Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

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
View PDF8 Cites 3 Cited by
  • 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 requires expensive instruments and equipment. And specific production environment and full-time staff, so this method is not suitable for industrialized production
[0007] Generally speaking, the drug is pulverized to obtain a smaller particle size, thereby improving the dissolution of the drug. However, for solid preparations containing glibenclamide, the high dissolution rate will make glibenclamide in the serum. The time to peak blood concentration of the drug in the blood becomes shorter, leading to hypoglycemia in the patient, which is life-threatening

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Granularityaaaaaaaaaa
Login to View More

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com