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What is Tranexamic acid
Is Tranexamic acid difficult ingredient to use
Which ingredients works well with Tranexamic acid
Do you know what Tranexamic Acid is? You’ve probably noticed that more and more skincare products now feature Tranexamic Acid on their packaging. It’s an incredibly effective ingredient—so effective, in fact, that it was originally used in pharmaceuticals before becoming a star component in cosmetics.
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Tranexamic acid is widely recognized as an effective ingredient for improving dark spots. Many people have already incorporated skincare products containing tranexamic acid into their routines. In this section, I will first explain what tranexamic acid is.
Tranexamic acid is a type of amino acid that was first introduced to the market in 1965. It functions by inhibiting plasmin, a proteolytic enzyme responsible for dissolving blood clots. In the medical field, it is used to promote hemostasis and to reduce inflammation and allergic reactions. More recently, its ability to suppress melanin production—the cause of dark spots and melasma—has attracted attention, leading to its common use in cosmetics, particularly for treating melasma. Tranexamic acid is widely used both as an oral medication to alleviate melasma and throat inflammation, and as an active ingredient in skincare products targeting dark spots and dullness. It is incorporated into everyday skincare products and is highly regarded among women of various age groups.
The Cosmetic Grade Tranexamic Acid market is experiencing significant growth, driven by increasing consumer awareness of skin health and the rising prevalence of hyperpigmentation concerns. This powerful ingredient is renowned for its ability to inhibit melanin production, making it a popular choice in various skincare formulations aimed at treating discoloration and promoting an even skin tone.
In this section, let me share some of the main effects of tranexamic acid. Understanding its benefits will help you decide which products to choose and how to effectively promote them.
One of the causes of melasma is the influence of female hormones. When the balance of these hormones is disrupted, plasmin is stimulated, which activates melanocytes and is believed to contribute to the development of melasma. Tranexamic acid, which inhibits plasmin activity, is therefore used as an effective treatment for melasma.
Additionally, plasmin plays a role in producing substances that activate melanocytes in the epidermis (the skin’s surface). When melanocytes are activated, they produce excessive melanin, leading to dark spots. By incorporating tranexamic acid, which has anti-plasmin properties, melanocyte activation is suppressed, making it effective in preventing dark spots and post-inflammatory hyperpigmentation, such as acne scars.
Plasmin generates cytokines—substances that promote inflammation—during the process of protein breakdown. This is thought to trigger inflammation and allergic reactions. Tranexamic acid inhibits this activity and is also expected to help prevent skin irritation.
Do you know that some countries do not allow the use of tranexamic acid in cosmetic products?
If you are asking a Japanese OEM company to add tranexamic acid to a cosmetic product, please note that this is not permitted. In Japan, tranexamic acid can only be used as an active ingredient in quasi-drug (医薬部外品) products, not in standard cosmetics. All products on the market that contain tranexamic acid are sold as quasi-drugs. This is an important point to keep in mind. However, as an alternative, if the OEM company already has an approved quasi-drug formula that contains tranexamic acid, you may be able to use it as a white-label option.
On the other hand, some countries do allow the use of tranexamic acid in regular cosmetic products. For example, in Indonesia, the maximum allowed concentration of tranexamic acid in ready-to-use topical cosmetics is 3.0%.
In the United States and Europe, tranexamic acid was originally used as a hemostatic agent and to prevent postoperative bleeding in dental treatments, and its adoption in the beauty industry expanded relatively later. In fact, the American Academy of Dermatology (AAD) has reported that, in addition to hydroquinone and retinoids, topical tranexamic acid is effective for improving hyperpigmentation. Based on this, many Western cosmetic brands now formulate serums and creams containing a few percent of tranexamic acid, often combined with ingredients such as vitamin C and niacinamide.
Given the information above, it is very important to check the most up-to-date regulations in your target country, so please use this information as a reference.
In this section, I would like to introduce some effective ingredients that pair well with tranexamic acid. Tranexamic acid itself is an active ingredient, and when combined with other beneficial ingredients, it can further enhance the product’s effectiveness.
Niacinamide, also referred to as Vitamin B3, is a water-soluble nutrient widely recognized for its versatile benefits in skincare. It helps reinforce the skin’s protective barrier, regulate sebum levels, minimize discoloration, and calm irritation—making it a great option for all skin types, particularly those that are sensitive or acne-prone. It has become a highly popular ingredient, and its effectiveness increases when paired with other supportive actives.
For instance, tranexamic acid works by suppressing melanin formation, while niacinamide prevents the transfer of melanin to the skin’s surface. Using them together offers a dual strategy for reducing dark spots and enhances overall brightening results. Furthermore, both ingredients are mild and non-irritating, making them well-suited for reactive or blemish-prone skin.
Vitamin C is a highly regarded ingredient in the fields of skincare, health, and overall wellness. Naturally present in citrus fruits and various vegetables, this nutrient—also known as ascorbic acid—functions as a potent antioxidant when applied to the skin. It helps shield the complexion from pollution, environmental stress, and even UV-induced damage, making it a key player in achieving a brighter and more luminous appearance.
Tranexamic acid and Vitamin C both help improve hyperpigmentation, dark spots, and uneven skin tone, but they operate in distinct ways. Vitamin C boosts radiance by strengthening antioxidant defenses and slowing melanin production, while tranexamic acid interferes with the signals that trigger excess pigment formation. Used together, they address discoloration from multiple pathways, offering a highly effective approach for tackling concerns like sun damage, melasma, and post-inflammatory marks. Additionally, the two ingredients are generally easy to combine in a routine, with a low chance of irritation when layered thoughtfully.
Glutathione is a naturally occurring antioxidant present in the skin, where it plays a crucial role in shielding against visible damage caused by environmental stressors. Its powerful antioxidant capacity offers several skin benefits: it helps combat long-term oxidative damage, supports the restoration of the skin barrier, and improves the appearance of discoloration for a more even tone. Research also shows that when applied directly to areas of hyperpigmentation, glutathione can visibly improve sun-induced dark spots.
The combination of tranexamic acid and glutathione is frequently used in skincare and dermatological treatments. Tranexamic acid helps reduce hyperpigmentation and melasma by slowing melanin production, while glutathione enhances skin health and brightness through its detoxifying and antioxidant effects. Together, they work synergistically to illuminate the complexion, fade dark spots, and promote a more uniform skin tone. This duo is also appreciated for its anti-aging benefits and may be incorporated into topical formulas, oral supplements, or professional treatments based on individual needs and expert recommendations.
In the final section, I would like to provide some more technical and professional information.
It is highly water-soluble. It dissolves freely in water, making it easy to incorporate into the water phase of serums, toners, and creams.
Tranexamic acid is not highly pH-dependent; it’s effective in pH ranges from 3–8 and seems to do best for skin when formulated in a product whose pH is between 5–7.
While this ingredient is considered relatively stable and is commonly used in cosmetic formulations, maintaining its efficacy requires selecting products in airtight packaging and minimizing exposure to ultraviolet light and air.
In general, concentrations of around 0.5% to 3% are considered effective, and ingredients listed toward the top of the ingredient list typically indicate a higher amount. For example, in Japan, tranexamic acid can only be used in quasi-drugs, which ensures that a certain effective concentration is secured. Regulations vary by country, so it is important to check the allowable concentration levels in each region. This is because higher concentrations do not necessarily lead to better results and may instead increase the risk of irritation.
Tranexamic acid is a highly effective ingredient for improving dark spots and uneven skin tone, supported by both research and real-world results. When combined with ingredients like niacinamide, vitamin C derivatives, and glutathione, its brightening effects become even stronger. While relatively stable and easy to formulate, proper concentration, packaging, and regulatory checks remain important.
Overall, tranexamic acid is a reliable and versatile option for achieving clearer, more radiant skin. I hope this article will help support your business and assist you on your journey in creating formulations and developing your own products.
トラネキサム酸とは何か？
トラネキサム酸の効果とは？
トラネキサム酸配合製品の特長とは？
この記事では、医薬品や医薬部外品の有効成分として使われるトラネキサム酸の効果や製品事例をまとめました。
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トラネキサム酸は1960年代に国内で開発され、肝斑の改善効果があることで知られています。
肝斑の改善だけでなく、抗プラスミン活性を示すプロテアーゼ阻害薬として、口内炎治療の薬や、歯磨き粉など幅広い製品に使われています。
タンパク質を構成する成分である必須アミノ酸のリシンを元に人工合成されたアミノ酸の一種です。
2002年に医薬部外品の美白有効成分に承認されましたが、
化粧品成分としては承認されていないため、化粧品への配合は認められていません。
医薬部外品（薬用化粧品）に配合される場合には、
プロスタグランジンおよびプラスミン生成抑制による色素沈着抑制作用（美白作用）、
肝斑改善による色素沈着抑制作用、プラスミン生成抑制による抗炎症作用です。
1. 紫外線を浴びる
2. 肌に存在する角化細胞(ケラチノサイト)から様々な情報伝達物質(メラニン産生刺激因子)が産生・分泌される
3. 情報伝達を受け取ったメラノサイトでチロシナーゼ活性化され、メラニンが産生される
4. メラノサイトで産生されたメラニンが、ケラチノサイトへ転送される
5. 微弱炎症の持続、新陳代謝の乱れにより色素沈着、シミとなる
トラネキサム酸はメラノサイト活性化因子であるプラスミンをブロックすることで、シミや肝斑の原因となるメラニンの発生を抑制する作用があるとされています。
肌荒れを起こす原因でもあるプラスミンというタンパク質分解酵素の生成を抑制し、炎症を抑えます。
トラネキサム酸は医薬部外品の美白・抗炎症効果の有効成分として用いられます。
株式会社OEMではトラネキサム酸とグリチルリチン酸ジカリウムを有効成分としてローションとクリームの汎用処方を持っており、こちらの処方を使うことにより早期の商品開発が可能です。
薬用美白化粧水・クリーム
有効成分：トラネキサム酸・グリチルリチン酸ジカリウム
トラネキサム酸は美白作用、グリチルリチン酸ジカリウムは抗炎症作用として配合しています。
その他、美容成分のビタミンA、ビタミンB5誘導体、ビタミンC誘導体、ビタミンEや保湿成分であるヒアルロン酸、コラーゲン、植物性セラミドを配合しています。
また、ビタミン類はナノ化した原料を使用しています。
トラネキサム酸を配合した製品はシミ予防の美白や抗炎症作用が期待できますが、化粧品への配合は認められていません。
医薬部外品をオリジナルで作るとなると、一から医薬部外品の処方を組み、申請をする必要があるため、時間もコストもかかります。
OEM会社の汎用処方を上手く利用することで、開発期間を短縮してトラネキサム酸を配合した製品の製造ができるのです。
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