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Baicalein nano-suspension and preparation method thereof

A nanosuspension, baicalein technology, applied in the directions of anti-inflammatory agents, antiviral agents, pharmaceutical formulations, etc., can solve the problem of no baicalein nanosuspension, inability to be directly made into injections, limited oil-phase drug-carrying capacity, etc. problems, to achieve the effect of increased drug loading, improved long-term stability, and high safety

Active Publication Date: 2018-10-16
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Baicalein has poor water solubility, the degree of solubility in water is 17.5 μg / mL, and the solubility in soybean oil is less than 0.3 mg / mL; the solubility in water tends to increase with the increase of pH value, but it is easy to degrade when the pH is above 7.0
Baicalein is rapidly metabolized in the body, and its oral bioavailability is low, so it cannot be directly made into injections
[0003] In the prior art, researches on baicalein preparations include emulsions, submicroemulsions, micellar injections, liposomes and other types of explorations, but there are various drawbacks, such as limited drug-loading capacity of the oil phase, and the use of Surfactants that are not commonly used for intravenous injection such as Solutol and SDS are used, and toxic organic solvents such as dimethyl sulfoxide are used, which have low safety and poor stability, etc.
There is no report of baicalein nanosuspension

Method used

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  • Baicalein nano-suspension and preparation method thereof
  • Baicalein nano-suspension and preparation method thereof
  • Baicalein nano-suspension and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] prescription:

[0073] Baicalein Phospholipid Complex 1g+3g

[0074] Phospholipids 10g

[0075] F-68 0.6g

[0076] Glycerin 5g

[0077] Water for injection to 100ml

[0078] Preparation Process:

[0079] 1) After adding baicalein, phospholipids, and tetrahydrofuran (1g:3g:70ml) into a three-necked bottle to dissolve, heat at 40°C, reflux for 1-2h, then vacuumize to remove THF, and dry in a vacuum oven (30°C) for 12h to obtain Scutellaria baicalensis phospholipid complex

[0080] 2) Stir the prescription amount of baicalein phospholipid complex, phospholipids, and glycerin, and mix to obtain a semi-solid dispersion; the prescription amount of F-68 is dissolved in water for injection;

[0081] 3) Add the semi-solid dispersion into the F-68 aqueous solution, and disperse into a coarse suspension under high-speed shearing under ice bath conditions;

[0082] 4) Place the coarse suspension in a high-pressure homogenizer, and homogenize at room temperature (400-800bar, 4-...

Embodiment 2

[0093] prescription:

[0094] Baicalein Phospholipid Complex 2g+6g

[0095] Phospholipids 10g

[0096] F-68 1g

[0097] Glycerin 2.25g

[0098] Water for injection to 200ml

[0099] Preparation Process:

[0100] 1) After adding baicalein, phospholipids, and tetrahydrofuran (1g:3g:70ml) into a three-necked bottle to dissolve, heat at 40°C, reflux for 1-2h, then vacuumize to remove THF, and dry in a vacuum oven (30°C) for 12h to obtain Scutellaria baicalensis phospholipid complex

[0101] 2) Stir the baicalein phospholipid complex, phospholipid, and glycerin, and mix well to obtain a semi-solid dispersion; the prescription amount F-68 is dissolved in water for injection

[0102] 3) Add the semi-solid dispersion into the F-68 aqueous solution, and disperse into a coarse suspension under high-speed shearing under ice bath conditions;

[0103] 4) Place the coarse suspension in a high-pressure homogenizer, and homogenize at room temperature (400-800bar, 4-10 times);

[0104]...

Embodiment 3

[0115] prescription:

[0116] Baicalein Phospholipid Complex 0.5g+1.5g

[0117] Phospholipids 10g

[0118] F-68 1.2g

[0119] Glycerin 5g

[0120] Water for injection to 100ml

[0121] Preparation Process:

[0122] 1) After adding baicalein, phospholipids, and tetrahydrofuran (1g:3g:70ml) into a three-necked bottle to dissolve, heat at 40°C, reflux for 1-2h, then vacuumize to remove THF, and dry in a vacuum oven (30°C) for 12h to obtain Scutellaria baicalensis phospholipid complex

[0123] 2) Stir the baicalein phospholipid complex, phospholipid, and glycerin, and mix well to obtain a semi-solid dispersion; the prescription amount F-68 is dissolved in water for injection

[0124] 3) Add the semi-solid dispersion into the F-68 aqueous solution, and disperse into a coarse suspension under high-speed shearing under ice bath conditions;

[0125] 4) Place the coarse suspension in a high-pressure homogenizer, and homogenize at room temperature (400-800bar, 4-10 times);

[01...

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PUM

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Abstract

The invention belongs to the field of pharmaceutical preparations and discloses a baicalein nano-suspension and a preparation method thereof. A prescription of the baicalein nano-suspension comprisesthe following substances in percentage by mass: 0.1 to 2 percent of baicalein-phospholipid complex, 0.05 to 10 percent of phospholipid, 0.1 to 3 percent of F-68, 1 to 10 percent of glycerol and the balance of water. The baicalein nano-suspension and the preparation method thereof, provided by the invention, have the advantages of simple technology, cost reducing and relatively low energy consumption; the drug-loading amount of the preparation is improved, the stability is improved and the safety is high.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a baicalein nanosuspension and a preparation method thereof. Background technique [0002] Baicalein is an important active ingredient of traditional Chinese medicine Scutellaria baicalensis, which has various pharmacological effects such as antibacterial, antiviral, anti-inflammatory, liver-protecting and choleretic, diuretic, and anti-cancer. Baicalein has poor water solubility, the solubility in water is 17.5μg / mL, and the solubility in soybean oil is less than 0.3mg / mL; the solubility in water tends to increase with the increase of pH value, but it is easy to degrade when the pH is above 7.0. Baicalein is rapidly metabolized in the body, and its oral bioavailability is low, so it cannot be directly made into injections. [0003] In the prior art, researches on baicalein preparations include emulsions, submicroemulsions, micellar injections, liposomes and other types ...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K47/24A61K47/10A61K31/352A61P31/04A61P31/12A61P29/00A61P1/16A61P7/10A61P35/00
CPCA61K9/10A61K31/352A61K47/10A61K47/24A61P1/16A61P7/10A61P29/00A61P31/04A61P31/12A61P35/00
Inventor 郭青龙柯学王卉陈默
Owner CHINA PHARM UNIV