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头孢氨苄单盐酸盐 | 105879-42-3

中文名称
头孢氨苄单盐酸盐
中文别名
盐酸头孢氨苄
英文名称
cephalexin hydrochloride monohydrate
英文别名
(6R,7R)-7-[[(2R)-2-amino-2-phenylacetyl]amino]-3-methyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid;hydron;chloride;hydrate
头孢氨苄单盐酸盐化学式
CAS
105879-42-3
化学式
C16H17N3O4S*ClH*H2O
mdl
——
分子量
401.871
InChiKey
YHJDZIQOCSDIQU-OEDJVVDHSA-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

  • 颜色/状态:
    CRYSTALS
  • 溶解度:
    SLIGHTLY SOL IN WATER; PRACTICALLY INSOL IN ALC, CHLOROFORM, ETHER
  • 稳定性/保质期:

    ACID-STABLE

  • 解离常数:
    PKA: 5.2, 7.3

计算性质

  • 辛醇/水分配系数(LogP):
    0.04
  • 重原子数:
    26
  • 可旋转键数:
    4
  • 环数:
    3.0
  • sp3杂化的碳原子比例:
    0.31
  • 拓扑面积:
    139
  • 氢给体数:
    5
  • 氢受体数:
    7

ADMET

毒理性
  • 相互作用
利尿剂苯溴马隆(Probenecid)能有效减缓尿液清除速度并增强头孢氨苄(Cephalexin)的系统抗菌活性持续时间。
PROBENECID IS EFFECTIVE IN SLOWING URINARY CLEARANCE & ENHANCING DURATION OF SYSTEMIC ANTIMICROBIAL ACTIVITY /OF CEPHALEXIN/.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
  • 相互作用
头孢菌素类...可能会受到同时使用...磺吡酮的影响。肾小管分泌减少...可能导致更高的和更持续的血清平,因此加强药物活性。/头孢菌素类/
...CEPHALOSPORINS...MAY BE AFFECTED BY CONCURRENT USE OF...SULFINPYRAZONE. DIMINISHED TUBULAR SECRETION...RESULT IN HIGHER & MORE SUSTAINED SERUM LEVELS & HENCE, INTENSIFICATION OF DRUG ACTIVITY. /CEPHALOSPORINS/
来源:Hazardous Substances Data Bank (HSDB)
毒理性
  • 相互作用
呋塞米可能增强头孢菌素的肾毒性。/头孢菌素/
FUROSEMIDE MAY ENHANCE NEPHROTOXICITY OF CEPHALOSPORINS. /CEPHALOSPORINS/
来源:Hazardous Substances Data Bank (HSDB)
毒理性
  • 相互作用
由于水杨酸盐和/或头孢菌素的大剂量引起的低凝血酶原血症,以及非甾体抗炎药(NSAIDs)、水杨酸盐或磺啦嗪的胃肠道溃疡性或出血倾向可能会增加出血的风险。/头孢菌素/
Hypoprothrombinemia induced by large doses of salicylates and/or cephalosporins, and the gastrointestinal ulcerative or hemorrhagic potential of nonsteroidal anti-inflammatory drugs (NSAIDs), salicylates, or sulfinpyrazone may increase the risk of hemorrhage. /Cephalosporins/
来源:Hazardous Substances Data Bank (HSDB)
毒理性
  • 解毒与急救
头孢克通过血液透析或腹膜透析有效地从循环中清除。
CEPHALEXIN IS EFFICIENTLY REMOVED FROM CIRCULATION BY HEMODIALYSIS OR PERITONEAL DIALYSIS.
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
小于10%至15%...与血浆蛋白结合,血浆药物浓度迅速下降...超过90%...在6小时内以原形通过尿液排出,主要是通过肾小管分泌。...即使在肾功能减退的病人尿液中,仍可达到治疗有效的浓度。
LESS THAN 10 TO 15%...IS BOUND TO PLASMA PROTEIN, & PLASMA DRUG CONCN FALL RAPIDLY... MORE THAN 90%...IS EXCRETED UNALTERED IN URINE WITHIN 6 HR, PRIMARILY BY RENAL TUBULAR SECRETION. ...THERAPEUTICALLY EFFECTIVE CONCN ARE STILL ACHIEVED IN URINE OF PT WITH DECR RENAL FUNCTION.
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
CEPHALEXIN(头孢克)从胃肠道吸收良好。口服250毫克和500毫克后,血药浓度峰值分别在大约1小时后达到大约9和18微克/毫升。食物的摄入可能会延迟吸收。
CEPHALEXIN...IS WELL ABSORBED FROM GI TRACT. PEAK PLASMA CONCN, REACHED @ ABOUT 1 HR AFTER INGESTION OF DRUG, ARE APPROX 9 & 18 UG/ML AFTER ORAL DOSES OF 250 & 500 MG, RESPECTIVELY. INGESTION OF FOOD MAY DELAY ABSORPTION.
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
CEPHALEXIN 也会排泄到胆汁中。
CEPHALEXIN IS ALSO EXCRETED INTO BILE.
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
新生儿的头孢克吸收和排泄都受到影响,其中24小时尿液中抗生素的回收量占每日口服剂量的5-66%。
BOTH ABSORPTION & EXCRETION OF CEPHALEXIN ARE IMPAIRED IN NEW-BORN INFANTS, WHERE 24-HR URINARY RECOVERY OF ANTIBIOTIC ACCOUNTED FOR 5-66% OF DAILY ORAL DOSE.
来源:Hazardous Substances Data Bank (HSDB)

SDS

SDS:07a723223402b15cbd10ad03f0cfbef7
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制备方法与用途

头孢氨苄盐酸盐合物是一种高效且口服活性的新型半合成头孢菌素抗生素,具有广泛的抗菌谱。它对多种革兰氏阳性菌和阴性菌都具有抗菌活性。这种药物以青霉素结合蛋白(PBP)为靶点,抑制细菌细胞壁组装。主要用于研究肺炎、链球菌性咽喉炎和细菌性心内膜炎等疾病。[1][2]

反应信息

  • 作为反应物:
    描述:
    头孢氨苄单盐酸盐甲醇 为溶剂, 生成 、 头孢氨苄
    参考文献:
    名称:
    Process for preparing cephalexin monohydrate
    摘要:
    通过对7-ADCA进行硅化反应制备的单水合头孢氨苄,当硅化步骤在沸点超过100度的溶剂中回流时,可以获得高产率和改善纯度的产物。
    公开号:
    US05142043A1
  • 作为产物:
    参考文献:
    名称:
    一种头孢氨苄原料及胶囊剂的制备方法
    摘要:
    本发明公开了一种头孢氨苄原料的制备方法,包括以下步骤:(1)将左旋苯甘氨酸酯类衍生物缓慢加入到7-ADCA水溶液中,加入固定化青霉素酰化酶反应;(2)调节反应液黏度,用青霉素酰化酶分离器分离出酶,将头孢氨苄混悬液进行离心过滤得到头孢氨苄粗粉和滤液;(3)将滤液洗涤酶,分离出酶,将头孢氨苄混悬液离心过滤得到头孢氨苄粗粉和滤液,合并头孢氨苄粗粉;(4)重复步骤(3),至流出料液澄清;(5)混合全部头孢氨苄粗粉和滤液,用硫酸调pH,0.45μm滤膜过滤得料液,将料液温度升高,用氨水调节料液pH,然后养晶、过滤、水洗涤、丙酮洗涤,最后干燥,得终产物头孢氨苄产品。本发明头孢氨苄制备方法使头孢氨苄与酶分离容易。
    公开号:
    CN105274177A
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文献信息

  • Dendrimers as molecular translocators
    申请人:Goodman Murray
    公开号:US20060216265A1
    公开(公告)日:2006-09-28
    Transport molecules include a dendrimer and a biologically active molecule. The dendrimer of such transport molecules includes at least one guanidine group, at least one protonated guanidine group, at least one protected guanidine group, at least one amidine group, at least one protonated amidine group, at least one protected amidine group, at least one ureido group, at least one protonated ureido group, at least one protected ureido group, at least one thioureido group, at least one protonated thioureido group, or at least one protected thioureido group. The biologically active molecule is bonded to the dendrimer. A method of increasing the bioavailability of a drug includes bonding the drug to a dendrimer of the invention.
    转运分子包括一种树枝状聚合物和一种生物活性分子。这些转运分子的树枝状聚合物包括至少一个基团、至少一个质子化的基团、至少一个保护的基团、至少一个酰胺基团、至少一个质子化的酰胺基团、至少一个保护的酰胺基团、至少一个基团、至少一个质子化的基团、至少一个保护的基团、至少一个硫脲基团、至少一个质子化的硫脲基团,或至少一个保护的硫脲基团。生物活性分子与树枝状聚合物结合。一种增加药物生物利用度的方法包括将药物与本发明的树枝状聚合物结合。
  • [EN] NANOPARTICLE FORMULATIONS AND USES THEROF<br/>[FR] FORMULATIONS DE NANOPARTICULES ET LEURS UTILISATIONS
    申请人:ABRAXIS BIOSCIENCE LLC
    公开号:WO2010118365A1
    公开(公告)日:2010-10-14
    The present invention provides compositions comprising nanoparticles comprising: 1) a drug, such as a hydrophobic drug derivative; and 2) a carrier protein. Also provided are methods of treating diseases (such as cancer) using the compositions, as well as kits and unit dosages.
    本发明提供了包含纳米粒子的组合物,其中包括:1)药物,如疏性药物衍生物;和2)载体蛋白。还提供了使用这些组合物治疗疾病(如癌症)的方法,以及套件和单元剂量。
  • Porous drug matrices and methods of manufacture thereof
    申请人:Acusphere Inc.
    公开号:US20020142050A1
    公开(公告)日:2002-10-03
    Drugs, especially low aqueous solubility drugs, are provided in a porous matrix form, preferably microparticles, which enhances dissolution of the drug in aqueous media. The drug matrices preferably are made using a process that includes (i) dissolving a drug, preferably a drug having low aqueous solubility, in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution and hydrophilic or hydrophobic excipients that stabilize the drug and inhibit crystallization, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of drug. Hydrophobic or hydrophilic excipients may be selected to stabilize the drug in crystalline form by inhibiting crystal growth or to stabilize the drug in amorphous form by preventing crystallization. The pore forming agent can be either a volatile liquid that is immiscible with the drug solvent or a volatile solid compound, preferably a volatile salt. In a preferred embodiment, spray drying is used to remove the solvents and the pore forming agent. The resulting porous matrix has a faster rate of dissolution following administration to a patient, as compared to non-porous matrix forms of the drug. In a preferred embodiment, microparticles of the porous drug matrix are reconstituted with an aqueous medium and administered parenterally, or processed using standard techniques into tablets or capsules for oral administration.
    药物,特别是低溶性药物,以多孔性矩阵形式提供,最好是微粒,这可以增强药物在性介质中的溶解。药物矩阵最好是使用包括以下步骤的过程制备的:(i)将药物,最好是低溶性药物,溶解在挥发性溶剂中形成药物溶液,(ii)将至少一种孔形成剂与药物溶液结合形成乳液、悬浮液或第二溶液和亲或疏的赋形剂,以稳定药物并抑制结晶,(iii)从乳液、悬浮液或第二溶液中除去挥发性溶剂和孔形成剂,以得到多孔性的药物矩阵。亲或疏的赋形剂可以被选择用于通过抑制晶体生长来稳定药物的晶体形式,或者用于通过防止结晶来稳定药物的非晶形式。孔形成剂可以是与药物溶剂不相溶的挥发性液体或挥发性固体化合物,最好是挥发性盐。在一个优选实施例中,喷雾干燥用于除去溶剂和孔形成剂。所得到的多孔性矩阵在给患者治疗后具有更快的溶解速率,与非多孔性药物矩阵形式相比。在一个优选实施例中,多孔性药物矩阵的微粒被重组性介质,并通过标准技术处理成口服片剂或胶囊剂进行口服给药。
  • [EN] TOPICAL FORMULATIONS BASED ON IONIC SPECIES FOR SKIN TREATMENT<br/>[FR] FORMULATIONS TOPIQUES A BASE D'ESPÈCES IONIQUES POUR LE TRAITEMENT DE LA PEAU
    申请人:UNIV CALIFORNIA
    公开号:WO2018044920A1
    公开(公告)日:2018-03-08
    Compositions containing a complex that contains a cation with alkyl chains and a macromolecule anion, and methods of making and using are disclosed. The compositions are typically charge neutral and a liquid at room temperature and standard pressure. The macromolecule anions may be nucleic acids, peptides, proteins, and/or carbohydrates. The compositions have enhanced penetration across the skin barrier (stratum corneum) and into the skin cells, delivering the macromolecules to the skin cells. The compositions are topically applied to the skin and are particularly useful for treatment of skin conditions.
    本发明揭示了含有含有烷基链阳离子和大分子阴离子的复合物的组合物及其制备和使用方法。这些组合物通常是电中性的,且在常温和标准压力下呈液态。大分子阴离子可以是核酸、肽、蛋白质和/或碳水化合物。这些组合物可以增强穿透皮肤屏障(角质层)并进入皮肤细胞,将大分子输送到皮肤细胞中。这些组合物可局部应用于皮肤,尤其适用于治疗皮肤状况。
  • Sustained release pharmaceutical formulation for inhalation
    申请人:——
    公开号:US20040105821A1
    公开(公告)日:2004-06-03
    Pharmaceutical formulations and methods are provided for the sustained delivery of a pharmaceutical agent to the lungs of a patient by inhalation. The formulation includes porous microparticles which comprise a pharmaceutical agent and a matrix material, wherein upon inhalation of the formulation a therapeutically or prophylactically effective amount of the pharmaceutical agent is released from the microparticles in the lungs for at least 2 hours. Preferably, a majority of the pharmaceutical agent is released from the microparticles by 24 hours following inhalation, for example where a majority of the pharmaceutical agent is released no earlier than about 2 hours and no later than about 24 hours following inhalation. Methods for delivering a pharmaceutical agent, such as a corticosteroid, to the lungs of a patient are also provided. For example, the method includes having the patient inhale a dry powder blend comprising the present microparticles and a pharmaceutically acceptable bulking agent.
    提供了一种药物制剂和方法,通过吸入将药物剂量持续释放到患者的肺部。该制剂包括多孔微粒,其中包括药物剂量和基质材料,吸入该制剂后,肺部至少释放出治疗或预防有效剂量的药物剂量,持续时间至少为2小时。最好,药物剂量的大部分在吸入后的24小时内从微粒中释放出来,例如,药物剂量的大部分在吸入后不早于约2小时,不晚于约24小时内释放。还提供了将药物剂量(例如皮质类固醇)传递到患者肺部的方法。例如,该方法包括让患者吸入包括当前微粒和药用可接受的增容剂的干粉混合物。
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同类化合物

(6R,7R)-7-苯基乙酰胺基-3-[(Z)-2-(4-甲基噻唑-5-基)乙烯基]-3-头孢唑啉-4-羧酸二苯甲基酯 顺式-4-(2,2-二甲氧基乙基)-3-邻苯二甲酰-2-氮杂环丁酮 顺式-3-氨基-1-(2,4-二甲氧基苄基)-4-甲氧羰基-2-氮杂环丁酮 顺式-1-(对甲苯基)-3-苄氧基-4-(对茴香基)-氮杂环丁烷-2-酮 顺式-1,4-二苯基-3-(甲基苯基氨基)-2-氮杂环丁酮 青霉酰聚赖氨酸 青霉素钾 青霉素钠 青霉素酶液体 青霉素杂质F氢化物 青霉素杂质C 青霉素亚砜酯(GESO) 青霉素V二苄乙二胺 青霉素G衍生物 青霉素G甲酯 青霉素G甲酯 青霉素G-D7 青霉素 V 钠 阿那白滞素 阿莫西林钠 阿莫西林三水合物 阿莫西林 阿立必利D5 阿度西林 铜(2+)酞菁-29,30-二负离子-2-(二甲氨基)乙醇(1:1:1) 钾(2S,5R,6R)-6-[[2-[(E)-3-氯丁-2-烯基]巯基乙酰基]氨基]-3,3-二甲基-7-氧代-4-硫杂-1-氮杂双环[3.2.0]庚烷-2-羧酸酯 钠6-[[3-(2-氯-6-氟苯基)-5-甲基1,2-恶唑-4-羰基]氨基]-3,3-二甲基-7-氧代-4-硫杂-1-氮杂双环[3.2.0]庚烷-2-羧酸盐水合物 钠(6S,7R)-3-(羟基甲基)-7-甲氧基-8-氧代-7-[(2-噻吩基乙酰基)氨基]-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸酯 钠(6R,7R)-7-[[(2Z)-2-(2-氨基-1,3-噻唑-4-基)-2-甲氧基亚氨基乙酰基]氨基]-8-氧代-3-[(2S)-四氢呋喃-2-基]-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸酯 钠(2S,5R,6R)-6-[(2-叠氮基-2-苯基乙酰基)氨基]-3,3-二甲基-7-氧代-4-硫杂-1-氮杂双环[3.2.0]庚烷-2-羧酸盐 酞氨西林 赖氨酸氯尼辛 萘夫西林钠 萘夫西林钠 萘夫西林杂质 苯磺酸,2-[(2-羟基-1-萘基)偶氮]-5-甲基-,盐(2:1)钡 苯甘孢霉素亚砜 苯氧乙基青霉素钾 苯并[b]噻吩-3-羧酸,2-[3-氯-2-(4-硝基苯基)-4-羰基-1-吖丁啶基]-4,5,6,7-四氢-,乙基酯 苯唑西林钠 苯唑西林杂质1 舒巴坦杂质19 舒他西林 脱乙酰基戊二酰 7-氨基头孢烷酸 脱乙酰基头孢噻肟 肟莫南 羰苄西林苯酯钠 美罗培南钠盐 美罗培南 美洛培南