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Glibenclamide nanocrystal preparation and preparation method thereof

A technology of nano-crystal and glyburide, which is applied in the field of preparation and preparation of glyburide nano-crystal, can solve the problems of unfavorable subsequent process of preparation, reduced patient's medication compliance, complicated prescription composition, etc., and achieves no immune stimulation. , good biocompatibility, no physiological toxicity effect

Inactive Publication Date: 2016-08-24
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
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Problems solved by technology

Chinese patent 01803639 discloses a glibenclamide and its composition. The application redefines the required scale range of glibenclamide: 25% of the sieved particles have a particle size of 3-11 microns, and 50% of the sieved The particle size of the sieved material is 6-23 microns, and the particle size of 75% of the sieves is 15-46 microns. However, the addition of fillers, binders, and disintegrants in the prescription makes the drug content in the preparation lower, which is not necessary. It is beneficial to the follow-up process of the preparation and reduces the compliance of patients taking medicine
At present, most of the stabilizers used in glibenclamide are complexes of polymers and surfactants to provide charge stabilization effect, steric stabilization effect and reduce particle sedimentation velocity respectively, and the composition of the formulation is relatively complicated.

Method used

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  • Glibenclamide nanocrystal preparation and preparation method thereof
  • Glibenclamide nanocrystal preparation and preparation method thereof
  • Glibenclamide nanocrystal preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Embodiment 1: Preparation of a kind of glibenclamide nano crystal suspension

[0039] First, prepare 10ml of water phase containing 80mg of HPMC-E5, suspend 1500mg of glibenclamide in the above water phase, and transfer it to a ball mill jar, add 20mL of 0.1mm zirconia ball mill balls at the same time, use planetary Grind in a ball mill for 100 min. Electron microscope results showed that the drug particles were irregular in shape, and the particle size was consistent with the measurement results. Add 500 mg of sucrose to the glibenclamide nanosuspension prepared above, then put it in a refrigerator at -80°C to -20°C, pre-freeze for 4-10 hours, and then freeze-dry it in a freeze-drying device for 15-24 hours. The solidified glibenclamide nanocrystalline preparation was obtained, and the average particle diameter measured after reconstitution was 193nm.

Embodiment 2

[0040] Embodiment 2: Preparation of a kind of glibenclamide nano crystal suspension

[0041]First prepare 10ml of water phase containing 40mg of HPMC-E5, suspend 1200mg of glibenclamide in the above water phase, and transfer it to a ball mill jar, add 20mL of 0.1mm zirconia ball mill balls at the same time, use planetary Grind in a ball mill for 100 min. Electron microscope results showed that the drug particles were irregular in shape, and the particle size was consistent with the measurement results. Add 500 mg of sucrose to the glibenclamide nanosuspension prepared above, then put it in a refrigerator at -80°C to -20°C, pre-freeze for 4-10 hours, and then freeze-dry it in a freeze-drying device for 15-24 hours. The solidified glibenclamide nanocrystalline preparation is obtained, and the average particle diameter measured after reconstitution is 206nm

Embodiment 3

[0042] Embodiment 3: Preparation of a kind of glibenclamide nano crystal suspension

[0043] First prepare 10ml of water phase containing 130mg of PVP K30, suspend 1200mg of glibenclamide in the above water phase, and transfer it to a ball mill jar, add 20mL of 0.1mm zirconia ball mill balls at the same time, use planetary ball mill Grind for 100min. Electron microscope results showed that the drug particles were irregular in shape, and the particle size was consistent with the measurement results. Add 500 mg of sucrose to the glibenclamide nanosuspension prepared above, then put it in a refrigerator at -80°C to -20°C, pre-freeze for 4-10 hours, and then freeze-dry it in a freeze-drying device for 15-24 hours. The solidified glibenclamide nanocrystalline preparation is obtained, and the average particle diameter measured after reconstitution is 238nm

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Abstract

The invention relates to a glibenclamide nanocrystal preparation and a preparation method and belongs to the technical field of pharmaceutical preparations. The glibenclamide nanocrystal preparation is prepared from, by weight, glibenclamide 35%-93%, a stabilizer 2%-7% and a freeze-drying protective agent 28-60%, wherein the ratio of the glibenclamide to the stabilizer is 30:1 to 15:1. The stabilizer is hydroxypropyl methyl cellulose, polyvinylpyrrolidone, poloxamer or a surface active agent. The glibenclamide nanocrystal preparation is controllable in particle size, good in stability and small in side and toxic effect and obviously improves the dissolution and bioavailability of the glibenclamide.

Description

technical field [0001] The invention relates to a glibenclamide nano crystal preparation and a preparation method, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Glyburide (Glyburide) is a second-generation sulfonylurea oral hypoglycemic drug, the chemical name is N-[2-[4-[[[(cyclohexylamino)carbonyl]amino]sulfonyl]phenyl]ethyl ]-2-methoxy-5-chlorobenzamide has the advantages of small dose, small toxic and side effects, and strong hypoglycemic effect. However, glibenclamide has low water solubility (the solubility in water at 25°C is 0.1mg / mL, and is insoluble according to the definition of Chinese Pharmacopoeia), and it has strong lipophilicity (LogP=4.5). It belongs to a typical BCSII drug, and its extremely low Bioavailability limits its clinical application. In order to improve the dissolution rate and bioavailability of glibenclamide, the traditional preparation process usually adopts the measure of adding amphiphilic ex...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/64A61K47/26A61K47/38A61K47/32A61P3/10
CPCA61K9/19A61K31/64A61K47/26A61K47/32A61K47/38
Inventor 付强何仲贵杨文倩国梦然郭志斌关诗嘉
Owner SHENYANG PHARMA UNIVERSITY
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