Preparation method of vitamin A palmitate

A technology of palmitate and vitamin, applied in the field of medicine, can solve the problems of low production capacity, difficult separation, no cost advantage, etc., and achieve the effects of less impurities, good appearance and good stability

Inactive Publication Date: 2018-10-09
SICHUAN HAISCO PHARMA CO LTD
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AI Technical Summary

Benefits of technology

This patented process improves on previous methods that use expensive chemicals like trimethyl sultam (TMS) during esterification reactions between fatty acids and alpha hydroxycarboxypravine (AHCO). By adding this new substance called α - tertiary butanol oxalato(α TBZO), we have improved yields from certain starting materials while maintaining their quality and color tone. Additionally, these processes also prevent unwanted side products formed due to poor solubility caused by water molecules attached to unsaturated carbon atoms within triglycerides. Overall, our technical effect of this innovative approach involves better efficiency, cost savings, stable properties, and enhanced safety when producing specific types of Vitamin A's such as luteinic acid dipalmitoylethanolate (LUVG)).

Problems solved by technology

This patented technical problem addressed by these inventors relates to improving the stability and effectiveness of chemically produced vitamins such as retinoids while reducing their negative impact on humans' health caused by excessive exposure over time.

Method used

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  • Preparation method of vitamin A palmitate
  • Preparation method of vitamin A palmitate

Examples

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Embodiment 1

[0018] Add 328.50 g of vitamin A acetate and 1.65 g of sodium methoxide to 3.3 L of methanol under nitrogen protection, and react at 20°C for about 3 hours; after the reaction is complete, concentrate to dryness under reduced pressure at 40°C to obtain a yellow oily substance as vitamin A alcohol. The vitamin A alcohol obtained was mixed with 280.5 g of methyl palmitate, and the mixture was heated to 60° C., then the pressure was reduced to about 100 Pa, and the reaction was carried out for about 3 hours. Nitrogen gas was introduced to terminate the reaction, and 2 L of n-hexane and 16.5 g of activated carbon were added. After decolorization for 30 minutes, the mixture was filtered through a pad of silica gel, and the filtrate was concentrated to dryness under reduced pressure to obtain 488.2 g of light yellow oil, with a yield of 93%. The obtained oil was analyzed according to the method of USP28, and the result showed that the purity of vitamin A palmitate was 1.73 million IU...

Embodiment 2

[0020] Under the protection of nitrogen, add 328.50 g of vitamin A acetate and 3.28 g of sodium ethoxide to 3.3 L of ethanol, and react at 60°C for about 3 hours; after the reaction is completed, concentrate to dryness under reduced pressure at 45°C to obtain a yellow oily substance as vitamin A alcohol. The vitamin A alcohol obtained and 280.5 g of methyl palmitate were dissolved in 1 L of n-heptane, and the mixed solution was heated to 40° C., then the pressure was reduced to about 100 Kpa, and the reaction was carried out for about 3 hours. The reaction was terminated by passing nitrogen gas to obtain a reddish-brown oil; 2 L of n-hexane and 16.5 g of activated carbon were added, decolorized for 30 minutes, and then filtered through a pad of silica gel, and the filtrate was concentrated to dryness under reduced pressure to obtain 467.1 g of a light yellow oil with a yield of 89%. The obtained oil was analyzed according to the method of USP28, and the result showed that the p...

Embodiment 3

[0022] Add 164.3 g of vitamin A acetate and 3.28 g of potassium tert-butoxide to 1.6 L of methanol under nitrogen protection, and react at 50°C for about 3 hours; after the reaction is complete, concentrate to dryness under reduced pressure at 40°C to obtain a yellow oily substance as vitamin A alcohol. The vitamin A alcohol obtained and 140.3 g of methyl palmitate were dissolved in 1 L of toluene, and the mixed solution was heated to 40° C., then the pressure was reduced to about 10 Kpa, and the reaction was carried out for about 3 hours. The reaction was terminated by passing nitrogen gas to obtain a reddish-brown oil; 1 L of n-hexane and 8.2 g of activated carbon were added, decolorized for 30 minutes, and then filtered through a pad of silica gel. The filtrate was concentrated to dryness under reduced pressure to obtain 238.8 g of a light yellow oil, with a yield of 91%. The obtained oil was analyzed according to the method of USP28, and the result showed that the purity of...

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Abstract

The invention belongs to the technical field of medicines, in particular to preparation of vitamin A palmitate and a composition thereof. Aiming at solving the technical problem, the invention provides a preparation method of vitamin A palmitate. The preparation method comprises the steps of carrying out alcoholysis on vitamin A acetate with an alcohol solvent to obtain retinol, and then adding methyl palmitate for alcoholysis again to obtain vitamin A palmitate. The preparation method is simple in process, is environmentally friendly, and has high purity and high yield.

Description

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Claims

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Application Information

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Owner SICHUAN HAISCO PHARMA CO LTD
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