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Preparation process for ultrafine glibenclamide particles

A fine-grained and granular technology, which is applied to the active ingredients of sulfonylureas, devices that make medicines into special physical or taking forms, and metabolic diseases, etc. To achieve the effect of easy transportation and storage, good stability, easy to scale up and large-scale production

Inactive Publication Date: 2012-04-04
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The solubility of glibenclamide in water medium is very small, and it is not easy to be absorbed in the gastrointestinal tract. In order to improve the bioavailability of glibenclamide, the traditional preparation process usually adopts the measure of adding hydrophilic excipients, but the preparation of this process The essence of the process is to physically mix raw materials and excipients

Method used

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  • Preparation process for ultrafine glibenclamide particles
  • Preparation process for ultrafine glibenclamide particles
  • Preparation process for ultrafine glibenclamide particles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] A: Weigh 0.5g glibenclamide bulk drug and dissolve it in 10ml DMF;

[0039] B: Weigh 0.5g of hydroxypropyl methylcellulose and 0.018g of sodium dodecylbenzenesulfonate and dissolve them in 300mL of water, put the beaker containing the aqueous solution in an ice-water bath, and control the temperature of the aqueous solution at about 2°C;

[0040] C: under the stirring condition of 2000rpm, pour the bulk drug solution prepared in step A into the aqueous solution of step B to obtain drug slurry;

[0041] D: the inlet temperature of the control spray dryer (SD-Basic, Labplant, UK) is 160°C, the outlet temperature is 83°C, the feed rate is 28ml / min, the compressed air pressure is 0.6MPa, and the drug slurry is spray-dried, and then The superfine glibenclamide drug composite powder is obtained.

[0042] figure 1 It is the scanning electron micrograph of glibenclamide API; figure 2 It is the scanning electron micrograph of the particles in the glibenclamide slurry of embo...

Embodiment 2

[0044] A: Weigh 0.5g glibenclamide bulk drug and dissolve it in 10ml DMF;

[0045] B: Weigh 0.5g of hydroxypropyl methylcellulose and dissolve it in 300mL of water, bathe the beaker containing the aqueous solution in ice water, and control the temperature of the aqueous solution at about 2°C;

[0046] C: under the stirring condition of 2000rpm, pour the bulk drug solution prepared in step A into the aqueous solution of step B to obtain drug slurry;

[0047] D: the inlet temperature of the control spray dryer (SD-Basic, Labplant, UK) is 160°C, the outlet temperature is 83°C, the feed rate is 28ml / min, the compressed air pressure is 0.6MPa, and the drug slurry is spray-dried, and then The superfine glibenclamide drug composite powder is obtained.

Embodiment 3

[0049] A: Weigh 4g glibenclamide bulk drug and dissolve it in 80ml DMF;

[0050] B: Weigh 4g of hydroxypropyl methylcellulose and 0.14g of sodium dodecylbenzenesulfonate and dissolve them in 2400mL of water, bathe the beaker containing the aqueous solution in ice water, and control the temperature of the aqueous solution at about 2°C;

[0051] C: under the stirring condition of 2000rpm, pour the bulk drug solution prepared in step A into the aqueous solution of step B to obtain drug slurry;

[0052] D: the inlet temperature of the control spray dryer (SD-Basic, Labplant, UK) is 160°C, the outlet temperature is 83°C, the feed rate is 28ml / min, the compressed air pressure is 0.6MPa, and the drug slurry is spray-dried, and then The superfine glibenclamide drug composite powder is obtained.

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Abstract

The invention discloses a preparation process for ultrafine glibenclamide particles, which belongs to the field of micronization of drugs. The process comprises the following steps: preparing an organic solution of glibenclamide; dissolving pharmaceutic adjuvants in water to form an aqueous solution and controlling the temperature of the aqueous solution to be 2 to 50 DEG C; mixing the above mentioned two solutions to prepare medicinal slurry, carrying out spray drying on the medicinal slurry, and controlling inlet temperature to be 100 to 170 DEG C, outlet temperature to be 60 to 95 DEG C, a feeding speed to be 5 to 40 ml / min and compressed air pressure to be 0.4 to 0.8 MPa so as to obtain ultrafine glibenclamide powder. The ultrafine powder provided in the invention has good stability, and more than 85% of the powder can be dissolved within 2.5 minutes; the process is simple and is easy to operate.

Description

Technical field: [0001] The invention relates to a preparation method of ultrafine glibenclamide particles, which belongs to the field of medicine micronization. Background technique [0002] Diabetes is a systemic chronic metabolic disease determined by genetics. Due to the relative or absolute deficiency of insulin in the body, it causes the disorder of sugar, fat and protein metabolism. On a global scale, with the continuous improvement of people's living standards, changes in diet structure, improvement in labor intensity, and increased stress, the incidence of diabetes in the world is increasing at an alarming rate. According to the prediction of international authoritative diabetes epidemiology experts, by 2010, global diabetes patients will increase to 239 million, and by 2025 it will reach 300 million, of which more than 90% are type II diabetes. The situation in our country is no exception. It increases rapidly at a rate of 0.1% every year, and type II diabetes pat...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/64A61P3/10A61J3/02
Inventor 陈建峰于雷乐园王洁欣
Owner BEIJING UNIV OF CHEM TECH
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