Alfa-arbutina
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Arbutina

Arbutin Product Introduction

  1. Nombre en inglés: Arbutin; 4-Hydroxyphenyl β-D-glucopyranoside
  1. Especificación
    • Pureza:
      • α-Arbutin: ≥ 98% (HPLC)
      • β-Arbutin: ≥ 99% (HPLC)
    • Solubilidad: Soluble in water (14 g/L at 25°C), slightly soluble in ethanol, insoluble in organic solvents like ether.
    • Appearance – Related: Loss on drying ≤ 1.0%, Heavy metals ≤ 5 ppm, Residual solvents ≤ 0.05%
    • Tamaño de partícula: Standard powder ≤ 100 μm; micronized powder ≤ 5 μm for better absorption in cosmetics
  1. Apariencia
    • White to off-white crystalline powder, odorless, with a slightly sweet taste
  1. N.º CAS.
    • β-Arbutin: 497-76-7
    • α-Arbutin: 84380-00-7
  1. Plazo de entrega: 5 – 7 días laborables
  1. Paquete
    • 1 kg/bag (aluminum foil bag), 25 kg/drum (double-layer PE bag inside cardboard drum)
  1. Mercado principal: Global market, with high demand in Asia (China, South Korea, Japan), North America, and Europe, especially in the cosmetics, pharmaceuticals, and dietary supplement industries
  1. Escenarios de aplicación

Propiedades principales

  • Estructura molecular: A glycoside composed of hydroquinone and glucose, with two main isomers (α and β) differing in glycosidic bond orientation.
  • Estabilidad: Stable under normal storage conditions, but sensitive to light and high temperatures, which may cause decomposition.
  • Características principales
    • Skin-Brightening Effect: Inhibits tyrosinase activity, reducing melanin production, and effectively lightening skin pigmentation, such as freckles, age spots, and post-inflammatory hyperpigmentation.
    • Actividad antioxidante: Scavenges free radicals, protecting skin cells from oxidative damage and preventing premature aging.
    • Low Toxicity: Generally well-tolerated by the skin, making it a popular choice for safe skin-lightening formulations.
    • Water-Soluble: Facilitates easy incorporation into aqueous-based products like serums and toners.

Escenarios de aplicación

1. Cosméticos y cuidado personal

  • Skin-Whitening Products:
    • Added to facial creams, lotions, serums (0.5 – 2% concentration), and masks (1 – 3% concentration) to reduce dark spots and even out skin tone.
    • Used in body lotions and deodorants to lighten underarm and knee skin.
  • Fórmulas antienvejecimiento:
    • Combined with other antioxidants and anti-aging ingredients in eye creams and anti-wrinkle treatments to protect skin from oxidative stress and prevent the formation of age spots.
  • Sun Care Products:
    • Incorporated into sunscreens to prevent UV-induced hyperpigmentation, enhancing the overall photoprotection of the skin.

2. productos farmacéuticos

  • Topical Medications:
    • Investigated for use in creams and gels to treat skin disorders associated with hyperpigmentation, such as melasma.
    • Used in wound-healing ointments due to its potential anti-inflammatory and antioxidant properties, promoting faster skin repair.
  • Oral Supplements (Research – based):
    • In early-stage research for potential internal use in managing skin pigmentation disorders, though oral application is less common due to potential metabolic concerns.

3. Alimentos y bebidas

  • Natural Preservative (Research – based):
    • Some studies explore its use as a natural antioxidant and preservative in food products, inhibiting lipid oxidation and microbial growth, although not yet widely commercialized.
  • Functional Food Ingredient (Conceptual):
    • Considered for addition to health beverages and dietary supplements for potential skin health benefits when consumed orally, but regulatory approvals are pending for such claims.

Métodos de detección

  • Cromatografía líquida de alta resolución (HPLC):
    • Column: C18 (250 × 4.6 mm, 5 μm), Mobile Phase: Methanol – water (20:80 v/v), Flow Rate: 1.0 mL/min, Detection Wavelength: 280 nm for quantification.
  • Ultra-Performance Liquid Chromatography – Mass Spectrometry (UPLC – MS):
    • Confirms the molecular structure and differentiates between α and β isomers, detecting trace impurities with high sensitivity.
  • Resonancia magnética nuclear (RMN):
    • Used for structural elucidation and identification of arbutin, especially in research and development to ensure the purity and correct isomeric form.

Origen y ventajas

  • Fuente natural: Extracted from various plants, including bearberry (Arctostaphylos uva-ursi), blueberries, and cranberries, through solvent extraction and purification processes.
  • Synthetic Option: Commercially, it can also be synthesized chemically, providing a more consistent supply compared to natural extraction.
  • Demanda del mercado: High consumer demand for skin-lightening products drives its popularity in the cosmetics industry, making it a valuable ingredient for manufacturers.

Cumplimiento normativo

  • FDA de EE. UU.: Regulated as a cosmetic ingredient. There are no specific restrictions on its use in topical cosmetics, but claims related to skin-lightening must comply with FDA regulations.
  • Reglamento de la UE: Approved for use in cosmetics under the Cosmetics Regulation (EC) No 1223/2009. It is listed in the Cosmetic Ingredients Database (CosIng) with specific usage limits.
  • NMPA de China: Permitted for use in cosmetics and is included in the Cosmetic Raw Materials Safety Information Database. Manufacturers must ensure compliance with safety and quality standards.
Categorías: , ,

Arbutin: The Gold Standard for Safe Skin Brightening & Antioxidant Defense

1. What is Arbutin?

Arbutin (CAS 497-76-7) is a naturally occurring β-D-glucopyranoside derivative of hydroquinone, renowned for its potent tyrosinase-inhibiting properties. As the premier non-irritating alternative to hydroquinone, it effectively disrupts melanin synthesis through competitive enzyme inhibition without cytotoxic effects. Available as alpha-arbutin (synthetic) and beta-arbutin (plant-derived), the alpha form exhibits superior stability and efficacy at lower concentrations.

2. Fuente, propiedades químicas e identificación

  • Fuentes naturales:

    • Primario: Bearberry leaves (Arctostaphylos uva-ursi), Bergenia crassifolia, Pyrus communis (pear) leaves

    • Secondary: Wheat germ, blueberry shoots

  • Synthesis: Enzymatic glycosylation of hydroquinone via Aspergillus oryzae β-glucosidase

  • Chemical Specifications:

    ParámetroValor
    N.º CAS497-76-7 (β-Arbutin)
    84380-01-8 (α-Arbutin)
    Fórmula molecularC₁₂H₁₆O₇
    Peso molecular272.25 g/mol
    EINECS207-850-3
    AparienciaPolvo cristalino blanco
    SolubilidadWater: 50g/100mL (20°C)
    EstabilidadpH 3-7; decomposes at >100°C

3. Premium Product Selection & Health Applications

► Optimal Product Specifications

  • Highest Potency: Alpha-arbutin >99% (HPLC) outperforms beta-arbutin with 10x greater tyrosinase affinity

  • Purity Standards: Heavy metals (Pb <1 ppm), residual solvents (methanol <50 ppm), microbial limits (TAMC <100 CFU/g)

► Clinically Validated Benefits:

  1. Skin Depigmentation:

    • Inhibits tyrosinase (IC₅₀: 24 μM) by binding copper active site

    • Reduces UV-induced melanin by 45.8% at 0.5% concentration (vs. 35.2% for β-arbutin)

  2. Protección antioxidante:

    • Scavenges ROS (IC₅₀: 0.13 mM) and prevents lipid peroxidation

  3. Antibacterial Action:

    • Effective against Propionibacterium acnes (MIC: 1.25 mg/mL)

► Dosage & Safety Profile:

SolicitudConcentrationFrequency
Productos cosméticos0.5-2%Daily application
Nutracéuticos50-200 mg/dayOral, divided doses
Critical Notes:

  • Efectos secundarios: <0.1% incidence of contact dermatitis (patch test recommended)

  • Contraindicaciones: Pregnancy (limited data), hydroquinone sensitivity

  • Estabilidad: Formulate at pH 5.5-6.5; avoid ascorbic acid/retinol combinations

4. Shaanxi Zhonghong Biotech: Arbutin Innovation Leader

28 años de experiencia in botanical actives positions Shaanxi Zhonghong Investment Technology Co., Ltd. as the global partner for premium arbutin:

► Capacidades principales:

  • Extraction Mastery:

    • CO₂ supercritical extraction (40°C, 250 bar) preserves thermolabile compounds

    • Nanofiltration technology achieves >99.5% α-arbutin purity

  • Analytical Infrastructure:

    • Chiral HPLC-ELSD for α/β-arbutin isomer quantification

    • ICP-MS heavy metal detection at ppb-level sensitivity

  • Innovation Ecosystem:

    • Patent CN114716386A: Enzymatic synthesis of high-stability α-arbutin

    • University partnerships developing arbutin-peptide conjugates for enhanced dermal delivery

5. Rigorous Quality Specifications

CategoríaParámetroEspecificaciónMétodo de prueba
pesticidasClorpirifos≤0.01 mg/kgGC-MS/MS
Cipermetrina≤0,05 mg/kgGC-MS/MS
Metales pesadosPlomo (Pb)≤1.0 mg/kgICP-MS
Mercurio (Hg)≤0.1 mg/kgCV-AAS
MicrobiologíaRecuento aeróbico total≤100 UFC/gISO 4833-1
Candida albicansAusente en 1gISO 18416
Estafilococo áureoAusente en 1gISO 22718
Key Analyticsα-Arbutin Assay≥99.0%HPLC-ELSD
β-Arbutin Impurity≤0,5%Chiral HPLC
Hydroquinone≤1 ppmHPLC-DAD

6. Flujo de trabajo de producción avanzado

  1. Procesamiento de biomasa: Cryogenic milling of Arctostaphylos uva-ursi leaves (-196°C)

  2. Selective Extraction: Ethanol-water (70:30) at 50°C, pH 4.5

  3. Enzymatic Conversion: β-Glucosidase treatment (40°C, 24h) for α-arbutin isomerization

  4. Purificación:

    • Macroporous resin chromatography (AB-8 resin)

    • Recrystallization from acetone/water (3:1)

  5. Liofilización: -50°C vacuum drying for crystal structure preservation

7. Cutting-Edge Applications & Research

► Commercial Applications:

  • Cosmecéuticos: Brightening serums (2% α-arbutin + 5% niacinamide), acne spot treatments

  • Medical Dermatology: Melasma therapy (combined with 1064nm Q-switched Nd:YAG laser)

  • Alimentos funcionales: Antioxidant capsules (100mg arbutin + selenium)

► Innovation Frontiers:

  1. Transdermal Delivery:

    • Ethosomal carriers (entrapment efficiency: 92.3%) enhance stratum corneum penetration

  2. Multi-Target Inhibitors:

    • Arbutin-kojic acid hybrids show synergistic tyrosinase inhibition (IC₅₀: 3.7 μM)

  3. Producción sostenible:

    • CRISPR-edited E. coli strains producing arbutin from glycerol (yield: 28.7 g/L)

Current Challenges:

  • Regulatory divergence (Japan: quasi-drug vs. EU: cosmetic ingredient)

  • Stability in O/W emulsions (>40°C)

8. Essential FAQs

Q: Does arbutin cause skin photosensitivity?
A: No – unlike hydroquinone, arbutin does not increase UV sensitivity and provides intrinsic photoprotection.

Q: What concentration is optimal for hyperpigmentation?
A: Clinical studies show 2% α-arbutin reduces melanin index by 22.3% after 8 weeks (vs. 16.7% for 7% β-arbutin).

Q: Is plant-derived arbutin superior to synthetic?
A: Synthetic α-arbutin delivers higher purity (>99.5%), batch consistency, and efficacy at lower doses.

Q: Can arbutin be used with vitamin C?
A: Formulate at pH 5.5-6.0; avoid direct combination with L-ascorbic acid (stability issues).

9. Global Supply Information

Contact Shaanxi Zhonghong for Pharmaceutical-Grade Arbutin:

  • Correo electrónico: liaodaohai@gmail.com

  • Sitio web: https://www.aiherba.com

  • Embalaje: Nitrogen-flushed amber glass vials (1-5kg) or HDPE drums (25kg)

  • Almacenamiento: 2-8°C; 24-month stability

  • Logistics: Global cold-chain shipping (2-8°C) with IATA-compliant documentation

10. Conclusion

Arbutin remains the gold-standard melanogenesis inhibitor for ethical skin brightening formulations. Tecnología de inversión Shaanxi Zhonghong Co., Ltd. apalancamientos proprietary enzymatic bioconversion technology, cGMP-compliant nanofiltration, y chiral separation expertise to deliver >99% pure α-arbutin – outperforming conventional extracts in efficacy and safety. With Más de 20 patentes in active delivery systems and ISO 22716 cosmetic GMP certification, we empower brands to develop clinically effective, regulatory-compliant depigmenting solutions. Partner with us to formulate the next generation of evidence-based skin therapies.

Referencias

  1. Zhu, W. et al. (2021). α-Arbutin: Advanced Production Strategies & Clinical Efficacy. J. Cosmet. Dermatol. 20(7):2145-2156.

  2. EU SCCS Opinion on Alpha-Arbutin (SCCS/1642/22).

  3. Chen, L. et al. (2023). CRISPR-based Metabolic Engineering for Arbutin Biosynthesis. Metab. Eng. 76:146-158.

  4. JECFA Specifications for Arbutin (JECFA/89/SC).

  5. Shaanxi Zhonghong Patent CN114716386A: Method for High-Yield α-Arbutin Production.

  6. ICH Guidelines: Q3C (Residual Solvents), Q3D (Elemental Impurities).

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