved, it is filled in the capsule shell
The preparation process is complex and uses a large amount of surfactants

Method used

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  • Preparation method of glimepiride tablets
  • Preparation method of glimepiride tablets
  • Preparation method of glimepiride tablets

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preparation example Construction

[0044] The preparation method of the glimepiride tablet announced by the patent of the present invention mainly relies on two ways to improve the dissolution rate of the main drug, one is micronization of the glimepiride raw material drug; the other is adding auxiliary materials that help to improve the dissolution rate, Specifically, adding a hydrophilic binder povidone and increasing the amount of water-soluble excipient lactose. The glimepiride raw material drug is pulverized to prepare glimepiride powder with a particle size of less than 10 μm by means of an airflow pulverization method.

[0045] The present invention also provides a glimepiride tablet prepared by the above method, the glimepiride tablet components include glimepiride raw material drug, lactose, povidone, sodium carboxymethyl starch, microcrystalline cellulose, stearin Magnesium acid magnesium, glimepiride raw material medicine, lactose, povidone, carboxymethyl starch sodium, microcrystalline cellulose, ma...

Embodiment 1

[0061] Preparation Method Ⅰ of Glimepiride Tablets (Experimental Group 1)

[0062] Micropowder the glimepiride raw material to below 10 μm, weigh 2kg of the glimepiride raw material, 55kg of lactose, 5.2kg of sodium carboxymethyl starch I (internal addition), 0.4kg of povidone, and 0.25kg of microcrystalline cellulose, Carboxymethyl starch sodium II (external addition) 1.9kg, magnesium stearate 0.325kg, glimepiride micropowder, lactose, carboxymethyl starch sodium I (internal addition) were added to the wet granulator and mixed for 20-30 minutes to obtain Glide meurea mixture;

[0063] Add povidone into 9.6kg water and dissolve to prepare 4% povidone aqueous solution (W / W);

[0064] Add 4% povidone aqueous solution to make soft material in the wet granulator, add 14 mesh screens to granulate with a swinging granulator, and dry the granules with a fluidized bed;

[0065] The dried granules are sized with 20 meshes, added with microcrystalline cellulose, sodium starch glycolat...

Embodiment 2

[0067] Glimepiride Tablets Preparation Method II (Experimental Group 2)

[0068] Micropowder the glimepiride raw material to below 10 μm, weigh 2kg of the glimepiride raw material, 55kg of lactose, 5.2kg of sodium carboxymethyl starch I (internal addition), 0.4kg of povidone, and 0.25kg of microcrystalline cellulose, Carboxymethyl starch sodium II (external addition) 1.9kg, magnesium stearate 0.325kg, glimepiride micropowder, lactose, carboxymethyl starch sodium I (internal addition) were added to the wet granulator and mixed for 20-30 minutes to obtain Glide meurea mixture;

[0069] Add povidone to 9.6kg of 75% ethanol (W / W) solution and dissolve to prepare 4% povidone ethanol solution (W / W);

[0070] Add 4% povidone ethanol solution to the wet granulator to make soft materials, add 14 mesh screens to granulate with a swing granulator, and dry the granules with a fluidized bed;

[0071] The dried granules are sized with 20 meshes, added with microcrystalline cellulose, sodi...

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Abstract

The invention discloses a preparation method of glimepiride tablets.The preparation method comprises the steps that a glimepiride raw material drug is smashed, an auxiliary material is added, a prescription process of the glimepiride tablets is optimized, the glimepiride raw material drug is micronized, the particle size of the glimepiride raw material drug powder is controlled to be smaller than 10 microns, the weight percentage of microcrystalline cellulose is controlled to be below 1%, meanwhile the weight percentage of the water-soluble auxiliary material lactose is kept above 60%, the usage amount of the water-soluble auxiliary material lactose is increased while a soft material is prepared by adopting a hydrophilic adhesive povidone aqueous solution or a povidone ethanol aqueous solution, the proportion of the microcrystalline cellulose is minimized, and meanwhile wet granulation is performed by adopting a povidone containing solution.By the adoption of the preparation method, the dissolution rate of the drug in a dissolution medium is improved, the particle size smaller than 10 microns of the raw materials can meet the requirements, energy consumption is reduced, the dissolution rate of a main drug is accelerated, the time is saved, and the drug dissolution and bioavailability are improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular, the invention relates to a preparation method of glimepiride tablets. Background technique [0002] Glimepiride, chemical name 1-[4-[2-(3-ethyl-4-methyl-2-oxo-3-pyrroline-1-carboxamido)ethyl]benzenesulfonyl ]-3-(trans-4-methylcyclohexyl)urea is a new sulfonylurea hypoglycemic drug developed by the German company HoechstMarionRoussel (HMR) and first listed in Sweden under the trade name Amaryl in September 1995 , was approved by the FDA to enter the US market in 1996. It is used to treat type 2 diabetes that cannot be controlled by diet and exercise. It is the first sulfonylurea drug approved by the FDA that can be used simultaneously with insulin. Because the drug has a short action time with the receptor, it shortens the time for insulin secretion, so it has a strong insulin-sparing effect and can overcome the secondary failure of islet cells to a certain extent. Glimepiride ha...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/64A61K47/26A61K47/38A61K47/32A61P3/10
CPCA61K9/2018A61K9/2027A61K9/2054A61K31/64
Inventor 胡瀚赵伟淑田建尹江
Owner CHONGQING CONQUER PHARML
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