β-lactam

克拉维酸和氨苄西林表现出协同抗菌活性（针对产生 β-内酰胺酶的微生物）[2]。
Ab11 和 Ab51 菌株在 MIC 为 2–8 μg/mL 时被克拉维酸抑制[3]。

克拉维酸（13 mg/kg，腹腔注射）可降低鲍曼不动杆菌感染的 C57BL/6 小鼠肺炎模型的肺部细菌负荷[3]。克拉维酸（13 mg/kg，ip）在 Ab51 感染的 C57BL/6 小鼠肺炎模型中的 t1/2 为 6.69 h，AUC 为 4.03 mg·h/L[3]。
角叉菜胶 (HY-125474) 引起的爪水肿在用克拉维酸（100–300 mg/kg，腹腔注射）治疗时表现出抗炎作用[4]。

Absorption, Distribution and Excretion
Clavulanic acid is well absorbed in the gastrointestinal tract after oral administration. In a study of four subjects, the minimum absorption rate was 73%, and the mean absolute bioavailability was 64%. In a pharmacokinetic study of eight healthy volunteers, the mean Cmax was 2.098 ± 0.441 μg/mL. The mean Tmax reported in this study was 1.042 ± 0.80 hours. Another pharmacokinetic study reported Tmax ranging from 40 to 120 minutes. Approximately 40% to 65% of clavulanic acid is excreted unchanged in the urine within 6 hours after administration. Metabolites of clavulanic acid are primarily excreted via urine, feces, and carbon dioxide in exhaled air. Clavulanic acid can be eliminated via renal and non-renal routes. Approximately 17% of the dose of radiolabeled clavulanic acid is excreted in exhaled air, and 8% is excreted in feces. A study of four healthy volunteers showed a volume of distribution of 12 liters after administration of radiolabeled clavulanic acid. Clavulanic acid is distributed in various tissues and interstitial fluids. Clinically significant concentrations have been detected in the gallbladder, abdomen, skin, fat, and muscle tissues. Therapeutic concentrations of clavulanic acid have also been detected in bile, pus, synovial fluid, and peritoneal fluid. Animal studies have shown that clavulanic acid can cross the placenta. A pharmacokinetic study in four healthy volunteers showed a clearance of 0.21 L/min after administration of radiolabeled clavulanic acid. Another study showed a mean clearance of 12.20 L/h/70 kg. Dosage adjustments may be necessary for patients with renal failure.

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Metabolism/Metabolites
Clavulanic acid is primarily metabolized to two metabolites: 2,5-dihydro-4-(2-hydroxyethyl)-5-oxo-1H-pyrrole-3-carboxylic acid and 1-amino-4-hydroxy-but-2-one. One pharmacokinetic study found that the first metabolite accounted for 15.6% of the dose, and the second metabolite accounted for 8.8%.

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Biological Half-Life
According to reports, clavulanic acid has a half-life similar to that of amoxicillin, lasting 45-90 minutes. A study of radiolabeled clavulanic acid in four healthy volunteers determined its half-life to be 0.8 hours.

Protein Binding
Amoxicillin has a plasma protein binding rate of approximately 25%.

[1]. Clavulanic acid: a review. Biotechnol Adv. Jul-Aug 2008;26(4):335-51

[2]. Clavulanic acid, a novel inhibitor of beta-lactamases. Antimicrob Agents Chemother. 1978 Nov;14(5):650-5.

[3]. In vitro activity and in vivo efficacy of clavulanic acid against Acinetobacter baumannii. Antimicrob Agents Chemother. 2009 Oct;53(10):4298-304.

[4]. Tannic acid exhibits anti-inflammatory effects on formalin-induced paw edema model of inflammation in rats. Hum Exp Toxicol. 2019 Nov;38(11):1296-1301.

Clavulanic acid is an antibiotic isolated from Streptomyces clavuligerus. It is a suicidal β-lactamase inhibitor that inhibits the activity of bacterial β-lactamases. Clavulanic acid has multiple effects, including antibacterial, anti-anxiety, and EC 3.5.2.6 (β-lactamase) inhibition. It is a conjugate of clavulanic acid. Clavulanic acid is a β-lactamase inhibitor, often used in combination with amoxicillin or ticarcillin. By preventing β-lactamases from degrading the antibiotic, it broadens the antibacterial spectrum against susceptible bacterial infections, thus combating antibiotic resistance. Clavulanic acid is derived from Streptomyces clavuligerus. When used in combination with amoxicillin, clavulanic acid is often called Augmentin, Co-Amoxiclav, or Clavulin. Clavulanic acid is a β-lactamase inhibitor. Clavulanic acid's mechanism of action is as a β-lactamase inhibitor. It has been reported to be present in Streptomyces cattleya and Streptomyces clavuligerus, with supporting data. Clavulanic acid is a semi-synthetic β-lactamase inhibitor isolated from Streptomyces. It contains a β-lactam ring that binds firmly to the active site of β-lactamase or its vicinity, thereby inhibiting enzyme activity. This protects other β-lactam antibiotics from β-lactamase catalysis, thus enhancing their antibacterial activity. This drug is often used in combination with antibiotics sensitive to β-lactamases (such as penicillin and cephalosporins) to treat infections caused by β-lactamase-producing microorganisms. Streptomyces clavuligerus is a β-lactam antibiotic produced by actinomycetes. It is a suicide inhibitor of bacterial β-lactamases. When used alone, it has weak antibacterial activity against most microorganisms, but when used in combination with other β-lactam antibiotics, it can prevent microbial β-lactamases from inactivating the antibiotics.

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Drug Indications
Clavulanic acid, when used in combination with other antibiotics, can prevent the emergence of drug-resistant strains and enhance their antibacterial therapeutic effects.
The following diseases, when the pathogens produce β-lactamases, can be treated with amoxicillin/clavulanic acid or ticarcillin/clavulanic acid in combination: acute otitis media caused by Haemophilus influenzae and Moraxella catarrhalis; sinusitis caused by Haemophilus influenzae and Moraxella catarrhalis; lower respiratory tract infections caused by Haemophilus influenzae, Staphylococcus aureus, Klebsiella spp., and Moraxella catarrhalis; skin and soft tissue infections caused by Staphylococcus aureus, Escherichia coli, and Klebsiella spp.; urinary tract infections caused by Escherichia coli, Klebsiella spp., Enterobacter spp., Serratia marcescens, or Staphylococcus aureus; and gynecological infections caused by various bacteria, including Pseudomonas melanogenans, Enterobacter spp., Escherichia coli, and Klebsiella spp. Septicemia caused by Staphylococcus aureus and Staphylococcus epidermidis; septicemia caused by various bacteria (including Klebsiella spp., Escherichia coli spp., Staphylococcus aureus, or Pseudomonas spp.); bone and joint infections caused by Staphylococcus aureus; intra-abdominal infections caused by Escherichia coli, Klebsiella pneumoniae, or Bacteroides fragilis. Regarding drug susceptibility: It is important to note that this product is only indicated for infections confirmed or highly suspected to be caused by susceptible bacteria. Bacterial culture and drug susceptibility testing should be performed whenever possible, and this should be used as the basis for determining whether to use this antibiotic. Clavulanic acid should not be used if β-lactamase production is not detected in microbiological testing. When these tests are not possible, the local infection pattern and drug susceptibility test results can be used to determine whether clavulanic acid is appropriate. Ticarcillin combined with clavulanate potassium has shown particular efficacy in mixed infections and can be used as empirical treatment before determining the drug susceptibility of the causative bacteria. The ticarcillin-clavulanate potassium combination may be an effective monotherapy for treating infections that usually require multiple drug combinations.

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Mechanism of Action
The structure of potassium clavulanate contains a β-lactam ring, which can irreversibly bind to β-lactamases, thereby preventing β-lactamases from inactivating certain β-lactam antibiotics and effectively treating infections caused by Gram-positive and Gram-negative bacteria that are sensitive to β-lactam antibiotics.

199.048

58001-44-8

Potassium clavulanate cellulose;Clavulanate lithium;61177-44-4;Clavulanate potassium;61177-45-5

5280980

Off-white to light yellow solid powder

1.7±0.1 g/cm3

545.8±50.0 °C at 760 mmHg

117.5-118
117.5 - 118 °C

283.9±30.1 °C

0.0±3.3 mmHg at 25°C

1.644

-1.98

87.07

2

5

2

14

324

2

C(=C/1\[C@H](C(=O)O)N2C(=O)C[C@H]2O1)/CO

HZZVJAQRINQKSD-PBFISZAISA-N

InChI=1S/C8H9NO5/c10-2-1-4-7(8(12)13)9-5(11)3-6(9)14-4/h1,6-7,10H,2-3H2,(H,12,13)/b4-1-/t6-,7-/m1/s1

(2R,3Z,5R)-3-(2-hydroxyethylidene)-7-oxo-4-oxa-1-azabicyclo[3.2.0]heptane-2-carboxylic acid

Clavulanate; Acide clavulanique; Acido clavulanico; Clavulansaeure; Antibiotic MM 14151; acidum clavulanicum;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： (1). 本产品在运输和储存过程中需避光。  (2). 请将本产品存放在密封且受保护的环境中（例如氮气保护），避免吸湿/受潮。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~13.89 mg/mL (~69.74 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (12.55 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (12.55 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: 10% DMSO+90% (20% SBE-β-CD in Saline): ≥ 2.5 mg/mL (12.55 mM)

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配方 4 中的溶解度: 12.5 mg/mL (62.76 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶 (<60°C).

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。