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📢 | 100% plant-derived beauty ingredients are blended according to skin problems! "Botanical Care Oil BC / AZ" (2 types in total) "is ...


Contains 100% plant-derived beauty ingredients for different skin problems! "Botanical Care Oil BC / AZ" (2 types in total) "is ...

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Contains plant-derived vitamin C derivatives that are non-greasy and lightly penetrate into the skin * 1.

RBG Co., Ltd. (Location: East ...), which develops a completely additive-free skin care brand "Sapmire" with 100% natural ingredients. → Continue reading


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    Vitamin C derivative

    Vitamin C derivativeWhat is (Vitamin C Derivatives)?Vitamin CImproved (L-ascorbic acid)Derivative. AlsoProvitamin CIt is,Living bodyAt the inner酵素What becomes vitamin C (L-ascorbic acid) by reaction[1]..Vitamin C is strongAntioxidantIt works but is unstable and its molecular structure is fragile.Therefore, vitamin C derivatives are stabilized as substances (hard to decompose), and have improved absorption into the skin and side effects of dry skin. In the 1940sFood additiveIn the 1960s, it was used for beauty purposes.PigmentationSuppression[2], Used for acne, etc.in JapanQuasi-drugWhitening Active Ingredients Approved as Contains Multiple Vitamin C Derivatives[3].Iontophoresis,[4],Chemical peelingWill be applied later[5].


    Vitamin CL-ascorbic acidIs an unstable molecule that dissolves well in waterStratum corneumIs said to have insufficient penetration into the skin because it repels water[6]..Ascorbic acid (vitamin C) needs to be pH 3.5 or less[7]..It is highly acidic (irritating to the skin).

    ProvitaminIs a substance that is converted to vitamins in the body. In this case, if it is converted to vitamin C, it is provitamin C, but whether or not it can be converted depends on the experimental conditions and animal species, so it should be judged accurately. There is also a difficult side[1].

    Vitamin C derivatives were studied as fat-soluble ones in the 1940s as food antioxidants.[2]..Provitamin C began to be used in the 1960s, and in cosmetics, whitening cosmetics were launched in Japan in 1962, giving consumers the impression that they are whitening ingredients.[1].. In 1961, an Italian researcher synthesized water-soluble magnesium ascorbic acid phosphate for external use.scurvyEffective against (vitamin C deficiency)[2]..In Japan, in 1967, instead of taking vitamin C internally, it was applied externally.Pigmentation,Melasma(Stain),Sparrow egg spotThe possibility of treating (freckles) was reported[8]..Vitamin C sulfate was extracted in 1969 and was first used in marine feed in Europe and the United States. It was also used in cosmetics in the 1980s, but it was rarely used in the 1990s.[2].

    In the 1990s, sodium ascorbic acid phosphate, 2-glucoside ascorbic acid (AA-2G), oily ascorbyl tetrahexyldecanoate (VC-IP), and glycerin-based derivatives appeared.[1]..Vitamin C, magnesium ascorbic acid phosphate, and sodium ascorbic acid phosphate tend to dry the skin, so VC-IP and APPS with palmitic acid and GOVC with glycerin have appeared.[9].

    Types of Vitamin C Derivatives

    Water soluble

    • Vitamin C Phosphate (AP)[Source of name 1]
      Hiroshi Ikeno, who has used vitamin C (AP) for treatment, refers to sodium phosphate-L-ascorbic acid and magnesium phosphate-L-ascorbic acid.[Source of name 1], May be used with Vitamin C (AP) Phosphate, mainly pointing towards sodium[10].
    These ascorbyl phosphates (ascorbyl-2-phosphate) are stable as substances up to pH 4.2, which is higher than pKa7 where ascorbic acid is stable, but the substance itself is not an antioxidant and is probably raw. In the bodyAlkaline phosphataseConverted to ascorbic acid by[11]..While the stability as a substance is improved, the electrification density is increased and the permeability through the skin is insufficient.[11].
    Magnesium ascorbic acid phosphate was synthesized in 1961, and since then sodium ascorbic acid phosphate, which is less likely to precipitate and crystallize and is easier to dissolve, has appeared and is widely used.[2].
    Ascorbic acid 2-glucoside (AA-2G) is stable to light and heat but acts as vitamin C by metabolismProvitaminAnd in JapanQuasi-drug OfWhiteningActive ingredient,Food additiveAuthorized as[12].
    Long-lasting conversion to vitamin C compared to other derivatives[2].
    Contact dermatitisMultipleCase reportThere is[14][15][16][13].

    Fat soluble

    Tetrahexyldecanoic acid is the display name and is also called isoparmitic acid.[17].. VC-IP is an oily liquid[2]..VC-IP came to be used for the next material instability of ascorbyl palmitate[17].
    Used in cosmetics and food additives[17].. AA-Pal does not protect ascorbic acid from oxidative degradation and is less stable as a substance than other forms[11]..It is thought that it is easy to penetrate through the skin due to the addition of fat-soluble groups, but some studies show that this is not the case.[11].
    Used in cosmetology dermatology in Europe and America[17], Widely used in body care products, etc., but in Japan, the amount used is small because it causes discoloration due to the problem of stability as a substance.[2].


    It has both water-soluble and oil-soluble properties.

    MoisturizingGlycerinAnd bactericidalOctanolAre combined[18].


    Quasi-drugWhitening active ingredient approved for whitening efficacy[3]

    Vitamin C ethyl, ascorbic acid glucoside
    Sodium ascorbyl phosphate, magnesium ascorbyl phosphate

    Compatibility with iontophoresis

    Vitamin C, SAP and APPS are negatively ionizedIontophoresisIt can be performed[2].. Since MAP has a strong ionic bond of magnesium, part of it is ionized in an acidic solution, but it is thought that part of MAP is ionized because the skin is weakly acidic.[2]..It has been reported that a moisturizer is required by prescribing up to 2% for normal skin and 1% for dry skin because the dryness of the skin increases as the absorption of vitamin C and MAP increases.[17].. GO-VC is nonionic but can also introduce ions[18].

    VC-IP is not suitable for iontophoresis[18].


    The Japanese Dermatological Association's 2017 acne treatment guidelines state that VC-IP and MAP are options but not covered by insurance.[19].

    Acne vulgaris(Acne) with 50 peopleRandomized controlled trial At (RCT), a 5% concentration of SAP lotion was more effective than placebo after 3 months and had the same frequency of side effects as placebo.[20].. SAP's topical drug suppresses sebum oxidation by ultraviolet A waves (UVA) in a 20-person study, and in an RCT of 5 people who applied a 1% lotion twice daily, acne occurred after 2 months. Found to be preventive and curative[21].. On RCTs, a milky lotion containing aqueous SAP and oily ascorbyl palmitate reduced sebum secretion after 3 months compared to a placebo-treated face half.[22]..RCTs of 45 acne patients (10-50 grade II to III lesions) with 5% SAP and 0.2%RetinolThe number of lesions was reduced by about 1-20% in 22 month and about 2% in 49 months, and by about 1% in 30 month and about 2% in 63 months, respectively. Was letting[23]..Excessive use of retinol promoted inflammation and sunburn, and SAP had less of this skin irritation.[23].

    Senile pigment spots(Nikko Kuroko, Senile Kuroko) with 27 peopleDouble blindIn this study, the 6% SAP-containing lotion significantly improved Nikko Kuroko over six months later than the SAP-free lotion, but to a lesser extent.[24].. After SAPTranexamic acidTheIontophoresisThe concentration of SAP in the skin then drops significantly, but in the reverse order it has no effect.[4].

    Melasma(Stain) with trichloroacetic acidChemical peelingAdding MAP was more effective than alone[5].. MAP-filled toothpaste reduced gingival inflammation in people with periodontitis in RCTs of 300 people[25].

    Image analysis was performed by RCT with 11 people, and one month after applying a lotion containing APPS at a concentration of 1% in the morning and evening,Hair follicleThe improvement of open "pores" reduced visible pores by 21.6% and darkened pores by 28.5%, a difference that was statistically significant compared to lotions without APPS, even with open pores. There was a similar downward trend, but the difference was not significant, and it was thought that the cause was a short period.[26]..In accordance with the anti-wrinkle product guidelines, 21 people used 1% APPS, and after 8 weeks without application on the half face, fine wrinkles and increased keratin moisture content due to drying were observed at the application site.[27].

    Tetrahexyldecyl Ascorbate[Source of name 11]And a cream containing both vitamin C (ascorbic acid)Light damagebyWrinkleIs improving[28].

    As a result of irradiating cultured human skin with a high-concentration sodium ascorbate aqueous solution (100,500 mM) dropped on the surface with UVB ultraviolet rays, the cell survival rate was improved and the stress against ultraviolet rays was reduced.The study also revealed the amount of sodium ascorbate permeated into the cell layer.[29]Also in this studyIt is more effective to take and apply vitamin C before exposure to UV rays.It was revealed that.[30][31]

    注 釈

    1. ^ a b Hiroshi Ikeno, "Skin Care and Vitamin Treatment for Sensitive Skin (Special Feature: Beauty by Dermatologists and Its Current Situation)," Fragrance Journal, Vol. 30, No. 2, February 2002, pp. 2-18. “Vitamin C Phosphate (AP) is, to be exact, Na Phosphate-L-Ascorbate or Mg Phosphate-L-Ascorbate”
    2. ^ a b Stamford 2012: "Ascorbyl 2-phosphates, usually formulated as their sodium (SAP) and magnesium (MAP) salts ... Sodium ascorbyl phosphate (SAP) ... Magnesium ascorbyl phosphate (MAP)" There are several articles that are described as magnesium acetate papers, and sodium is also matched to this.
    3. ^ Stamford 2012: "ascorbyl 2-glucoside (AA-2G) ... Ascorbyl glucoside (AA-2G)" In Japanese papers, "ascorbic acid 2-glucoside", "ascorbic acid 2 glucoside", "AA-2G", etc.
    4. ^ Ascorbyl ethyl Cosmetic-info.jp "Display name Ascorbic Acid ... Revised display name 3-O-Ethyl Ascorbic Acid ... INCI 3-O-Ethyl Ascorbic Acid (former name) ETHYL ASCORBIC ACID"
    5. ^ Stamford 2012: "3-O-ethyl ascorbic acid (EAC)"
    6. ^ Samurai Misono, Shunsuke Yamaguchi, Satoru Hashimoto "Improvement of Damaged Hair Using Oil-Soluble Vitamin C (Ascorbyl Tetrahexyl Decanoate)", Journal of Japan Cosmetic Engineers, Vol. 52, No. 3, 2018, pp. 205-209, two:10.5107 / sccj.52.205.. "Ascorbyl tetrahexyl decanoate; VC-IP"
    7. ^ Stamford 2012: "tetra-isopalmitoyl ascorbate (VC-IP) ... Ascorbyl tetraisopalmitate (VC-IP)"
    8. ^ Stamford 2012: "ascorbyl 6-palmitate (AA-Pal) ... Ascorbyl palmitate (AA-PAL)"
    9. ^ Stamford 2012: "ascorbyl 2-phosphate 6-palmitate (APPS). ... Ascorbyl 2-phosphate 6-palmitate (APPS)"
    10. ^ Appreciation Showa Denko: "Ascorbyl palmitate 3Na / Trisodium Ascorbyl Palmitate Phosphate L-ascorbyl 2-phasphate 6-sodium palmitate / trisodium L-ascorbyl 3-phasphate 2-palmitate <chemical name>"
    11. ^ Tetrahexyl decyl ascorbic acid Cosmetic-Info.jp: "INCI Tetrahexyldecyl Ascorbate"


    1. ^ a b c d Shinobu Ito, "Hundred Flowers Campaign, The Age of Provitamin C," Fragrance Journal, Vol. 43, No. 9, September 2015, pp. 9-14.
    2. ^ a b c d e f g h i j k l Shinobu Ito, "Provitamin C (13) Whitening and Provitamin C: Vitamin C Derivatives and Hyperpigmentation Suppression," Fragrance Journal, Vol. 40, No. 11, November 2012, pp. 11-66.
    3. ^ a b Ando H, Matsui MS, Ichihashi M. (2010-6). “Quasi-drugs developed in Japan for the prevention or treatment of hyperpigmentary disorders”. International journal of molecular sciences 11 (6): 2566–2575. two:10.3390 / ijms11062566. PMID 20640168. https://www.ncbi.nlm.nih.gov/pmc/articles/pmid/20640168/. 
    4. ^ a b c Akiko Miyake, Tatsuya Okumura, Toru Okamoto, "Ordering Effects of Tranexamic Acid and Sodium Ascorbic Acid on Iontophoresis," Skin Science, Vol. 7, No. 4, 2008, pp. 421-427, two:10.11340 / skinresearch.7.4_421.
    5. ^ a b Murtaza F, Bangash AR, Khushdil A; et al (2016-7). “Efficacy of Trichloro-Acetic Acid Peel Alone Versus Combined Topical Magnesium Ascorbyl Phosphate for Epidermal Melasma”. Journal of the College of Physicians and Surgeons 26 (7): 557–561. PMID 27504543. 
    6. ^ Firas Al-Niaimi, Nicole Yi Zhen Chiang (2017-7). “Topical Vitamin C and the Skin: Mechanisms of Action and Clinical Applications”. The Journal of clinical and aesthetic dermatology 10 (7): 14–17. PMC 5605218. PMID 29104718. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5605218/. 
    7. ^ SR Pinnell, H. Yang, M. Omar; et al (2001-2). “Topical L-ascorbic acid: percutaneous absorption studies”. Dermatologic surgery: official publication for American Society for Dermatologic Surgery [et al.] 27 (2): 137–142. PMID 11207686. 
    8. ^ Masaru Takeuchi, Kazuo Aso, Kenji Kawase, Hiroshi Ichikawa "20. Vitamin C research in the field of dermatology: (VI) Transdermal absorption and clinical application of stable vitamin C ointment (summary of general research presentation)"Vitamin," Vol. 35, No. 6, 1967, p. 502, two:10.20632 / vso.35.6_502_2.
    9. ^ Shinobu Ito, "Effects of Provitamin C on Pore Abnormalities," Fragrance Journal, Vol. 45, No. 2, February 2017, pp. 2-39.
    10. ^ Hiroshi Ikeno, "Effects of Vitamin C Phosphate on Improvement of Abnormal Pore Keratosis," Fragrance Journal, Vol. 33, No. 9, September 2005, pp. 9-39. “L-ascorbyl-47-phosphate (APS)”
    11. ^ a b c d Stamford 2012.
    12. ^ a b Yamamoto "The journey from the invention of stable and long-lasting vitamin C to the launch of a university-launched venture and the birth of health functional foods"Journal of Pharmacology, Japan, Vol. 132, No. 3, March 2008, 9, pp. 1-160," two:10.1254 / fpj.132.160.
    13. ^ a b Yagami, Akiko; Suzuki, Kayoko; Morita, Yusuke; et al (2014). “Allergic contact dermatitis caused by 3-o-ethyl-l-ascorbic acid (vitamin C ethyl)”. Contact Dermatitis 70 (6): 376–377. two:10.1111 / cod.12161. PMID 24846587. 
    14. ^ Numata, Takafumi; Kobayashi, Yuko; Ito, Tomonobu; et al (2015). “Two cases of allergic contact dermatitis due to skin-whitening cosmetics”. Allergology International 64 (2): 194–195. two:10.1016 / j.alit.2014.10.007. PMID 25838099. https://doi.org/10.1016/j.alit.2014.10.007. 
    15. ^ Victoria-Martínez, Ana M .; Mercader-García, Pedro (2017). “Allergic Contact Dermatitis to 3-o-Ethyl-L-Ascorbic Acid in Skin-lightening Cosmetics”. Dermatitis 28 (1): 89. two:10.1097 / DER.0000000000000260. PMID 28002235. 
    16. ^ Mamodaly, Myriam; Dereure, Olivier; Raison-Peyron, Nadia (2019). “A new case of allergic contact dermatitis caused by 3-o-ethyl ascorbic acid in facial antiageing cosmetics”. Contact Dermatitis. two:10.1111 / cod.13307. PMID 31066077. 
    17. ^ a b c d e Shinobu Ito, "Provitamin C (4) Provitamin C and Acne," Fragrance Journal, Vol. 39, No. 5, May 2011, pp. 5-49.
    18. ^ a b c Ichiro Kurokawa, "Effects of New Vitamin C Derivatives on Acne," Fragrance Journal, Vol. 43, No. 9, September 2015, pp. 9-26.
    19. ^ Nobukazu Hayashi, Fukumi Furukawa, Minami Furumura and others "Acne Vulgaris Treatment Guidelines 2017"Journal of the Japanese Dermatological Association, Vol. 127, No. 6, 2017, pp. 1261-1302," two:10.14924 / dermatol.127.1261, NOT 130007040253.
    20. ^ Woolery-Lloyd, Heather; Baumann, Leslie; Ikeno, Hiroshi (2010). “Sodium L-ascorbyl-2-phosphate 5% lotion for the treatment of acne vulgaris: a randomized, double-blind, controlled trial”. Journal of Cosmetic Dermatology 9 (1): 22–27. two:10.1111 / j.1473-2165.2010.00480.x. PMID 20367669. 
    21. ^ Klock J, Ikeno H, Ohmori K; et al (June 2005). “Sodium ascorbyl phosphate shows in vitro and in vivo efficacy in the prevention and treatment of acne vulgaris”. Int J Cosmet Sci (3): 171–6. two:10.1111 / j.1467-2494.2005.00263.x. PMID 18492184. 
    22. ^ Khan, H .; Akhtar, N .; Ali, A. (2016). “Assessment of Combined Ascorbyl Palmitate (AP) and Sodium Ascorbyl Phosphate (SAP) on Facial Skin Sebum Control in Female Healthy Volunteers”. Drug Research 67 (1): 52–58. two:10.1055 / s-0042-118171. PMID 27756097. 
    23. ^ a b Ruamrak, C .; Lourith, N .; Natakankitkul, S. (2009). “Comparison of clinical efficacies of sodium ascorbyl phosphate, retinol and their combination in acne treatment”. International Journal of Cosmetic Science 31 (1): 41–46. two:10.1111 / j.1468-2494.2008.00479.x. PMID 19134126. 
    24. ^ Ishikawa, Yuko; Niwano, Takao; Hirano, Shinichi; et al (2019). “Whitening effect of l-ascorbate-2-phosphate trisodium salt on solar lentigos”. Archives of Dermatological Research 311 (3): 183–191. two:10.1007 / s00403-019-01892-2. PMID 30778667. 
    25. ^ Shimabukuro, Yoshio; Nakayama, Yohei; Ogata, Yorimasa; et al (2015). “Effects of an Ascorbic Acid–Derivative Dentifrice in Patients With Gingivitis: A Double-Masked, Randomized, Controlled Clinical Trial”. Journal of Periodontology 86 (1): 27–35. two:10.1902 / jop.2014.140138. PMID 25277459. 
    26. ^ INUI, Shigeki; ITAMI, Satoshi (2007). “Perifollicular pigmentation is the first target for topical vitamin C derivative ascorbyl 2-phosphate 6-palmitate (APPS): Randomized, single-blinded, placebo-controlled study”. The Journal of Dermatology 34 (3): 221–223. two:10.1111 / j.1346-8138.2007.00256.x. PMID 17291309. 
    27. ^ Eiko Kato, Risa Iguchi, Yuko Saeki "Water-soluble Vitamin C Derivatives with Lipophilicity: Ascorbyl Palmitate Phosphate (APPS)", Fragrance Journal, Vol. 43, No. 9, September 2015, pp. 9-51.
    28. ^ Richard E. Fitzpatrick, Elizabeth F. Rostan (2002-3). “Double-blind, half-face study comparing topical vitamin C and vehicle for rejuvenation of photodamage”. Dermatologic surgery: official publication for American Society for Dermatologic Surgery [et al.] 28 (3): 231–236. PMID 11896774. 
    29. ^ Kawashima, Saki; Funakoshi, Tomoko; Sato, Yasunori; Saito, Norikatsu; Ohsawa, Hajime; Kurita, Katsumi; Nagata, Kisaburo; Yoshida, Masayuki et al. (2018-11-01). “Protective effect of pre- and post-vitamin C treatments on UVB-irradiation-induced skin damage” (English). Scientific Reports 8 (1): 16199. two:10.1038 / s41598-018-34530-4. ISSN 2045-2322. https://www.nature.com/articles/s41598-018-34530-4. 
    30. ^ "Vitamin C application to the skin is effective before exposure to ultraviolet rays”. Incorporated Administrative Agency Tokyo Metropolitan Geriatric Health and Longevity Medical Center. 2021/6/28Browse.
    31. ^ "Examination of percutaneous absorption of ascorbic acid in human cultured epidermis and prevention and recovery effect against cell damage caused by ultraviolet UVB". 2021/6/28Browse.


    • Stamford, Nicholas PJ (2012). “Stability, transdermal penetration, and cutaneous effects of ascorbic acid and its derivatives”. Journal of Cosmetic Dermatology 11 (4): 310–317. two:10.1111 / jocd.12006. PMID 23174055. 

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