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Vitamin K1 medicine with novel dosage form, and preparation method thereof

A vitamin and new dosage form technology, applied in the field of vitamin K1 micellar drug loading system and its preparation, can solve the problems of restricted application and high price, achieve high drug loading, less toxic and side effects, and avoid adverse reactions

Inactive Publication Date: 2016-11-02
SPH NO 1 BIOCHEM & PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, polyethylene glycol phosphatidylethanolamine (PEG-PE) is widely used in foreign countries, but the price is expensive, which restricts its wide application to a certain extent.

Method used

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  • Vitamin K1 medicine with novel dosage form, and preparation method thereof
  • Vitamin K1 medicine with novel dosage form, and preparation method thereof
  • Vitamin K1 medicine with novel dosage form, and preparation method thereof

Examples

Experimental program
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Effect test

preparation example Construction

[0017] The invention provides a preparation method of vitamin K1-mPEG-PE, the steps are as follows:

[0018] (a). Preparation of mPEG-PE by chemical reaction: under the protection of nitrogen, add the tetrahydrofuran solution of diacylglycerol dropwise at 0°C to the tetrahydrofuran solution of diisopropylethylamine and phosphorus oxychloride, after the addition is complete Stirring was continued for 2 h. At 0° C., the solution of polyethylene glycol monomethyl ether and pyridine in tetrahydrofuran was continued to be added dropwise. After the addition was completed, the mixture was reacted at room temperature for 6 h. Filtrate, add water in an equimolar amount to phosphorus oxychloride to the filtrate, stir for 1-2 hours, evaporate the solvent to obtain a solid, and obtain mPEG-PE after precipitation and dialysis with diethyl ether.

[0019] (b). After mixing mPEG-PE and vitamin K1 in a certain ratio, add an appropriate amount of chloroform to dissolve, remove the chloroform b...

Embodiment 1

[0022] Example 1. Preparation of vitamin K1-mPEG-PE micelles by film hydration method

[0023] Precisely weigh 1g of vitamin K1 and 6g of mPEG-PE (prepared by the above chemical reaction) and dissolve them in 300mL of chloroform, and remove the chloroform by rotary evaporation to form a polymer drug mixed film, and dry it in vacuum overnight to remove the residual organic solvent . Add 100mL of water for injection, ultrasonicate in a water bath at 25°C for 40min, filter through a 0.22µm sterile microporous membrane, and freeze-dry to obtain the product.

Embodiment 2

[0024] Example 2. Preparation of vitamin K1-mPEG-PE micelles by film hydration method

[0025] Precisely weigh 1g of vitamin K1 and 6g of mPEG-PE (prepared by the above chemical reaction) and dissolve them in 300mL of chloroform, and remove the chloroform by rotary evaporation to form a polymer drug mixed film, and dry it in vacuum overnight to remove the residual organic solvent . Add 100mL of water for injection, ultrasonicate in a water bath at 37°C for 40min, filter through a 0.22µm sterile microporous membrane, and freeze-dry to obtain the product.

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Abstract

The invention discloses a vitamin K1 medicine with novel dosage form, a formed micelle medicine loading system and a preparation method of the system. The vitamin K1 micelle medicine loading system is a vitamin K1 and pegylated phospholipid copolymer, and can form self-assembled nanoparticles in water. The vitamin K1 is innovatively entrapped in mPEG-PE polymer micelles in order to improve the solubility of the vitamin K1 in water, so polysorbate 80 and other toxicity and allergy inducing auxiliary materials are avoided, the untoward effects of vitamin K1 injection are reduced or avoided, and the safety of the medicine is increased.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a safe and stable vitamin K1 micellar drug-loading system and a preparation method thereof. Background technique [0002] Vitamin K1 is a mixture of trans and cis isomers of 2-methyl-3-(3,7,11,15-tetramethyl-2-hexadecenyl)-1,4-naphthalenedione, It is also the main form of vitamin K in plants, and its structural formula is as follows: figure 1 shown. [0003] Vitamin K1 belongs to the fat-soluble vitamin drugs, which are necessary for the synthesis of factors in the liver. Supplementing an appropriate amount of vitamin K1 can promote the synthesis of prothrombin in the liver and play a role in hemostasis. At present, vitamin K1 is mainly prepared into injections, which are clinically used in the treatment of diseases such as hypoprothrombin, vitamin K1 deficiency, neonatal spontaneous bleeding. However, vitamin K1 injections currently used clinically have ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K9/19A61K31/122A61K47/34A61P7/04C08G65/338C08G65/327C08G65/332C08G65/331
CPCA61K9/107A61K9/19A61K31/122A61K47/24C08G65/327C08G65/331C08G65/332C08G65/338
Inventor 顾春燕刘蓓黄臻辉
Owner SPH NO 1 BIOCHEM & PHARMA CO LTD
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