ECTOIN
化妆品中 四氢甲基嘧啶羧酸 (ECTOIN) 的全球法规限值与配方应用标准是什么?
四氢甲基嘧啶羧酸(标准 INCI: ECTOIN,CAS 号: 96702-03-3)是化妆品配方中主要用作皮肤调理剂的核心成分。受中国 NMPA(已使用/准用)、韩国 MFDS(未列管)及欧盟 CosIng(未列管)等 6 大法域法定标准监管,常规建议添加量为 0.3–5%(最佳稳定窗口 pH 3–9)。
全球 7 轨官方全成分标签名称对照表
严格采用各国政府官方目录原名 · 严禁机器翻译| 法域与监管轨道 | 官方公告全成分标准名称 | 一键复制 |
|---|---|---|
| ① 韩国 (MFDS 化妆品标准名称) | ECTOIN (KR MFDS Registered) | |
| ② 韩国旧名称历史 (301 重定向) | — | — |
| ③ 欧盟 (EU CosIng EC 1223/2009) | ECTOIN | |
| ④ 美国普通化妆品 (US PCPC / MoCRA INCI) | ECTOIN | |
| ⑤ 美国 OTC 防晒/祛痘专论活性物名称 (FDA OTC) | — (非美国 OTC 专论活性成分 / 普通化妆品原料) | — |
| ⑥ 中国 (NMPA《已使用化妆品原料目录 IECIC》标准中文名) | 四氢甲基嘧啶羧酸 | |
| ⑦ 日本普通化妆品 / 医药部外品 (JCIA / MHLW) | エクトイン · [QD: エクトイン] |
Layer 1 — 全球 6 大法域法定限值与监管状态
| 法域 | 监管状态 | 法定限值 | 适用条件与法定依据来源 |
|---|---|---|---|
| 韩国 (MFDS) | 未列管 | GMP | 已列入官方化妆品原料目录 (按 GMP 规范使用) |
| 欧盟 (EU) | 未列管 | GMP | 已列入官方化妆品原料目录 (按 GMP 规范使用) |
| 美国 (FDA) | 未列管 | GMP | 已列入官方化妆品原料目录 (按 GMP 规范使用) |
| 中国 (NMPA) | 已使用/准用 | GMP | IECIC Entry #6443 |
| 日本 (MHLW) | 未列管 | GMP | 已列入官方化妆品原料目录 (按 GMP 规范使用) |
| 东盟 (ACD) | 未列管 | GMP | 已列入官方化妆品原料目录 (按 GMP 规范使用) |
Layer 2 — 毒理评估与历史最高使用量 (CN IECIC / US CIR / EU SCCS)
“欧盟 SCCS 安全评估上限”代表消费者安全科学委员会判定安全边际 (MoS≥100) 的毒理阈值;“美国 CIR 市售最高报告浓度”与“中国 IECIC 最高历史使用量”代表已上市化妆品的最高实际使用浓度。
| 安全评估依据 | 适用范围与剂型 | 评估浓度范围 | 评估结论与文献档案 |
|---|---|---|---|
| 中国 IECIC 最高历史使用量 | leave_on | ≤ 7% | 安全判定 (MoS≥100)NMPA IECIC (2025) Entry 06285 (2025) |
| 中国 IECIC 最高历史使用量 | rinse_off | ≤ 2% | 安全判定 (MoS≥100)NMPA IECIC (2025) Entry 06285 (2025) |
Layer 3 Formulation Concentration Box-Plot vs. Statutory Limit
Layer 3 — 剂型常规配比指南与理化配伍性
| 剂型分类 | Min – Q1 – Median – Q3 – Max (%) | 配方作用与机理 | Source ID |
|---|---|---|---|
| 剂型组 A — 水剂爽肤水 / 精华液 / 安瓶 | 0.3% · 0.5% · 1% · 2% · 5% | Extremolyte hydration-shell cell protectant & anti-inflammatory active | bitop Ectoin natural Monograph & PubMed Clinical Trials |
| 剂型组 B — 乳液 / 面霜 (O/W · W/O) | 0.3% · 0.5% · 1% · 2% · 7% | Barrier-repair dermatological cream active (up to 7% in clinical studies) | bitop Ectoin Clinical Dossier & CN IECIC |
Stratum Corneum Penetration Depth & Bio-Spicule Transdermal Delivery
Under passive topical application, molecules diffuse tortuously through intercellular lipids. Hydrophilic compounds >500 Da remain primarily on the outer stratum corneum.
pH Stability Window (0–14), Thermal Limit & HLB Colloidal Phase Behavior
Outside pH 3–9, risk of hydrolysis, viscosity loss, or ionic dissociation increases.
Thermally stable up to 85°C during standard emulsification.
Cellular & Molecular Target Mechanism Flow
Interactive Synergy Pairings (Solid) & Incompatibility Warnings (Dashed)
Click any green synergy node to jump directly to its monograph, or click a red dashed node to inspect the chemical incompatibility mechanism.
商品名仅供配方师识别原料规格参考,商标权归各原厂商所有。
学术与毒理综合摘要
Tier 1 Synthesis本综述严格基于与该原料关联的 NIH PubMed 同行评审文献摘要及官方毒理学评估档案编写。
关联同行评审文献 (NIH PubMed) (5)
In vivo assessment of Ectoin: a randomized, vehicle-controlled clinical trial [PMID: 17519560 · 2007]
The aim of the study was to assess an Ectoin formulation with regard to the antiageing properties. The study was designed as a monocentric, randomized, double-blind application test, in order to ensure the compatibility and the efficacy of Ectoin in comparison to a vehicle emulsion. A total of 104 voluntary healthy female test subjects were included in the study. Moisturizing properties as well as other parameters of skin ageing, like skin surface structure and skin elasticity, were determined for treatment A (vehicle) and treatment B (with 2% Ectoin) versus an untreated control. Statistical evaluations according to the Wilcoxon rank-sum test indicate a general preference for the Ectoin treatment by the test subjects in both the application and the efficacy tests. None of the participating test subjects had any side effects throughout the study. In terms of antiageing properties, previous in vitro studies could be confirmed by this clinical trial, clarifying that the natural cell protection concept of Ectoin is transferable to skin care with manifold benefits.
Testing an Ectoin Containing Emollient for Atopic Dermatitis [PMID: 30987568 · 2019]
To describe the methodology in studying patient's acceptability and efficacy of an ectoin containing emollient for atopic dermatitis (AD). We described the methodology that we used in studying emollients and moisturisers, and patient acceptability of a group of AD patients before and following usage of an ectoin-containing proprietary emollient. These data were also compared with other brand emollients that we previously reported, namely Restoradom®, Ezerra® and Ezerra plus®. 30 subjects (50% Male, Mean (SD) age: 9.8 (3.6) years with AD used the trial emollient W for four weeks. AD severity of subjects (by objective SCORAD) was moderate (n=22) and severe (n=8). Compliance was good and patients generally managed to use the moisturisers daily, with individual reports of a 'tingly' sensation by some subjects when applied to inflamed wounds. 63% reported "very good" or "good", whereas 37% reported "fair" or "poor" acceptability of the moisturisers. Following use of the trial emollient, area affected, disease intensity and severity significantly improved, as demonstrated in objective SCORAD (p=0.002). There were also significant improvements in POEM (p=0.035), and PADQLQ scores (p=0.017). For skin measurements, only transepidermal water loss had improved (p=0.035) after the treatment. There was no significant improvement of itch or sleep scores, skin hydration, pH, S. aureus colonization status, or need for use of topical medications. When compared with historical data of other emollients, the mean age of patients on emollient W was younger; efficacy and acceptability among these emollients were similar. Methodology of emollient research is described. Doctors should provide evidencebased information about the efficacy of emollients. The ectoin-containing proprietary emollient improves disease and quality of life following its use in 4 weeks. Efficacy and acceptability are similar among 4 proprietary emollients.
Strategies for the biological production of ectoine by using different chassis strains [PMID: 38157997 · 2024]
As an amino acid derivative and a typical compatible solute, ectoine can assist microorganisms in resisting high osmotic pressure. Own to its long-term moisturizing effects, ectoine shows extensive applications in cosmetics, medicine and other fields. With the rapid development of synthetic biology and fermentation engineering, many biological strategies have been developed to improve the ectoine production and simplify the production process. Currently, the microbial fermentation has been widely used for large scaling ectoine production. Accordingly, this review will introduce the metabolic pathway for ectoine synthesis and also comprehensively evaluate both wild-type and genetically modified strains for ectoine production. Furthermore, process parameters affecting the ectoine production efficiency and adoption of low cost substrates will be evaluated. Lastly, future prospects on the improvement of ectoine production will be proposed.
Ectoine in the Treatment of Irritations and Inflammations of the Eye Surface [PMID: 33628826 · 2021]
The ocular surface is facing various unspecific stress factors resulting in irritation and inflammation of the epithelia, causing discomfort to the patients. Ectoine is a bacteria-derived extremolyte with the ability to protect proteins and biological membranes from damage caused by extreme environmental conditions like heat, UV-light, high osmolarity, or dryness. Evidence from preclinical and clinical studies attest its effectiveness in treating several epithelium-associated inflammatory diseases, including the eye surface. In this review, we analysed 16 recent clinical trials investigating ectoine eye drops in patients with allergic conjunctivitis or with other unspecific ocular inflammations caused by e.g. ophthalmic surgery. Findings from these studies were reviewed in context with other published work on ectoine. In summary, patients with irritations and unspecific inflammations of the ocular surface have been treated successfully with ectoine-containing eye drops. In these patients, significant improvement was observed in ocular symptoms of allergic rhinoconjunctivitis, postoperative secondary dry eye syndrome, or ocular reepithelisation after surgery. Using ectoine as an add-on therapy to antihistamines, in allergy patients accelerated symptom relief by days, and its use as an add-on to antibiotics resulted in faster wound closure. Ectoine is a natural substance with an excellent tolerability and safety profile thus representing a helpful alternative for patients with inflammatory irritation of the ocular surface, who wish to avoid local reactions and side effects associated with pharmacological therapies or wish to increase the efficacy of standard treatment regimen.
Topical Ectoine: A Promising Molecule in the Upper Airways Inflammation-A Systematic Review [PMID: 31534961 · 2019]
To date, topical therapies guarantee a better delivery of high concentrations of pharmacologic agents to the mucosa of the upper airways (UA). Recently, topical administration of ectoine has just been recognized as adjuvant treatment in the Allergic Rhinitis (AR) and Rhinosinusitis (ARS). The aim of this work is to review the published literature regarding all the potential therapeutic effects of ectoine in the acute and chronic inflammatory diseases of UA. Pertinent studies published without temporal limitation were selected searching on MEDLINE the following terms: "ectoine" and "nasal spray," "oral spray," "upper respiratory tract infections," "rhinosinusitis," "rhinitis," "rhinoconjunctivitis," "pharyngitis," and "laryngitis." At the end of our selection process, six relevant publications were included: two studies about the effect of ectoine on AR, one study about ARS, one study about rhinitis sicca anterior, and two studies about acute pharyngitis and/or laryngitis. Due to its moisturizing and anti-inflammatory properties, topical administration of ectoine could play a potential additional role in treatment of acute and chronic inflammatory diseases of UA, in particular in the management of sinonasal conditions improving symptoms and endoscopic findings. However, these results should be viewed cautiously as they are based on a limited number of studies; some of them were probably underpowered because of their small patient samples.
常见问题解答 (FAQ)
- Q1. 四氢甲基嘧啶羧酸 (ECTOIN) 在全球 7 大法域的官方全成分标签名称是什么?
- 中国 NMPA《已使用化妆品原料目录 (IECIC)》标准中文名为 '四氢甲基嘧啶羧酸',美国 PCPC 与欧盟 CosIng 标准 INCI 为 'ECTOIN',日本 JCIA 表示名称为 'エクトイン'。
- Q2. 四氢甲基嘧啶羧酸 (ECTOIN) 在中、韩、欧、美、日、东盟的法定监管状态 (Layer 1) 如何?
- 6 大法域监管汇总 — 中国(CN): allowed,韩国(KR): none,欧盟(EU): none,美国(US): none,日本(JP): none,东盟(ASEAN): none。
- Q3. 四氢甲基嘧啶羧酸 (ECTOIN) 的常规配方添加量 (Layer 3) 与最佳稳定 pH 窗口是多少?
- 在代表性剂型 (aqueous_serum) 中常规添加量为 0.3%–5%(中位数 1%),最佳稳定 pH 范围为 3–9。
- Q4. 四氢甲基嘧啶羧酸 (ECTOIN) 有哪些配伍禁忌 (Incompatibilities) 与协同增效组合?
- 推荐协同组合包括 CERAMIDE NP, PANTHENOL, HYDROXYECTOIN, NIACINAMIDE;配伍禁忌注意:Exceptionally stable against heat, light, and pH extremes; compatible with acrylic rheology modifiers。