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Silibinin injection and preparation method thereof

A technology for silibinin and injections, which is applied in the direction of pharmaceutical formulas, medical preparations containing active ingredients, etc., and can solve the problems of low oral bioavailability, poor water solubility of silybin, and difficulties And other issues

Inactive Publication Date: 2011-01-26
TIANJIN TASLY PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are various oral dosage forms of silibinin on the market, but due to the poor water solubility of silibinin, the oral bioavailability is low, usually around 5%, and there are large individual differences
Although silibinin salts can be prepared to increase the water solubility of silibinin, it is difficult to prepare silibinin salts as injections due to their instability in water and high pH

Method used

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  • Silibinin injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] 1. Preparation of drug powder injection

[0037] Preparation of phospholipid complex: Add 1 g of silibinin and 2 g of soybean lecithin into 60 ml of absolute ethanol, dissolve in a water bath at 45°C, and then remove the ethanol by rotary evaporation, and the obtained powder is the phospholipid complex of silibinin.

[0038] Preparation of liquid before lyophilization: Take the preparation of 70mL liquid as an example. Dissolve 1.05 g of silibinin phospholipid complex in tert-butanol and dilute to 50 ml; dissolve 3.5 g of sucrose in water for injection and dilute to 20 ml; mix the above liquids evenly and filter with a 0.22 μm microporous membrane, The filtrate was divided into vials of 2ml per bottle.

[0039] Freeze-drying: Let the solution be pre-frozen at -45°C for 3 hours, then vacuumize at 100 mTorr, dry at -45~-5°C for 10 hours, continue drying at 0~35°C for 3 hours, vacuum Degree remains unchanged, vacuum plugging, that is.

[0040] 2. Preparation of solubili...

Embodiment 2

[0044] 1. Preparation of drug powder injection

[0045] Preparation of phospholipid complex: 1 g of silibinin and 1.8 g of soybean lecithin were added to 84 ml of absolute ethanol, dissolved in a water bath at 40°C, and then the ethanol was removed by rotary evaporation, and the obtained powder was the phospholipid complex of silibinin.

[0046] Preparation of liquid before freeze-drying: take the preparation of 80mL liquid as an example. Dissolve 1.5g of silibinin phospholipid complex in tert-butanol to 50ml; take 2.1g of sucrose, dissolve it in water for injection, and dilute to 30ml; mix the above liquids evenly and filter with a 0.22μm microporous membrane , and the filtrate was divided into vials of 2ml each.

[0047] Freeze-drying: Let the solution be pre-frozen at -40°C for 3.5 hours, then vacuumize at 90 mTorr, dry at -40~-5°C for 12 hours, continue drying at 0~30°C for 2.5 hours, vacuum Degree remains unchanged, vacuum plugging, that is.

[0048] 2. Preparation of ...

Embodiment 3

[0052] 1. Preparation of drug powder injection

[0053] Preparation of phospholipid complex: add 1 g of silibinin and 2.5 g of soybean lecithin to 70 ml of absolute ethanol, dissolve in a water bath at 50 ° C, and then remove the ethanol by rotary evaporation, and the obtained powder is the phospholipid complex of silibinin .

[0054] Preparation of liquid before lyophilization: Take the preparation of 80mL liquid as an example. Dissolve 1.12g of silibinin phospholipid complex in tert-butanol and dilute to 50ml; dissolve 2.5g of sucrose and 1.5g of trehalose in water for injection and dilute to 30ml; Pore ​​membrane filtration, and the filtrate was divided into vials of 2ml each.

[0055] Freeze-drying: Let the solution be pre-frozen at -42°C for 2.5 hours, then vacuumize at 90 mTorr, dry at -42~-5°C for 8 hours, continue drying at 0~35°C for 6 hours, vacuum Degree remains unchanged, vacuum plugging, that is.

[0056] 2. Preparation of solubilizer solution

[0057] Taking...

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Abstract

The invention discloses a silibinin injection and a preparation method thereof. The silibinin injection comprises a silibinin powder injection and the solution of compatibilizer. The preparation method comprises the following steps of: (1) preparing a silibinin phospholipid compound; (2) preparing solution before freeze drying or spray drying; and (3) performing freeze drying or spray drying. A method for preparing the solution of the compatibilizer comprises the following steps of: dissolving injection water for bile salt; uniformly mixing the dissolved injection water and solution of absolute ethanol of phospholipid; passing the mixture through a 0.22-mu m microporous filtering film; filling the mixture into an ampoule bottle with the volume of 5 milliliters; and sterilizing at the temperature of between 115 and 121 DEG C for 15 to 35 minutes. After being dissolved by the solution of the compatibilizer, a medicinal powder injection is diluted in 5 percent or 10 percent glucose injection for instillation, so that the storage stability of a medicament and the solubility and water stability of silibinin can be enhanced.

Description

technical field [0001] The invention relates to a traditional Chinese medicine injection and a preparation method thereof, in particular to a silybin injection and a preparation method thereof, belonging to the field of traditional Chinese medicine. Background technique [0002] Milk thistle, also known as milk thistle, milk thistle, pheasant, and mouse, is a plant in the family Asteraceae; its whole plant or seeds are used for medicinal purposes. Silymarin (SL) is a mixture of flavonoids extracted and refined from milk thistle seeds, composed of silibinin, silidianim and silichristim3 There are two isomers, and silybin has another isomer, which is called isosillbinin, isosilybin. Studies have found that silibinin has obvious protective effects on the liver, and its effects are reflected in scavenging active oxygen, resisting lipid peroxidation, inhibiting nitric oxide (NO) production, inhibiting 5-lipoxygenase, Anti-glutathione (GsH) emptying effect, and pharmacological e...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/19A61K31/357A61K47/36A61K47/26A61K47/10A61K47/24A61K47/28A61P1/16A61K31/192
Inventor 陈建明朱永宏陈明高保安张兰兰赵颖周水平
Owner TIANJIN TASLY PHARMA CO LTD