Novel ultraviolet-resistant and oxygen-resistant precursor micelle solid preparation and production method thereof

Abstract

The invention discloses a novel ultraviolet-resistant and oxygen-resistant precursor micelle solid preparation which is prepared from the following raw material components in parts by mass: 0.1-95 parts of an active material, 0.5-95 parts of a micelle agent, 0.1-90 parts of a filler, 0.1-20 parts of an antioxidant, 0-10 parts of a pH regulator, 0.1-5 parts of a complexing agent and 0-30 parts of an isoosmotic adjusting agent, the raw material components are prepared into solid particles or powder, and precursor micelles are dissolved in deionized water to obtain clear and transparent water liquid. According to the precursor micelle preparation provided by the invention, one or more beneficial water-soluble or indissolvable active ingredients such as vitamin C, salicylic acid, ferulic acid, p-hydroxyacetophenone and raspberry ketone can be prepared into a precursor micelle solid preparation, and the precursor micelle solid preparation is dissolved in water to form a transparent aqueous liquid, so that the precursor micelle solid preparation is fully utilized and the maximum effect of the precursor micelle solid preparation is brought into play; the bioavailability is improved, the waste of high-value active ingredients can be reduced, and the environment-friendly value is realized.

Description

Technical Field

[0001] The present invention relates to the technical field of precursor micelle preparations, in particular to a novel ultraviolet-resistant and oxygen-resistant precursor micelle solid preparation and a production method thereof. Background Art

[0002] Vitamin C is vulnerable to UV rays and easily oxidizes. Therefore, it must be stored in a dark and oxygen-free environment for use in food, pharmaceuticals, and cosmetics. This is highly inconvenient and prone to deterioration, posing risks or hazards to human health. There is an urgent need to find a formula or method to address this issue. During extensive experimentation, I stumbled upon the discovery that by encapsulating vitamin C in micelles and combining them with antioxidants and chelating agents, vitamin C and salicylic acid can be rendered UV- and oxygen-resistant. Further research subsequently revealed that treatment with this micellar agent significantly improved the stability and water solubility of easily oxidized ingredients, such as salicylic acid, ferulic acid, p-hydroxyacetophenone, and raspberry ketone. Summary of the Invention

[0003] The object of the present invention is to provide a novel UV-resistant and oxygen-resistant precursor micelle solid preparation and a production method thereof, so as 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 UV-resistant and oxygen-resistant precursor micelle solid preparation comprises the following raw material components in parts by weight: 0.1-95 parts of active material, 0.5-95 parts of micellar agent, 0.1-90 parts of filler, 0.1-20 parts of antioxidant, 0-10 parts of pH regulator, 0.1-5 parts of complexing agent, and 0-30 parts of isotonicity regulator. The solid preparation is made into solid particles or powder. The precursor micelles are dissolved in deionized water to obtain a clear and transparent aqueous solution.

[0006] Preferably, the active ingredient includes one or more of vitamin C, salicylic acid, ferulic acid, p-hydroxyacetophenone, and raspberry ketone.

[0007] Preferably, the micellar agents include one or more of glycyrrhizic acid, glycyrrhizic acid salts such as monopotassium glycyrrhizate, dipotassium glycyrrhizate, tripotassium glycyrrhizate, monoammonium glycyrrhizate, diammonium glycyrrhizate, triammonium glycyrrhizate, monosodium glycyrrhizate, disodium glycyrrhizate, trisodium glycyrrhizate, and magnesium isoglycyrrhizate.

[0008] Preferably, the isotonicity regulator includes one or more of mannitol, trehalose, and glucose.

[0009] Preferably, the mass ratio of the active material to the micellar agent is in the range of 40:1 to 1:99.

[0010] Preferably, the filler is bosine, and the ratio of bosine to vitamin C is in the range of 10:1 to 1:99.

[0011] Preferably, the antioxidant is anhydrous sodium sulfite, p-hydroxyacetophenone, raspberry ketone, sodium metabisulfite, sodium thiosulfate, or sodium bisulfite; and the complexing agent is EDTA-2Na.

[0012] Preferably, the pH regulator includes arginine, lysine, histidine, sodium hydroxide, potassium hydroxide, triethanolamine, meglumine, anhydrous sodium carbonate, sodium bicarbonate, disodium hydrogen phosphate, and sodium citrate, so that the pH value of the system is controlled between 2.5 and 7.

[0013] The preparation method of the novel UV-resistant and oxygen-resistant precursor micelle solid preparation comprises the following steps:

[0014] For vitamin C, the above materials are mixed in order, and 3 to 30 times of deionized water are added, stirred to fully dissolve, filtered, freeze-dried, discharged, crushed, and bagged; this precursor micelle material is diluted with water by a certain multiple, such as 10 times, 20 times, 30 times, or 50 times, to obtain a transparent gel, a transparent emulsion, or a transparent aqueous solution in sequence; or the above materials are physically mixed, or the materials other than the active ingredient, such as vitamin C, are first dissolved in a certain concentration, such as 10% to 95% of aqueous ethanol or anhydrous ethanol, stirred evenly, the ethanol is removed under reduced pressure, vacuum dried, crushed, and then mixed evenly with the vitamin C before bagging;

[0015] For salicylic acid, the materials were physically mixed;

[0016] For ferulic acid, p-hydroxyacetophenone and raspberry ketone, various materials are heated with ethanol of appropriate concentration to fully dissolve, concentrated under reduced pressure, ethanol is recovered, vacuum dried, crushed, sieved and bagged.

[0017] The beneficial effects of the present invention are:

[0018] (1) The precursor micelle preparation provided by the present invention can prepare one or more beneficial active ingredients that are easily soluble or poorly soluble in water, such as vitamin C, salicylic acid, ferulic acid, p-hydroxyacetophenone, raspberry ketone, etc., into a precursor micelle solid preparation, and dissolve it in water to form a transparent aqueous 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 transparent water, transparent emulsion, transparent paste, transparent gel and other dosage forms with aesthetic value in appearance, expand the application of these active materials in cosmetics, medicines, food, animal medicines, feed, etc., and have great social value and economic value.

[0019] (2) The preparation method of the precursor micelle preparation provided by the present invention is simple to operate, has stable technology, and the raw materials are easily available. The prepared solid raw materials are convenient to store and transport. The preparation method of the precursor micelle solid preparation for preparing transparent, clear water, transparent emulsion, transparent paste, transparent gel, etc. after adding water is also relatively simple and energy-saving, and has great promotion value. DETAILED DESCRIPTION

[0020] In order to make the technical means, creative features, purpose and efficacy of the present invention easy to understand, the present invention is further described below in conjunction with specific examples, but the following examples are only preferred embodiments of the present invention, not all. Based on the examples in the embodiments, other embodiments obtained by those skilled in the art without making creative work are within the scope of protection of the present invention. The experimental methods in the following examples, unless otherwise specified, are conventional methods, and the materials, reagents, etc. used in the following examples, unless otherwise specified, can be obtained from commercial channels.

[0021] Example 1

[0022] This example provides a method for preparing a UV-resistant and oxygen-resistant precursor micelle solid preparation using this solution. The raw material components and mass ratios used in this example are as follows:

[0023] 1. Vitamin C precursor micellar solid preparation formula:

[0024]

[0025]

[0026] 2. Preparation method:

[0027] The materials for preparing the drug-excipient precursor micelle preparation are weighed according to the mass ratio, mixed, and 9 times the amount of deionized water is added. The mixture is heated to 40-50 degrees Celsius, stirred to mix thoroughly, and filtered while hot to obtain a colorless to light yellow clear liquid. The liquid is freeze-dried to obtain a block solid, which is crushed, sieved, and bagged.

[0028] 3. Comparative experiment on the resistance of vitamin C to ultraviolet light and oxygen

[0029] The materials of Example 1, Comparative Example 1 and Comparative Example 2 were weighed according to the proportions in Table 1, slightly heated, stirred and mixed evenly, filtered, and placed in colorless transparent glass bottles, sealed, and placed according to corresponding storage conditions. The color and transparency were observed and recorded.

[0030]

[0031]

[0032]

[0033] Example 2

[0034] This example provides a method for preparing a UV-resistant and oxygen-resistant precursor micelle solid preparation using this solution. The raw material components and mass ratios used in this example are as follows:

[0035] 1. The formula and proportion of the ferulic acid precursor micelle preparation are as follows:

[0036]

[0037] 2. Preparation method:

[0038] The precursor micelle preparation materials prepared above were weighed and mixed according to their mass ratio. A 10%-50% aqueous ethanol solution (approximately 10 times the mass) was added. The mixture was heated, controlled at 30-70°C, and stirred until transparent. The mixture was filtered while hot to obtain a light yellow, clear liquid. The ethanol and water were removed by vacuum distillation. The mixture was then vacuum dried, crushed, sieved, and barreled.

[0039] 3. Comparative experiment on ultraviolet and oxygen resistance of ferulic acid

[0040] The materials of Example 2, Comparative Example 3 and Comparative Example 4 were weighed according to the proportions in Table 2, slightly heated, stirred and mixed evenly, filtered, and placed in colorless transparent glass bottles, sealed, and placed according to corresponding storage conditions. The color and transparency were observed and recorded.

[0041]

[0042]

[0043] Example 3

[0044] This example provides a method for preparing a precursor micelle formulation using this method and dissolving it in water so that the proportion of salicylic acid in the final product remains above 0.5% and a transparent gel at room temperature is obtained. The raw material components and their mass ratios used in this example are as follows:

[0045] 1. The formula and proportion of the salicylic acid precursor micelle preparation are as follows:

[0046]

[0047] 2. Preparation Method

[0048] The materials for preparing the precursor micelle solid preparation of drug-excipient combination are weighed according to the mass ratio, crushed, sieved, mixed in increasing order for 1 hour to 2 hours, discharged, and barreled.

[0049] 3. Comparative experiment on salicylic acid's resistance to ultraviolet light and oxygen

[0050] The materials of Example 3, Comparative Example 5 and Comparative Example 6 were weighed according to the proportions in Table 3, slightly heated, stirred and mixed evenly, filtered, and placed in colorless transparent glass bottles, sealed, and placed according to corresponding storage conditions. The color and transparency were observed and recorded.

[0051]

[0052]

[0053] Example 4

[0054] The raw material components and mass ratios used in this embodiment are as follows:

[0055] 1. The formula and proportion of the precursor micelle solid preparation of p-hydroxyacetophenone and raspberry ketone are as follows:

[0056]

[0057]

[0058] 2. Preparation Method

[0059] Weigh the above materials according to their mass ratio, mix them, add about 10 times the amount of 10%-50% aqueous ethanol, heat at a temperature of 30-70°C, stir until transparent, and filter while hot to obtain a light yellow, clear liquid. Distill under reduced pressure to remove the ethanol and water, then vacuum dry, crush, sieve, and barrel.

[0060] 3. Comparative experiment on UV resistance and oxygen resistance of p-hydroxyacetophenone and raspberry ketone

[0061] The materials of Example 4, Comparative Example 7 and Comparative Example 8 were weighed according to the proportions in Table 4, slightly heated, stirred and mixed evenly, filtered, and placed in colorless transparent glass bottles, sealed, and placed according to corresponding storage conditions. The color and transparency were observed and recorded.

[0062]

[0063]

[0064]

[0065] 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 to the above embodiments. The above embodiments and descriptions are merely preferred examples of the present invention and are not intended to limit the present invention. Various changes and improvements may be made to the present invention without departing from the spirit and scope of the present invention. Such changes and improvements fall within the scope of the present invention. The scope of protection claimed in the present invention is defined by the appended claims and their equivalents.

Claims

1. A novel UV-resistant and oxygen-resistant precursor micelle solid preparation, characterized by: The preparation comprises the following raw material components in parts by weight: 0.1 to 95 parts of active material, 0.5 to 95 parts of micellar agent, 0.1 to 90 parts of filler, 0.1 to 20 parts of antioxidant, 0 to 10 parts of pH regulator, 0.1 to 5 parts of complexing agent, and 0 to 30 parts of isotonicity regulator, and is made into solid particles or powder. The precursor micelles are dissolved in deionized water to obtain a clear and transparent aqueous solution.

2. The novel UV-resistant and oxygen-resistant precursor micelle solid preparation according to claim 1, characterized in that: The active material comprises one or more of vitamin C, salicylic acid, ferulic acid, p-hydroxyacetophenone and raspberry ketone.

3. The novel UV-resistant and oxygen-resistant precursor micelle solid preparation according to claim 1, characterized in that: The micellar agents include one or more of glycyrrhizic acid, glycyrrhizic acid salts such as monopotassium glycyrrhizate, dipotassium glycyrrhizate, tripotassium glycyrrhizate, monoammonium glycyrrhizate, diammonium glycyrrhizate, triammonium glycyrrhizate, monosodium glycyrrhizate, disodium glycyrrhizate, trisodium glycyrrhizate, and magnesium isoglycyrrhizate.

4. The novel UV-resistant and oxygen-resistant precursor micelle solid preparation according to claim 1, characterized in that: The isotonicity regulator includes one or more of mannitol, trehalose and glucose.

5. The novel UV-resistant and oxygen-resistant precursor micelle solid preparation according to claim 1, characterized in that: The mass ratio of the active material to the micellar agent is in the range of 40:1 to 1:

99.

6. The novel UV-resistant and oxygen-resistant precursor micelle solid preparation according to claim 2, characterized in that: The filler is bosera, and the ratio of bosera to vitamin C is in the range of 10:1 to 1:

99.

7. The novel UV-resistant and oxygen-resistant precursor micelle solid preparation according to claim 1, characterized in that: The antioxidant is anhydrous sodium sulfite, p-hydroxyacetophenone, raspberry ketone, sodium metabisulfite, sodium thiosulfate, and sodium bisulfite; and the complexing agent is EDTA-2Na.

8. The novel UV-resistant and oxygen-resistant precursor micelle solid preparation according to claim 1, characterized in that : PH regulators include arginine, lysine, histidine, sodium hydroxide, potassium hydroxide, triethanolamine, meglumine, anhydrous sodium carbonate, sodium bicarbonate, disodium hydrogen phosphate, and sodium citrate to control the pH value of the system between 2.5 and 7.

9. The method for preparing the novel UV-resistant and oxygen-resistant precursor micelle solid preparation according to any one of claims 1 to 8, characterized in that: Here are the steps: For vitamin C, the above materials are mixed in order, and 3 to 30 times of deionized water are added, stirred to fully dissolve, filtered, freeze-dried, discharged, crushed, and bagged; this precursor micelle material is diluted with water by a certain multiple, such as 10 times, 20 times, 30 times, or 50 times, to obtain a transparent gel, a transparent emulsion, or a transparent aqueous solution in sequence; or the above materials are physically mixed, or the materials other than the active ingredient, such as vitamin C, are first dissolved in a certain concentration, such as 10% to 95% of aqueous ethanol or anhydrous ethanol, stirred evenly, the ethanol is removed under reduced pressure, vacuum dried, crushed, and then mixed evenly with the vitamin C before bagging; For salicylic acid, the materials were physically mixed; For ferulic acid, p-hydroxyacetophenone and raspberry ketone, various materials are heated with ethanol of appropriate concentration to fully dissolve, concentrated under reduced pressure, ethanol is recovered, vacuum dried, crushed, sieved and bagged.

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