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Baicalin nanometer crystal and preparation method thereof

A baicalin nanometer and nanocrystal technology, applied in the field of medicine, can solve the problems of low drug loading, complicated process, large amount of auxiliary materials, etc.

Inactive Publication Date: 2014-03-19
NINGXIA MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these technologies still generally have limitations such as complex process, low drug loading, and large amount of excipients.

Method used

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  • Baicalin nanometer crystal and preparation method thereof
  • Baicalin nanometer crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Embodiment 1: Weigh 50 mg of baicalin, dissolve it in 1 mL of DMSO, inject it into 20 mL of 0.5% lecithin aqueous solution under high-speed shear at 30,000 rpm, and continue high-speed shear for 12 minutes in an ice-water bath to obtain baicalin nano Suspension, the average particle size is 286 nm. Take the newly prepared baicalin nanosuspension and add water to dilute it in an appropriate amount, and measure the particle size distribution with a laser particle size analyzer (attached figure 1 ); the sample was dropped on the copper grid, and after the sample was dried, it was observed and photographed under a transmission electron microscope (attached figure 2 ).

Embodiment 2

[0037] Example 2: Weigh 70 mg of baicalin, dissolve it in 1 mL of glycerol, inject it into 20 mL of 0.5% poloxamer 188 aqueous solution under high-speed shear at 30,000 rpm, and continue high-speed shear at room temperature for 10 min. The baicalin nanosuspension was obtained, and the average particle diameter was 400nm.

Embodiment 3

[0038] Example 3: Weigh 100 mg of baicalin, disperse it in 1 mL of ethanol, inject it into 20 mL of 0.5% polyvinyl alcohol aqueous solution under high-speed shear at 16000 rpm, and continue high-speed shear for 8 minutes to obtain baicalin nanosuspension Liquid, the average particle size is 759nm.

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Abstract

The invention discloses a baicalin nanometer crystal which comprises a raw material and an auxiliary material, wherein the raw material is baicalin. The preparation method of the baicalin nanometer crystal comprises the following steps: (1) dispersing a stabilizing agent into water to obtain a system A; (2) dispersing the baicalin into a good solvent to obtain system B; (3) dispersing the system B into the system A under the action of high-speed shearing to obtain a nanometer suspension C; (4) after the nanometer suspension C is centrifugalized at high speed, discarding supernatant, adding a small amount of the system A, and dispersing again through the high-speed shearing to obtain a concentrated suspension D; (5) adding a protective agent to the nanometer suspension C obtained from the step (3) or the concentrated suspension D obtained from the step (4), and drying to obtain the baicalin solid-state nanometer crystal. The baicalin nanometer crystal disclosed by the invention can be used for overcoming the defect that the baicalin is difficult to dissolve in water; compared with a raw material drug, the prepared baicalin nanometer crystal is significantly enhanced in saturated solubility.

Description

technical field [0001] The invention relates to the field of medicine, in particular to the field of pharmaceutical preparations, in particular to a method for preparing baicalin nanocrystals technical background [0002] Baicalin is the main active ingredient extracted from the traditional Chinese medicine Scutellaria baicalensis, belonging to flavonoids, with molecular formula C 21 h 18 o 11 , the molecular weight is 446.35. It is a yellow crystal with a melting point of 223 ℃, almost insoluble in water, and has certain fat solubility. [0003] Studies have shown that baicalin has pharmacological effects such as anti-tumor, anti-pathogen, protection of liver damage, improvement of diabetic nephropathy, repair and protection of brain damage, improvement of retinopathy, and anti-allergy. However, due to the poor solubility of baicalin, unstable aqueous solution, and poor oral absorption, the preparations usually have disadvantages such as low bioavailability and short ha...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K9/14A61K31/7048A61P35/00A61P31/04A61P1/16A61P3/10A61P13/12A61P25/00A61P37/08A61P27/02
Inventor 王文苹张秋菊王虹胡进刘艳华随宏魏世杰
Owner NINGXIA MEDICAL UNIV
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