Drometrizole trisiloxane (Mexoryl XL)   中文名称: 甲酚曲唑三硅氧烷

Absorption, Distribution and Excretion
Drometrizole trisiloxane is reported as having little to no absorption through the skin. At this time, however, studies demonstrate that the components of most commonly used sunscreens are likely absorbed into the skin at least to some extent - although penetration to deeper tissues and the cutaneous circulation remains limited. Despite the extensive use of sunscreen products around the world, there have been few reports of adverse effects related to their use.
Drometrizole trisiloxane is reported as having little to no absorption through the skin. The systemic presence of the compound is consequently expected to be minimal.
Drometrizole trisiloxane is reported as having little to no absorption through the skin. The systemic presence of the compound is consequently expected to be minimal.
Drometrizole trisiloxane is reported as having little to no absorption through the skin. The systemic presence of the compound is consequently expected to be minimal.

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Metabolism / Metabolites
Drometrizole trisiloxane is reported as having little to no absorption through the skin. The systemic presence of the compound is consequently expected to be minimal.

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Biological Half-Life
Drometrizole trisiloxane is reported as having little to no absorption through the skin. The systemic presence of the compound is consequently expected to be minimal.

Protein Binding
Drometrizole trisiloxane is reported as having little to no absorption through the skin. The systemic presence of the compound is consequently expected to be minimal.

Drometrizole trisiloxane is a photostable UVA and UVB light filter. The compound is a lipophilic benzotriazole derivative marketed as Meroxyl XL by L'Oreal, although sunscreens with drometrizole trisiloxane are currently only approved for use in the EU, Canada, Australia, and Japan, among other countries. Despite being used elsewhere in the world with relatively few reports of adverse reactions, the FDA continues to cite that the existing scientific record is not sufficient to establish the compound as being generally recognized as safe and effective for over-the-counter sunscreen use.
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Drug Indication
Drometrizole trisiloxane is used as an active ingredient in various sunscreens for the indication of protecting the skin by absorbing the damaging UV radiation of sunlight.

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Mechanism of Action
Ultraviolet radiation is the invisible energy component to sunlight and consists of three wavelength ranges: (a) UVA is long-range UV radiation between 320-400nm. Although not as energetic as UVB, UVA can penetrate deep into the dermis. UVA can cause immediate tanning, premature skin aging, and can also play a role in the formation of some skin cancers. Approximately 95% of UVA from the sun passes through Earth's ozone layer. (b) UVB is short-wavelength UV radiation between 280-320nm. It is capable of penetrating the outer protective layer of the skin and is responsible for delayed tanning, sunburns, and most skin cancers. A large amount of UVB is absorbed by the ozone layer, however, as only 5% reaches the Earth's surface. (c) UVC is comprised of wavelengths between 100-280nm and is very energetic. It is very dangerous to all forms of life, even when the exposure is short. However, UVC radiation is generally filtered out by the ozone layer and never reaches the Earth. Ultimately, the shorter the wavelength, the more harmful the UV radiation - although shorter wavelength UV radiation is less able to penetrate the skin. Subsequently, drometrizole trisiloxane is a broad spectrum lipophilic benzotriazole derivative chemical sunscreen that is capable of absorbing UVA and UVB radiation. It is also photostable, meaning that it will not degrade in the presence of sunlight, unlike other UV filters like the widely used UVA absorber avobenzone. When combined with the UV blocker ecamsule, it has been shown that the two UV blockers elicit a synergistic effect involving an enhanced protective action for the skin against UVA and UVB radiation. Additionally, drometrizole trisiloxane is usually combined with other active sunscreen agents like titanium dioxide, avobenzone, and others to ensure the combined product covers or protects against as broad a spectrum of UV radiation as possible, considering drometrizole trisiloxane does not absorb against the entire range of UV radiation. And finally, at the molecular level, it is believed that the general structure of various UV blockers like drometrizole trisiloxane as aromatic molecules conjugated with carbonyl groups is capable of absorbing high energy ultraviolet rays and then consequently releasing that energy as less harmful, lower energy rays.

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Pharmacodynamics
As an active ingredient in sunscreen products, drometrizole trisiloxane is applied directly onto human skin where it acts as a chemical sunscreen layer between skin and sunlight that also directly absorbs the UV sunlight radiation. Since drometrizole trisiloxane is also considered to have little to no absorption through the skin, little systemic exposure and pharmacokinetics are expected and users can freely wash off and re-apply the compound as necessary.

C24H39N3O3SI3

501.85

501.23

155633-54-8

9848888

White to off-white solid powder

6.388

69.4

1

5

9

33

613

0

CC1=CC(CC(C[Si](O[Si](C)(C)C)(C)O[Si](C)(C)C)C)=C(O)C(N2N=C3C=CC=CC3=N2)=C1

HUVYTMDMDZRHBN-UHFFFAOYSA-N

InChI=1S/C24H39N3O3Si3/c1-18-14-20(15-19(2)17-33(9,29-31(3,4)5)30-32(6,7)8)24(28)23(16-18)27-25-21-12-10-11-13-22(21)26-27/h10-14,16,19,28H,15,17H2,1-9H3

2-(benzotriazol-2-yl)-4-methyl-6-[2-methyl-3-[methyl-bis(trimethylsilyloxy)silyl]propyl]phenol

OR-10154; OR10154; Silatrizole

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。