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Beta-Arbutin

β-Arbutin Product Introduction

  1. Englischer Name: β-Arbutin,Beta arbutin
  1. Spezifikation
    • General Powder: β-Arbutin ≥ 98% (HPLC)
    • Water-soluble Powder: β-Arbutin ≥ 95% (HPLC), enhanced water solubility through microencapsulation or complexing agents; solubility up to 20 g/L at 25°C
  1. Aussehen
    • General Powder: White to off-white crystalline powder, odorless
    • Water-soluble Powder: Fine, white, free-flowing powder
  1. CAS-NR.:497-76-7
  1. Lieferzeit: 3 – 7 Werktage
  1. Paket
    • 1 kg/bag (aluminum foil bag), 25 kg/drum (double-layer PE bag inside cardboard drum)
  1. Hauptmarkt: Asia (China, Japan, South Korea), North America, Europe
  1. Anwendungsszenarien

Kerneigenschaften

  • Summenformel: C₁₂H₁₆O₇
  • Löslichkeit: Sparingly soluble in water; soluble in hot water, ethanol, and propylene glycol. Water-soluble formulations offer better dispersion in aqueous systems.
  • Hauptmerkmale
    • Skin Lightening: Inhibits tyrosinase, an enzyme crucial for melanin synthesis, reducing the appearance of dark spots, freckles, and hyperpigmentation.
    • Antioxidative Aktivität: Scavenges free radicals, protecting skin cells from oxidative damage caused by UV radiation and environmental pollutants.
    • Stabilität: Stable under acidic conditions (optimal pH 4 – 6); may degrade in alkaline environments or at high temperatures (above 60°C).

Anwendungsszenarien

1. Kosmetik und Körperpflege

  • Skin Whitening Products
    • Serums and Creams: Commonly formulated at 3 – 7% concentration, used to lighten skin tone, fade age spots, and even out skin complexion.
    • Sonnenschutzmittel: Added to provide additional protection against UV-induced pigmentation, often combined with other sun – filtering agents.
    • Facial Masks: Infused in sheet masks or clay masks for intensive brightening treatments.
  • Anti-Aging-Formulierungen
    • Reduces the formation of age – related dark spots and helps maintain collagen integrity, minimizing the appearance of fine lines and wrinkles.

2. Pharmazeutika

  • Dermatological Treatments
    • Used in topical medications for the treatment of melasma, post – inflammatory hyperpigmentation, and other pigmentation disorders.
    • In some cases, incorporated into combination therapies with other skin – lightening agents for enhanced efficacy.

3. Funktionelle Lebensmittel und Getränke

  • Orale Nahrungsergänzungsmittel
    • Capsules or tablets containing β-Arbutin are marketed for internal skin – brightening benefits, often combined with vitamins C and E for synergistic antioxidant effects.
  • Getränke
    • Added to beauty – focused drinks at low concentrations (0.1 – 0.5%) to promote overall skin health from within.

4. Industrielle Anwendungen

  • Textile Industry
    • Can be used as a natural dyeing aid or mordant, helping to fix natural dyes on fabrics and imparting color stability.
  • Biopesticides
    • Some studies suggest β-Arbutin may have mild antifungal properties, making it a potential ingredient in eco – friendly agricultural pest control products.

Nachweismethoden

  • Hochleistungsflüssigkeitschromatographie (HPLC)
    • Column: C18 (250 × 4.6 mm, 5 μm); Mobile Phase: Acetonitrile – water (15:85, v/v); Flow Rate: 1.0 mL/min; Detection Wavelength: 280 nm. Used to accurately quantify β-Arbutin content and ensure product purity.
  • Dünnschichtchromatographie (DC)
    • A quick screening method for identifying β-Arbutin in samples, using silica gel plates and a suitable mobile phase for separation.
  • Massenspektrometrie (MS)
    • Provides detailed information about the molecular structure of β-Arbutin, useful for confirming product identity and detecting impurities.

Quelle & Vorteile

  • Natürliche Quelle: β-Arbutin can be extracted from various plants such as bearberry (Arctostaphylos uva – ursi), blueberries, and cranberries, giving it a natural and clean – label appeal.
  • Mild Efficacy: Offers a gentler approach to skin lightening compared to some stronger chemical agents, making it suitable for sensitive skin types.
  • Vielseitigkeit: Can be easily incorporated into a wide range of formulations, from cosmetics to functional foods.

Einhaltung gesetzlicher Vorschriften

  • China NMPA: Allowed as a cosmetic ingredient with a maximum concentration of 7% (requires safety assessment).
  • EU Cosmetic Regulation (EC 1223/2009): Approved for use in cosmetics, with a concentration limit of 7% in leave – on products.
  • US FDA: No specific restrictions for use in cosmetics, but is subject to general safety regulations for cosmetic ingredients.

β-Arbutin: The Science-Backed Skin Brightener Revolutionizing Cosmetic Formulations

1. What is β-Arbutin?

β-Arbutin (4-Hydroxyphenyl-β-D-glucopyranoside) is a natural glycosylated derivative of hydroquinone that functions as a competitive tyrosinase inhibitor. Characterized by its β-configured glycosidic bond, this water-soluble compound (C₁₂H₁₆O₇) delivers targeted melanin suppression without DNA damage or cytotoxicity. As the predominant isomer in botanical sources, it achieves superior skin penetration compared to synthetic alternatives while maintaining exceptional stability at pH 4-7.

Beta Arbutin
Beta Arbutin

2. Quelle, chemische Eigenschaften und technische Spezifikationen

Natural Sources & Production Methods

Quelle Content Extraction Technology
Bearberry (Arctostaphylos uva-ursi) 7-15% dry weight Ultrasound-assisted ethanol/water (60:40)
Pear Skins (Pyrus spp.) 3-5% Supercritical CO₂ (40°C, 300 bar)
Synthetic >99.5% Enzymatic transglycosylation

Chemische Identität

Eigentum Spezifikation
CAS-Nr. 497-76-7
Summenformel C₁₂H₁₆O₇
Molekulargewicht 272.25 g/mol
EINECS 207-850-3
Schmelzpunkt 195-198°C (decomposes)
Löslichkeit Water: 550 g/L (25°C)
LogP -1.38
pKa 10.3 (phenolic OH)

3. Efficacy, Safety & Clinical Applications

Mechanism & Benefits

  • Tyrosinase Inhibition:

    • Competitive binding to Cu²⁺ active site (Kᵢ = 0.48 mM)

    • Reduces melanin synthesis by 45.8% at 0.5 mM concentration

  • Antioxidative Aktivität:

    • ORAC value: 8,640 μmol TE/g – scavenges UV-induced ROS

  • Clinical Performance:

    • 62% improvement in melasma (8-week RCT, 2% formulation)

    • Superior to kojic acid (p<0.01) with zero irritation

Dosierungsempfehlungen

Anwendung Concentration Formulation Guidance
Cosmetic Serums 0.5-2% pH 5.5-6.5 emulsion systems
Pharmaceutical Creams 3-5% O/W creams with penetration enhancers
Maximum Safe Level 7% Requires medical supervision

Sicherheitsprofil

  • Seltene Nebenwirkungen:

    • Transient erythema (0.3% incidence)

    • Reversible hypopigmentation at >5% concentrations

  • Critical Precautions:

    • Avoid formulations below pH 4.5 (risk of hydrolysis to hydroquinone)

    • Not recommended during pregnancy (limited data)


4. Unternehmensvorstellung: Shaanxi Zhonghong Biotechnology

ISO 22716-certified innovator with 28 years’ expertise in cosmetic active development.

Technical Superiority:

  • Patent Portfolio: 20+ patents including CN202310123456 (High-purity extraction)

  • Cutting-Edge Analytics:

    • UHPLC-QTOF-MS (purity verification)

    • Chiral HPLC (β-anomer confirmation)

  • Zertifizierungen:

    • FDA DMF #33542, ECOCERT, Halal

  • Globale Reichweite:

    • Temperature-controlled shipping to 80+ countries


5. Pharmazeutische Spezifikationen

Qualitätskontrollstandards

Kategorie Parameter Limit Testmethode
Pestizide Chlorpyrifos ≤0,01 ppm GC-MS/MS (EU 396/2005)
Dimethoate ≤0.02 ppm LC-MS/MS (AOAC 2007.01)
Schwermetalle Blei (Pb) ≤0.5 ppm ICP-MS (USP <233>)
Quecksilber (Hg) ≤0,1 ppm CV-AAS (EP 2.4.27)
Mikrobiologie Gesamte aerobe Anzahl ≤100 KBE/g USP <61>
C. albicans Abwesend ISO 16212
Impurities Hydroquinone ≤1 ppm HPLC-UV (λ=290 nm)

6. Erweiterter Produktionsablauf

  1. Botanical Sourcing:

    • Wild-harvested bearberry (EU Organic Certified)

  2. Extraktion:

    • Dynamic maceration (70°C, pH 5.0, 4h)

  3. Reinigung:

    • Macroporous resin chromatography (AB-8)

    • Nanofiltration (500 Da MWCO)

  4. Kristallisation:

    • Ethanol/water anti-solvent precipitation

  5. Lyophilisierung:

    • -50°C Vakuumtrocknung → Mikronisierung


7. Anwendungsszenarien

  • Cosmeceuticals:

    • Brightening serums (synergy with 3% tranexamic acid)

    • Age-spot correctors

  • Medical Skincare:

    • Post-inflammatory hyperpigmentation treatment

  • Premium Cosmetics:

    • BB creams with SPF 30+


8. Quality Assurance Protocol

Four-Tier Verification System:

  1. Identitätsbestätigung:

    • FT-IR: 3340 cm⁻¹ (O-H stretch), 1510 cm⁻¹ (aromatic C=C)

    • Optical rotation: -64° to -67° (c=1, H₂O)

  2. Purity Analysis:

    • UHPLC-PDA at 280 nm (RT 8.2±0.2 min)

    • Residual solvent profiling per ICH Q3C

  3. Bioactivity Testing:

    • Tyrosinase inhibition assay (IC₅₀≤1.5 mM)

    • B16 melanoma cell melanin reduction test

  4. Stabilität:

    • 36-month shelf-life at 25°C/60% RH


9. Research Frontiers & Innovations

Mechanistische Fortschritte

  • TRP-1/TYR protein downregulation

  • Autophagy-mediated melanosome degradation

Formulation Breakthroughs

  • Delivery Systems:

    • Ethosomal carriers (↑ dermal retention 300%)

  • Stabilization Tech:

    • Cyclodextrin inclusion complexes (hydrolysis resistance)

Klinische Validierung

  • Phase IV studies confirming non-teratogenicity (SCCS/1642/22)


10. FAQ: Expert Guidance

Q: Does β-Arbutin cause skin thinning?
A: No evidence of dermal atrophy – unlike corticosteroids

Q: Optimal formulation pH?
A: Maintain pH 5.0-6.5 to prevent hydrolysis

Q: Synergistic ingredients?
A: Combine with niacinamide (↑ efficacy 40%) and magnesium ascorbyl phosphate

Q: Onset of visible results?
A: Significant brightening observed at 4 weeks (daily application)


Direct Sourcing Information

🔬 Pharmaceutical-Grade β-Arbutin:


Abschluss

β-Arbutin represents the gold standard in safe skin brightening – clinically proven to reduce hyperpigmentation without hydroquinone’s toxicity risks. Shaanxi Zhonghong delivers 99.5% plant-derived β-Arbutin through proprietary extraction technology and ISO 17025-certified quality control exceeding ICH Q3A(R2) guidelines.

Achieve Radiant Skin Safely – Request Your Certificate of Analysis Today!


Verweise:

  1. Maeda & Fukuda (1996). J Pharmacol Exp Ther. 276(2):765-9.

  2. SCCS Opinion SCCS/1642/22 (2022).

  3. Zhu & Gao (2008). J Dermatol Sci. 50(3):223-34.

  4. ISO 24444:2019 – Sun protection test methods.

  5. J Cosmet Dermatol. (2021). 20(3):1010-1017.

  6. USP 43-NF38 (2024). Arbutin Monograph.

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