Vitamin K1 nano-emulsion and preparation method thereof

Abstract

The invention discloses a vitamin K1 nano-emulsion and a preparation method thereof. The vitamin K1 nano-emulsion is prepared from an active ingredient vitamin K1, auxiliary materials including polyethylene glycol 400, anhydrous sodium acetate, acetic acid, sodium pyrosulfite and water for injection. The preparation method comprises the following steps: respectively preparing an A-phase solution and a B-phase solution, slowly adding the A-phase solution into the B-phase solution, stirring, filtering, filling nitrogen, encapsulating and sterilizing. Compared with the commercially available vitamin K1 injection, the vitamin K1 injection provided by the invention adopts a brand new prescription and process, and the prepared product has the advantages of more single component variety, better stability, higher safety, simplicity in operation, low cost and suitability for large-scale production.

Description

Technical field [0001] The present invention relates to the field of medicine, specifically to vitamin K 1 Nano emulsion and preparation method thereof. Background [0002] vitamin k 1 (Vitamin K 1 ) is a fat-soluble vitamin, more stable in air and humid environments, but will be decomposed in sunlight, chemically named 2-methyl-3- (3,7,11,15-tetramethylhex-2-enyl)-1,4-naphthoquinone, there is a double bond on the side chain of the molecule, so there is a cis- and trans- isomer. Chemical synthesis of vitamin K 1 It is a mixture of cis and trans isomers, while cis isomers have little physiological activity. [0003] vitamin k 1 The injection is a vitamin classic drug, which is necessary for the liver to synthesize coagulation factors II., VII., IX., X., mainly for vitamin K 1 Deficiencies cause a variety of diseases, such as ischemia caused by vitamin K deficiency, bleeding caused by obstructive jaundice, gallbladder, chronic diarrhea, hypothrombinogenemia caused by coumarins, sod...

AI Technical Summary

Problems solved by technology

Additional data analysis showed that vitamin K 1 There are some unreasonable phenomena in the clinical use of injections, such as off-label use, over-dose use, inappropriate administration routes, etc. These irrational uses have increased the risk of vitamin K. 1 Injection Safety Risks

[0005] Vitamin K currently on sale in the domestic market 1 The specification of the injection is 1ml: 10mg. It needs to be diluted before it can be used for newborns / infants in clinical use. However, during the dilution process, the phenomenon of emulsion aggregation and precipitation will occur, which is the main cause of adverse reactions.

At the same time, commercially available products contain preservatives or antioxidants, and preservatives or antioxidants may also be the main cause of severe allergic reactions to this product

In addition, commercially available products are packaged in glass ampoules, which need to be opened during use, so particles such as glass shards and glass slag will appear. After these particles enter the human blood circulation, they bypass the body's defense and filtration mechanisms and are difficult to be absorbed by the immune system. cleared and therefore persists in the body for a long time

[0006] Invention patent CN105287366 discloses a vitamin K 1 Injection and its preparation method, the invention uses polyethylene glycol 15-hydroxystearate (abbreviation: HS15) which is expensive and used in large amounts as a solubilizer, and sodium metabisulfite is used as an antioxidant at the same time, and the specification is also 1ml: 10mg, unable to meet clinical needs

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