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أربوتين

Arbutin Product Introduction

  1. الاسم الانجليزي: Arbutin; 4-Hydroxyphenyl β-D-glucopyranoside
  1. مواصفة
    • نقاء:
      • α-Arbutin: ≥ 98% (HPLC)
      • β-Arbutin: ≥ 99% (HPLC)
    • الذوبانية: 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%
    • حجم الجسيمات: Standard powder ≤ 100 μm; micronized powder ≤ 5 μm for better absorption in cosmetics
  1. مظهر
    • White to off-white crystalline powder, odorless, with a slightly sweet taste
  1. رقم CAS
    • β-Arbutin: 497-76-7
    • α-Arbutin: 84380-00-7
  1. مهلة: 5 – 7 أيام عمل
  1. طَرد
    • 1 كجم/كيس (كيس رقائق الألومنيوم)، 25 كجم/برميل (كيس مزدوج الطبقة من البولي إيثيلين داخل برميل من الورق المقوى)
  1. السوق الرئيسي: 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. سيناريوهات التطبيق

الخصائص الأساسية

  • البنية الجزيئية: A glycoside composed of hydroquinone and glucose, with two main isomers (α and β) differing in glycosidic bond orientation.
  • استقرار: Stable under normal storage conditions, but sensitive to light and high temperatures, which may cause decomposition.
  • الميزات الرئيسية
    • Skin-Brightening Effect: Inhibits tyrosinase activity, reducing melanin production, and effectively lightening skin pigmentation, such as freckles, age spots, and post-inflammatory hyperpigmentation.
    • النشاط المضاد للأكسدة: 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.

سيناريوهات التطبيق

1. مستحضرات التجميل والعناية الشخصية

  • 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.
  • تركيبات مضادة للشيخوخة:
    • 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.
  • منتجات العناية بالشمس:
    • Incorporated into sunscreens to prevent UV-induced hyperpigmentation, enhancing the overall photoprotection of the skin.

2. المستحضرات الصيدلانية

  • 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. المأكولات والمشروبات

  • 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.

طرق الكشف

  • كروماتوغرافيا السائل عالية الأداء (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.
  • كروماتوغرافيا السوائل فائقة الأداء - مطيافية الكتلة (UPLC – MS):
    • Confirms the molecular structure and differentiates between α and β isomers, detecting trace impurities with high sensitivity.
  • الرنين المغناطيسي النووي (NMR):
    • Used for structural elucidation and identification of arbutin, especially in research and development to ensure the purity and correct isomeric form.

المصدر والمزايا

  • مصدر طبيعي: 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.
  • Market Demand: High consumer demand for skin-lightening products drives its popularity in the cosmetics industry, making it a valuable ingredient for manufacturers.

الامتثال التنظيمي

  • إدارة الغذاء والدواء الأمريكية: 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.
  • لائحة الاتحاد الأوروبي: 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.
  • الصين NMPA: 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.

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. المصدر والخصائص الكيميائية والتعريف

  • المصادر الطبيعية:

    • أساسي: Bearberry leaves (Arctostaphylos uva-ursi), Bergenia crassifoliaPyrus communis (pear) leaves

    • Secondary: Wheat germ, blueberry shoots

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

  • Chemical Specifications:

    المعلمةقيمة
    رقم CAS497-76-7 (β-Arbutin)
    84380-01-8 (α-Arbutin)
    الصيغة الجزيئيةC₁₂H₁₆O₇
    الوزن الجزيئي272.25 g/mol
    إينكس207-850-3
    مظهرWhite crystalline powder
    الذوبانيةWater: 50g/100mL (20°C)
    استقرارpH 3-7; decomposes at >100°C

3. Premium Product Selection & Health Applications

► Optimal Product Specifications

  • Highest PotencyAlpha-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. الحماية المضادة للأكسدة:

    • 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:

طلبConcentrationFrequency
مستحضرات التجميل0.5-2%Daily application
المكملات الغذائية50-200 mg/dayOral, divided doses
Critical Notes:
  • تأثيرات جانبية: <0.1% incidence of contact dermatitis (patch test recommended)

  • موانع الاستعمال: Pregnancy (limited data), hydroquinone sensitivity

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


4. Shaanxi Zhonghong Biotech: Arbutin Innovation Leader

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

► القدرات الأساسية:

  • 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

فئةالمعلمةمواصفةطريقة الاختبار
المبيدات الحشريةالكلوربيريفوس≤0.01 mg/kgكروماتوغرافيا الغاز-مطياف الكتلة/مطياف الكتلة
سايبرمثرين≤0.05 mg/kgكروماتوغرافيا الغاز-مطياف الكتلة/مطياف الكتلة
المعادن الثقيلةالرصاص (Pb)≤1.0 mg/kgICP-MS
الزئبق (Hg)≤0.1 ملغ/كغCV-AAS
علم الأحياء الدقيقةإجمالي عدد التمارين الهوائية≤100 وحدة تشكيل مستعمرة/جمISO 4833-1
Candida albicansغائب في 1 جرامISO 18416
المكورات العنقودية الذهبيةغائب في 1 جرامISO 22718
Key Analyticsα-Arbutin Assay≥99.0%HPLC-ELSD
β-Arbutin Impurity≤0.5%كروماتوغرافيا السائل عالي الأداء (HPLC)
Hydroquinone≤1 ppmHPLC-DAD

6. سير عمل الإنتاج المتقدم

  1. Biomass Processing: Cryogenic milling of Arctostaphylos uva-ursi leaves (-196°C)

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

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

  4. طهارة:

    • Macroporous resin chromatography (AB-8 resin)

    • Recrystallization from acetone/water (3:1)

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


7. Cutting-Edge Applications & Research

► التطبيقات التجارية:

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

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

  • الأغذية الوظيفية: 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. الإنتاج المستدام:

    • CRISPR-edited الإشريكية القولونية 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:

  • بريد إلكترونيliaodaohai@gmail.com

  • موقع إلكترونيhttps://www.aiherba.com

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

  • تخزين: 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. شركة شنشي تشونغهونغ للاستثمار والتكنولوجيا المحدودة الروافع المالية proprietary enzymatic bioconversion technologycGMP-compliant nanofiltration، و chiral separation expertise to deliver >99% pure α-arbutin – outperforming conventional extracts in efficacy and safety. With أكثر من 20 براءة اختراع 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.


مراجع

  1. Zhu, W. et al. (2021). α-Arbutin: Advanced Production Strategies & Clinical EfficacyJ. 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 BiosynthesisMetab. 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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