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Sucralfate | 54182-58-0

中文名称
——
中文别名
——
英文名称
Sucralfate
英文别名
——
Sucralfate化学式
CAS
54182-58-0
化学式
C12H54Al9O55S8
mdl
——
分子量
1577.9
InChiKey
YZPQNHUVIVIUCT-JTJNLBSYSA-F
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:
    >220°C (dec.)
  • 沸点:
    1990℃ at 101.325kPa
  • 密度:
    0.338 at 20℃
  • 溶解度:
    几乎不溶于水、乙醇(96%)和二氯甲烷。溶于无机酸和碱金属氢氧化物的稀溶液。
  • LogP:
    1.46 at 25℃ and pH7

计算性质

  • 辛醇/水分配系数(LogP):
    -27.32
  • 重原子数:
    84
  • 可旋转键数:
    37
  • 环数:
    2.0
  • sp3杂化的碳原子比例:
    1.0
  • 拓扑面积:
    536
  • 氢给体数:
    20
  • 氢受体数:
    55

ADMET

代谢
这种药物以非常小的量被吸收,并且不被显著代谢。
This drug is absorbed in very small quantities and is not significantly metabolized.
来源:DrugBank
毒理性
  • 毒性总结
过量服用:在给予几种动物最大剂量达12克/千克/体重的情况下,并未观察到死亡,因此无法确定其致死剂量。人类过量服用胃溃宁可能导致便秘,建议采取支持性治疗。 孕妇使用:该药物被认为是妊娠B类药物。在啮齿类动物和兔子上进行了剂量高达推荐人类剂量50倍的研究,未观察到对胎儿的危害。尚未在孕妇中进行足够且控制良好的临床试验。由于动物研究的结果并不总是与人类反应相关,因此胃溃宁只有在认为对母亲健康至关重要时才应在孕期使用。 哺乳期使用:目前尚不清楚该药物是否会在人类乳汁中排泄。许多药物都会在乳汁中排泄,因此,如果给哺乳期妇女服用胃溃宁,应谨慎。 致癌性:在啮齿类动物中进行了为期24个月的毒性研究,胃溃宁的剂量达到了1克/千克(相当于推荐人类剂量的12倍),未观察到与胃溃宁相关的肿瘤迹象。
**Overdose** Overdosage has never been observed with sucralfate. It is unlikely, as administering a maximum dose of up to 12 g/kg/body weight in several animal species did not result in death. The lethal dose could not be determined in these studies. It is likely that overdose of sucralfate in humans would result in constipation, and supportive treatment would be advised. **Use in pregnancy** This drug is considered a pregnancy Category B drug. Studies have been performed in rodents and rabbits at doses up to 50 times the recommended human dose. No harm to the fetus has been observed in the abovementioned studies. Sufficient and well-controlled clinical trials have not been performed in pregnant women. Due to the fact that the results of animal studies are not always relevant to human response, sucralfate should be used during pregnancy only if it is deemed essential for the mother's health. **Use in nursing** Whether this drug is excreted in human milk is currently unknown. Many drugs are excreted in breast milk, therefore, if sucralfate is administered to a lactating and nursing woman, caution should be observed. **Carcinogenesis** 24 month toxicity studies were performed in rodents, and the dose of sucralfate reached up to 1 g/kg (equivalent to 12 times the recommended human dose). No signs of sucralfate-related tumors were noted.
来源:DrugBank
毒理性
  • 药物性肝损伤
Sucralfate
Compound:sucralfate
来源:Drug Induced Liver Injury Rank (DILIrank) Dataset
毒理性
  • 药物性肝损伤
DILI 注释:无 DILI(药物性肝损伤)担忧
DILI Annotation:No-DILI-Concern
来源:Drug Induced Liver Injury Rank (DILIrank) Dataset
毒理性
  • 药物性肝损伤
标签部分:无匹配
Label Section:No match
来源:Drug Induced Liver Injury Rank (DILIrank) Dataset
毒理性
  • 药物性肝损伤
参考文献:M Chen, V Vijay, Q Shi, Z Liu, H Fang, W Tong. 美国食品药品监督管理局批准的药物标签用于研究药物诱导的肝损伤,《药物发现今日》,16(15-16):697-703, 2011. PMID:21624500 DOI:10.1016/j.drudis.2011.05.007 M Chen, A Suzuki, S Thakkar, K Yu, C Hu, W Tong. DILIrank:按人类发展药物诱导肝损伤风险排名的最大参考药物清单。《药物发现今日》2016, 21(4): 648-653. PMID:26948801 DOI:10.1016/j.drudis.2016.02.015
References:M Chen, V Vijay, Q Shi, Z Liu, H Fang, W Tong. FDA-Approved Drug Labeling for the Study of Drug-Induced Liver Injury, Drug Discovery Today, 16(15-16):697-703, 2011. PMID:21624500 DOI:10.1016/j.drudis.2011.05.007 M Chen, A Suzuki, S Thakkar, K Yu, C Hu, W Tong. DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. Drug Discov Today 2016, 21(4): 648-653. PMID:26948801 DOI:10.1016/j.drudis.2016.02.015
来源:Drug Induced Liver Injury Rank (DILIrank) Dataset
吸收、分配和排泄
  • 吸收
这种药物从胃肠道吸收的量非常少。吸附的硫酸化双糖通过尿液排出。该药物含有铝,在每天四次服用1克硫糖铝后,大约有0.001%到0.017%的铝含量被肾功能正常的患者吸收。预计这个数字在肾功能受损的患者中会增加。
This drug is absorbed from the gastrointestinal tract in very minimal quantities. The adsorbed sulfated disaccharide is excreted in the urine. This drug contains aluminum and after the administration of 1 g of sucralfate 4 times per day, about 0.001% to 0.017% of this aluminum content is absorbed in patients with normal renal function. This number is expected to increase in those with impaired renal function.
来源:DrugBank
吸收、分配和排泄
  • 消除途径
这种药物被吸收的微不足道的量主要在48小时内通过尿液排出。
The negligible amount of this drug that is absorbed is excreted mainly in the urine within 48 hours.
来源:DrugBank
吸收、分配和排泄
  • 分布容积
这种药物吸收量非常小,通常局限于发炎的胃肠病变部位。
This drug is absorbed in a very small quantity, and normally localizes to inflamed gastrointestinal lesions.
来源:DrugBank
吸收、分配和排泄
  • 清除
Sucralfate含有铝。在非透析慢性肾衰竭患者中给予Sucralfate需要治疗医师仔细考虑,因为吸收的铝的排泄可能会减少,可能导致可能的铝中毒。在诊断为慢性肾衰竭的透析患者中,已经观察到并报告了与Sucralfate相关的铝中毒。在与其他也含有铝的药物(包括各种抗酸药)联合使用Sucralfate之前,应仔细检查每日铝摄入量(包括Sucralfate)。
Sucralfate contains aluminum. The administration of sucralfate in non-dialyzed chronic renal failure patients warrants careful consideration from the treating physician as the excretion of absorbed aluminum may be decreased, causing possible aluminum toxicity. In dialyzed patients diagnosed with chronic renal failure, aluminum toxicity related to sucralfate has been observed and reported. The daily amount of aluminum ingestion (including sucralfate) should be carefully examined before administering sucralfate in combination with other drugs also containing aluminum, including various antacids.
来源:DrugBank

安全信息

  • WGK Germany:
    2
  • 海关编码:
    29400090
  • 危险品运输编号:
    NONH for all modes of transport
  • 危险性防范说明:
    P261,P305+P351+P338
  • 危险性描述:
    H302,H315,H319,H335

制备方法与用途

硫糖铝性状

硫糖铝为白色无定形粉末,无臭,几乎无味,并具有引湿性。它在稀盐酸和氢氧化钠中溶解,但几乎不溶于水、乙醇及氯仿。

适应症

硫糖铝适用于胃及十二指肠溃疡、胃炎、胃一食管反流病以及胃酸过多等病症的治疗。

作用机制

硫糖铝在酸性环境中解离成八硫酸盐蔗糖聚合物,可黏附于溃疡底部与胃黏膜蛋白结合,形成保护屏障。此外,它还能与胃蛋白酶结合,抑制其蛋白分解活动,并具有持久的中和胃酸作用。

动力学

口服后,硫糖铝释放出铝离子及硫酸蔗糖复合离子,少量可被胃肠道吸收并通过尿液排出。在慢性肾功能不全患者中,血清及尿中的铝浓度显著升高。

生物活性

Sucralfate 是一种蔗糖硫酸-铝复合体,能够与溃疡面结合形成物理屏障,从而保护胃肠道免受胃酸腐蚀,并阻止黏液降解。

体外研究

研究表明,Sucralfate 可能通过位阻效应干扰肠上皮细胞与胶原I的粘附,抑制肠上皮细胞的运动性。它还能保护RGM1细胞免受酸性和胃蛋白酶损害。

体内研究

体内的研究显示,Sucralfate 对抗急性辐射结肠炎的作用可能是通过抑制由p53介导的凋亡过程,并保护结肠上皮干细胞来实现的。

用途

硫糖铝用于治疗胃溃疡及十二指肠溃疡、制酸以及抑制胃蛋白酶的作用。