傳明酸水膠面膜的配方與品管方法的開發

The Development of Formula and Quality Control Method for Tranexamic Acid Hydrogel Mask

盧佳葆(Jia-Bau Lu)

指導教授 ： 許世興

朝陽科技大學/理工學院/應用化學系/碩士(2010年)

摘要

Tranexamic acid 是皮膚美白化妝品配方的重要試劑，及抑制分解纖維蛋白凝塊的抗血紅蛋白藥物，早期具有止血抗炎的藥理效果。
Tranexamic acid 對紫外光、可見光波長 190~800 nm 之吸光性非常弱，以致於無法以紫外光、可見光偵測器直接予以檢測之。本實驗以 FMOC ( 9-Fluorenylmethyl chloroformate )衍生試劑，在鹼性之緩衝水溶液中與 Tranexamic acid 之胺基反應成衍生物，並建立一套新的HPLC分析方法來檢測水膠面膜中Tranexamic acid的美白成分；移動相為10mM NH4OAc 緩衝水溶液pH 6.7/ 甲醇比例為30 / 70，撘配ODS Hypersil 250×4.6 mm(5 μm)的層析管柱，偵測波長為268 nm，流速為1.0 mL/min，注射量為20 μL，此分析方法可在9分鐘內完成。
在分析方法確效方面，Tranexamic acid的線性迴歸係數R2 = 0.9999，精密度實驗的相對標準偏差( RSD )介於0.01 % ~ 0.31 %之間，準確度實驗的回收率則介於98.0 % ~ 100.0 %。
在經皮穿透試驗方面，將自製的 Tranexamic acid 水膠面膜在 Nylon 濾膜及豬皮進行穿透性實驗，Tranexamic acid 在 3 hr 後的釋離率分別為 17.35 % 和 6.53 %，而相對標準偏差( RSD)分別在 5.71 % 和 8.60 % 以下，穿透試驗的結果可以當作藥物經皮使用的參考依據。

將自製的 Tranexamic acid 水膠面膜在室溫( 25±2℃)及加速( 40±2℃)的安定性試驗條件下進行6個月實驗，室溫試驗的Tranexamic acid含量衰退至94.92 %，而加速試驗的Tranexamic acid含量衰退至90.72 %。

關鍵字

傳明酸 ； 高效能液相層析儀

並列摘要

Tranexamic acid is an important reagent in cosmetic skin-whitening formulation, and is an antifibrinolytic drug that inhibits breakdown of fibrin clots, early in the pharmacological of anti-inflammatory effect with bleeding.
The molecule of tranexamic acid has very week absorption at the ultraviolet and visible wavelength from 190 to 800 nm, so that it is impossible to directly detect tranexamic acid with the UV-Vis detector.
In this research, the derivative reagent of FMOC (9-fluorenylmethyl chloroformate) was to use to react with the amino functional group of tranexamic acid at the alkaline condition and to form the UV detectable compound. A HPLC method was developed to determine the whitening ingredient of tranexamic acid in hydrogel mask. The mobile phases were prepared with 10mM NH4OAc buffer solution adjusted at pH 6.7 and methanol with the ratio of 30 to 70. Chromatographic methods was performed with a HPLC system equipped with ODS Hypersil 250×4.6mm(5 μm) column with UV/Vis absorption set at 268 nm, flow rate set at 1.0 mL/min and an injection of 20 μL as well as each runtime about nine minutes.
In the result of analytical validation, the linear regression coefficient (R2) was 0.9999, the relative standard deviations(RSD) of precision experiment were between 0.01 %~0.31 %, and the recoveries of the accuracy experiment were between 98.0 %~100.0 %.
In the tests of transdermal penetration, the hydrogel masks of tranexamic acid were placed in nylon membrane and pig skin to do penetrating experiments, the release rates of tranexamic acid for three hours for nylon membrane and pig skin were 17.35 % and 6.53 %, respectively. The relative standard deviations(RSD) of penetration tests for nylon membrane and pig skin were 5.71 % and 8.60 % below, respectively. The results of penetration tests can be used as the reference of transdermal medicine.
In this experiment, the tranexamic acid hydrogel mask was placed in the room temperature condition(25±2℃) and the accelerated condition (40±2℃) for six-month stability tests, the content of tranexamic acid was declined to 94.92 % in the room temperature test and was declined to 90.72 % in the accelerated test.

並列關鍵字

Tranexamic acid ； HPLC

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