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Stable fat-soluble vitamin C preparation and preparation method thereof

A fat-soluble vitamin and vitamin technology, which can be applied to non-central analgesics, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., can solve problems such as gastrointestinal disorders and urinary stones, and achieve improvement and stability. performance, simple preparation method and good adhesion

Inactive Publication Date: 2020-10-09
嘉兴市爵拓科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But on the other hand, the gastrointestinal function may be disturbed by taking a large amount of vitamin C, and more serious cases may cause urinary stones

Method used

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  • Stable fat-soluble vitamin C preparation and preparation method thereof
  • Stable fat-soluble vitamin C preparation and preparation method thereof
  • Stable fat-soluble vitamin C preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1 novel vitamin C succinate derivative

[0028] synthetic route:

[0029]

[0030] Preparation method: Dissolve 1mol (176g) of vitamin C and 1.1mol of succinic acid in 200mL of water, heat up to 40°C, add 8.8g of lipase and mix, microwave treatment (power 800W) and stir for 5 hours, remove the solvent under reduced pressure, Pour the mixture into a mixture of ethyl acetate and ice water, the volume ratio of ethyl acetate and ice water in the mixture of ethyl acetate and ice water is 1:1, stir and wash for 10 min, filter, wash with distilled water, and dry under vacuum at 50°C. The obtained solid powder is a novel vitamin C succinate derivative, and the yield is 95%.

[0031] NMR results: 1 H NMR (300MHz, DMSO) δ15(s, 2H), 5.5(d, 1H), 5.18(m, 1H), 4.2(d, 2H), 2.63-2.66(m, 4H). ESMS calculated value C 10 h 10 o 8 (M+H)+: 259.04; Found: 259.0.

Embodiment 2

[0032] Embodiment 2 novel vitamin C succinate derivatives

[0033] synthetic route:

[0034]

[0035] Preparation method: Dissolve 1mol (176g) of vitamin C and 1.3mol of succinic acid in 200mL of water, heat up to 45°C, add 35.2g of lipase and mix, microwave treatment (power 1200W) and stir for 10h, then remove the solvent under reduced pressure, Pour the mixture into a mixture of ethyl acetate and ice water, the volume ratio of ethyl acetate and ice water in the mixture of ethyl acetate and ice water is 1:1, stir and wash for 10 min, filter, wash with distilled water, and vacuum dry at 70°C. The obtained solid powder is a novel vitamin C succinate derivative, and the yield is 92%.

Embodiment 3

[0036] Embodiment 3 novel vitamin C succinate derivatives

[0037] synthetic route:

[0038]

[0039] Preparation method: Dissolve 1mol (176g) of vitamin C and 1.2mol of succinic acid in 200mL of water, heat up to 42°C, add 20g of lipase and mix, microwave treatment (power 1000W) and stir for 7 hours, remove the solvent under reduced pressure, and The mixture was poured into a mixture of ethyl acetate and ice water, the volume ratio of ethyl acetate and ice water in the mixture of ethyl acetate and ice water was 1:1, stirred and washed for 10 min, filtered, washed with distilled water, and dried under vacuum at 60°C to obtain The solid powder is a novel vitamin C succinate derivative, and the yield is 93%.

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PUM

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Abstract

The invention provides a stable fat-soluble vitamin C preparation, which contains a novel vitamin C succinate derivative, and the novel vitamin C succinate derivative has a structure shown as a formula I in the specification. The novel vitamin C succinate derivative synthesized by the invention is simple in preparation method, improves the stability, fat solubility and biocompatibility of vitaminC, can organically combine the effects of vitamin C and vitamin C, enables the effects of vitamin C and vitamin C succinate to be more excellent, reduces the preparation cost, improves the absorptioneffect, and has a wide application prospect.

Description

technical field [0001] The invention relates to the technical field of biological preparations, in particular to a stable fat-soluble vitamin C preparation and a preparation method thereof. Background technique [0002] Vitamin C has high medicinal value, but vitamin C also has a shortcoming, that is, its stability is very poor. A way to convert vitamin C into a stable substance has been sought by human beings for a long time, but at present Looking at it, turning it into a derivative is the only way. In recent years, the new physiological functions and medicinal value of vitamin C have been continuously developed, so it has attracted widespread attention in the world. Researchers have applied it to the research of treating various diseases, expecting more important discoveries, But the application of vitamin C is still limited by its natural properties. Because vitamin C is very unstable to physical and chemical factors, and it is relatively hydrophilic and difficult to p...

Claims

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Application Information

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IPC IPC(8): A61K31/375A61K31/194A61K47/54A61K47/55A61K47/38A61K47/36A61K47/40A61K9/20A61K9/16A61P39/06A61P29/00A61P13/02
CPCA61K9/205A61K9/2054A61K9/2059A61K9/4866A61K31/194A61K31/375A61K47/542A61K47/55A61P13/02A61P29/00A61P39/06A61K2300/00
Inventor 不公告发明人
Owner 嘉兴市爵拓科技有限公司
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