Method for producing sterols - lanosterol and cholesterol from wooly fat

FIELD: medicinal industry, sterols.

SUBSTANCE: invention relates, in particular, to the improved method for producing sterols - lanosterol and cholesterol from wooly fat that can be used in preparing medicinal and cosmetic preparations. Method is carried out by alkaline hydrolysis of raw, extraction of unsaponifiable substances, removal of solvent and successive isolation of lanosterol and cholesterol. Alkaline hydrolysis of raw is carried out with a mixture of ethanol, sodium hydroxide, pyrogallol and water at temperature 70°C for 4 h at stirring in the following ratio of components: raw : ethanol : sodium hydroxide : pyrogallol : water = 100.0:(300.0-350.0):(30.0-35.0):(0.01-0.05):(7.5-12.0), respectively, with the indicated mixture with addition of toluene in the following ratio: raw : ethanol : sodium hydroxide : pyrogallol : toluene : water = 100.0:(220.0-255.0):(30.0-38.0):(0.05-0.12):(100.0-137.0):(2.5-7.0), respectively, and lanosterol is isolated by precipitation from mixture of methylene chloride and ethanol in the ratio = 1:1. Before removal of solvent unsaponifiable substances are extracted at temperature 50°C for 2-3 h at stirring. Invention provides increasing yield of the end product, enhancing qualitative indices and reducing cost of production.

EFFECT: improved producing method.

2 cl, 3 ex

 

The technical field to which the invention relates.

The invention relates to the medical industry, in particular to a method of production of sterols: lanosterol and cholesterol from wool fat, and can be used for the preparation of medical and cosmetic products.

The level of technology

A method of obtaining cholesterol from wool fat with the aim of providing raw materials of vitamin D3 with the utilization of other components of wool fat, which includes hydrolysis of raw materials, extraction of the unsaponifiable substances, removing the solvent and consistent allocation of cholesterol (see research Report NGO "Vitamins" Minmemory the USSR. - Develop a method of obtaining cholesterol from wool fat with the aim of providing raw materials of vitamin D3 with the utilization of other components of wool fat, № state registration 01840025671, M., 1985).

The disadvantage of this method is the low yield of the target product.

The closest in technical essence and the achieved positive effect and adopted by the authors for the prototype is the method of extraction of cholesterol from wool fat by saponification, which consists in the fact that wool fat dissolve in any organic solvent, is subjected to deep saponification with alkali, for example sodium, separate mileau part by filtration, centrifugation or other under the service method, unsaponifiable part, in the solvent, is treated with metal salts, such as manganese, calcium, iron, chromium, drop-down sediment, complex compounds of cholesterol with metal salts are separated by filtration, by centrifugation and washed with the same solvent, and then the filtrate is evaporated, the residue containing uncovered cholesterol and other parts of unsaponifiable wool fat, used separately, then integrated connection of cholesterol with metal salts decompose when adding water to the solvent, cholesterol precipitates, after which he precrystallization and dried (see A.S. the USSR # 94246, CL 23a, 5, publ. in BI No. 9 1952).

The disadvantage of this method is the low yield and high cost of production.

Disclosure of inventions

The task of the invention is to develop a method of production of sterols: lanosterol and cholesterol from wool fat more cheap, with high quality and yield of the target products.

The technical result that can be obtained using the present invention is to increase the yield of the target product and qualitative indicators, the cost of production method.

The technical result is achieved by using a method of production of sterols: lanosterol and the lobby is of Terra from wool fat, including alkaline hydrolysis of raw materials, extraction of the unsaponifiable substances, removing the solvent and selects lanosterol and cholesterol, while alkaline hydrolysis of the raw material is carried out with a mixture of sodium hydroxide and water, with the mixture for carrying out the alkaline hydrolysis of the raw material is injected ethanol and pyragollole, and alkaline hydrolysis of the feedstock is carried out at a temperature of 70°C for 4 hours under stirring for 15 min in the following ratio: raw material : ethanol : caustic sodium : pyragollole : water 100,0 : (300,0-350,0) : (30,0-35,0) : (0,05-0,01) : (7,5-12,0) or the mixture with the addition of toluene in the ratio of raw materials : ethanol : caustic sodium : pyragollole : toluene : water 100,0 : (220,0-225,0) : (30,0-38,0) : (0,05-0,12) : (100,0-137,0) : (2,5-7,0), followed by separation of lanosterol, deposition from a mixture of methylene chloride and ethanol in the ratio 1:1, and before removal of solvent unsaponifiables extracted for 2-3 hours at a temperature of 50°under stirring.

The essence of the proposed method

The essence of the proposed method of production of sterols: lanosterol and cholesterol from wool fat, is as follows.

Spend alkaline hydrolysis of raw materials, extraction of the unsaponifiable substances, removing the solvent and selects lanosterol and cholesterol, while alkaline hydrolysis of the raw material is carried out with a mixture of ethanol, sarcastically what about the sodium, pyragollole and water at a temperature of 70°C for 4 hours with stirring in the following ratio: raw material : ethanol : caustic sodium : pyragollole : water 100,0 : (300,0-350,0) : (30,0-35,0) : (0,05-0,01) : (7,5-12,0) or the mixture with the addition of toluene in the ratio of raw materials: ethanol : caustic sodium : pyragollole : toluene : water 100,0 : (220,0-255,0) : (30,0-38,0) : (0,05-0,12) : (100,0-137,0) : (2,5-7,0), and lanosterol allocate deposition from a mixture of methylene chloride and ethanol in the ratio 1:1, and before removal of solvent unsaponifiables extracted for 2-3 hours at a temperature of 50°under stirring.

The implementation of the invention

Examples of specific performance of the method of production of sterols: lanosterol and cholesterol from wool fat.

Example 1. Into the reactor containing the reflux condenser, a stirrer and a water jacket, placed 100 g of wool fat and heated to 45°C. Here also is poured a mixture consisting of 30 g of sodium hydroxide, 7.5 ml of water, 300 ml of ethanol and 45 mg pyragollole B, preheated to 45°C. mix Well for 10 minutes, Increase the temperature to 60°and carry out the alkaline hydrolysis of wool fat for 3.5 h under stirring. Then let the mixture cool to 20°and determine the amount of residual alkali. With this objective, 0.5 g of the obtained mass was added to 2.5 ml of ethanol, 7.5 ml of benzene, 7.5 ml of water and 5 drops of 0.1%-g is the solution of phenolphthalein in ethanol. Titrate with 0.1 N. HCl solution. The products of hydrolysis, in the reactor, heated to 35°add 1000 ml of acetone and addition of 14.5 ml of acetic acid to neutralize the residual alkali. The temperature was raised to 50°and unsaponifiables extracted for 20 hours with stirring. Sodium salt of fatty acid is filtered off, again placed in a reactor, add 500 ml of acetone and extracted in the same conditions. The extract was filtered and sodium salts of fatty acids are washed with 500 ml of acetone, preheated to 35°C. the Acetone extracts are combined and evaporated in vacuum at 50°With dryness. Sodium salts of fatty acids are used as classic emulsifier. Newmiley balance is 50.0 g or 50% of the taken sample of the feedstock. Unsaponifiables are dissolved in 200 ml of methylene chloride at 35°and add an equal volume of ethanol and left at 20°C for 1 h, not more, for the deposition of lanosterol. The precipitate is filtered, washed with 2 times 50 ml of ice-cold methylene chloride and dried in a vacuum desiccator at 35°C. Receive a white amorphous crystals having a melting point of 140-141°With the output of lanosterol 10.0 g, i.e. for 10.3% of the initial raw material.

The filtrate after separation of lanosterol evaporated in vacuum at 50°With dryness, dissolved in 250 ml of ethanol and left at 0°With those who tell 3 h for crystallization of cholesterol. The precipitate is filtered off, the filtrate is evaporated in vacuum at 50°With dryness, the residue is dissolved in 150 ml of ethanol and again precipitated residual quantity of cholesterol at 0°C for 2 hours the Precipitate is filtered off and added to the original draft of cholesterol. The filtrate is evaporated in vacuum at 50°With dryness, it is a concentrate of aliphatic alcohols mixed with hydroxy-, oxo -, and methyl-sterols.

The obtained crystals of cholesterol are combined and subjected to recrystallization twice. To this end, the crystals of cholesterol dissolved by heating to 60°With 100 ml of ethanol, then cooled and maintained at 0°C for 2 hours the Precipitate is filtered off, dissolved in 100 ml of acetone at 50°s and maintained at 0°C for 2 hours the Precipitate is filtered off, washed twice on the filter with 30 ml of ice-cold acetone. Get white crystals of cholesterol, the melting point of 144-145°C. Impurities are 3.0% (2% methylcholantrene, 1% lanosterol). The output of cholesterol 8.0 g, i.e. 8,0% of the feedstock.

Example 2. Carried out analogously to example 1, but with addition of toluene.

Put 100 g of wool fat, heat it to 50°C. Here also is poured a mixture of 30.0 g of NaOH, 4.5 mg pyragollole B, 300 ml of ethanol, 100 ml of toluene and 7.5 ml of water, previously heated to 50°C. Alkaline hydrolysis with stirring Prov is out for 3.8 hours at 70° C. Then added to the mixture of 230 ml of water, 120 ml of toluene and 200 ml of ethanol. The contents of the reactor are stirred for 10 min and left to settle at 60°C for 30 min the Lower aqueous layer was drained and at the same temperature, washed with 50 ml of toluene. Toluene rinse attached to the main toluene-methanol extract. The extract was evaporated in vacuum at 70°With up to a volume of 100 ml To the volume poured 600 ml of acetone, the mixture is stirred for 15 min and the precipitate sodium salts of the fatty acid is filtered off, washed twice with 70 ml of acetone, heated to 35°C. the Entire filtrate evaporated in vacuum to dryness. If the odor of toluene to the residue was added 2 times 100 ml of acetone and evaporated to dryness at 50°C. the Sodium salt is then used as a classic emulsifier.

The output of unsaponifiable fractions is 51% of the feedstock. A further selection of lanosterol and cholesterol and cleaning is carried out, as in example 1.

The output of lanosterol of 11.0 g, i.e. for 11% of the feedstock, and cholesterol 9,0,, ie 9% of the original raw materials.

Example 3. Carried out analogously to examples 1 and 2, but with increasing ratios of components.

Put 100 g of wool fat and heated to 50°C. Here also is poured a mixture consisting of 40 g NaOH, 15 ml of water, 400 ml of ethanol, 150 mg pyragollole B, pre-heat the th up to 50° C. a Well-stirred for 15 minutes Raise the temperature to 70°and carry out the alkaline hydrolysis of wool fat for 4 h under stirring. Then the mass is cooled to 20°and determine the amount of residual alkali, as in example 1. The products of hydrolysis, in the reactor, heated to 35°add 1000 ml of acetone and 18, 70 ml of acetic acid to neutralize the residual alkali. The temperature was raised to 50°and unsaponifiables extracted for 2, 3 h under stirring. Sodium salt of fatty acid is filtered off, again placed in a reactor, add 500 ml of acetone and extracted in the same conditions. The extract was filtered and sodium salts of fatty acids are washed with 500 ml of acetone, preheated to 35°C. the Acetone extracts are combined and evaporated in vacuum at 50°With dryness. Sodium salts of fatty acids are used as classic emulsifier. The output of the unsaponifiable fraction is 52% of the original raw materials.

A further selection of lanosterol and cholesterol and cleaning carried out as in example 1. The output of lanosterol 12.0 g, ie 12%, cholesterol 10.0 g, i.e 10% of the original raw materials.

The proposed method provides higher output of cholesterol to 8-10% and lanosterol up to 10-12% of the original raw materials, and reduces the time to obtain the target product (twice).

Cu is IU, the method preserves coproducts: fatty acids and aliphatic alcohols used for the preparation of medical and cosmetic products.

Thus, using this method of production of sterols: lanosterol and cholesterol from wool fat, not only increased the output of lanosterol and cholesterol, but also qualitative indicators.

Qualitative indicators of lanosterol:

1. DESCRIPTION - white crystalline powder with a yellowish, odorless.

2. TRANSPARENCY AND CHROMA - 2% solution in acetone is transparent and has a visible light white color, the degree of turbidity corresponds to the standard No. 4 State of pharmacotherapy XI edition.

3. The LOSS IN WEIGHT on DRYING 0,71%

4. ASH TOTAL of 1.24%

5. ASH SULFATE 3,68%

6. HEAVY METALS IN SULFATE ASH does not exceed 0,005%

7. RADIOACTIVITY (gamma radiation) was 13.8±0,5 Mr/h

(background - 13,3±0,5 Mr/h,

a valid natural background level up to 60 μr/h).

8. MELTING point 138-140°

9. SPECIFIC ROTATION (10% solution in acetone) +58°

10. QUANTITATIVE CONTENT (polarimetry) 98,0%

11. IMPURITIES by means of gas-liquid, thin-layer chromatography and UV spectrophotometry was not found.

Qualitative indicators of cholesterol:

1. DESCRIPTION white crystallize the cue powder, odorless.

2. TRANSPARENCY AND CHROMA - 2% solution in acetone is transparent and colorless.

3. The LOSS IN WEIGHT on DRYING 1,59%

4. ASH TOTAL 0,28%

5. ASH SULFATE 0,36%

6. HEAVY METALS IN SULFATE ASH does not exceed 0,005%

7. RADIOACTIVITY (gamma radiation) - 12,8±0,4 R/h

(background - 13,3±0,5 Mr/h,

a valid natural background level up to 60 μr/h).

8. MELTING point 147-149°

9. SPECIFIC ROTATION (10% solution in acetone) -38,2°

10. QUANTITATIVE CONTENT (polarimetry) 98,1%

11. IMPURITIES by means of gas-liquid, thin-layer chromatography and UV spectrophotometry was not found.

When high quality drugs lanosterol and cholesterol has the following results:

The drug lanosterol" contains: 37% lanest-8-EN-3β-Ola,

5% of cholesterol-7-EN-3β-Ola,

1% cholestadiene-3-ol.

The present invention in comparison with the prototype and other known technical solution has the following advantages:

- high yield of the target products;

- cheaper method of production of sterols;

- improve the quality of lanosterol and cholesterol;

- improvement of the environmental pollution in the production method of sterols.

Method for the production of sterols: lanosterol and cholesterol from cher is these fat, including alkaline hydrolysis of raw materials, extraction of the unsaponifiable substances, removing the solvent and selects lanosterol and cholesterol, while alkaline hydrolysis of the raw material is carried out with a mixture of sodium hydroxide and water, characterized in that the mixture for carrying out the alkaline hydrolysis of the raw material is injected ethanol and pyragollole, while alkaline hydrolysis of the feedstock is carried out at a temperature of 70°C for 4 h under stirring for 15 min in the following ratio of raw materials:ethanol:caustic sodium:pyragollole:water 100,0: (300,0-350,0): (30,0-35,0): (0,05-0,01): (7,5-12,0), or the mixture with the addition of toluene in the ratio of raw materials:ethanol:caustic sodium:pyragollole:toluene:water 100,0: (220,0-225,0): (30,0-38,0): (0,05-0,12): (100,0-137,0): (2,5-7,0), followed by separation of lanosterol, deposition from a mixture of methylene chloride and ethanol in the ratio 1:1, and before removal of solvent unsaponifiables extracted for 2-3 hours at a temperature of 50°under stirring.



 

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