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A kind of baicalein injection freeze-dried powder injection

A technology for freeze-dried powder injection and baicalein, which is applied in the field of pharmaceutical preparations and can solve the problems of insolubility of baicalein, poor light and pH stability, and the like

Inactive Publication Date: 2018-04-13
HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The technical problem to be solved by the present invention is to overcome the defects that baicalein is insoluble in water and has poor stability to light and pH, and to provide a new dosage form of baicalein, that is, freeze-dried powder for injection, which is characterized in that lecithin and nonionic The mixed micelle system formed by compounding surfactants under certain conditions can increase the degree of dispersion of the drug and improve the stability of the drug

Method used

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  • A kind of baicalein injection freeze-dried powder injection
  • A kind of baicalein injection freeze-dried powder injection
  • A kind of baicalein injection freeze-dried powder injection

Examples

Experimental program
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Effect test

Embodiment 1

[0033] (1) Preparation of the organic phase: Dissolve 5000 mg of lecithin S100 and 5000 mg of polyethylene glycol lithium lauryl hydroxystearate in 8 mL of methanol, add 500 mg of baicalein, and dissolve the drugs completely for later use.

[0034] (2) Preparation of water phase: Disperse 7500 mg lecithin S100 in 250 g water and set aside.

[0035] (3) Preparation of freeze-dried powder injection: Slowly pour the organic phase into the water phase, sonicate with a cell pulverizer, 200 W, for 5 minutes, add 8% lactose, pass through a 0.22 μm microporous membrane, and freeze-dry.

Embodiment 2

[0037] (1) Preparation of the organic phase: Dissolve 9000 mg of lecithin S100 and 4500 mg of polyethylene glycol lauryl hydroxystearate in 15 mL of absolute ethanol, add 600 mg of baicalein, and dissolve the drugs completely for later use.

[0038] (2) Preparation of water phase: Disperse 5000 mg lecithin S100 in 265 g water and set aside.

[0039] (3) Preparation of freeze-dried powder injection: Slowly pour the organic phase into the water phase, ultrasonicate the cell pulverizer, 300 W, 3 min, add 3% trehalose, pass through a 0.22 μm microporous membrane, and freeze-dry.

Embodiment 3

[0041] (1) Preparation of the organic phase: 16500 mg lecithin S100 and 5500 mg polyethylene glycol lauryl hydroxystearate were dissolved in 20 mL absolute ethanol, 660 mg baicalein was added, and the drugs were completely dissolved for later use.

[0042] (2) Preparation of water phase: Disperse 3000 mg lecithin S100 in 274 g water and set aside.

[0043] (3) Preparation of freeze-dried powder injection: Slowly pour the organic phase into the water phase, sonicate with a cell pulverizer, 400 W, for 1 min, add 10% mannitol, pass through a 0.22 μm microporous membrane, and freeze-dry.

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Abstract

The invention discloses a freeze-dried powder injection of baicalein. The freeze-dried powder injection is prepared by the following steps: dissolving a baicalein medicinal raw material, lecithin and a non-ionic surface active agent into an organic solvent, then mixing together with a water phase, carrying out ultrasonic treatment, and freeze-drying so as to prepare the freeze-dried powder injection. Before use, the freeze-dried powder injection is redissolved by water for injection so as to form a mixed micellar system with the particle size of (110+ / -8)nm. The method can be used for overcoming the problems of poor water solubility of baicalein and difficulty in parenteral administration, and meanwhile can improve the medicine stability.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, in particular to a baicalein injection freeze-dried powder, which belongs to the technical field of medicine. Background technique [0002] The chemical name of baicalein is 5,6,7-trihydroxyflavone, which is one of the main active ingredients in the dry root of Scutellaria baicalensis Georgi, a plant of Labiatae. Its chemical structure is shown in the figure. [0003] [0004] Recent studies have shown that baicalein has a wide range of pharmacological effects, including antibacterial, antiviral, hepatoprotective and diuretic, scavenging free radicals and anti-oxidation, anticoagulant and antithrombotic, inhibiting pancreatic enzyme activity and the effect on biofilms, Anti-cancer, dual regulation of smooth muscle, inhibition of adhesion molecule expression and other pharmacological effects. It is mainly used clinically for antiviral, antibacterial, anti-inflammatory and anti-infective (Gao Yan...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/352A61K47/24A61K47/14A61P31/12A61P31/00A61P31/04
Inventor 高子彬张晓博张丽男谷艳玲齐献利孙勇军吴韶梅谢英花刘磊
Owner HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY