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    • 5. 发明授权
    • Highly purified tocopheryl phosphate, process for producing the same,
analytical method therefor and cosmetic
    • 高纯度生育磷酸酯,其生产方法,分析方法和化妆品
    • US6046181A
    • 2000-04-04
    • US342228
    • 1999-06-29
    • Yutaka OonishiTsutomu NozawaTakami OoeKeisuke ManoNaoaki MisuYohei KurataShinobu ItoEiji Ogata
    • Yutaka OonishiTsutomu NozawaTakami OoeKeisuke ManoNaoaki MisuYohei KurataShinobu ItoEiji Ogata
    • A61K8/02A61K8/67A61Q1/02A61Q1/04A61Q5/02A61Q7/00A61Q11/00A61Q19/00A61Q19/10C07F9/655G01N30/02G01N30/88G01N33/82A61K7/035A61K7/00A61K7/02A61K7/021A61K7/027
    • G01N33/82A61K8/0212A61K8/678A61Q19/00C07F9/65522A61Q1/02A61Q1/04A61Q11/00A61Q19/10A61Q5/02A61Q7/00G01N2030/884G01N30/02Y10S514/846
    • Disclosed herein are a highly purified tocopheryl phosphate and/or a salt thereof (tocopheryl phosphates) wherein a P,P'-bistocopheryl hypophosphate and/or a salt thereof (P,P'-bistocopheryl diphoshates) is contained in a proportion of not higher than 3% by weight; a process for producing a highly purified tocopheryl phosphate and/or a salt thereof, which comprises the steps of reacting a tocopherol with an oxyphosphorus trihalide followed by treating with an acid or basic aqueous solution to thereby form tocopheryl phosphates (i) in which P,P'-bistocopheryl diphoshates (ii) formed as by-products are contained, hydrolyzing the P,P'-bistocopheryl diphoshates (ii) under acid condition, and, optionally, rendering the hydrolyzate neutral or basic under basic condition; and a method of analyzing tocopheryl phosphates, comprising analyzing a sample containing components (i) and (ii) with the use of a high-performance liquid chromatograph column packed with a gel of a polymethacrylate having, bonded thereto, long-chain alkyl groups. None or only an extremely minute amount of P,P'-bistocopheryl diphoshates are contained in the highly purified tocopheryl phosphates, so that the highly purified tocopheryl phosphates exhibit antioxidant and blood circulation promoting effects, have excellent water solubility, are powdery so that the handling thereof is extremely easy, are free from cutaneous irritation and allergenecity and ensure dermal safety. Therefore, the highly purified tocopheryl phosphates are useful as cosmetic ingredients. The amounts of components (i) and (ii) can be simply measured with high accuracy by the above method.
    • 本文公开了高纯度的生育磷酸酯和/或其盐(生育磷酸酯),其中P,P'-二生育酚低磷酸盐和/或其盐(P,P'-二生育基二磷酸酯)的含量不高于 超过3%重量; 一种生产高纯度生育磷酸酯和/或其盐的方法,其包括使生育酚与三卤氧磷反应,然后用酸或碱性水溶液处理,从而形成生育磷酸酯(i),其中P, 含有作为副产物形成的P'-二生育基二磷酸酯(ⅱ),在酸性条件下水解P,P'-二生育基二磷酸酯(ⅱ),任选地在碱性条件下使水解产物中性或碱性。 以及分析生育磷酸酯的方法,包括使用填充有与其键合的聚甲基丙烯酸酯的凝胶的高效液相色谱柱分析含有成分(i)和(ii)的样品的长链烷基。 高纯度的生育磷酸酯中没有或仅有非常少量的P,P'-二生育基二磷酸酯,因此高纯度的生育磷酸酯表现出抗氧化和促进血液循环的作用,具有优异的水溶性,是粉末状的, 它非常容易,没有皮肤刺激和过敏原,并确保皮肤安全。 因此,高纯度的生育磷酸酯可用作化妆品成分。 组分(i)和(ii)的量可以通过上述方法以高精度简单地测量。
    • 8. 发明授权
    • Ascorbic acid drugs for intracerebral administration
    • 抗坏血酸药物用于脑内给药
    • US5869525A
    • 1999-02-09
    • US647767
    • 1996-05-15
    • Shinobu ItoEiji OgataNobuhiko Miwa
    • Shinobu ItoEiji OgataNobuhiko Miwa
    • A61K31/375A61K31/34A61K31/70A61K31/715
    • A61K31/375
    • An L-ascorbic acid drug for intracerebral administration comprising one or more stable activity L-ascorbic acid compounds and one or more blood brainbarrier deobstruents. Also disclosed is a method for increasing intracerebral concentration of L-ascorbic acid in a human being comprising administering by injection an L-ascorbic acid drug comprising one or more stable activity L-ascorbic acid compounds. Additionally disclosed is a method for increasing intracerebral concentration of L-ascorbic acid in a human being comprising administering by injection an L-ascorbic acid drug comprising one or more stable activity L-ascorbic acid compounds and one or more blood brainbarrier deobstruents. Also disclosed is a method for treating diseases or disorders that result from intracerebral bloodstream inhibition or intracerebral bloodstream lowering comprising administering by injection to a person in need of such treatment, a dosage effective amount of an L-ascorbic acid drug comprising one or more stable activity L-ascorbic acid compounds. Additionally disclosed is a method for treating diseases or disorders that result from intracerebral bloodstream inhibition or intracerebral bloodstream lowering comprising administering by injection to a person in need of such treatment, a dosage effective amount of an L-ascorbic acid drug comprising one or more stable activity L-ascorbic acid compounds and one or more blood brainbarrier deobstruents.
    • 一种用于脑内给药的L-抗坏血酸药物,其包含一种或多种稳定的活性L-抗坏血酸化合物和一种或多种血液脑阻滞剂。 还公开了增加人体中L-抗坏血酸的脑内浓度的方法,包括通过注射施用包含一种或多种稳定活性L-抗坏血酸化合物的L-抗坏血酸药物。 另外公开了一种增加人抗坏血酸的脑内浓度的方法,包括通过注射施用包含一种或多种稳定的活性L-抗坏血酸化合物和一种或多种血脑屏障去除剂的L-抗坏血酸药物。 还公开了一种用于治疗由脑内血流抑制或脑内血流降低引起的疾病或病症的方法,其包括通过注射给予需要这种治疗的人,剂量有效量的包含一种或多种稳定活性的L-抗坏血酸药物 L-抗坏血酸化合物。 另外公开了一种治疗由脑内血流抑制或脑内血流降低引起的疾病或病症的方法,其包括通过注射给予需要这种治疗的人,剂量有效量的包含一种或多种稳定活性的L-抗坏血酸药物 L-抗坏血酸化合物和一种或多种血脑屏障阻断剂。