Vitamin K1 micelle injection and preparation method thereof

A vitamin and injection technology, applied in blood diseases, pharmaceutical formulations, emulsion delivery, etc., can solve the problems of insolubility, large side effects of intravenous administration, low oral bioavailability, etc., to achieve low preparation cost and reduce adverse reactions. , the effect of prolonged time

Inactive Publication Date: 2016-10-12
HEFEI HUAFANG PHARMA SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The purpose of the present invention is to overcome the disadvantages of insoluble vitamin K1, low oral bioavailability, large side effects of intravenous administration, etc., to prepare a vitamin K1 that can greatly improve its bioavailability and low cost, simple preparation process, suitable for industrial production, and safe Potent Vitamin K1 Micellar Injection

Method used

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  • Vitamin K1 micelle injection and preparation method thereof
  • Vitamin K1 micelle injection and preparation method thereof
  • Vitamin K1 micelle injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Each bottle contains vitamin K1 10mg, and the composition of 1000 bottles of vitamin K1 micellar injection is:

[0034]

[0035] The specific operation process is as follows:

[0036] (1) Weigh each component according to the ratio, add vitamin K1, sodium glycocholate, and soybean lecithin into 2-methyl-2-propanol and water (volume ratio 4:1), and stir , dissolved until clear;

[0037] (2) Put the solution in step (1) into a lyophilizer, cool down to -40°C±2°C, keep it warm for 2h to 4h, then evacuate until the pressure of the freeze-drying box is lower than 10Pa, and then use 4°C / h Raise the temperature to -25°C ± 2°C for sublimation drying, keep it warm for 10 hours, raise the temperature to 30°C ~ 35°C, keep it warm for 2 hours, freeze-drying is over, and it will be loose and dry.

[0038] (3) Add the prescribed amount of purified water to the powder, stir at room temperature until the sample is clear and transparent, adjust the pH value to 5.5-6.5 with hydrochl...

Embodiment 2

[0042] Each bottle contains vitamin K1 10mg, and the composition of 1000 bottles of vitamin K1 micellar injection is:

[0043]

[0044]

[0045] The specific operation process is as follows:

[0046] (1) Weigh each component according to the stated ratio, add vitamin K1, sodium taurocholate, and soybean lecithin to 2-methyl-2-propanol and water (volume ratio 4:1), stir, dissolve until clear;

[0047] (2) Put the solution in step (1) into a lyophilizer, cool down to -40°C±2°C, keep it warm for 2h to 4h, then evacuate until the pressure of the freeze-drying box is lower than 10Pa, and then use 4°C / h Raise the temperature to -25°C ± 2°C for sublimation drying, keep it warm for 10 hours, raise the temperature to 30°C ~ 35°C, keep it warm for 2 hours, freeze-drying is over, and it will be loose and dry.

[0048] (3) Add the prescribed amount of purified water to the powder, stir at room temperature until the sample is clear and transparent, adjust the pH value to 5.5-6.5 wi...

Embodiment 3

[0052] Each bottle contains vitamin K1 10mg, and the composition of 1000 bottles of vitamin K1 micellar injection is:

[0053]

[0054] The specific operation process is as follows:

[0055] (1) Weigh each component according to the stated ratio, add vitamin K1, sodium glycocholate, and soybean lecithin into 2-methyl-2-propanol and water (volume ratio 3:1), and stir , dissolved until clear;

[0056] (2) Put the solution in step (1) into a lyophilizer, cool down to -40°C±2°C, keep it warm for 2h to 4h, then evacuate until the pressure of the freeze-drying box is lower than 10Pa, and then use 4°C / h Raise the temperature to -25°C ± 2°C for sublimation drying, keep it warm for 10 hours, raise the temperature to 30°C ~ 35°C, keep it warm for 2 hours, freeze-drying is over, and it will be loose and dry.

[0057] (3) Add the prescribed amount of purified water to the powder, stir at room temperature until the sample is clear and transparent, adjust the pH value to 5.5-6.5 with h...

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Abstract

The invention discloses a vitamin K1 micelle injection and a preparation method thereof, and belongs to the field of micelle injection and preparation thereof. The invention discloses a vitamin K1 micelle for the first time. The vitamin K1 micelle is prepared from vitamin K1, cholate, phospholipid, a pH regulator and water for injection. The preparation method of the vitamin K1 micelle injection comprises the steps that an organic solvent freezing and drying method is adopted, a mixed micelle composed of phospholipid and cholate is adopted as a carrier, and the vitamin K1 is entrapped in hydrophobic nuclei of the mixed micelle. Due to the fact that the vitamin K1 is not dissolved into water, the solubility of the vitamin K1 in water is remarkably improved through the cholate/phospholipid mixed micelle preparation technology, polysorbate-80 and propylene glycol are not added into the vitamin K1 micelle injection, only phospholipid and cholate named as physiological excipient are adopted as auxiliary materials, and compared with vitamin K1 injections on sale currently, the preparation can reduce adverse drug effect and improve the clinic application safety.

Description

technical field [0001] The invention relates to a preparation method of the vitamin K1 micellar injection, and belongs to the field of micellar injection preparations and preparation thereof. Background technique [0002] Vitamin K1 is a yellow to orange-yellow transparent viscous liquid, odorless or almost odorless, easy to decompose when exposed to light; refractive index: 1.525-1.528; easily soluble in chloroform, ether or vegetable oil, slightly soluble in ethanol , insoluble in water; its chemical name is: trans and cis of 2-methyl-3-(3,7,11,15-tetramethyl-2-hexadecenyl)-1,4-naphthalenedione A mixture of isomers of formula; its molecular formula: C 31 h 46 o 2 ;Molecular weight: 450.71, the structural formula is: [0003] [0004] Vitamin K is an active drug for procoagulation factors, and its main function is to participate in the synthesis of coagulation factors II, VII, IX, and X in the liver. With the participation of vitamin K, the γ-hydroxylation of the gl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/122A61K47/28A61K47/24A61P7/04
CPCA61K9/0019A61K9/1075A61K31/122A61K47/24A61K47/28
Inventor 杨贤龙何勇张亮亮
Owner HEFEI HUAFANG PHARMA SCI & TECH
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