Preparation method of allyl isothiocyanate nanometer lipid carrier

A technology of nano-lipid carrier and isothiocyanate, which is applied in the directions of non-active ingredients such as medical preparations, pharmaceutical formulations, ester active ingredients, etc. Limit the application and other problems to achieve the effect of prolonging the local aggregation, high drug loading, and clear targeting

Active Publication Date: 2013-12-25
上海海虹实业(集团)巢湖今辰药业有限公司
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  • Abstract
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AI Technical Summary

Problems solved by technology

[0005] Due to the low solubility of allyl isothiocyanate in aqueous solution, it is highly irritating to the body after injection and has a short half-life in vivo, which limits its clinical application. Therefore, it is necessary to use modern preparation technology to effectively increase the concentration of allyl isothiocyanate. The solubility of propyl ester reduces irritation, prolongs the drug's action time and local aggregation in the body, and better exerts its anticancer effect
[0006] Nanostructured lipid carriers (NLC) is a new type of drug loading developed from solid lipid nanoparticles (SLN), which can effectively avoid drug efflux during placement and has a low encapsulation efficiency. The problem with the solid lipid nanoparticle (SLN) system is that it is made of a single lipid material, and after high-pressure homogeneous cooling during the preparation process, the lipid tends to form more regular crystals, causing the trapped Drug efflux or crystallization in the dispersed aqueous phase of SLN

Method used

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  • Preparation method of allyl isothiocyanate nanometer lipid carrier
  • Preparation method of allyl isothiocyanate nanometer lipid carrier

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preparation example Construction

[0034] When the allyl isothiocyanate nano lipid carrier of the present invention is prepared, its preparation method comprises the following steps:

[0035] (1) Dissolve allyl isothiocyanate, solid lipid material, liquid oil, and fat-soluble emulsifier in an organic solvent, then remove the organic solvent by vacuum rotary evaporation or vacuum drying, and heat to 60~ Melting at 100°C to form the organic phase;

[0036] (2) Dissolve long-circulation excipients, water-soluble emulsifiers, and additives in water for injection, and heat to 60-100°C to form the water phase;

[0037] (3) mixing the organic phase and the aqueous phase under stirring or high shear conditions at a temperature of 60-100° C. to prepare colostrum;

[0038] (4) Ultrasonic or high-pressure homogenization is performed on the colostrum to prepare the allyl isothiocyanate nano-lipid carrier.

[0039] The obtained allyl isothiocyanate nano-lipid carrier can be further lyophilized or kept sealed at 4°C, where...

Embodiment 1

[0041] An allyl isothiocyanate nano lipid carrier, which is composed of: allyl isothiocyanate 5mg, GMS60mg, MCT20uL, lecithin 150mg, absolute ethanol 5mL, PEG200020mg, Tween8040mg, water for injection 50mL.

[0042] The preparation method is as follows:

[0043] Dissolve allyl isothiocyanate, GMS, MCT, and lecithin in absolute ethanol, remove the absolute ethanol by rotary evaporation under reduced pressure, and heat to 80°C to melt to form an organic phase; dissolve PEG2000 and Tween80 in water for injection and heated to 80°C to form the water phase; at a temperature of 80°C, the organic phase and the water phase were mixed under stirring conditions to prepare colostrum; the colostrum was subjected to high-pressure homogenization , and poured into ice water to prepare allyl isothiocyanate nano lipid carrier.

[0044] The drug loading and encapsulation efficiency of allyl isothiocyanate nano-lipid carriers were determined to be 7.82% and 87.6% respectively

Embodiment 2

[0046] A nano-lipid carrier of allyl isothiocyanate, which is composed of: 5 mg of allyl isothiocyanate, 60 mg of GMS, 20 uL of MCT, 150 mg of lecithin, 5 mL of absolute ethanol, 20 mg of PEG2000, 40 mg of Tween8040 mg, and 100 mL of water for injection.

[0047] The preparation method is as follows:

[0048] Dissolve allyl isothiocyanate, GMS, MCT, and lecithin in absolute ethanol, remove the absolute ethanol by rotary evaporation under reduced pressure, and heat to 80°C to melt to form an organic phase; dissolve PEG2000 and Tween80 in water for injection and heated to 80°C to form an aqueous phase; at a temperature of 80°C, the organic phase and the aqueous phase were mixed under stirring conditions to prepare colostrum; the colostrum was subjected to high-pressure homogenization , and poured into ice water to prepare allyl isothiocyanate nano lipid carrier.

[0049] The drug loading and encapsulation efficiency of allyl isothiocyanate nanolipid carriers were determined to ...

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Abstract

The invention discloses a preparation method of an allyl isothiocyanate nanometer lipid carrier. The preparation method comprises the following steps of dissolving allyl isothiocyanate, a solid lipid material, liquid oil, and a lipid soluble emulsifier in an organic solvent, removing the organic solvent, and heating the resulting product to 60-100 DEG C for melting to obtain an organic phase; dissolving a long-circulating adjuvant, a water soluble emulsifier, and an additive in injection water, and heating the resulting solution to 60-100 DEG C to obtain a water phase; and mixing the organic phase and the water phase at the temperature of 60-100 DEG C to prepare a pre-emulsion; and carrying out ultrasonic or high-pressure homogenizing treatment on the pre-emulsion, and pouring the homogenized product into ice water so as to obtain the allyl isothiocyanate nanometer lipid carrier comprising the following ingredients in percentages by weight: 0.01-8% of allyl isothiocyanate, 0.50-15% of solid lipid material, 0-15% of liquid oil, 0.10-15% of emulsifier, 0-15% of long-circulating adjuvant, 0-15% of additive and the balance of injection water.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, and discloses a preparation method of allyl isothiocyanate nano-lipid carrier, more specifically, the invention relates to a method that helps avoid phagocytosis of the reticuloendothelial system in the body and can stabilize Preparation method of allyl isothiocyanate nano-lipid carrier for storage. Background technique [0002] Allyl isothiocyanate (AITC) is the main taste substance of mustard oil. Due to its unique taste and antibacterial properties, recent studies have found that it can inhibit the growth of cancer cells and can also be used in agriculture. Instead of methyl bromide, it is used as a soil disinfectant, so allyl isothiocyanate has broad application prospects in food additives, food antibacterial and antiseptic, medical anticancer and soil disinfection. [0003] Allyl isothiocyanate is a compound with high antitumor activity. It has a wide antibacterial spectrum and lo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K31/26A61K47/26A61K47/34A61K47/36A61K47/32A61P35/00
Inventor 陈卫东王雷方国民张先文朱婷婷林彤远罗晴蔡晓蕾
Owner 上海海虹实业(集团)巢湖今辰药业有限公司
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