抗生素头孢泊肟（头孢泊肟酸）对革兰氏阴性厌氧菌（Bacteroidetesceae）的最低抑菌浓度（MIC）为0.125-4 mg/L。观察到头孢泊肟抑制小韦荣球菌的 MIC 值为 0.25-8 mg/L。头孢泊肟可抑制糖酵解链球菌、微小消化链球菌和布氏瘤胃球菌，最低抑制浓度 (MIC) 低于每升 2 毫克 [1]。头孢泊肟或头孢泊肟酸可抑制肺炎链球菌和化脓性链球菌的菌群。菌落形成单位[2]。

在治疗方面，小鼠对头孢菌素（2.5 至 50 mg/kg；口服；每 8 小时一次；连续 48 小时）反应良好 [3]。

Animal/Disease Models: Female Swiss CD1 mice [3]
Doses: 2.5, 5, 10, 25, 40 and 50 mg/kg
Route of Administration: Oral;
Route of Administration: Oral. Every 8 hrs (hrs (hours)); 48 hour
Experimental Results: Efficacy value >350 obtained.

Absorption, Distribution and Excretion
Cefpodoxime proxetil is a prodrug that is absorbed from the gastrointestinal tract and then deesterified to its active metabolite, cefpodoxime. In fasting subjects, approximately 50% of the administered dose of 100 mg cefpodoxime proxetil is absorbed systemically. Within the recommended dose range (100 to 400 mg), approximately 29% to 33% of the administered dose is excreted unchanged in the urine within 12 hours. Biological Half-Life 2.09 to 2.84 hours

Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation
Limited information suggests that low concentrations of cefpodoxime in breast milk are not expected to have any adverse effects on breastfed infants. There are reports that cephalosporins occasionally disrupt the infant's gut microbiota, leading to diarrhea or thrush, but these effects have not been adequately assessed. Cefpodoxime is safe for use by breastfeeding women.
◉ Effects on Breastfed Infants
No published information found as of the revision date.
◉ Effects on Lactation and Breast Milk
A 40-year-old non-pregnant woman developed hyperprolactinemia and bilateral galactorrhea after taking cefpodoxime 200 mg twice daily for two days. Seven days after discontinuation of the medication, the galactorrhea resolved, and serum prolactin levels significantly decreased to the normal range. One month later, prolactin levels decreased further. Since no other cause was found, the authors believe that the galactorrhea and hyperprolactinemia were most likely caused by cefpodoxime. A 22-year-old woman was taking extended-release venlafaxine 150 mg/day for 3 months. Two weeks ago, she started taking cefpodoxime 200 mg/day for 14 days. Afterward, she experienced bilateral breast engorgement and galactorrhea, lasting for 3 days. Laboratory tests and a head CT scan were normal, with only a slight increase in alkaline phosphatase and elevated serum prolactin levels. Within two weeks, her galactorrhea began to lessen and disappeared after three weeks, during which time the venlafaxine dose remained unchanged. Her serum prolactin levels also returned to normal. The authors believe that her symptoms and hyperprolactinemia were likely caused by cefpodoxime. Prolactin levels in mothers who have established lactation may not affect their ability to breastfeed. Serum protein binding rate: 22% to 33%, plasma protein binding rate: 21% to 29%.

[1]. Werner H, et, al. Comparative in vitro activity of cefpodoxime against anaerobes other than Bacteroides fragilis. Infection. 1991 Sep-Oct;19(5):377-9.
[2]. Valentini S, et, al. In-vitro evaluation of cefpodoxime. J Antimicrob Chemother. 1994 Mar;33(3):495-508.
[3]. Pérez-Trallero E, et, al. Prediction of in-vivo efficacy by in-vitro early bactericidal activity with oral beta-lactams, in a dose-ranging immunocompetent mouse sepsis model, using strains of Streptococcus pneumoniae with decreasing susceptibilities to penicillin. J Chemother. 2001 Apr;13(2):118-25.

Cefpodoxime is a third-generation cephalosporin antibiotic. Its cephalosporin skeleton has methoxymethyl and (2Z)-2-(2-amino-1,3-thiazolyl)-2-(methoxyimino)acetamino substituents at positions 3 and 7, respectively. It is administered orally as an ester prodrug for the treatment of acute otitis media, pharyngitis, and sinusitis. It is an antibacterial drug. It belongs to the cephalosporin and carboxylic acid classes. Cefpodoxime is an oral third-generation cephalosporin antibiotic effective against most Gram-positive and Gram-negative bacteria. Cefpodoxime proxetil is commonly used to treat acute otitis media, pharyngitis, and sinusitis. It is a prodrug that is deesterified into cefpodoxime after absorption through the intestinal mucosa. Cefpodoxime is a cephalosporin antibacterial drug. Cefpodoxime is a third-generation semi-synthetic cephalosporin and also a β-lactam antibiotic with bactericidal activity. Cefpodoxime's mechanism of action involves binding to penicillin-binding proteins (PBPs) located on the bacterial cell membrane. Upon binding, transpeptidase activity is inhibited, preventing the cross-linking of the pentaglycine bridge to the fourth amino acid residue of the pentapeptide, thereby blocking peptidoglycan chain synthesis. Therefore, cefpodoxime inhibits the synthesis of bacterial septa and cell walls. Cefpodoxime is a third-generation cephalosporin antibiotic. Its cephalosporin core contains a methoxy group at the C-3 position. See also: cefpodoxime proxetil (active ingredient); cefpodoxime sodium (active ingredient). Indications: For the treatment of mild to moderate infections caused by susceptible strains of specified microorganisms. FDA Label: Cefpodoxime is effective against a variety of Gram-positive and Gram-negative bacteria. Cefpodoxime is stable in the presence of β-lactamases. Therefore, many microorganisms resistant to penicillin and cephalosporins due to the production of β-lactamases may be sensitive to cefpodoxime. Cefpodoxime is inactivated by certain extended-spectrum β-lactamases. The bactericidal activity of cefpodoxime stems from its inhibition of cell wall synthesis. The active metabolite of cefpodoxime preferentially binds to penicillin-binding protein 3, thereby inhibiting the synthesis of peptidoglycan (a major component of bacterial cell walls).

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Pharmacodynamics
Cefpodoxime is effective against most Gram-positive and Gram-negative bacteria, but ineffective against Pseudomonas aeruginosa, Enterococcus, and Bacteroides fragilis.

C15H17N5O6S2

427.46

427.062

80210-62-4

Cefpodoxime-d3;2477791-28-7

6335986

White to off-white solid powder

1.8±0.1 g/cm3

200-202ºC

1.780

0.94

209.98

3

11

7

28

744

2

C(C1=C(COC)CS[C@@H]2[C@@H](C(N12)=O)NC(=O)/C(/C1=CSC(N)=N1)=N\OC)(=O)O

WYUSVOMTXWRGEK-HBWVYFAYSA-N

InChI=1S/C15H17N5O6S2/c1-25-3-6-4-27-13-9(12(22)20(13)10(6)14(23)24)18-11(21)8(19-26-2)7-5-28-15(16)17-7/h5,9,13H,3-4H2,1-2H3,(H2,16,17)(H,18,21)(H,23,24)/b19-8-/t9-,13-/m1/s1

5-Thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7-(((2-amino-4-thiazolyl)(methoxyimino)acetyl)amino)-3-(methoxymethyl)-8-oxo-, (6R-(6alpha,7beta(Z)))-

U76253AR-3746 U-76253AR3746 R 3763 U 76253AR-3763 R3763

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中，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 : ~250 mg/mL (~584.85 mM)

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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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。