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Allyl isothiocyanate micelle preparation

A technology of isothiocyanate and allyl ester, applied in the direction of ester active ingredients, medical preparations of non-active ingredients, antineoplastic drugs, etc., can solve the problems of limited application, large body irritation, and low solubility, and achieve Eliminate allergies and improve safety

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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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0020] The preparation method of the allyl isothiocyanate micelle preparation of the present invention, the steps are as follows: allyl isothiocyanate and pharmaceutically acceptable carrier materials are added in the organic solvent for dissolution, and the organic solvent is evaporated under reduced pressure in a water bath After forming a film, add PBS buffer solution containing additives, stir to hydrate, vortex or sonicate, adjust the pH with a pH regulator, and filter through a membrane to obtain the product.

[0021] The organic solvent is ethanol, ethyl acetate, acetone, tetrahydrofuran, dichloromethane and any combination thereof. The temperature of the water bath is 45 to 55° C., and the hydration time is 2 to 3 hours. The pore size of the filter membrane is 0.22 μm.

[0022] Allyl isothiocyanate micelle preparation of the present invention has the following advantages:

[0023] In the present invention, PEG derivatized phospholipids and other phospholipids are sel...

Embodiment 1

[0026] A micellar preparation of allyl isothiocyanate, which consists of: 1 mg of allyl isothiocyanate, 4 mg of DSPE-PEG, 4 mL of absolute ethanol, 50 mL of PBS buffer, 0.5 mg of glucose, and 0.1 mg of oxalic acid.

[0027] The preparation method is as follows:

[0028] Add allyl isothiocyanate and DSPE-PEG to absolute ethanol to dissolve, evaporate the absolute ethanol in a water bath at 50°C under reduced pressure to form a film, add PBS buffer containing glucose, stir for 2.5 hours of hydration, and ultrasonically dissolve , adjust the pH to 6 with oxalic acid, and filter it through a 0.22 μm filter membrane.

[0029] The encapsulation efficiency and drug loading of allyl isothiocyanate were determined to be 80.2% and 9.1%, respectively.

Embodiment 2

[0031] A micellar preparation of allyl isothiocyanate, which is composed of: 1 mg of allyl isothiocyanate, 6 mg of DSPE-PEG, 4 mL of absolute ethanol, 50 mL of PBS buffer, 0.5 mg of glucose, and 0.2 mg of oxalic acid.

[0032] The preparation method is as follows:

[0033] Add allyl isothiocyanate and DSPE-PEG to absolute ethanol to dissolve, evaporate the absolute ethanol in a water bath at 50°C under reduced pressure to form a film, add PBS buffer containing glucose, stir for 2.5 hours of hydration, and ultrasonically dissolve , adjust the pH to 5 with oxalic acid, and filter it through a 0.22 μm filter membrane.

[0034] The encapsulation efficiency and drug loading of allyl isothiocyanate were determined to be 84.1% and 7.3%, respectively.

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Abstract

The invention discloses an allyl isothiocyanate micelle preparation. The allyl isothiocyanate micelle preparation comprises the following components in percentage by weight: 1-4% of allyl isothiocyanate, 2-16% of pharmaceutically acceptable carrier material, 0-15% of PBS (phosphate buffered saline), 0.10-6% of additives and 0.10-4% of pH regulator, wherein the pH regulator is used for regulating pH. According to the allyl isothiocyanate micelle preparation disclosed by the invention, PEG (polyethylene glycol)-derived phospholipids and other phospholipids are selected, then a micelle is self-assembled by amphiphilic derivatives in a water solution, the allyl isothiocyanate is simultaneously encapsulated, polyoxyethylene and other surfactant type solubilizers do not need to be used, adverse reactions of allergy and the like caused by traditional solvents are eliminated, and the safety of medicaments is greatly improved.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, and discloses a micellar preparation of allyl isothiocyanate. More specifically, the invention relates to a kind of isothiocyanate that helps avoid phagocytosis of the reticuloendothelial system in the body and can be stored stably. Allyl cyanate micellar formulation. 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 low toxicity. It can selectively a...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/26A61K47/34A61K47/24A61P35/00
Inventor 陈卫东朱婷婷方国民张先文林彤远罗晴蔡晓蕾
Owner 上海海虹实业(集团)巢湖今辰药业有限公司
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