Novel oil-soluble precursor micelle preparation and production method thereof
By mixing the active material with alcohols, surfactants and oils in a specific proportion, heating and diluting, forming a transparent oily liquid, the problem of the active material being difficult to dissolve in oil is solved, and the bioavailability and application range are improved.
Patent Information
- Application Number
- CN202510136526.0
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2025-02-07
- Publication Date
- 2025-05-16
AI Technical Summary
Active materials such as bosein and ferulic acid are difficult to dissolve in oil, resulting in limited use range and unstable in aqueous systems.
Using a new oil-soluble precursor micelle preparation, the active material that is difficult to dissolve in oil is mixed with alcohols, surfactants and oils in a specific proportion, heated and diluted to form a transparent oily liquid.
The effective dissolution of the active material in the oil is achieved, forming a transparent oily liquid, improving bioavailability, reducing the waste of active ingredients, and expanding its application scope in the fields of medicines, cosmetics, food, etc.
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Abstract
Description
Technical Field
[0001] The invention relates to the field of precursor micelle preparations, in particular to a novel oil-soluble precursor micelle preparation and a production method thereof. Background Art
[0002] The oil solubility of active materials such as bosaicin, ferulic acid, glycyrrhizic acid, ammonium glycyrrhizinate, glabridin, phenethyl resorcinol, dimethoxytoluene propyl resorcinol, isobutylamido thiazolyl resorcinol, dihydroavenous alkaloids, ergothioneine, etc. has been plaguing the pharmaceutical industry, food industry, cosmetics industry, agriculture and other fields, resulting in the limited use of these active materials and the inability to be better promoted and used. In addition, active materials such as ergothioneine are prone to become unstable in aqueous systems and are greatly affected by oxygen and pH value. If they are dissolved in oil, these defects will be reduced and the system will be more stable. Summary of the invention
[0003] The purpose of the present invention is to provide a novel oil-soluble precursor micelle preparation and a production method thereof to solve the above technical problems.
[0004] In order to solve the above technical problems, the present invention adopts the following technical solutions:
[0005] A novel oil-soluble precursor micelle preparation comprises the following raw material components in parts by weight: 0.01 to 90 parts of an active material that is poorly soluble in oil, 0 to 65 parts of alcohols, 0.01 to 90 parts of surfactants, and 0 to 90 parts of oils and fats.
[0006] Preferably, the insoluble active material in oil comprises one or more of bosacene, ferulic acid, glycyrrhizic acid, ammonium glycyrrhizinate, glabridin, phenethyl resorcinol, dimethoxytoluene propyl resorcinol, isobutylamidothiazolyl resorcinol, dihydroavenous alkaloids, and ergothioneine.
[0007] Preferably, the surfactants include one or more of lecithin and its derivatives, hydrogenated lecithin and its derivatives, egg yolk lecithin and its derivatives, and also include a variety of water-in-oil emulsifiers.
[0008] Preferably, the water-in-oil emulsifier includes Span 60 / 80 / 120, tri(polyglycerol-3, lauryl) hydrogenated trimer linoleate, sorbitan sesquioleate, sorbitan olivate, sorbitan isostearate, and monoglyceride.
[0009] Preferably, the alcohols include one or more of 1,2-pentanediol, hexylene glycol, 1,2-hexanediol, 1,6-hexanediol, cyclohexylglycerol, dimethyl isosorbide, isopropyl glycerol, glycerol acetone acetal, and ethanol.
[0010] Preferably, the mass ratio of the insoluble active material in oil to the surfactant is in the range of 30:1 to 1:99.
[0011] Preferably, the mass ratio of the active material to the alcohol is in the range of 10:1 to 1:99.
[0012] Preferably, the oils used include squalane, caprylic decanoic acid glyceride, GTCC, isononyl isononanoate, corn oil, soybean oil, jojoba oil, sunflower seed oil, and cactus seed oil.
[0013] A novel method for preparing an oil-soluble precursor micelle preparation is characterized in that it comprises the following steps: mixing the above-mentioned active materials, alcohols, surfactants and oils in order, heating them, and controlling the temperature in the range of 30 to 99 degrees. After the mixture is evenly mixed, discharging the materials, taking the precursor micelle material and diluting it with oils by a certain multiple to obtain a transparent oil preparation.
[0014] A novel application of an oil-soluble precursor micelle preparation, a transparent oil prepared based on the novel precursor micelle, and then an emulsion, ointment, cream, lipstick, eye shadow, jelly, injection prepared by adding appropriate colorants, flavors, antioxidants, preservatives, thickeners, gelling agents, and flavoring agents, which is used for preparing food, medicine, cosmetics, pesticides, feed, and veterinary drugs.
[0015] The beneficial effects of the present invention are:
[0016] (1) The oil-soluble precursor micelle preparation provided by the present invention can dissolve one or more beneficial active ingredients that are difficult to dissolve in oil, such as bosacene, ferulic acid, glycyrrhizic acid, ammonium glycyrrhizinate, glycyrrhizin, phenethyl resorcinol, dimethoxytoluene propyl resorcinol, isobutylamidothiazolyl resorcinol, dihydroavenate alkaloids, ergothioneine, etc., in oil to form a transparent oily liquid, so as to fully utilize and maximize its efficacy, improve its bioavailability, reduce the waste of high-value active ingredients, and have environmental value; at the same time, it can prepare dosage forms such as transparent oils and transparent oil gels that have appreciation value in appearance, expand the application of these active materials in cosmetics, medicines, foods, pesticides, feeds, etc., and have great social value and economic value.
[0017] (2) The preparation method of the oil-soluble precursor micelle preparation provided by the present invention is simple to operate, has stable technology, and has readily available raw materials. The prepared paste or solid raw materials are convenient for storage and transportation. The preparation method of preparing transparent, clear transparent oil, transparent oil gel, etc. after adding oil to the paste or solid is also relatively simple and energy-saving, and has great promotion value. DETAILED DESCRIPTION
[0018] In order to make the technical means, creative features, objectives and effects achieved by the present invention easy to understand, the present invention is further described below in conjunction with specific embodiments, but the following embodiments are only preferred embodiments of the present invention, not all. Based on the embodiments in the implementation mode, other embodiments obtained by those skilled in the art without creative work all belong to the protection scope of the present invention. The experimental methods in the following embodiments, unless otherwise specified, are conventional methods, and the materials, reagents, etc. used in the following embodiments, unless otherwise specified, can all be obtained from commercial channels.
[0019] Example 1
[0020] This embodiment provides a method for preparing a transparent oil-soluble precursor micelle preparation using this scheme, and dissolving it in oil so that the proportion of isobutyrylaminothiazolylresorcinol in the final product is still more than 0.1% [it can also be other concentrations such as 0.2%, etc., and the same is true for the following embodiments], and a transparent liquid at room temperature can still be obtained. The raw material components and mass proportions used in this embodiment are as follows:
[0021] 1. Transparent oil-soluble precursor micelle preparation formula:
[0022] 12.5 parts of isobutyrylaminothiazolylresorcinol
[0023] 37.5 parts of egg yolk lecithin
[0024] 1,2-Hexanediol 50 parts
[0025] 2. Diluting oil
[0026] Isononyl isononanoate, the proportion is 5900 parts
[0027] 3. Preparation method:
[0028] This embodiment also provides a method for preparing the above transparent oil-soluble precursor micelle preparation, the steps are as follows:
[0029] Weigh the materials for preparing the transparent oil-soluble precursor micelle preparation according to the mass ratio, mix, heat, control the temperature in the range of 30-99°C, stir to make it uniform, filter while hot, and obtain a yellow-brown clear and transparent liquid. High-pressure homogenization can be performed if necessary. Weigh a certain amount of this transparent oil-soluble precursor micelle preparation and a corresponding proportion of dilution oil [oil temperature in the range of 50-99 degrees], mix, filter while hot, and after cooling, obtain a light yellow transparent oil.
[0030] Example 2
[0031] This example provides a method for preparing a transparent oil-soluble precursor micelle preparation using this scheme, and dissolving it in oil so that the proportion of ammonium glycyrrhizinate in the final product is still more than 0.1%, and a transparent liquid at room temperature can still be obtained. The components and mass proportions of the raw and auxiliary materials used in this example are as follows:
[0032] 1. The formula and proportion of the transparent oil-soluble precursor micelle preparation are as follows:
[0033]
[0034] 2. Diluting oil
[0035] GTCC [caprylic acid triglyceride], the proportion is 9000 parts
[0036] 3. Preparation method:
[0037] Weigh the materials for preparing the oil-soluble precursor micelle preparation according to the mass ratio, mix, heat, control the temperature in the range of 30-99°C, stir, make transparent, filter while hot, and obtain a light yellow clear liquid. Weigh a certain amount of this oil-soluble precursor micelle preparation and a corresponding proportion of GTCC [oil temperature in the range of 70-99 degrees], mix, and obtain a slightly light yellow transparent oil.
[0038] Example 3
[0039] This example provides a method for preparing a transparent oil-soluble precursor micelle preparation using this scheme, and dissolving it in oil so that the proportion of glycyrrhizic acid in the final product is still more than 0.1%, and a transparent liquid at room temperature can still be obtained. The raw material components and mass proportions used in this example are as follows:
[0040] 1. The formula and proportion of the transparent oil-soluble precursor micelle preparation are as follows:
[0041]
[0042] 2. Diluting oil
[0043] Isononyl isononanoate, the proportion is 9000 parts
[0044] 3. Preparation method:
[0045] Weigh the materials for preparing the oil-soluble precursor micelle preparation according to the mass ratio, mix, heat, control the temperature in the range of 30-99°C, stir, make transparent, filter while hot, and obtain a light yellow clear and transparent liquid. Weigh a certain amount of this oil-soluble precursor micelle preparation and a corresponding proportion of isononyl isononanoate [oil temperature in the range of 70-99 degrees], mix, and obtain a slightly light yellow transparent oil.
[0046] Example 4
[0047] This example provides a method for preparing a transparent oil-soluble precursor micelle preparation using this scheme, and dissolving it in oil so that the proportion of bosine in the final product is still more than 1%, and a transparent liquid at room temperature can still be obtained. The components and mass proportions of the raw and auxiliary materials used in this example are as follows:
[0048] 1. The formula and proportion of the transparent oil-soluble precursor micelle preparation are as follows:
[0049]
[0050] 2. Diluting oil
[0051] Isononyl isononanoate, the proportion is 900 parts
[0052] 3. Preparation method:
[0053] Weigh the materials for preparing the oil-soluble precursor micelle preparation according to the mass ratio, mix, heat, control the temperature in the range of 30-99°C, stir, make transparent, filter while hot, and obtain a light brown-red clear and transparent liquid. Weigh a certain amount of this oil-soluble precursor micelle preparation and a corresponding proportion of isononyl isononanoate [oil temperature in the range of 70-99 degrees], mix, and obtain a slightly light yellow transparent oil.
[0054] Example 5
[0055] This example provides a method for preparing a transparent oil-soluble precursor micelle preparation using this scheme, and dissolving it in oil so that the proportion of dihydroavenate alkaloids in the final product is still more than 0.2%, and a transparent liquid at room temperature can still be obtained. The components and mass proportions of the raw and auxiliary materials used in this example are as follows:
[0056] 1. The formula and proportion of the transparent oil-soluble precursor micelle preparation are as follows:
[0057] 20 parts of dihydroavenous alkaloids
[0058] 100 parts of anhydrous ethanol
[0059] 80 servings of egg yolk lecithin
[0060] 2. Diluting oil
[0061] Isononyl isononanoate, the proportion is 9000 parts
[0062] 3. Preparation method:
[0063] Weigh the materials for preparing the oil-soluble precursor micelle preparation according to the mass ratio, mix, heat, control the temperature in the range of 30-99°C, stir, make transparent, filter while hot, and obtain a light brown-yellow clear and transparent liquid. Recover ethanol under reduced pressure to obtain a brown-yellow fluid paste. Weigh a certain amount of this fluid paste and a corresponding proportion of isononyl isononanoate [oil temperature in the range of 70-99 degrees], mix, and obtain a slightly light yellow transparent oil.
[0064] The above shows and describes the basic principles, main features and advantages of the present invention. Those skilled in the art should understand that the present invention is not limited by the above embodiments. The above embodiments and descriptions are only preferred examples of the present invention and are not intended to limit the present invention. Without departing from the spirit and scope of the present invention, the present invention may have various changes and improvements, which fall within the scope of the present invention. The scope of protection of the present invention is defined by the attached claims and their equivalents.
Claims
1. A novel oil-soluble precursor micelle preparation, characterized in that: The invention comprises the following raw material components in parts by weight: 0.01 to 90 parts of active materials insoluble in oil, 0 to 65 parts of alcohols, 0.01 to 90 parts of surfactants and 0 to 90 parts of oils and fats.
2. A novel oil-soluble precursor micelle preparation according to claim 1, characterized in that: The active material that is insoluble in oil includes one or more of bosacene, ferulic acid, glycyrrhizic acid, ammonium glycyrrhizinate, glabridin, phenethyl resorcinol, dimethoxytoluene propyl resorcinol, isobutylamidothiazolyl resorcinol, dihydroavenous alkaloids, and ergothioneine.
3. A novel oil-soluble precursor micelle preparation according to claim 1, characterized in that: The surfactants include one or more of lecithin and its derivatives, hydrogenated lecithin and its derivatives, egg yolk lecithin and its derivatives, and also include a variety of water-in-oil emulsifiers.
4. A novel oil-soluble precursor micelle preparation according to claim 3, characterized in that: The water-in-oil emulsifier includes Span 60 / 80 / 120, tri(polyglycerol-3, lauryl) hydrogenated trimer linoleate, sorbitan sesquioleate, sorbitan olive oil ester, sorbitan isostearate, and monoglyceride.
5. The novel oil-soluble precursor micelle preparation according to claim 1, characterized in that: The alcohols include one or more of 1,2-pentanediol, hexylene glycol, 1,2-hexanediol, 1,6-hexanediol, cyclohexylglycerol, dimethyl isosorbide, isopropylidene glycerol, glycerol acetone acetal, and ethanol.
6. A novel oil-soluble precursor micelle preparation according to claim 1, characterized in that: The mass ratio of the insoluble active material to the surfactant is in the range of 30:1 to 1:
99.
7. A novel oil-soluble precursor micelle preparation according to claim 1, characterized in that: The mass ratio of the active material to the alcohol is in the range of 10:1 to 1:
99.
8. A novel oil-soluble precursor micelle preparation according to claim 1, characterized in that: The oils used include squalane, caprylic / capric glyceride, GTCC, isononyl isononanoate, corn oil, soybean oil, jojoba oil, sunflower seed oil, and cactus seed oil.
9. A method for preparing the novel oil-soluble precursor micelle preparation according to any one of claims 1 to 8, characterized in that: The method comprises the following steps: mixing the above active materials, alcohols, surfactants and oils in order, heating them, controlling the temperature in the range of 30 to 99 degrees, discharging the materials after they are evenly mixed, taking the precursor micelle materials and diluting them with oils by a certain multiple to obtain a transparent oil agent.
10. Application of a novel oil-soluble precursor micelle preparation, characterized in that: The transparent oil prepared based on the above-mentioned novel precursor micelles is then used to prepare emulsions, ointments, creams, lipsticks, eye shadows, jellies, and injections by adding appropriate colorants, flavors, antioxidants, preservatives, thickeners, gelling agents, and flavoring agents, which are used to prepare foods, medicines, cosmetics, pesticides, feeds, and veterinary drugs.