Sultamicillin
(Synonyms: 舒他西林) 目录号 : GC64190
Sultamicillin is a newly developed antibiotic in which ampicillin and the β-lactamase inhibitor sulbactam are linked as an ester.
Cas No.:76497-13-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Sultamicillin is a newly developed antibiotic in which ampicillin and the β-lactamase inhibitor sulbactam are linked as an ester.
| Cas No. | 76497-13-7 | SDF | Download SDF |
| 别名 | 舒他西林 | ||
| 分子式 | C25H30N4O9S2 | 分子量 | 594.66 |
| 溶解度 | DMSO : 100mg/mL | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6816 mL | 8.4082 mL | 16.8163 mL |
| 5 mM | 0.3363 mL | 1.6816 mL | 3.3633 mL |
| 10 mM | 0.1682 mL | 0.8408 mL | 1.6816 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Sultamicillin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use
Drugs 1989 Apr;37(4):491-522.PMID:2661196DOI:10.2165/00003495-198937040-00005.
Sultamicillin is the tosylate salt of the double ester of sulbactam plus ampicillin. Sulbactam is a semisynthetic beta-lactamase inhibitor which, in combination with ampicillin, extends the antibacterial activity of the latter to include some beta-lactamase-producing strains of bacteria that would otherwise be resistant. The combination of sulbactam plus ampicillin for parenteral use has previously been shown to be clinically and bacteriologically effective in a variety of infections. The chemical linkage of sulbactam and ampicillin has now produced an orally effective compound, Sultamicillin, with antibacterial activity and clinical efficacy which are similar to those of the parenteral formulation. Sultamicillin has been shown to be clinically effective in non-comparative trials in patients with infections of the respiratory tract, ears, nose and throat, urinary tract, skin and soft tissues, as well as in obstetric and gynaecological infections, and in the treatment of gonorrhoea. In a small number of controlled trials, Sultamicillin has shown comparable clinical efficacy to phenoxymethyl penicillin (penicillin V) and to amoxycillin (alone and in combination with clavulanic acid) in the treatment of paediatric streptococcal pharyngitis and acute otitis media, respectively; to cefaclor in the treatment of acute otitis media in adults; and to bacampicillin, cloxacillin and flucloxacillin plus ampicillin in skin and soft tissue infections in adults, children and adult diabetic patients, respectively. Sultamicillin was superior in efficacy to bacampicillin in the treatment of chronic respiratory infections, to cefaclor in the treatment of acute otitis media in adults, and to cefadroxil in the treatment of patients with complicated urinary tract infections. However, in single-dose treatment of uncomplicated gonorrhoea, Sultamicillin (1500mg plus probenecid 1g) was inferior to a 2g intramuscular dose of spectinomycin. While in several studies the incidence of diarrhoea associated with Sultamicillin was greater than that with comparative antibacterials, sultamicillin-associated diarrhoea was generally mild and transitory, although occasionally severe enough to necessitate discontinuation of treatment. Further studies in larger groups of patients are needed to clarify the therapeutic efficacy and safety of Sultamicillin in comparison with other antibacterial regimens, and to determine the optimum single dosage for the treatment of gonorrhoea. Nonetheless, Sultamicillin appears to provide a similar pharmacodynamic and pharmacokinetic profile to that of parenteral sulbactam plus ampicillin and, as such, will extend the therapeutic efficacy of ampicillin, with the further advantage of allowing treatment of patients with an oral formulation, thus avoiding the potentially adverse clinical and financial effects of prolonged parenteral therapy.
The pharmacokinetics of Sultamicillin
APMIS Suppl 1989;5:17-22.PMID:2660866doi
Sultamicillin is a mutual prodrug of ampicillin and sulbactam, a beta-lactamase inhibitor. When administered orally, Sultamicillin is readily absorbed and rapidly hydrolyzed to provide high levels of its two constituents in the peripheral circulation. Peak serum concentrations of ampicillin are achieved that are approximately three and one-half times those obtained with an equivalent amount of oral ampicillin. Equimolar concentrations of sulbactam are also provided, with both ampicillin and sulbactam being widely distributed among various body fluids and tissues. The pharmacokinetic parameters of the two components are similar, both being eliminated primarily by renal excretion. Although the elimination half-lives of ampicillin and sulbactam are each approximately 1 hour, the high serum concentrations achieved coupled with their synergistic bactericidal activity permit twice-daily dosing.
Worldwide clinical experience with Sultamicillin
APMIS Suppl 1989;5:23-34.PMID:2660868doi
Sultamicillin at an adult dose of 375-750 mg twice daily or a pediatric dose of 50 mg/kg/d provides effective outpatient/office therapy for community-acquired infections of the upper and lower respiratory tract, urinary tract, and skin/soft tissue structures. Given the incidence of Haemophilus influenzae and Branhamella catarrhalis in otitis media and the frequent occurrence of beta-lactamase-producing strains, it is particularly appropriate for the therapy of otitis media in infants and children. The increasing prevalence of beta-lactamase-producing pathogens in these infections, coupled with the fact that diagnostic bacteriology is often not available or practical in office practice, suggests that the broad use of Sultamicillin might be desirable. Several factors support such usage: 1) the superiority of Sultamicillin compared with the ampicillin commercial dosage form as a delivery system for ampicillin; 2) the possible occurrence at the infection site of beta-lactamase-producing organisms, not themselves pathogens, which nevertheless impair the activity of the beta-lactam antibiotic against sensitive pathogens; 3) the complementary binding of penicillin-binding proteins by ampicillin and sulbactam in ampicillin-sensitive organisms; 4) the lack of resistance development following repeated exposure of strains sensitive to sulbactam/ampicillin suggested by in vitro studies; and 5) the inability of sulbactam to induce beta-lactamase production. In addition to broad use in community-acquired infections, oral therapy with Sultamicillin should also provide convenient outpatient follow-up for initial parenteral sulbactam/ampicillin therapy. Extensive testing of various laboratory parameters has revealed no evidence of systemic toxicity with Sultamicillin. The only significant side effect of Sultamicillin is diarrhea/loose stools, which, although a frequent complaint in some studies, is of mild to moderate severity and results in a low discontinuation rate.
In vitro evaluation of 99m Tc-sultamicillin for infection imaging
Biopharm Drug Dispos 2021 Jun;42(6):285-293.PMID:33904176DOI:10.1002/bdd.2281.
Early detection of the site of infection non-invasively with radiolabeled molecules is important for the success of treatment. Technetium-99m labeled antibiotics have the potential to discriminate between bacterial infection and sterile inflammation. Sultamicillin is the tosylate salt of the double ester of sulbactam plus ampicillin. In this study, Sultamicillin was labeled with 99m Tc according to the stannous chloride method. Quality control studies of radiolabeled Sultamicillin were performed by radiochromatographic methods. In vitro binding assays were performed in live and heat-killed gram-positive Staphylococcus aureus and gram-negative Escherichia coli strains. The radiolabeling yield of 99m Tc-sultamicillin was determined as 97.8% ± 3.1% (n = 5). The maximum bacterial uptake of 99m Tc-sultamicillin was 80.7% ± 11.00% at 4 h for living S. aureus and 93.2% ± 4.40% at 2 h for E. coli. Bacterial uptake study results show that Sultamicillin has the potential to be a nuclear imaging agent, especially in infections caused by gram-negative E. coli and gram-positive S. aureus.
Sultamicillin experiences in the field of internal medicine
APMIS Suppl 1989;5:51-6.PMID:2660872doi
Sultamicillin is a substance in which sulbactam, a beta-lactamase inhibitor, is covalently linked through an ester group to ampicillin. This paper describes the results of a clinical trial with Sultamicillin in the infectious diseases encountered in internal medicine. In an open segment of the trial, 426 adult patients were treated orally with Sultamicillin. The efficacy rates achieved were 86.1% (136/158) in acute respiratory infections, 67.5% (137/203) in chronic respiratory infections, 92.9% (39/42) in acute urinary tract infections, 76.9% (10/13) in chronic urinary tract infections, and 70.0% (7/10) in other types of infections. The bacteriological efficacy of Sultamicillin was 83.8% (62/74) for Gram-positive and 74.0% (159/215) for Gram-negative bacteria. Efficacy was similar, 81% (17/21), for those strains that were high producers of beta-lactamase. Adverse reactions were observed in 10.1% of the patients in the open phase of the trial. In the double-blind segment, Sultamicillin was compared with bacampicillin in respiratory infections, including pneumonia, lung abscesses, and chronic respiratory tract infections. One tablet of either drug was given orally three times a day for 14 d. Evaluation of clinical effectiveness by the trial committee revealed efficacy rates of 82.8% (96/116) for Sultamicillin and 69.8% (81/116) for bacampicillin, indicating a significant superiority for Sultamicillin. All of this difference resulted from the superior efficacy of Sultamicillin (89.2%) over that of bacampicillin (63.2%) in patients with chronic respiratory infections. Efficacy in pneumonia was the same for both agents. Adverse reactions to Sultamicillin and bacampicillin were observed in 16.3% (21/129) and 6.3% (8/127) of the cases, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)