Micronized glibenclamide and composition thereof

A technology of micronization and composition, applied in the field of medicine, can solve the problems of high energy, shortened time to peak blood concentration of glibenclamide, and life-threatening problems

Inactive Publication Date: 2014-10-15
SHENYANG PHARMA UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above report is to use the grinding method to improve the particle size of the glibenclamide raw material drug. However, the grinding method takes a long time and consumes a lot of energy. Not only the cost is high, but the yield is also low, and it is not suitable for industrial production; Patent No. The Chinese patent authorization of CN1210258C discloses a glibenclamide and its composition with a specific particle size distribution, which defines the particle size by sieving. The preparation of particles of such a size generally require...

Method used

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  • Micronized glibenclamide and composition thereof
  • Micronized glibenclamide and composition thereof
  • Micronized glibenclamide and composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Take an appropriate amount of unmicronized and micronized glibenclamide raw materials, and investigate whether the raw materials of two particle sizes are in 0.1M hydrochloric acid solution, pH4.5 acetate buffer, pH6.8 phosphate buffer, pH7.4 The saturation solubility in phosphate buffer and pH8.5 phosphate buffer, the test results are shown in Table 1.

[0043] The glibenclamide was injected into the ultrafine pulverizer and crushed by high-speed airflow. The working pressure of the superfine pulverizer was 2.3 MPa, the internal working temperature was 0-10° C., and the pulverization time was 20 minutes. The obtained micronized glibenclamide with a particle size of 0.5 μm-5 μm accounted for 75%.

[0044] Table 1 Saturation solubility test results of glibenclamide raw materials in buffer solutions with different pH values

[0045]

[0046] From the test results, it can be known that glibenclamide bulk drug is insoluble in 0.1M hydrochloric acid solution, and its sol...

Embodiment 2

[0048]

[0049] Mix the micronized glibenclamide powder with Tween 80, microcrystalline cellulose and lactose according to the method of equal addition, and then mix it with sodium carboxymethyl starch, add 25ml of starch slurry containing 5% to make granules, and heat at 60°C Ventilate and dry, granulate, add magnesium stearate, mix evenly, and compress into tablets.

Embodiment 3

[0051]

[0052] Mix the micronized glibenclamide powder with Tween 80, microcrystalline cellulose and lactose according to the method of equal addition, and then mix it with sodium carboxymethyl starch, add 25ml of starch slurry containing 5% to make granules, and heat at 60°C Ventilate and dry, granulate, add magnesium stearate, mix evenly, and compress into tablets.

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Abstract

The invention relates to composition containing micronized glibenclamide. Particle sizes d0.5 of the micronized glibenclamide are in a range of 0.2 mu m-5 mu m, and the micronized glibenclamide is combined with a carrier to prepare a preparation with the proper dissolution rate. The invention further relates to a method for preparing the micronized glibenclamide solid preparation. By the aid of the method, the solubility of the glibenclamide is improved, the bioavailability is improved, and clinical effects of the pharmaceutical preparation are increased.

Description

technical field [0001] The invention relates to a micronized glibenclamide and its composition, in particular to a solid preparation made of micronized glibenclamide and pharmaceutically acceptable additives made by ultrafine pulverization technology, belonging to field of medical technology. Background technique [0002] Glibenclamide (Glibenclamide) is a second-generation sulfonylurea drug, and its oral preparation has the advantages of fast absorption and high protein binding rate (95%). It is currently the first-line drug for the treatment of type Ⅱ diabetes, and its effect is stronger than that of tolbutamide 100-200 times, so the dosage is significantly reduced. This product can stimulate islet β cells to secrete insulin and lower blood sugar. The prerequisite is that the pancreatic β cells still have a certain function of synthesizing and secreting insulin; this product can also inhibit the decomposition of liver glycogen by increasing the level of portal vein insuli...

Claims

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Application Information

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IPC IPC(8): C07C311/59A61K31/64A61P3/10
Inventor 孙进马攀勤杨亚军刘晓红王永军
Owner SHENYANG PHARMA UNIVERSITY
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