A composition for treating skin pigmentation, a method of forming the composition, and a method of treating skin pigmentation are disclosed. The composition comprises at least one pharmaceutically acceptable additive. The composition further comprises at least one melanin production inhibitor, which may be a depigmentation agent. The melanin production inhibitor is present in an amount effective to inhibit melanin production in human skin cells of a subject that is administered the composition. The melanin production inhibitor is selected from the group consisting of cyclovirobuxine D, lipoic acid, nuciferine, peimisine, oleuropein, Rhodiola algida extract, Rhodiola kirilowii (Regel) Maxim extract, Glycyrrhizae Radix et Rhizoma extract, Cirsii japonici herba extract, Platycladi semen extract, Synotis erythropappa extract, Astragali complanati semen extract, Plantaginis semen extract, Lycopi herba extract, Euryales semen extract, Cuscutae semen extract, Amomi fructus extract, Tara seed extract, Platycladi cacumen extract, Eucommiae cortex extract, Dioscoreae rhizoma extract, Cirsii herba extract, and combinations thereof.揭露了用以治療皮膚色素沉著的組成物、形成該組成物的方法、及治療皮膚色素沉著的方法。組成物包含至少一藥學上可接受添加劑。組成物更包含至少一黑色素生成抑制劑,其可為一脫色素劑。黑色素生成抑制劑存在量有效抑制在施以組成物的一受試者的人體皮膚細胞中的黑色素生成。黑色素生成抑制劑係選自由以下所組成的群組:環常綠黃楊鹼D(cyclovirobuxine D)、硫辛酸(lipoic acid)、荷葉鹼(nuciferine)、貝母辛鹼(peimisine)、橄欖苦苷(oleuropein)、唐古紅景天(Rhodiola algida)抽出物、狹葉紅景天(Rhodiola kirilowii(Regel)Maxim)抽出物、甘草根及根莖(Glycyrrhizae Radix et Rhizoma)抽出物、大薊(Cirsii japonici herba)抽出物、柏子仁(Platycladi semen)抽出物、紅纓合耳菊(Synotis erythropappa)抽出物、沙苑子(Astragali complanati semen)抽出物、車前子(Plantaginis semen)抽出物、澤蘭(Lycopi herba)抽出物、芡實(Euryales semen)抽出物、菟絲子(Cuscutae semen)抽出物、豆蔻(Amomi fructus)抽出物、塔拉籽(Tara seed)抽出 物、側柏葉(Platycladi cacumen)抽出物、杜仲(Eucommiae cortex)抽出物、山藥(Dioscoreae rhizoma)抽出物、小薊(Cirsii herba)抽出物、及其組合。