Mezlocillin (sodium salt)
(Synonyms: 美洛西林钠) 目录号 : GC47671
A β-lactam antibiotic
Cas No.:59798-30-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Mezlocillin is a β-lactam antibiotic and derivative of ampicillin .1,2 It is active against B. fragilis, E. lentum, P. morbillorum, and F. nucleatum (MICs = 8, 4, 2, and 4 µg/ml, respectively).2 Mezlocillin (32 µg/ml) is also active against 10 strains of S. faecalis.1 In vivo, mezlocillin (240 mg/kg) increases survival and reduces bacteremia in a rabbit model of S. faecalis endocarditis. It completely eliminates lung P. morbillorum, E. lentum, and F. nucelatum, but not B. fragilis, in a rabbit model of pulmonary P. morbillorum, E. lentum, F. nucelatum, and B. fragilis infection when administered at a dose of 300 mg/kg.2 Formulations containing mezlocillin have been used in the treatment of various bacterial infections.
1.Fass, R.J., and Wright, C.A.Comparative efficacies of mezlocillin and ampicillin alone or in combination with gentamicin in the treatment of Streptococcus faecalis endocarditis in rabbitsAntimicrob. Agents Chemother.25(4)408-410(1983) 2.Chandrasekar, P.H., Rolston, K.V.I., Chokkavelu, C., et al.Comparative efficacy of four antibiotics in anaerobic pulmonary infection. An experimental model in rabbitsChemotherapy30(5)331-336(1984)
| Cas No. | 59798-30-0 | SDF | |
| 别名 | 美洛西林钠 | ||
| Canonical SMILES | O=C(N1CCN(S(C)(=O)=O)C1=O)NC(N[C@H](C2=CC=CC=C2)C(N[C@@H]3C(N4[C@]3([H])SC(C)(C)[C@@H]4C([O-])=O)=O)=O)=O.[Na+] | ||
| 分子式 | C22H25N6O9S2.Na | 分子量 | 604.6 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,PBS (pH 7.2): 10 mg/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 | 1.654 mL | 8.2699 mL | 16.5399 mL |
| 5 mM | 0.3308 mL | 1.654 mL | 3.308 mL |
| 10 mM | 0.1654 mL | 0.827 mL | 1.654 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。
Stability of Mezlocillin sodium as determined by high-performance liquid chromatography
J Pharm Sci 1983 Dec;72(12):1479-81.PMID:6663491DOI:10.1002/jps.2600721230.
The stability of Mezlocillin sodium solutions in water with either phosphate buffers or other ingredients used in intravenous admixtures (dextrose, fructose, and sodium chloride) has been studied using a stability-indicating high-performance liquid chromatographic method. This assay shows a relative standard deviation of 1.42% based on six injections. The optimum stability was shown at an approximate pH of 4.8, and solutions in dextrose (5%) and sodium chloride (0.9%) were stable for up to 4 days at 25 degrees, 36 days at 5 degrees, and for 60 days at -10 degrees. When refrigerated, the solutions in 5% fructose and 10% dextrose were as stable as those in 5% dextrose.
Compatibility of verapamil hydrochloride with penicillin admixtures during simulated Y-site injection
Am J Hosp Pharm 1988 Jan;45(1):142-5.PMID:3348228doi
The compatibility of verapamil hydrochloride during simulated Y-site injection with i.v. admixtures containing 11 different penicillins was studied. Admixtures of penicillin G potassium (62.5 mg/mL), nafcillin sodium (40 mg/mL), oxacillin sodium (40 mg/mL), ampicillin sodium (40 mg/mL), carbenicillin disodium (40 mg/mL), methicillin sodium (40 mg/mL), ticarcillin sodium (40 mg/mL), azlocillin sodium (40 mg/mL), Mezlocillin sodium (40 mg/mL), piperacillin sodium (40 mg/mL), and amdinocillin (20 mg/mL) were prepared in both 5% dextrose injection and 0.9% sodium chloride injection in minibags. Verapamil hydrochloride injection 4 mL (10 mg) was then added to each admixture, and the admixtures were examined macroscopically and microscopically for precipitate immediately and at 15 minutes and 24 hours after mixing. To simulate Y-site injection of verapamil, verapamil hydrochloride injection 1 mL (2.5 mg) was added to 1 mL of each penicillin admixture in a test tube. For admixtures in which precipitates formed, the pH was recorded before and after verapamil was added to the admixtures. Loss of verapamil hydrochloride when mixed with the penicillin admixtures was determined using reverse-phase high-performance liquid chromatography. Addition of verapamil hydrochloride to admixtures containing nafcillin sodium, oxacillin sodium, ampicillin sodium, and Mezlocillin sodium resulted in substantial loss of verapamil hydrochloride. The results for the Y-site injection study showed visible precipitation with the same penicillin admixtures. Because a precipitate formed when verapamil hydrochloride was added to nafcillin sodium, oxacillin sodium, ampicillin sodium, or Mezlocillin sodium in the diluents studied, we recommended that verapamil hydrochloride be administered separately or that the i.v. tubing be flushed thoroughly before and after this drug is administered through a Y-injection site with these penicillin admixtures.
Compatibility of gemcitabine hydrochloride with 107 selected drugs during simulated Y-site injection
J Am Pharm Assoc (Wash) 1999 Jul-Aug;39(4):514-8.PMID:10467816DOI:10.1016/s1086-5802(16)30471-5.
Objective: To evaluate the physical compatibility of gemcitabine hydrochloride (Gemzar-Eli Lilly and Company) with 107 selected drugs. Design: Controlled experimental trial. Setting: Laboratory. Interventions: Samples of 5 mL gemcitabine (as the hydrochloride salt) 10 mg/mL in 0.9% sodium chloride injection were mixed with 5 mL samples of the selected drugs diluted in 0.9% sodium chloride injection or, if necessary to avoid incompatibilities with the diluent, 5% dextrose injection. Main outcome measures: Visual examinations of the samples were performed in normal fluorescent light with the unaided eye and using a Tyndall beam (high-intensity monodirectional light) to enhance visualization of small particles and low-level haze. The turbidity of each sample was measured as well. In selected samples, electronic particle content assessment was performed. All of the samples were assessed initially and at 1 and 4 hours. Results: Most of the drugs were physically compatible with gemcitabine hydrochloride during the 4-hour observation period. However, 15 drug combinations had incompatibilities that included color change, increase in haze or turbidity, particulate formation, and gross precipitation: acyclovir sodium, amphotericin B, cefoperazone sodium, cefotaxime sodium, furosemide, ganciclovir sodium, imipenem-cilastatin sodium, irinotecan, methotrexate sodium, methylprednisolone sodium succinate, Mezlocillin disodium, mitomycin, piperacillin sodium, piperacillin sodium/tazobactam sodium, and prochlorperazine edisylate. Conclusion: Gemcitabine hydrochloride 10 mg/mL admixed in a compatible infusion solution is physically compatible for 4 hours at room temperature with 92 of 107 tested drugs. Simultaneous Y-site administration of gemcitabine hydrochloride with the 15 drugs resulting in incompatibilities should be avoided.
[Pharmacokinetics of Mezlocillin. Comparison with ampicillin and influence of probenecid (author's transl)]
Nouv Presse Med 1982 Feb 4;11(5 Pt 2):347-52.PMID:6460974doi
In a randomized cross-over study 10 healthy male volunteers received a single 1 g dose of 6-[R]-2-3-methylsulfonyl -2- oxo-imidazolisine -1- carboxamido) -2- phenyl-acetamido]-penicillanic acid sodium salt (Mezlocillin) and of ampicillin, either intravenously or intramuscularly. Following the intravenous loading dose, mean peak serum levels of 101 micrograms/ml for Mezlocillin and 91.5 micrograms/ml for ampicillin were recorded. The ultimate half-life t 1/2 of Mezlocillin (46.4 min) was slightly shorter than that of ampicillin (52.4 min). Similarly, the total volume of distribution of Mezlocillin (24.1 l) was slightly inferior to that of ampicillin (29.4 l). The proportions of the dose administered recovered in the urine of 24 hours were 50.4 % for Mezlocillin and 69.9 % for ampicillin. The total clearances of the two antibiotics were not significantly different, but the renal clearance of Mezlocillin (186.6 ml/min/1.73 m2) was significantly lower than that of ampicillin (309.5 ml/min/1.73 m2). Following intramuscular injection, the mean peak serum levels obtained were 15.6 microgram/ml with Mezlocillin and 15.1 micrograms/ml with ampicillin. The half-lives of the antibiotics were 50.0 min and 57.2 min respectively. The bioavailable fractions of Mezlocillin and ampicillin, as measured from the areas under the serum concentration curves wer 63 % and 75 % respectively of the values determined after intravenous injection. The oral administration of 1 g probenecid one hour before an intramuscular injection of Mezlocillin increased the peak serum level and area under the curve by 65 % and decreased the total clearance, renal clearance and apparent volume of distribution by 38 %, 52 %, and 35 % respectively. However, the ultimate half-life was not significantly altered (50.5 min without, and 52.0 min with probenecid).
Local tolerance of i.m. Mezlocillin injection
Arzneimittelforschung 1979;29(12a):1985-7.PMID:543907doi
To evaluate the intensity of the localized pain caused by intramuscular administration of 6-[(R)-2-[3-methylsulfonyl-2-oxo-imidazolidine-1-carboxamido]-2-phenyl-acetamido]-penicillanic acid sodium salt (Mezlocillin, Baypen), the pain was compared to that caused by ampicillin in a blind test. Ampicillin served as reference because of its extensive use. 50 patients were given 1 g of Mezlocillin and 1 g of ampicillin successively, in both gluteal regions. Ampicillin is significantly more painful than Mezlocillin. However, substantial pain is produced by both drugs. In a second study, to reduce the pain, 50 patients were given 1 g of Mezlocillin twice, one injection was given in a period of 5-7 s, and the other in a 12-15 s period. The slower injection is significantly less painful than the faster one. In conclusion, i.m. administration of Mezlocillin is less painful than that of ampicillin, and the slow injection reduces the pain of Mezlocillin administration.