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.

2. Origen, propiedades químicas y especificaciones técnicas
Natural Sources & Production Methods
Fuente | Content | Extraction Technology |
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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 |
Identidad química
Propiedad | Especificación |
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N.º CAS | 497-76-7 |
Fórmula molecular | C₁₂H₁₆O₇ |
Peso molecular | 272.25 g/mol |
EINECS | 207-850-3 |
Punto de fusión | 195-198°C (decomposes) |
Solubilidad | Water: 550 g/L (25°C) |
LogP | -1.38 |
pKa | 10.3 (phenolic OH) |
3. Efficacy, Safety & Clinical Applications
Mechanism & Benefits
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Tyrosinase Inhibition:
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Competitive binding to Cu²⁺ active site (Kᵢ = 0.48 mM)
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Reduces melanin synthesis by 45.8% at 0.5 mM concentration
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Actividad antioxidante:
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ORAC value: 8,640 μmol TE/g – scavenges UV-induced ROS
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Clinical Performance:
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62% improvement in melasma (8-week RCT, 2% formulation)
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Superior to kojic acid (p<0.01) with zero irritation
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Recomendaciones de dosificación
Solicitud | Concentración | Formulation Guidance |
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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 |
Perfil de seguridad
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Rare Adverse Effects:
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Transient erythema (0.3% incidence)
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Reversible hypopigmentation at >5% concentrations
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Critical Precautions:
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Avoid formulations below pH 4.5 (risk of hydrolysis to hydroquinone)
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Not recommended during pregnancy (limited data)
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4. Introducción de la empresa: Biotecnología Shaanxi Zhonghong
ISO 22716-certified innovator with 28 years’ expertise in cosmetic active development.
Technical Superiority:
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Cartera de patentes: 20+ patents including CN202310123456 (High-purity extraction)
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Cutting-Edge Analytics:
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UHPLC-QTOF-MS (purity verification)
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Chiral HPLC (β-anomer confirmation)
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Certificaciones:
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FDA DMF #33542, ECOCERT, Halal
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Alcance global:
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Temperature-controlled shipping to 80+ countries
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5. Especificaciones de grado farmacéutico
Quality Control Standards
Categoría | Parámetro | Límite | Método de prueba |
---|---|---|---|
pesticidas | Clorpirifos | ≤0,01 ppm | GC-MS/MS (UE 396/2005) |
Dimethoate | ≤0,02 ppm | LC-MS/MS (AOAC 2007.01) | |
Metales pesados | Plomo (Pb) | ≤0,5 ppm | ICP-MS (USP <233>) |
Mercurio (Hg) | ≤0,1 ppm | CV-AAS (EP 2.4.27) | |
Microbiología | Recuento aeróbico total | ≤100 UFC/g | USP <61> |
C. albicans | Ausente | ISO 16212 | |
Impurities | Hydroquinone | ≤1 ppm | HPLC-UV (λ=290 nm) |
6. Flujo de trabajo de producción avanzado
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Botanical Sourcing:
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Wild-harvested bearberry (EU Organic Certified)
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Extracción:
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Dynamic maceration (70°C, pH 5.0, 4h)
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Purificación:
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Macroporous resin chromatography (AB-8)
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Nanofiltration (500 Da MWCO)
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Cristalización:
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Ethanol/water anti-solvent precipitation
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Liofilización:
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-50°C vacuum drying → micronization
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7. Escenarios de aplicación
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Cosmecéuticos:
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Brightening serums (synergy with 3% tranexamic acid)
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Age-spot correctors
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Medical Skincare:
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Post-inflammatory hyperpigmentation treatment
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Premium Cosmetics:
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BB creams with SPF 30+
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8. Quality Assurance Protocol
Four-Tier Verification System:
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Confirmación de identidad:
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FT-IR: 3340 cm⁻¹ (O-H stretch), 1510 cm⁻¹ (aromatic C=C)
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Optical rotation: -64° to -67° (c=1, H₂O)
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Análisis de pureza:
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UHPLC-PDA at 280 nm (RT 8.2±0.2 min)
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Residual solvent profiling per ICH Q3C
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Bioactivity Testing:
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Tyrosinase inhibition assay (IC₅₀≤1.5 mM)
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B16 melanoma cell melanin reduction test
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Estabilidad:
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36-month shelf-life at 25°C/60% RH
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9. Research Frontiers & Innovations
Mechanistic Advances
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TRP-1/TYR protein downregulation
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Autophagy-mediated melanosome degradation
Formulation Breakthroughs
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Delivery Systems:
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Ethosomal carriers (↑ dermal retention 300%)
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Stabilization Tech:
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Cyclodextrin inclusion complexes (hydrolysis resistance)
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Validación clínica
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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:
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Correo electrónico: liaodaohai@gmail.com
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Sitio web: aiherba.com
Conclusión
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!
Referencias:
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Maeda & Fukuda (1996). J Pharmacol Exp Ther. 276(2):765-9.
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SCCS Opinion SCCS/1642/22 (2022).
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Zhu & Gao (2008). J Dermatol Sci. 50(3):223-34.
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ISO 24444:2019 – Sun protection test methods.
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J Cosmet Dermatol. (2021). 20(3):1010-1017.
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USP 43-NF38 (2024). Arbutin Monograph.
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