CN105919928A - Method for preparing advanced alkanol aqueous solution - Google Patents
Method for preparing advanced alkanol aqueous solution Download PDFInfo
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- CN105919928A CN105919928A CN201610254989.8A CN201610254989A CN105919928A CN 105919928 A CN105919928 A CN 105919928A CN 201610254989 A CN201610254989 A CN 201610254989A CN 105919928 A CN105919928 A CN 105919928A
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- high triacontanol
- aqueous solution
- alkanol
- triacontanol
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/08—Solutions
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
Abstract
The invention provides a method for preparing an advanced alkanol aqueous solution. The method comprises the following steps: smashing advanced alkanol, and sieving the obtained powder; preparing an anionic surfactant, advanced alkanol and water, wherein the ratio of the anionic surfactant to the advanced alkanol to the water is (1-50) to 1 to (200-499) (w/w/w); uniformly mixing the anionic surfactant and the advanced alkanol, adding water into the mixture, and adjusting the pH of the solution to be 3-4 by adopting 5% of citric acid; and heating the solution prepared in the step (3) to 85-100 DEG C, preserving the heat, stirring the solution for 20-60 min till the advanced alkanol is dissolved, and carrying out natural cooling, thus obtaining the advanced alkanol aqueous solution. The method provided by the invention is reasonable in design, simple in technological process, and convenient to operate, advanced alkanol can be completely dissolved into water, so that the advanced alkanol aqueous solution is obtained, and therefore, the development in liquid preparations and study on the cell engineering of the advanced alkanol are expanded.
Description
Technical field
The present invention relates to the Application way of high triacontanol.A kind of method preparing high triacontanol aqueous solution.
Background technology
High triacontanol refer to amount of carbon atom at 20-34 straight chain saturated unitary primary alconol, molecular formula is CH3-(CH2)n-
CH2OH, the high triacontanol being primarily present in nature be hexacosanol, octacosanol, triacontanol, n-Dotriacontanol,
Inearnatyl alcohol.The oils and fats of these high triacontanols plant presented in wax ester or epidermis wax ester, the lipid of insect secretory, dynamic
In the fur of thing, sebum and internal organs.As: the main ester formed by hexadecanoic acid and triacontanol of Cera Flava, real estate Cera Flava contains
Having the total alkanol of 31%, the alcohols that wherein dissociates is 1%, and the total alkanol in Cera Flava has an effect of lipotropism, the most predominantly 28
Alkanol, triacontanol and n-Dotriacontanol, containing free alcohol in Cera Flava is n-Dotriacontanol (1.25%) and inearnatyl alcohol
(3.97%).The primary alconol carbon chain lengths that different species produce is different with content, the primary alconol carbon chain lengths that wherein free form exists
For C26, C28, C30, C32.Alkanol as middle-and-high-ranking in sugarcane wax mainly includes hexacosanol, octacosanol, triacontanol, its
Content is 19%, and wax insect middle-and-high-ranking alkanol main component is hexacosanol and octacosanol, its content 45%-56% respectively
And 34%-38%.These high triacontanols all have good pharmacologically active.As octacosanol has reduction cholesterol, resisting fatigue, increase
Add physical ability, stamina intensifying, improve muscular strength, reduce the oxygen consumption of myocardial cell, improve metabolism, blood circulation promoting, enhancing
Skin activity.Document is reported, octacosanol has good curative effect to parkinson, atherosclerosis.For these diseases one
As be required for oral formulations.Liquid preparation belongs to the one of oral formulations, because liquid preparation has dispersion greatly, absorbs fast, gives
Medicine approach is many, easy divided dose taking convenience, the advantages such as medicine irritation is little, therefore becomes the focus of current research.
Owing to high triacontanol mixture and one matter thereof are the most water insoluble, constrain high triacontanol mixture and list thereof
One material in the exploitation of water soluble preparation product and is studied on a cellular level, and high triacontanol mixture and one matter thereof
Research to the mechanism of action of specified disease.
In terms of drug research, people increasingly pay attention to illustrating the mechanism of action of medicine from cellular level.By to carefully
The technology such as the cultivation of born of the same parents, cell fusion, allow rapid screening out the action site of medicine.But, cell is mostly to cultivate at liquid
In.Therefore, high triacontanol mixture and one matter thereof are dissolved in water, are convenient for people on cell level study worm senior
Alkanol mixture and the one matter research to the specified disease mechanism of action thereof.
Summary of the invention
In order to develop high triacontanol mixture and one matter water soluble preparation and expand its answering in cell engineering
With, the present invention provides the technical scheme of a kind of method preparing high triacontanol aqueous solution.
Technical scheme: a kind of method preparing high triacontanol aqueous solution, it is characterised in that concrete steps are such as
Under:
(1) high triacontanol is pulverized, cross 200 mesh sieves
(2) anion surfactant, high triacontanol and water are prepared, anion surfactant and high triacontanol, the ratio of water
For；(1-50): 1:(200-499) (w/w/w)；
(3) anion surfactant is mixed with high triacontanol, add water, with the pH3-4 of concentration 5% citric acid regulating solution；
(4) the solution heating-up temperature 85 DEG C-100 DEG C that step (3) is made, insulation, stirring 20-60min dissolves to high triacontanol,
Natural cooling, for high triacontanol aqueous solution.
Described high triacontanol is high triacontanol mixture and one matter, and described high triacontanol one matter is 20
Six alkanols, octacosanol, triacontanol, n-Dotriacontanol, inearnatyl alcohol；Described high triacontanol mixture is 26
Alkanol and octacosanol mixing, wherein hexacosanol content is: 45%-56% (w/w), and octacosanol content is: 44%-
55% (w/w)。
Anion surfactant described in step (2) and high triacontanol, water be preferably in a proportion of 5:1:245 (w/w/w).
Nonionic surfactant described in step (2) is: tween 80, tween 20, moors sieve Pehanorm, Arlacel-80, department
Dish-20.
Described nonionic surfactant is preferably tween 80.
Heating-up temperature described in step (5) preferably 91 DEG C-95 DEG C.
Worm high triacontanol is dissolved in water, can be convenient for people to from cell level study high triacontanol and specified disease is made
With the research of mechanism, but high triacontanol has water-fast characteristic, and for these characteristics of high triacontanol, the present invention uses
Optimum high triacontanol is dissolved in the cosolvent anion surfactant of water, in numerous anion surfactants
It is chosen to be: tween 80, tween 20, moors sieve Pehanorm, Arlacel-80, Arlacel-20;It is preferably tween 80.Anion surface active
Agent is the surfactant the most not producing ion, is divided into polyoxyethylene-type and polyol type by its structure hydrophilic group
Two classes, wherein polyoxyethylene-type anion surfactant is polyethylene oxide and the compound addition compound product containing active hydrogen.This
Analog anion surfactants contains can adsorb the polar group of particle in water, forms particle and builds bridge.Have and accelerate solution
The effect of clarification.This kind of anionic surfactant is broadly divided into sorbitan ester and sucrose ester, wherein anhydrous sorbitol
Ester includes Tweens and spans.
The present invention is that high triacontanol is dissolved in water and devises anion surfactant, senior by substantial amounts of experimentation
Alkanol and the optimal proportion of water.Experiment proves that anion surfactant is the highest with the ratio of high triacontanol, high triacontanol molten
Xie Du is the best, and stability is the strongest, and the content of high triacontanol is the lowest.Comprehensive each side factor, anion surfactant is with senior
The ratio of alkanol is optimal with 5:1.High triacontanol is found through experiments easy in acid aqueous solution of anionic surfactant
Dissolving, when aqueous solution of anionic surfactant pH=3-4 solute effect is best, high triacontanol is using 5% citric acid regulation
In aqueous solution of anionic surfactant, solute effect is more preferable.Under room temperature, high triacontanol is solid state, 85 DEG C and more than
Cera Chinensis is liquid condition, and High Temperature And Velocity stirring has the Brownian movement promoting molecule, the beneficially dissolving of high triacontanol.In system
During Bei, stirring helps speed up the dissolving of high triacontanol, has a significant effect the stability of high triacontanol aqueous solution.Experiment
Prove that the content of water is little on dissolubility impact in preparation process, but the content of water can not very little, when water very little time, senior
By not re-dissolved after alkanol is saturated.The method of the present invention can make high triacontanol be completely dissolved in aqueous.Molten by observing
The outward appearance of liquid, it can be seen that do not had undissolved high triacontanol powder in solution, high triacontanol aqueous solution is milky or wax
Opaque or the translucent or transparent solution of white.
High triacontanol also known as pole long-chain fatty alcohol, refer to amount of carbon atom 20-34 straight chain saturated unitary primary alconol [1],
Molecular formula is CH3-(CH2)n-CH2OH.The former characteristic with amphiphilic of high fatty alcohol, has hydrophobic group the most hydrocarbon the most in the molecule
Chain, has again hydrophilic group such as hydroxyl.But owing to the dissolubility in water is the lowest, it is necessary to add hydrophilic group or hydroxyl is changed into sulphuric acid
Base, after making hydrophile-lipophile balance value reach necessary numerical value, fatty alcohol derivative has had enough hydrophilic groups can be allowed to be dissolved in water.
Citric acid is 2-hydroxy propane-1,2,3-tricarboxylic acids, a normal band water of crystallization in three carboxyls of citric acid, reacts many with alcohol
Number can form friendship fat, polyhydroxy-alkanoate or network-type polyester.Under strongly acidic conditions, esters hydrolyzes.Esters exists
Hydrolyzed under acidic conditions reaction is reversible.Therefore, add nonionic surfactant, utilize surfactant in critical temperature
Micelle can be formed, alcohol and acid are wrapped in micelle, stop it to regenerate esters, thus increase molten in water of high triacontanol
Xie Du.
The method of the present invention is reasonable in design, and technological process is simple, easy to operate, and high triacontanol can be made to be dissolved completely in water
In, become high triacontanol aqueous solution, study in terms of expanding high triacontanol exploitation in terms of liquid preparation and cell engineering.
Detailed description of the invention
Below by specific embodiment, technical scheme is further described.
A kind of method preparing high triacontanol aqueous solution, the design parameter of embodiment 1-14 is shown in Table 1, specifically comprises the following steps that
(1) high triacontanol is pulverized, cross 200 mesh sieves；
(2) anion surfactant, high triacontanol and water are prepared, anion surfactant and high triacontanol, the ratio of water
For；(1-50): 1:(200-499) (w/w/w)；Described anion surfactant and high triacontanol, being preferably in a proportion of of water
5:1:245 (w/w/w).Described high triacontanol is high triacontanol mixture and one matter, and described high triacontanol is 20
Six alkanols, octacosanol, triacontanol, n-Dotriacontanol, inearnatyl alcohol；Described high triacontanol mixture is 26
Alkanol and octacosanol mixing, wherein, the hexacosanol content in hexacosane alcohol mixture is: 45%-56%；28
Octacosanol content in alkanol mixture is: 44%-55%；Described nonionic surfactant is: tween 80, tell
Temperature-20, moors sieve Pehanorm, and Arlacel-80, Arlacel-20, described nonionic surfactant is preferably tween 80.
(3), after being mixed with high triacontanol by anion surfactant, water is added, with concentration 5% citric acid regulating solution
pH3-4；
(4) the solution heating-up temperature 85 DEG C-100 DEG C that step (3) is made, heating-up temperature preferably 91 DEG C-95 DEG C, insulation, stirring
Dissolve to high triacontanol, natural cooling；For high triacontanol aqueous solution.
The design parameter of table 1 embodiment 1-14
The dissolving situation of the middle-and-high-ranking alkanol of high triacontanol aqueous solution that inspection embodiment 1-14 obtains and stability thereof, be specifically shown in Table
2.By observe solution outward appearance, it can be seen that in solution without do not have dissolving high triacontanol powder, solution be milky or
Opaque or the translucent or transparent solution of wax.Anion surfactant is the highest with the ratio of high triacontanol, solution
Color is the whitest, and transparency is the highest.
The dissolving situation of table 2 high triacontanol and stability test thereof
Conclusion:
1, anion surfactant is the highest with the ratio of high triacontanol, and the dissolubility of high triacontanol is the best, and stability is the strongest, high
The content of level alkanol is the lowest.Embodiment proves that the anion surfactant ratio with high triacontanol is with 5:1((w/w) optimal.
2, in high triacontanol one matter, hexacosanol, octacosanol and triacontanol all have good dissolving to imitate
Really, in high triacontanol mixture be hexacosanol and octacosanol mixing solute effect preferable.
3, tween 80, tween 20 in nonionic surfactant, moors sieve Pehanorm, and Arlacel-80 and Arlacel-20 are for senior
Alkanol all has good solute effect.Embodiment proves that non-ionic surfactant Tween-80 effect is best.
4, high triacontanol dissolubility in the environment of slant acidity is higher, and embodiment proves that pH value is optimal with pH=3.5.PH adjusts
Joint agent is best with the effect of 5% citric acid.The high triacontanol aqueous solution that embodiment 1-14 obtains is in strict accordance with 1-4 of the present invention
Prepared by the preparation method of step, be adjusted the pH value of high triacontanol aqueous solution the most again.From testing result it can be seen that
The stability of high triacontanol aqueous solution is reliable, particularly embodiment 3, the optimal parameter or close that embodiment 6,7 and 8 uses
Product room temperature prepared by optimal parameter is placed 1 month and is still kept white clear to half a year, and has no precipitation.
5, high triacontanol dissolubility in the anion surfactant of heating is higher, and embodiment proves that heating-up temperature is with 91
DEG C-95 DEG C are preferred.
5, in preparation process, stirring helps speed up the dissolving of high triacontanol, has bright to the stability of high triacontanol solution
Development rings.Embodiment proves stirring more than 30min, and the stability of solution increases.
6, anion surfactant is the highest with the ratio of high triacontanol, and the transparency of solution is the highest.
7, in preparation process, the content of water is little on dissolubility impact, but the content of water can not very little, when water very little
Time, by not re-dissolved after the middle-and-high-ranking alkanol of solution is saturated.
Claims (6)
1. the method preparing high triacontanol aqueous solution, it is characterised in that specifically comprise the following steps that
(1) high triacontanol is pulverized, cross 200 mesh sieves；
(2) anion surfactant, high triacontanol and water are prepared, anion surfactant and high triacontanol, the ratio of water
For；(1-50): 1:(200-499) (w/w/w)；
(3) anion surfactant is mixed with high triacontanol, add water, with the pH3-4 of concentration 5% citric acid regulating solution；
(4) the solution heating-up temperature 85 DEG C-100 DEG C that step (3) is made, insulation, stirring 20-60min dissolves to high triacontanol,
Natural cooling, for high triacontanol aqueous solution.
A kind of method preparing high triacontanol aqueous solution the most according to claim 1, it is characterised in that described senior alkane
Alcohol is high triacontanol mixture and one matter, described high triacontanol one matter be hexacosanol, octacosanol, three
Ten alkanols, n-Dotriacontanol, inearnatyl alcohol；Described high triacontanol mixture is that hexacosanol and octacosanol mix
Closing, wherein hexacosanol content is: 45%-56% (w/w), and octacosanol content is: 44%-55% (w/w).
A kind of method preparing high triacontanol aqueous solution the most according to claim 1, it is characterised in that step (2) is described
Anion surfactant and high triacontanol, water be preferably in a proportion of 5:1:245 (w/w/w).
A kind of method preparing high triacontanol aqueous solution the most according to claim 1, it is characterised in that step (2) is described
Nonionic surfactant be: tween 80, tween 20, moor sieve Pehanorm, Arlacel-80, Arlacel-20.
A kind of method preparing high triacontanol aqueous solution the most according to claim 4, it is characterised in that described nonionic
Surfactant is preferably tween 80.
A kind of method preparing high triacontanol aqueous solution the most according to claim 1, it is characterised in that step (5) is described
Heating-up temperature preferably 91 DEG C-95 DEG C.
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| CN201610254989.8A CN105919928A (en) | 2016-04-25 | 2016-04-25 | Method for preparing advanced alkanol aqueous solution |
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| CN201610254989.8A CN105919928A (en) | 2016-04-25 | 2016-04-25 | Method for preparing advanced alkanol aqueous solution |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113057941A (en) * | 2021-03-26 | 2021-07-02 | 中国林业科学研究院资源昆虫研究所 | Higher alkanol liposome for improving learning memory and preparation method thereof |
| CN113080350A (en) * | 2021-04-19 | 2021-07-09 | 超元素(广州)食品科技有限公司 | Formula and application for soothing nerves and aiding sleep and preparation method of water-phase liquid beverage |
| CN113197977A (en) * | 2021-04-19 | 2021-08-03 | 超元素(广州)食品科技有限公司 | Rice bran fatty alkanol aqueous phase solution and preparation method thereof |
-
2016
- 2016-04-25 CN CN201610254989.8A patent/CN105919928A/en active Pending
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113057941A (en) * | 2021-03-26 | 2021-07-02 | 中国林业科学研究院资源昆虫研究所 | Higher alkanol liposome for improving learning memory and preparation method thereof |
| CN113057941B (en) * | 2021-03-26 | 2022-06-17 | 中国林业科学研究院资源昆虫研究所 | Higher alkanol liposome for improving learning memory and preparation method thereof |
| CN113080350A (en) * | 2021-04-19 | 2021-07-09 | 超元素(广州)食品科技有限公司 | Formula and application for soothing nerves and aiding sleep and preparation method of water-phase liquid beverage |
| CN113197977A (en) * | 2021-04-19 | 2021-08-03 | 超元素(广州)食品科技有限公司 | Rice bran fatty alkanol aqueous phase solution and preparation method thereof |
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