Clear aqueous composition of dihydroartemisinin
By encapsulating dihydroartemisinin with fatty alcohol sulfate salts/fatty alcohol polyoxyethylene ether sulfate salts to form a transparent aqueous formulation, the solubility and stability issues in aqueous media are resolved, enabling its effective application in cosmetics.
Patent Information
- Application Number
- CN202410713460.2
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2024-06-03
- Publication Date
- 2025-12-05
AI Technical Summary
Dihydroartemisinin is poorly soluble in water and other aqueous media, and its molecule contains a special peroxide group, making it unstable to heat and easily decomposed by moisture, heat, and reducing substances, which limits its application in cosmetics.
Dihydroartemisinin is encapsulated with fatty alcohol sulfate salts/fatty alcohol polyoxyethylene ether sulfate salts to form a transparent aqueous formulation. An anionic surfactant is used to form micelles in water to solubilize and slowly release dihydroartemisinin.
This improves the solubility and stability of dihydroartemisinin in aqueous systems, ensures the composition maintains a transparent appearance under high and low temperature conditions, and has a sustained-release effect, thus expanding its application in cosmetics.
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Abstract
Description
TECHNICAL FIELD
[0001] The present application relates to the field of natural pharmaceutical chemistry and the field of cosmetics, in particular to a transparent aqueous emulsion composition of dihydroartemisinin encapsulated by fatty alcohol sulfate / fatty alcohol polyoxyethylene ether sulfate. BACKGROUND
[0002] Cosmetics that take into account both efficacy and safety are increasingly favored by consumers. Among the many effective raw materials, natural sources of effective raw materials have more advantages than a variety of traditional non-natural sources of effective active substances.
[0003] Dihydroartemisinin (DHA) is an extremely important derivative of artemisinin, which has higher bioavailability and easier metabolism than artemisinin, greatly improving its pharmaceutical value. According to research in the medical field, DHA has good effects in the aspects of anti-malaria, anti-tumor, anti-virus, anti-inflammatory, anti-other parasites, anti-fibrosis, antihypertensive, and immune regulation. Existing research has found that dihydroartemisinin not only has the above medical effects, but also has a good inhibitory effect on malassezia, and can be used as a natural source of safe and efficient anti-dandruff ingredient to replace traditional anti-dandruff agents.
[0004] Wei Qiang et al. in "Dihydroartemisinin improves mouse psoriasis-like skin inflammation by inhibiting the proliferation of keratinocytes and the production of pro-inflammatory factors", Chinese Journal of Immunology, 2020(5):543-548, found that dihydroartemisinin can improve the inflammatory response of mouse psoriasis-like skin induced by imiquimod, and its possible mechanism is to inhibit the excessive proliferation of keratinocytes and the cytokines secreted by them through the MAPK / NF-κB signaling pathway.
[0005] Chinese patent CN109939105A discloses the use of artemisinin and its derivatives in the preparation of drugs and cosmetics for improving the barrier function of the skin's stratum corneum and preventing and treating skin inflammation.
[0006] Chinese patent CN116019734A discloses the anti-dandruff application of dihydroartemisinin. The patent research found that dihydroartemisinin has a clear inhibition zone at a concentration of 5mM and 10mM, and the inhibition zone of 10mM is greater than the positive control OCT, indicating that dihydroartemisinin has a good inhibitory effect on malassezia.
[0007] However, DHA is poorly soluble in water and other aqueous media, and contains special peroxy groups in the molecule, which is not stable to heat, and is easily decomposed by moisture, heat and reducing substances. In order to improve the water solubility and stability of DHA and reduce its toxicity, the common method in the medical field at present is to encapsulate DHA into drug-loaded materials. For example, Chiara Righeschi et al. prepared two kinds of DHA-loaded liposomes with egg yolk lecithin and cholesterol, which can significantly reduce the toxicity of DHA to normal cells while improving the water solubility of DHA. Chen Fangwei et al. used hydroxypropyl-β-cyclodextrin (HP-β-CD) as a carrier to encapsulate DHA, and revealed the feasibility of encapsulation by molecular simulation. The results showed that HP-β-CD encapsulated DHA was not only feasible but also could significantly improve the water solubility of DHA. The above cases are all from the field of pharmacy, and there is no new report in the field of daily chemical industry. It is of great significance to expand the application field if DHA can be applied to cosmetic formulations and can stably exert its effect.
[0008] The present application surprisingly found that fatty alcohol sulfate / fatty alcohol polyoxyethylene ether sulfate can solubilize DHA, thereby greatly improving the solubility of DHA in aqueous system, and the combination of the two has a stable transparent appearance under high and low temperature and normal temperature conditions. Therefore, the present application provides a transparent aqueous DHA composition encapsulated by fatty alcohol sulfate / fatty alcohol polyoxyethylene ether sulfate. SUMMARY
[0009] In one aspect, the present application provides a transparent aqueous DHA composition, which comprises, based on the total weight of the composition:
[0010] 0.01-1% by weight of DHA;
[0011] 5-88% by weight of anionic surfactant selected from the group consisting of fatty alcohol sulfate, fatty alcohol polyoxyethylene ether sulfate, or a combination thereof; and
[0012] an aqueous carrier acceptable in personal care field.
[0013] In a preferred embodiment, the composition of the present application comprises 0.1-0.5% by weight of DHA.
[0014] In a preferred embodiment, the composition of the present application comprises 5-72% by weight of anionic surfactant, more preferably 7-30% by weight of anionic surfactant, and most preferably 7-28% by weight of anionic surfactant.
[0015] In a preferred embodiment, the anionic surfactant is selected from the group consisting of C 12-22 fatty alcohol sulfate, C 12-22fatty alcohol ether sulfate or a combination thereof. More preferably, the anionic surfactant is selected from the group consisting of sodium lauryl sulfate, sodium laureth sulfate or a combination thereof. Most preferably, the anionic surfactant is selected from the group consisting of sodium lauryl sulfate, sodium laureth sulfate or a combination thereof.
[0016] In another aspect, the present application also relates to a personal care product comprising the composition of the present application. In a preferred embodiment, the personal care product is selected from the group consisting of a shampoo, a body wash, a facial cleanser. BRIEF DESCRIPTION OF DRAWINGS
[0017] Figure 1 Stability photos of 4-week samples of Examples 1-5 are shown.
[0018] Figure 2 Stability photos of 4-week samples of Examples 7-11 are shown.
[0019] Figure 3 Stability comparison photos of 4-week samples of Example 6, Example 12 and Comparative Example 1 are shown. DETAILED DESCRIPTION
[0020] The present application provides a transparent aqueous composition. The composition is formed by a combination of fatty alcohol sulfate / fatty alcohol ether sulfate and dihydroartemisinin (DHA), and the composition has a stable colorless transparent appearance and can be used in efficacy-type daily-use products.
[0021] When the concentrations of sodium lauryl sulfate and sodium laureth sulfate in water are higher than their CMC values, stable transparent micellar particles are formed in the aqueous solution, which can encapsulate hydrophobic ingredients and have a solubilizing effect. Meanwhile, during the process of dilution, the concentration of the surfactants becomes lower and lower, and the micellar form changes. When the concentration is lower than the CMC value, the micelles open, and the encapsulated ingredients can be slowly released, thus, the surfactants also have a slow-release effect on the active ingredients.
[0022] The micelles formed by sodium lauryl sulfate and sodium laureth sulfate have the effects of encapsulation, solubilization and slow release, which not only increase the water solubility of DHA, but also improve the stability of DHA and reduce the cytotoxicity of DHA. Therefore, the composition of the present application greatly expands the application scenarios of DHA.
[0023] For the sake of providing a more concise description, some numerical recitations herein are not modified with the term "about." It should be understood that whether or not the term "about" is expressly used, every quantity given herein is intended to refer to the actual given value, and also to be approximated by a reasonable amount that is near to or close to the stated value, including values that are due to experimental and / or measurement conditions.
[0024] For the sake of providing a more concise description, some numerical recitations herein are recited as a range from about X amount to about Y amount. It should be understood that when a range is recited, the range is not limited to the recited upper and lower limits, but encompasses any amount there-between, or therefrom, including the recited amounts.
[0025] Dihydroartemisinin
[0026] Dihydroartemisinin (DHA) is an extremely important derivative of artemisinin, which has higher bioavailability and easier metabolism compared to artemisinin. According to research in the medical field, DHA has good effects in anti-malaria, anti-tumor, anti-virus, anti-inflammatory, anti-other parasites, anti-fibrosis, antihypertensive, and immune regulation, etc. Existing research has found that dihydroartemisinin not only has the above medical effects, but also has a good inhibitory effect on malassezia, and can be used as a natural source of safe and efficient anti-dandruff ingredient to replace traditional anti-dandruff agents.
[0027] In some embodiments, the composition of the present application comprises 0.01-1% by weight of dihydroartemisinin. In preferred embodiments, the composition of the present application comprises 0.01-0.6% by weight of dihydroartemisinin. In more preferred embodiments, the composition of the present application comprises 0.1-0.5% by weight of dihydroartemisinin.
[0028] Anionic surfactant
[0029] Fatty alcohol sulfates and fatty alcohol polyoxyethylene ether sulfates are low-cost anionic surfactants with excellent detergency, emulsification, foaming properties, and easy thickening, and are widely used in daily chemical, textile, papermaking, leather, machinery, oil exploitation, etc. When the concentration of fatty alcohol sulfates and fatty alcohol polyoxyethylene ether sulfates in water is higher than the CMC value, stable and transparent micellar particles are formed in the aqueous solution, which can encapsulate hydrophobic ingredients and have a solubilizing effect. At the same time, in the process of cleaning and dilution, the concentration of surfactants becomes lower and lower, and the micellar form changes. When the concentration is lower than the CMC value, the micelles open, and the encapsulated ingredients can be slowly released, so it also has a slow-release effect on active ingredients.
[0030] The present application finds that fatty alcohol sulfate / fatty alcohol polyoxyethylene ether sulfate can solubilize DHA, thereby greatly improving its solubility in aqueous system, and the combination of the two has a stable transparent appearance under high and low temperature and normal temperature conditions, indicating that DHA is wrapped by the micelles of fatty alcohol sulfate / fatty alcohol polyoxyethylene ether sulfate, and the stability is improved. The composition has a good inhibitory effect on Malassezia, and can be used in anti-dandruff products to replace traditional anti-dandruff agents.
[0031] In some embodiments, the fatty alcohol sulfate salt employed in the composition of the present application is C 12-22 fatty alcohol sulfate salt. In preferred embodiments, the fatty alcohol sulfate salt employed in the composition of the present application is C 12-20 fatty alcohol sulfate salt, preferably C 12-18 fatty alcohol sulfate salt, preferably C 12-16 fatty alcohol sulfate salt. In specific embodiments, the fatty alcohol sulfate salt employed in the composition of the present application is sodium lauryl sulfate. In specific embodiments, the present application employs sodium lauryl sulfate available from Jiangsu Youyang Pharmaceutical Co., Ltd. under the trade name sodium dodecyl sulfate.
[0032] In some embodiments, the fatty alcohol polyoxyethylene ether sulfate salt employed in the composition of the present application is C 12-22 fatty alcohol polyoxyethylene ether sulfate salt. In preferred embodiments, the fatty alcohol polyoxyethylene ether sulfate salt employed in the composition of the present application is C 12-20 fatty alcohol polyoxyethylene ether sulfate salt, preferably C 12-18 fatty alcohol polyoxyethylene ether sulfate salt, preferably C 12-16 fatty alcohol polyoxyethylene ether sulfate salt. In specific embodiments, the fatty alcohol polyoxyethylene ether sulfate salt employed in the composition of the present application is sodium lauryl polyoxyethylene ether sulfate. In specific embodiments, the present application employs sodium lauryl polyoxyethylene ether sulfate available from BASF (China) Co., Ltd. under the trade name N 70.
[0033] In some embodiments, the composition of the present application comprises 5-88% by weight of anionic surfactant. In preferred embodiments, the composition of the present application comprises 7-72% by weight of anionic surfactant, more preferably 7-30% by weight, more preferably 7-28% by weight of anionic surfactant. In a specific embodiment, the composition of the present application comprises 15% by weight of anionic surfactant.
[0034] In some embodiments, the composition of the present application comprises 5-88 wt.% of fatty alcohol sulfate salt. In preferred embodiments, the composition of the present application comprises 7-30 wt.% of fatty alcohol sulfate salt. In most preferred embodiments, the composition of the present application comprises 15 wt.% of fatty alcohol sulfate salt.
[0035] In some embodiments, the composition of the present application comprises 5-72 wt.% of fatty alcohol polyoxyethylene ether sulfate salt. In preferred embodiments, the composition of the present application comprises 7-28 wt.% of fatty alcohol polyoxyethylene ether sulfate salt. In most preferred embodiments, the composition of the present application comprises 15 wt.% of fatty alcohol polyoxyethylene ether sulfate salt.
[0036] Aqueous dosage form composition
[0037] The present application provides a multifunctional transparent aqueous composition which greatly improves the solubility and stability of DHA in aqueous system, and can be applied in efficacy type daily chemical products. The present technology can greatly expand the application of natural active ingredient-dihydroartemisinin in other fields.
[0038] In addition to the above components, the composition of the present application also contains a balance of water. Therefore, the composition of the present application can also contain water or other aqueous carriers.
[0039] In preferred embodiments, the composition of the present application has a water content of at least 50 wt.%. For example, the composition of the present application has a water content of greater than 50 wt.%, greater than 55 wt.%, greater than 60 wt.%, greater than 65 wt.%, greater than 70 wt.%, greater than 75 wt.%, or greater than 80 wt.%. In some embodiments, the composition of the present application has a water content of 50-95 wt.%, preferably 60-90 wt.%, 60-88 wt.%, 65-88 wt.%, 70-88 wt.%, or 75-88 wt.%.
[0040] Personal care product
[0041] The present application also relates to personal care products which can comprise the composition of the present application. In some specific embodiments, such personal care products can be in the form of facial cleanser, body wash, shampoo, etc. In preferred embodiments, the personal care product is a shampoo product.
[0042] The product can be applied to the skin or hair of a user in any desired manner. In some aspects, the product can be applied directly by hand, or a device such as a towel, sponge, or other apparatus can be used to apply the product. The composition is advantageously applied to wetted hair or skin to facilitate application. The composition can be left on the area of application for a desired level of time, such as from about 5 seconds to about 5 minutes, and then washed off with water to remove from the area of application.
[0043] EMBODIMENT
[0044] The application will be further described in conjunction with specific examples. It is necessary to point out here that the examples are only used to further illustrate the application and cannot be understood as limiting the scope of protection of the application. Those skilled in the art can make some non-essential improvements and adjustments according to the content of the application described above. The test methods in the following examples are not specified, which are generally in accordance with the conventional conditions or in accordance with the conditions recommended by the manufacturers. Unless otherwise specified, all percentages and parts are by weight.
[0045] The experimental materials used in the embodiments of the application are as follows:
[0046] Dihydroartemisinin, purity > 90%, provided by Institute of Chinese Medicine, Chinese Academy of Chinese Medical Sciences;
[0047] Sodium lauryl sulfate, trade name sodium dodecyl sulfate, active content 100%, purchased from Jiangsu Youyang Pharmaceutical Co., Ltd.;
[0048] Sodium lauryl ether sulfate, trade name N 70, active content 70%, purchased from BASF (China) Co., Ltd.;
[0049] Disodium lauryl ether sulfosuccinate, trade name Ucefactant MES L30, active content 30%, purchased from Guangzhou Xingye Science and Technology Co., Ltd.
[0050] Example 1: Preparation of a transparent water type composition of dihydroartemisinin wrapped by fatty alcohol polyether sulfate salt
[0051] 21.43 parts by mass of sodium lauryl ether sulfate was weighed and added to a beaker containing 50 parts by mass of deionized water, and mixed and stirred at a speed of 200 rpm at room temperature until completely dissolved; 0.01 parts by mass of dihydroartemisinin was placed in the beaker, and mixed and stirred at 200 rpm until the dihydroartemisinin was completely dissolved, then deionized water was added to make up to 100 parts, and continued to be stirred at a speed of 200 rpm for 10 minutes until completely dispersed and uniform.
[0052] Example 2: Preparation of a transparent water type composition of dihydroartemisinin wrapped by fatty alcohol polyether sulfate salt
[0053] Take 21.43 parts by mass of sodium lauryl ether sulfate, add to a beaker containing 50 parts by mass of deionized water, mix and stir at room temperature at a speed of 200 rpm until completely dissolved; take 0.05 parts by mass of dihydroartemisinin and place it in the beaker, mix and stir at 200 rpm until dihydroartemisinin is completely dissolved, then make up to 100 parts with deionized water, continue to stir at a speed of 200 rpm for 10 minutes until completely dispersed and uniform.
[0054] Example 3: Preparation of a transparent aqueous formulation composition of dihydroartemisinin wrapped by a fatty alcohol polyether sulfate salt
[0055] Take 21.43 parts by mass of sodium lauryl ether sulfate, add to a beaker containing 50 parts by mass of deionized water, mix and stir at room temperature at a speed of 200 rpm until completely dissolved; take 0.1 parts by mass of dihydroartemisinin and place it in the beaker, mix and stir at 200 rpm until dihydroartemisinin is completely dissolved, then make up to 100 parts with deionized water, continue to stir at a speed of 200 rpm for 10 minutes until completely dispersed and uniform.
[0056] Example 4: Preparation of a transparent aqueous formulation composition of dihydroartemisinin wrapped by a fatty alcohol polyether sulfate salt
[0057] Take 21.43 parts by mass of sodium lauryl ether sulfate, add to a beaker containing 50 parts by mass of deionized water, mix and stir at room temperature at a speed of 200 rpm until completely dissolved; take 0.4 parts by mass of dihydroartemisinin and place it in the beaker, mix and stir at 200 rpm until dihydroartemisinin is completely dissolved, then make up to 100 parts with deionized water, continue to stir at a speed of 200 rpm for 10 minutes until completely dispersed and uniform.
[0058] Example 5: Preparation of a transparent aqueous formulation composition of dihydroartemisinin wrapped by a fatty alcohol polyether sulfate salt
[0059] Take 21.43 parts by mass of sodium lauryl ether sulfate, add to a beaker containing 50 parts by mass of deionized water, mix and stir at room temperature at a speed of 200 rpm until completely dissolved; take 0.6 parts by mass of dihydroartemisinin and place it in the beaker, mix and stir at 200 rpm until dihydroartemisinin is completely dissolved, then make up to 100 parts with deionized water, continue to stir at a speed of 200 rpm for 10 minutes until completely dispersed and uniform.
[0060] Example 6: Preparation of a transparent aqueous formulation composition of dihydroartemisinin wrapped by a fatty alcohol polyether sulfate salt
[0061] Take 21.43 parts by mass of sodium lauryl ether sulfate, add to a beaker containing 50 parts by mass of deionized water, mix and stir at room temperature at a speed of 200 rpm until completely dissolved; take 0.5 parts by mass of dihydroartemisinin and place it in a beaker, mix and stir at 200 rpm until dihydroartemisinin is completely dissolved, then make up to 100 parts with deionized water, continue to stir at a stirring speed of 200 rpm for 10 minutes until completely dispersed and uniform.
[0062] Test Example 1: Stability Test
[0063] The appearance of Test Examples 1-6 was observed for stability.
[0064] The stability evaluation method is as follows: the transparent composition prepared in Examples 1-5 was placed in an incubator at high temperature (40°C), low temperature (4°C), and room temperature (25°C) for 30 days. The samples were observed every week for the presence of solid particles, jellification, layering, color change, etc. If the sample showed no change before and after a certain time within 30 days, it was considered to have "passed"; the presence of solid particles was considered to have "precipitated"; the presence of a viscous gel that was not easy to flow was considered to have "jellified"; the presence of two layers of liquid was considered to have "layered"; and the presence of a color change was considered to have "changed color". The results are shown in the following table.
[0065] Table 1: Stability of different prepared compositions
[0066]
[0067]
[0068] As can be seen from Table 1, when the amount of dihydroartemisinin added is between 0.01 and 0.6 parts, it can be completely dissolved in an aqueous solution containing 21.43 parts of sodium lauryl ether sulfate to form a colorless transparent aqueous liquid with no viscosity, and the formed composition can maintain a stable colorless transparent appearance at high temperature (40°C), low temperature (4°C), and room temperature (25°C) for 1-4 weeks.
[0069] Example 7: Preparation of a transparent aqueous composition of dihydroartemisinin encapsulated by a fatty alcohol sulfate salt
[0070] Take 15 parts by mass of sodium lauryl ether sulfate, add to a beaker containing 50 parts by mass of deionized water, mix and stir at room temperature at a speed of 200 rpm until completely dissolved; take 0.01 parts by mass of dihydroartemisinin and place it in a beaker, mix and stir at 200 rpm until dihydroartemisinin is completely dissolved, then make up to 100 parts with deionized water, continue to stir at a stirring speed of 200 rpm for 10 minutes until completely dispersed and uniform.
[0071] Example 8: Preparation of a transparent aqueous formulation of dihydroartemisinin encapsulated by fatty alcohol sulfate
[0072] Take 15 parts by mass of sodium dodecyl sulfate, add to a beaker containing 50 parts by mass of deionized water, mix and stir at room temperature at a speed of 200 rpm until completely dissolved; take 0.1 parts by mass of dihydroartemisinin, place in the beaker, mix and stir at 200 rpm until the dihydroartemisinin is completely dissolved, then make up to 100 parts with deionized water, continue to stir at a speed of 200 rpm for 10 minutes until completely dispersed and uniform.
[0073] Example 9: Preparation of a transparent aqueous formulation of dihydroartemisinin encapsulated by fatty alcohol sulfate
[0074] Take 15 parts by mass of sodium dodecyl sulfate, add to a beaker containing 50 parts by mass of deionized water, mix and stir at room temperature at a speed of 200 rpm until completely dissolved; take 0.2 parts by mass of dihydroartemisinin, place in the beaker, mix and stir at 200 rpm until the dihydroartemisinin is completely dissolved, then make up to 100 parts with deionized water, continue to stir at a speed of 200 rpm for 10 minutes until completely dispersed and uniform.
[0075] Example 10: Preparation of a transparent aqueous formulation of dihydroartemisinin encapsulated by fatty alcohol sulfate
[0076] Take 15 parts by mass of sodium dodecyl sulfate, add to a beaker containing 50 parts by mass of deionized water, mix and stir at room temperature at a speed of 200 rpm until completely dissolved; take 0.3 parts by mass of dihydroartemisinin, place in the beaker, mix and stir at 200 rpm until the dihydroartemisinin is completely dissolved, then make up to 100 parts with deionized water, continue to stir at a speed of 200 rpm for 10 minutes until completely dispersed and uniform.
[0077] Example 11: Preparation of a transparent aqueous formulation of dihydroartemisinin encapsulated by fatty alcohol sulfate
[0078] Take 15 parts by mass of sodium dodecyl sulfate, add to a beaker containing 50 parts by mass of deionized water, mix and stir at room temperature at a speed of 200 rpm until completely dissolved; take 0.6 parts by mass of dihydroartemisinin, place in the beaker, mix and stir at 200 rpm until the dihydroartemisinin is completely dissolved, then make up to 100 parts with deionized water, continue to stir at a speed of 200 rpm for 10 minutes until completely dispersed and uniform.
[0079] Example 12: Preparation of a transparent aqueous formulation of dihydroartemisinin encapsulated by fatty alcohol sulfate
[0080] Take 15 parts by mass of sodium dodecyl sulfate, add to a beaker containing 50 parts by mass of deionized water, mix and stir at room temperature at a rotation speed of 200 rpm until completely dissolved; take 0.5 parts by mass of dihydroartemisinin and place it in the beaker, mix and stir at 200 rpm until the dihydroartemisinin is completely dissolved, then make up to 100 parts with deionized water, continue to stir at a stirring speed of 200 rpm for 10 minutes until completely dispersed and uniform.
[0081] Test Example 2: Stability Test
[0082] The appearance of Test Examples 7-12 was observed, and their stability was investigated.
[0083] The stability evaluation method is as follows: the transparent composition prepared in Examples 7-12 was placed in an incubator at high temperature (40°C), low temperature (4°C), and room temperature (25°C) for 30 days. The samples were observed every week for the presence of solid particles, jellification, delamination, color change, and the like. If the sample showed no change before and after a certain time within 30 days, it was considered to have "passed"; the presence of solid particles was considered to have "precipitated"; the presence of a viscous gel that was not easy to flow was considered to have "jellified"; the presence of two layers of liquid was considered to have "delaminated"; and the presence of a color change was considered to have "changed color". The results are shown in the following table.
[0084] Table 2: Stability Investigation of Different Prepared Compositions
[0085]
[0086] As shown in Table 2, when the amount of dihydroartemisinin added is between 0.01 and 0.6 parts, it can be completely dissolved in an aqueous solution containing 15 parts of sodium dodecyl sulfate to form a colorless, transparent, and non-viscous aqueous formulation liquid, and the composition of the two can maintain a stable colorless transparent appearance at high and low temperatures and room temperature for 1-4 weeks.
[0087] Comparative Example 1: Preparation of a Sodium Lauryl Ether Sulfosuccinate Disodium and Dihydroartemisinin Composition
[0088] Take 50 parts by mass of sodium lauryl ether sulfosuccinate disodium and place it in a beaker, slowly add 0.5 parts by mass of dihydroartemisinin at a stirring speed of 200 rpm, mix and stir until the dihydroartemisinin is completely dissolved, then make up to 100 parts with deionized water, continue to stir at a stirring speed of 200 rpm for 10 minutes until completely dispersed and uniform.
[0089] Test Example 3: Stability Test
[0090] The appearance of Comparative Example 1 was observed, and its stability was investigated.
[0091] The stability evaluation method is as follows: the transparent composition prepared in Comparative Example 1 is placed in a constant temperature oven at high temperature (40°C), low temperature (4°C), and room temperature (25°C), and observed for 30 days to observe whether solid particles are precipitated, whether the sample is jellied, whether it is layered, whether it is discolored, and the like. If the sample is normal with no change before and after a certain time within 30 days, it is indicated as "pass", the appearance of solid particles is indicated as "precipitation", the appearance of a viscous gel that is not easy to flow is indicated as "jelly", the appearance of two layers of liquid is indicated as "layering", and the appearance of color change is indicated as "discoloration". The results are shown in the following table.
[0092] Table 3: Stability evaluation of the composition prepared in Comparative Example 1
[0093]
[0094] As can be seen from the results of Comparative Example 1, the composition of 50% lauryl alcohol polyether sulfosuccinate disodium and 0.5% dihydroartemisinin appears yellowing at room temperature (25°C) and high temperature (40°C), and the higher the temperature, the more obvious the discoloration. Although Comparative Example 1, Example 6, and Example 12 are all anionic surfactants, and the effective content of the anionic surfactants is 15%, and the dihydroartemisinin is 0.5%, the lauryl alcohol polyether sulfosuccinate disodium and dihydroartemisinin of Comparative Example 1 cannot form a composition with stable appearance, while the lauryl alcohol polyether sulfates and lauryl alcohol sulfates in the examples can.
Claims
1. A clear aqueous lotion composition comprising, based on total weight of the composition: 0.01-1 wt.% of dihydroartemisinin; 5-88 wt.% of an anionic surfactant selected from the group consisting of a fatty alcohol sulfate, a fatty alcohol polyoxethylene ether sulfate, or a combination thereof; and an aqueous carrier acceptable for personal care.
2. The composition of claim 1, wherein The composition comprises 0.1-0.5 wt.% of dihydroartemisinin.
3. The composition of claim 1, wherein The composition comprises 5-72 wt.% of an anionic surfactant.
4. The composition of claim 3, wherein The composition comprises 7-30 wt.% of an anionic surfactant.
5. The composition of claim 4, wherein The composition comprises 7-28 wt.% of an anionic surfactant.
6. The composition of claim 1, wherein The anionic surfactant is selected from the group consisting of: C 12-22 fatty alcohol sulfate, C 12-22 fatty alcohol polyoxyethylene ether sulfate, or combinations thereof.
7. The composition of claim 6, wherein The anionic surfactant is selected from the group consisting of sodium lauryl sulfate, sodium lauryl polyoxethylene ether sulfate, or a combination thereof.
8. The composition of claim 7, wherein The anionic surfactant is selected from the group consisting of sodium lauryl sulfate, sodium lauryl polyoxethylene ether sulfate, or a combination thereof.
9. A personal care product comprising the composition of any one of claims 1-8.
10. The personal care product of claim 9, which is a shampoo product, a body wash, or a facial cleanser.
Citation Information
Patent Citations
Application of artemisinin and derivatives thereof
CN109939105A
Anti-dandruff application of dihydroartemisinin
CN116019734A
