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泊洛沙姆188EP标准品 | 53637-25-5

中文名称
泊洛沙姆188EP标准品
中文别名
聚氧丙烯聚氧乙烯共聚物(固体);P123聚环氧乙烷-聚环氧丙烷-聚环氧乙烷三嵌段共聚物;环氧乙烷与甲基环氧乙烷的嵌段聚合物;普流罗尼F-108;聚(丙二醇)-嵌-聚(乙二醇)-嵌-聚(丙二醇)
英文名称
Poloxamer
英文别名
2-methyloxirane;oxirane
泊洛沙姆188EP标准品化学式
CAS
53637-25-5;9003-11-6;106392-12-5
化学式
C5H10O2
mdl
——
分子量
102.13
InChiKey
RVGRUAULSDPKGF-UHFFFAOYSA-N
BEILSTEIN
——
EINECS
——
  • 物化性质
  • 计算性质
  • ADMET
  • 安全信息
  • SDS
  • 制备方法与用途
  • 上下游信息
  • 反应信息
  • 文献信息
  • 表征谱图
  • 同类化合物
  • 相关功能分类
  • 相关结构分类

物化性质

  • 熔点:
    57-61 °C
  • 密度:
    1.05 g/mL at 20 °C
  • 物理描述:
    Liquid
  • 颜色/状态:
    Liquid
  • 稳定性/保质期:
    常温常压下稳定,避免潮湿、高温和湿热环境。

计算性质

  • 辛醇/水分配系数(LogP):
    0.42
  • 重原子数:
    7
  • 可旋转键数:
    0
  • 环数:
    2.0
  • sp3杂化的碳原子比例:
    1.0
  • 拓扑面积:
    25.1
  • 氢给体数:
    0
  • 氢受体数:
    2

ADMET

代谢
一个单一的代谢物,HW1,其分子量大约为16000道尔顿,在狗和人的药代动力学研究中被检测到。在狗和人体中,HW1分别占母体化合物稳态下的10-20%和40%。然而,有建议称,嵌段聚合物不被代谢,并以原样形式通过尿液和粪便排出,HW1可能是P188高分子量分布的一个组成部分,由于其清除率较低,在血浆中浓缩。
A single metabolite, HW1, with a molecular weight of approximately 16000 Daltons was detected in a pharmacokinetic study in dogs and man. HW1 was present in 10-20 and 40% of the parent compound at steady state in dogs and humans, respectively. However, it is suggested that block polymers are not metabolized and are excreted unchanged in the urine and feces, and HW1 may be a component of the higher molecular weight distribution of P188 that concentrates in the plasma due to its lower clearance rate.
来源:DrugBank
毒理性
  • 毒性数据
大鼠LC50 = 320毫克/立方米/4小时
LC50 (rat) = 320 mg/m3/4h
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
毒理性
  • 非人类毒性摘录
实验室动物:急性暴露/为了表征多克酸407(普朗尼克F-127)对大鼠各种器官系统的潜在毒性,每天一次连续4天将0.33克/千克/天(10% w/w溶液)或1.0克/千克/天(30% w/w溶液)的多克酸407通过多次腹腔注射给大鼠。与对照组动物相比,注射0.33克/千克/天多克酸407的大鼠在脾脏、肝脏或总体重方面没有显著增加或减少。与对照组相比,连续4天注射0.33克/千克/天的大鼠单核细胞数量显著增加。连续4天注射1.0克/千克/天与对照组动物相比,出现了明显的脾肿大。观察到体重显著减少,淋巴细胞百分比、红细胞、血红蛋白和血细胞比容百分比显著下降。同一组大鼠中白细胞数量和单核细胞百分比显著增加。因此,连续4天重复腹腔注射1.0毫克/千克/天的多克酸407会导致大鼠脾肿大和体重减少。
/LABORATORY ANIMALS: Acute Exposure/ To characterize any potential toxicities of poloxamer 407 (Pluronic F-127) to various organ systems in the rat, multiple intraperitoneal (IP) injections of 0.33 g/kg/day (10% w/w solution) or 1.0 g/kg/day (30% w/w solution) of poloxamer 407 were administered once daily for 4 consecutive days to rats. When compared to control animals, rats injected with 0.33 g/kg/day of poloxamer 407 did not show a significant increase or decrease in spleen, liver, or total body weight. Rats injected with 0.33 g/kg/day for 4 days demonstrated a significant increase in the number of monocytes when compared to controls. Administration of 1.0 g/kg/day for 4 days demonstrated distinct splenomegaly when compared to control animals. A significant reduction in body weight and significant decrease in the percent of lymphocytes, red blood cells, hemoglobin, and percent hematocrit were noted. A significant increase in the number of white blood cells and the percent monocytes was observed in this same group of rats. It was concluded that repetitive IP 1.0 mg/kg/day injections of poloxamer 407 to rats for 4 days results in splenomegaly and total body weight reduction.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
  • 非人类毒性摘录
实验室动物:急性暴露/研究了4种潜在聚氧乙烯醇注射载体的肌肉毒性,通过注射到兔肌肉中进行组织的大体形态检查和监测注射后随着时间的推移肌酸磷酸激酶水平的变化。将结果与已接受的肌内注射载体获得的结果进行比较。
/LABORATORY ANIMALS: Acute Exposure/ The muscle toxicity caused by 4 potential poloxamer injection vehicles was investigated following injection into rabbit muscles via gross morphological examination of tissue and monitoring of creatine phosphokinase levels as a function of time following injection. Results were compared to those obtained for accepted intramuscular vehicles.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
  • 非人类毒性摘录
实验室动物:急性暴露/研究了疏水表面活性剂,聚氧化烯2930对大鼠脂质吸收的影响。在急性条件下,与脂质餐一起通过十二指肠内输注表面活性剂,吸收的脂质在肠细胞中异常积聚。这种效果在停止治疗后很快逆转。
/LABORATORY ANIMALS: Acute Exposure/ Effect of hydrophobic surfactant, poloxalene 2930, on lipid absorption was studied in rats. Under acute conditions with surfactant infused intraduodenally with a lipid meal absorbed lipid accumulated abnormally in the enterocytes. This effect was quickly reversed after terminating treatment.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
  • 非人类毒性摘录
实验室动物:亚慢性或前慢性暴露/多聚氧化烯2930,一种疏水性表面活性剂,被加入到动脉硬化饮食中,剂量水平为饮食的0.5%和1%,并喂养给兔子10周。另一组仅接受普通动脉硬化饮食,对照组则喂养普通饲料。在此期间后,通过离心分离血清脂蛋白并进行分析。动脉硬化饮食的兔子的脂蛋白组成异常。每个脂蛋白分组的胆固醇:甘油三酯比例显著增加,极低密度脂蛋白的胆固醇:蛋白比例也是如此。补充多聚氧化烯2930可以预防这些变化。在所有动脉硬化饮食组中,极低密度脂蛋白(VLDL)和高密度脂蛋白(HDL)中的载脂蛋白E的百分比增加。在多聚氧化烯处理的兔子中,即使血清胆固醇水平正常或略有增加,这种情况也会发展。可以得出结论,多聚氧化烯2930对脂蛋白具有全身性影响,这可能有助于其抗动脉硬化作用。
/LABORATORY ANIMALS: Subchronic or Prechronic Exposure/ Poloxalene 2930, a hydrophobic surfactant, was incorporated into an atherogenic diet at dose levels, 0.5% and 1% of the diet, and fed to rabbits for 10 weeks. Another group received plain atherogenic diet alone and a control group was fed chow. After this period, serum lipoproteins were separated by centrifugation and analyzed. The composition of lipoproteins from rabbits on atherogenic diet was abnormal. The cholesterol: triglyceride ratio of every lipoprotein fraction was significantly increased as was the cholesterol: protein ratio of very low density lipoproteins. Supplementing the diet with Poloxalene 2930 prevented these alterations. In all groups on the atherogenic diet the percentage of apolipoprotein E in VLDL and HDL increased. In the case of Poloxalene-treated rabbits this developed even though serum cholesterol levels were normal or slightly increased. It is concluded that Poloxalene 2930 has a systemic effect on lipoproteins which may contribute to its antiatherogenic action.
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
  • 吸收
在健康志愿者中,经过48小时的连续静脉输注纯化后的P188,稳态浓度(Css)的平均值为522 ± 118 mg/L,负荷剂量结束时的最高浓度大约为909 ± 165 mg/L。血浆浓度与剂量成正比。
Following a 48-hour continuous intravenous infusion of purified P188 in healthy volunteers, the mean concentration of P188 at steady state concentration (Css) was 522 ± 118 mg/L and the maximum concentration occurring at the end of the loading dose was approximately 909 ± 165 mg/L. The plasma concentrations were dose-proportional.
来源:DrugBank
吸收、分配和排泄
  • 消除途径
在健康的男性受试者中,肾清除率占总血浆清除率的90%。
Renal clearance accounted for 90% of total plasma clearance in healthy male subjects.
来源:DrugBank
吸收、分配和排泄
  • 分布容积
在连续静脉输注500毫克/千克P188的第7天,怀孕雌性大鼠的稳态分布容积(Vss)约为2.13毫升/千克。在接受720毫克/千克/天剂量的狗中,Vss为876毫升/千克。
The volume of distribution at steady state (Vss) after a continuous intravenous infusion of 500 mg/kg of P188 on day 7 was approximately 2.13 mL/kg in pregnant female rats. Vss was 876 mL/kg in dogs receiving a dose of 720 mg/kg/day.
来源:DrugBank
吸收、分配和排泄
  • 清除
在健康志愿者中,经过48小时的连续静脉输注纯化后的P188,仅使用血浆浓度数据估算出的平均总身体清除率为4.40 ± 0.77升/小时。从尿液中排出的P-188的量估算出的平均肾清除率为5.21 ± 1.28升/小时。单个代谢物HW1的清除速度慢于母化合物。
Following a 48-hour continuous intravenous infusion of purified P188 in healthy volunteers, the mean total body clearance was estimated to be 4.40 ± 0.77 L/h when using the plasma concentration data only. Estimated mean renal clearance from the amount of P-188 excreted in urine was 5.21 ± 1.28 L/h. The clearance of a single metabolite HW1 was slower than the parent compound.
来源:DrugBank
吸收、分配和排泄
14C-Poloxalene 2930(PX)的吸收和排泄,PX 是一种大分子量的非离子疏水表面活性剂,通过胆瘘大鼠进行研究。大约一半的剂量通过十二指肠内输注被吸收,部分被吸收的表面活性剂随胆汁排出。其余部分通过尿液排出。在研究结束时,仅在肝脏和尸体中回收到微量的14C-PX。还进行了两项研究,将14C-PX掺入饮食中。在为期7天的第一次喂养研究中,大多数药剂在停止治疗后的72小时内通过胃肠道排出。在第二项研究中,大鼠被喂养含14C-PX的饮食7、14或23天,以确定随着测试期的延长,表面活性剂是否继续在体内积累。在第七天和第十四天之间确实发生了进一步积累,但当喂养持续总共23天时,并未发生。在喂养23天后摄入的14C-PX量中,基本上在停止治疗后的7天内全部排出。这些研究表明,尽管14C-PX的大分子量约为3,000,但仍有部分被吸收。此外,吸收的物质会迅速通过胆汁和尿液排出,体内组织中保留很少。
Absorption and excretion of 14C-Poloxalene 2930 (PX), a nonionic hydrophobic surfactant of large molecular weight, were studied using bile fistula rats. Approximately half of the dose infused intraduodenally was absorbed and some of the absorbed surfactant was excreted in bile. The remainder was excreted in urine. Only trace quantities of the 14C-PX were recovered in liver and carcass at termination of the study. Two studies were also performed with 14C-PX incorporated into the diet. In the first feeding study of 7 days duration, most of the agent was excreted via the gastrointestinal tract within 72 hr of discontinuing treatment. In the second study, rats were fed dietary 14C-PX for 7, 14, or 23 days to determine whether the surfactant continued to accumulate in the body as the test period was extended. Further accumulation did occur between the 7th and 14th days but not when feeding was continued for a total of 23 days. Of the amount of 14C-PX ingested after 23 days of feeding, essentially all was excreted by the end of 7 days after discontinuing treatment. These studies indicate that despite its large molecular weight of about 3,000 some 14C-PX is absorbed. Furthermore, absorbed material is promptly excreted in bile and urine with little retained in body tissues.
来源:Hazardous Substances Data Bank (HSDB)

制备方法与用途

简介

聚氧丙烯聚氧乙烯共聚物溶液(PEO-PPO-PEO),是一种通过共价键连接亲水的PEO链段与疏水的PPO链段形成的高分子化合物,属于非离子型的高分子表面活性剂。其商品名包括Pluronic(由BASF公司生产)或Poloxamer(由ICI公司生产)。然而,由于聚氧丙烯聚氧乙烯共聚物溶液本身结构中端羟基的活性较小,限制了其在多个领域的广泛应用。因此,对其端羟基进行修饰化,制备系列衍生物非常必要。其中一个重要的方法是将聚氧丙烯聚氧乙烯共聚物溶液进行羧基化。

应用

作为高分子非离子表面活性剂,聚氧丙烯聚氧乙烯共聚物溶液广泛应用于消泡剂、乳化剂、破乳剂、润滑剂、增稠剂、洗涤剂以及化妆品、食品和药品的添加剂等领域。与低分子表面活性剂相比,这类共聚物具有更低的临界胶束浓度、多样化的分子化学组成结构及由此导致的不同两亲性质,并具备极低的毒性、良好的生物相容性和蛋白抗性等优势。这使得它们在废水处理、介孔材料制备、生物医用材料、药物载体研究、动物细胞培养和生物大分子分离等方面展现出广泛的应用前景。

反应信息

  • 作为反应物:
    描述:
    参考文献:
    名称:
    IN SITU BULKING COMPOSITION
    摘要:
    本发明涉及一种水合的、生物相容的组织增强化合物及其植入哺乳动物组织的方法。该组织增强化合物由活体组织、可选的体液和至少一种由有机多异氰酸酯衍生的NCO-末端亲水性聚氨酯预聚物和含氧乙烯基二醇或多元醇组成,其中基本上所有的羟基都被聚异氰酸酯封顶。
    公开号:
    US20110135700A1
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文献信息

  • Esters of aromatic alkoxylated alcohols and fatty carboxylic acids
    申请人:——
    公开号:US20030181744A1
    公开(公告)日:2003-09-25
    Esters of alkoxylated aromatic alcohol and fatty carboxylic acid are provided. The esters are especially suitable as additives for personal care and cosmetic products. The preferred esters having an aromatic nucleus, an alkoxy spacer, an ester carboxylic group, and a fatty alkyl group, in which the aromatic nucleus and the oxygen atom of the ester carboxylic group are connected to the alkoxy spacer, and the fatty alkyl group is attached to the carbon atom of the ester carboxylic group, are also provided. Certain of the esters of alkoxylated aromatic alcohol and fatty carboxylic acid having certain skin spread factor or viscosity are also provided.
    提供了烷氧基化芳香醇和脂肪羧酸的酯。这些酯特别适用于个人护理和化妆品产品的添加剂。优选酯具有芳香核、烷氧间隔、酯羧基和脂肪烷基,其中芳香核和酯羧基的氧原子连接到烷氧间隔,脂肪烷基附着在酯羧基的碳原子上。还提供了具有特定皮肤扩散因子或粘度的某些烷氧基化芳香醇和脂肪羧酸的酯。
  • Surfactant treated polyolefinic microporous materials capable of
    申请人:Celanese Corporation
    公开号:US04501793A1
    公开(公告)日:1985-02-26
    Disclosed are hydrophilic polyolefinic microporous materials and a method for the preparation thereof. Such materials are prepared by impregnating a normally hydrophobic polyolefinic microporous substrate material with a solution of a nonionic alkylphenoxy poly(ethyleneoxy) ethanol surfactant having an HLB of from about 10 to 15 in a solvent system comprising from about 55 to about 65 volume percent methanol or acetone and from about 35 to about 45 volume percent water. It has been discovered that polyolefinic microporous materials rendered hydrophilic by this technique not only wet rapidly, but in addition may be multiply re-wet with aqueous solutions, such as aqueous alkali solutions, with excellent retention of their hydrophilic properties. The hydrophilic polyolefinic microporous materials of this invention find particular application as battery separators and as membranes for use in various chemical, medical and biotechnical processes.
    本发明涉及亲水性聚烯烃微孔材料及其制备方法。这种材料是通过将非离子烷基苯氧基聚(乙氧基)乙醇表面活性剂的HLB值在大约10到15之间的溶液浸渍到通常具有疏水性的聚烯烃微孔基材料中,在包含大约55至65体积%甲醇或丙酮和大约35至45体积%水的溶剂体系中制备的。发现通过这种技术使聚烯烃微孔材料变得亲水性不仅能够快速湿润,而且可以用水溶液,如水性碱溶液,多次重复湿润,并保持其亲水性能。本发明的亲水性聚烯烃微孔材料特别适用于用作电池隔膜和用于各种化学、医学和生物技术过程的膜。
  • Compositions containing esters of aromatic alkoxylated alcohols and fatty carboxylic acids
    申请人:——
    公开号:US20030161792A1
    公开(公告)日:2003-08-28
    A personal care or cosmetic product composition that includes from about 0.1% to about 99% of at least one ester of alkoxylated aromatic alcohol and fatty carboxylic acid, and from about 0.1% to 60% of at least one functional ingredient is provided. The functional ingredients in the composition may include active ingredients and additional ingredients. Especially suitable active ingredients are sunscreen active ingredients and antiperspirant active ingredients. Preferred compositions are sunscreen product formulations and antiperspirant products. In one preferred embodiment, the composition further includes at least one cyclomethicone compound present in the amount of from about 1% to 99% by weight of the composition. A method of improving the protection of human or animal skin or hair from radiation and a method of improving the protection of human or animal skin or hair from perspiration are also provided.
    提供一种个人护理或化妆品组合物,其中包括约0.1%至约99%的至少一种醚化芳香醇和脂肪羧酸酯,以及约0.1%至60%的至少一种功能性成分。组合物中的功能性成分可以包括活性成分和附加成分。特别适合的活性成分是防晒活性成分和止汗活性成分。首选组合物是防晒产品配方和止汗产品。在一种首选实施例中,该组合物进一步包括至少一种环甲基硅氧烷化合物,其重量占组合物的约1%至99%。还提供了一种改善人类或动物皮肤或头发对辐射的保护的方法和一种改善人类或动物皮肤或头发对汗水的保护的方法。
  • Linear polydimethylsiloxane-polyoxyalkylene block copolymers linked via Si-C groups and via carboxylic ester groups, a process for preparing them and their use
    申请人:Evonik Goldschmidt GmbH
    公开号:US07754778B2
    公开(公告)日:2010-07-13
    The invention provides linear polydimethylsiloxane-polyoxyalkylene block copolymers containing Si—C groups and carboxylic ester groups and having repeating (A1BA2B) units where A1 and A2 are two different polydimethylsiloxane units of the general formula (I) with a number of Si atoms N=(n+2) of 15≦N≦30 and NA1≠NA2 and B is a unit of the formula (II) —CH2—CH2—(CH2)a—CO[O—CH2—CH(R)]c—O-[D-O]e—[—CH2—CH(R)—O]d—OC—(CH2)b—CH2—CH2— (II) where R independently at each occurrence is H, —CH3 or —C2H5, a and b independently of one another are 0 to 20, c and d independently of one another are values≧1, e is 0 or 1 and D is a hydrocarbon radical having 2 to 10 C atoms, the overall molar weight of the unit of the formula II being from 600 to 10 000 g/mol, with the proviso that the average mixed molar weight of the polydimethylsiloxane units (A1+A2) is from >1665 to <1998 g/mol and the fraction of [O—CH2—CH(R)] with R═H is >0% to ≦50% by weight, based on the overall weight of [O—CH2—CH(R)] in B, a process for preparing them and their use.
    本发明提供了含有Si-C基团和羧酸酯基团的线性聚二甲基硅氧烷-聚氧烷嵌段共聚物,其具有重复的(A1BA2B)单元,其中A1和A2是通式(I)的两个不同的聚二甲基硅氧烷单元,其具有Si原子数N =(n + 2)为15≦N≦30和NA1≠NA2,B是通式(II)的一个单元 -CH2-CH2-(CH2)a-CO [O-CH2-CH(R)] c-O- [D-O] e- [—CH2-CH(R) -O] d-OC-(CH2)b-CH2-CH2-(II),其中R在每次出现时独立地是H,-CH3或-C2H5,a和b彼此独立地为0至20,c和d彼此独立地为值≧1,e为0或1,D是具有2至10个C原子的碳氢基团,式II的单元的总摩尔质量为600至10,000 g / mol,但前提是聚二甲基硅氧烷单元(A1 + A2)的平均混合摩尔质量为> 1665至<1998 g / mol,[O-CH2-CH(R)]的分数,其中R = H的重量占B中[O-CH2-CH(R)]的总重量的> 0%至≦50%,以其制备的过程及其用途。
  • Ink, ink cartridge and ink jet recording process
    申请人:CANON KABUSHIKI KAISHA
    公开号:US09388322B2
    公开(公告)日:2016-07-12
    The invention provides an ink for use in an ink jet recording process in which an ink is ejected from a recording head by the action of thermal energy, the ink comprising a pigment, a water-soluble polyurethane polymer, a compound represented by a general formula (1) having a weight-average molecular weight of 1,000 or more and 8,500 or less, and a polyethylene oxide alkyl ether, the alkyl group of which has 12 or more carbon atoms, wherein, based on the total mass of the ink, the content (mass %) of the compound represented by the general formula (1) is 0.4 times or more and 10.0 times or less in terms of mass ratio with respect to the content (mass %) of the polyethylene oxide alkyl ether.
    该发明提供了一种用于喷墨记录过程的墨水,其中墨水通过热能作用从记录头中喷出,所述墨水包括颜料、水溶性聚氨酯聚合物、由重量平均分子量为1,000或更多且不超过8,500的通式(1)表示的化合物和聚乙烯氧化物烷基醚,其中烷基的碳原子数为12或更多,基于墨水的总质量,所述通式(1)表示的化合物的含量(质量%)相对于聚乙烯氧化物烷基醚的含量(质量%)以质量比为0.4倍或更多,但不超过10.0倍。
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