Scutellarin nanosuspension and preparation method thereof

A nano-suspension, scutellarin technology, applied in the directions of liquid delivery, pharmaceutical formulation, emulsion delivery, etc., can solve the problems of organic solvent residue, large polydispersity index, uneven particle size of nano-suspension, etc. The effect of improving availability and increasing solubility

Inactive Publication Date: 2013-04-03
MACAU UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The media grinding method and emulsification method will have organic solvent residues; the nanosuspension prepared by the precipitation method has uneven particle size and large polydispersity index; the high-pressure homogenization method must pre-powder the drug

Method used

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  • Scutellarin nanosuspension and preparation method thereof
  • Scutellarin nanosuspension and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] In the scutellarin nanosuspension described in this example, the stabilizer is 1.4g, including 0.8g poloxamer 188 and 0.6g Cremophor EL; scutellarin (purity: 90% (w / w) above) is 0.3g, stabilizer: scutellarin is 4.7:1.

[0024] The preparation method of the scutellarin nanosuspension described in the present embodiment is as follows:,

[0025] (1) Weigh 0.3g scutellarin and dissolve it in 100mL phosphate buffer (pH7.4) as a good solvent;

[0026] (2) Dissolve 0.8g of Poloxamer 188 and 0.6g of Cremophor EL in 100mL of phosphoric acid aqueous solution (pH2.0) as a poor solvent.

[0027] (3) Drop the good solvent into the poor solvent at a dropping rate of 0.5mL / min, stir and disperse with a high-shear mixing emulsifier, control the stirring speed at 100r / min, and continue stirring for 1 hour to form a pre-nanosuspension ;

[0028] (4) Place the pre-nanosuspension in a high-pressure micro-fluidic homogenizer, control the pressure at 800 bar, and circulate 15 times to pre...

Embodiment 2

[0030] In the scutellarin nanosuspension described in this embodiment, the stabilizer is 1g, including 0.4g polyethylene glycol 400 and 0.6g Labrasol; scutellarin is 0.1g, and the stabilizer: scutellarin is 10:1 .

[0031] The preparation method of the scutellarin nanosuspension described in the present embodiment is as follows:

[0032] (1) Weigh 0.1g scutellarin and dissolve it in 100mL sodium hydroxide solution (pH6.8) as a good solvent;

[0033] (2) Dissolve 0.4g polyethylene glycol 400 and 0.6g Labrasol in 100mL hydrochloric acid aqueous solution (pH2.0) as a poor solvent;

[0034] (3) Drop the good solvent into the poor solvent at a dropping rate of 5mL / min, mechanically stir to disperse, and control the stirring speed at 500r / min, after dropping, continue stirring for 30 minutes to form a pre-nanosuspension;

[0035] (4) Place the pre-nanosuspension in a high-pressure micro-fluidic homogenizer, control the pressure at 1500 bar, and circulate 5 times to prepare the nan...

Embodiment 3

[0037] In the scutellarin nanosuspension described in the present embodiment, the stabilizer is 1.5g, including 0.5g hydroxypropyl methylcellulose K100 and 1g Cremophor RH40; scutellarin is 0.2g, and the stabilizer: scutellarin is 7.5:1.

[0038] The preparation method of the scutellarin nanosuspension described in the present embodiment is as follows:

[0039] (1) Weigh 0.2g scutellarin and dissolve it in 100mL potassium hydroxide solution (pH7.5) as a good solvent;

[0040] (2) Dissolve 0.5g of hydroxypropylmethylcellulose K100 and 1g of Cremophor RH40 in 100mL of acetic acid aqueous solution (pH3) as a poor solvent;

[0041] (3) Drop the good solvent into the poor solvent at a dropping rate of 2mL / min, stir magnetically to disperse, and control the stirring speed at 800r / min, after dropping, continue stirring for 45min to form a pre-nanosuspension;

[0042] (4) Place the pre-nanosuspension in a high-pressure micro-fluidic homogenizer, control the pressure at 1000 bar, and...

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and relates to a scutellarin nanosuspension and a preparation method thereof. The scutellarin nanosuspension is prepared from a stabilizer and scutellarin in a weight ratio of (1:1)-(10:1). The preparation method is implemented through dissolving the scutellarin into an alkaline solution and then adding the obtained mixture into an acid solution containing the stabilizer, so that due to the solubility difference of the scutellarin in the acid solution and the alkaline solution, the scutellarin is oversaturated and then crystallized by separating; and carrying out homogenization on the obtained product by using a high-pressure micro jet homogenizer so as to obtain the scutellarin nanosuspension, wherein the particle size of the scutellarin nanosuspension is 100-500 nm, and the polydispersity index is 0.1-0.5. The scutellarin nanosuspension and preparation method thereof disclosed by the invention have the significant advantages that the nanosuspension improves the solubility of the scutellarin and increases the oral bioavailability of the scutellarin; the scutellarin nanosuspension can be solidified through freeze drying or spray drying, and applied to dosage forms such as tablets, capsules, granules, oral suspensions and the like; and the scutellarin nanosuspension is simple in preparation process, and convenient for industrial production.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a scutellarin nanosuspension and a preparation method thereof. Background technique [0002] Scutellarin is the main active ingredient of breviscapine, and its chemical name is 4',5,6-trihydroxyflavone-7-O-β-D-glucuronide. Clinically, it is mainly used to treat cerebral thrombosis, cerebral infarction, paralysis after stroke, coronary heart disease and other diseases. Because scutellarin is almost insoluble in water, its oral absorption is poor, and its bioavailability is low, so its clinical application is greatly limited. Currently clinically used breviscapine preparations mainly include tablets, powder injections, injections and the like. The oral bioavailability of ordinary tablets is low, and the half-life of ordinary injections and powder injections is short and eliminated rapidly in the body. [0003] In order to improve the solubility and bioavailab...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/7048A61K47/38A61P9/10
Inventor 易涛汤丽华李良
Owner MACAU UNIV OF SCI & TECH
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