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Glimepiride tablet and preparation method thereof

A technology of glimepiride tablet and urea tablet, which is applied in the field of medicine, can solve the problems of lowering the qualified rate of glimepiride, poor repeatability of treatment effect, poor disintegration rate and dissolution rate, etc., so as to improve bioavailability , Reduce the effect of strong hygroscopicity and good solubility

Pending Publication Date: 2022-04-12
YANGTZE RIVER PHARM GRP GUANGZHOU HAIRUI PHARM CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Yet because glimepiride is a hydrophobic substance, it is difficult to dissolve in water, so that the conventional oral preparations containing glimepiride, especially the disintegration rate and dissolution rate of glimepiride tablets are all poor, and the bioavailability low, which leads to poor repeatability of the treatment effect, and the hygroscopicity of glimepiride is strong, and the problem of sticking, punching and splitting is prone to occur during the production process of glimepiride tablets, which greatly reduces the effect of glimepiride. pass rate

Method used

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  • Glimepiride tablet and preparation method thereof
  • Glimepiride tablet and preparation method thereof

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preparation example Construction

[0073] The present application also provides a preparation method of a glimepiride tablet, which is used for preparing the glimepiride tablet described in any of the above-mentioned embodiments. The preparation method of the glimepiride tablet comprises the following steps: performing a first grinding operation on glimepiride and trehalose to obtain a first grinding product; adding phospholipids to the first grinding material to perform a second grinding operation to obtain a second grinding product Grinding product; dry granulation operation is performed on the second grinding product to obtain glimepiride tablet.

[0074] The preparation method of the above-mentioned glimepiride tablet makes glimepiride and trehalose carry out the first grinding operation, which effectively weakens the hygroscopicity in the pulverization process of glimepiride, and in the grinding process, trehalose and Glimepiride forms a mixed system with better uniformity. In addition, under the condition...

Embodiment 1

[0089] Add 3-ethyl-4-methyl-2-pyrrolidone into n-heptane, the mass ratio of 3-ethyl-4-methyl-2-pyrrolidone to n-heptane is 1:10~18, heat up to 70°C Dissolve, add phenylethyl isocyanate dropwise, the molar ratio of phenylethyl isocyanate to 3-ethyl-4-methyl-2-pyrrolidone is 1:1, heat to 100°C, react for 8 hours, and drop to At room temperature, the crude product of Compound A was obtained, and then methyl tert-butyl ether with the same mass as n-heptane was added, stirred for 25 minutes, filtered, and dried to obtain the pure product of Compound A;

[0090] Add pure compound A to chlorosulfonic acid, the mass ratio of chlorosulfonic acid to 3-ethyl-4-methyl-2-pyrrolidone is 2.5:1, the reaction temperature is 5°C, stir for 3.5h, add 5°C water, and crystal, filtered to obtain compound B;

[0091] Add compound B to saturated ammonia water, the solid-to-liquid ratio of saturated ammonia water to 3-ethyl-4-methyl-2-pyrrolidone is 1g:18ml, the reaction temperature is 35°C, stirred f...

Embodiment 2

[0097] Add 3-ethyl-4-methyl-2-pyrrolidone into n-heptane, the mass ratio of 3-ethyl-4-methyl-2-pyrrolidone to n-heptane is 1:12, heat up to 85°C to dissolve, Add phenylethyl isocyanate dropwise, the molar ratio of phenylethyl isocyanate to 3-ethyl-4-methyl-2-pyrrolidone is 1:1.2, heat to 90°C, react for 10h, and cool down to room temperature after completion, To obtain the crude product of Compound A, add methyl tert-butyl ether equal in quality to n-heptane, stir for 20 min, filter, and dry to obtain the pure product of Compound A;

[0098] Add pure compound A to chlorosulfonic acid, the mass ratio of chlorosulfonic acid to 3-ethyl-4-methyl-2-pyrrolidone is 2.8:1, the reaction temperature is 10°C, stir for 3h, add 10°C water, crystallize , filtered to obtain compound B;

[0099] Add compound B to saturated ammonia water, the solid-to-liquid ratio of saturated ammonia water to 3-ethyl-4-methyl-2-pyrrolidone is 1g:15ml, the reaction temperature is 30°C, stirred for 2.5h, filtere...

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Abstract

The invention provides a glimepiride tablet and a preparation method thereof. The glimepiride tablet comprises glimepiride, trehalose and phospholipid which are mixed and ground. The glimepiride tablet disclosed by the invention is relatively good in dissolution rate and relatively high in qualified rate of preparation.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a glimepiride tablet and a preparation method thereof. Background technique [0002] Glimepiride is a third-generation sulfonylurea long-acting antidiabetic drug. Its mechanism of action is to bind to sulfonylurea receptors on the surface of pancreatic β-cells, prompting the closure of adenosine triphosphate-sensitive potassium channels, causing depolarization of the cell membrane. to open voltage-dependent calcium channels, Ca 2+ Influx promotes the release of insulin and inhibits the synthesis of hepatic glucose. Since the interaction time between glimepiride and receptors is short, the insulin secretion time is shortened, which can effectively save insulin. At the same time, it also has high efficiency, long-acting, It is clinically evaluated as the best sulfonylurea hypoglycemic drug due to the advantages of less dosage and less side effects. [0003] Yet because glimepiri...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K47/36A61K47/24A61K31/64A61P3/10
CPCY02A50/30
Inventor 夏春森任亚东施猛刘志强汪刘恒袁海成
Owner YANGTZE RIVER PHARM GRP GUANGZHOU HAIRUI PHARM CO LTD
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