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Ticarcillin disodium (Ticarcillin disodium salt) Sale

(Synonyms: 替卡西林二钠) 目录号 : GC32164

A semi-synthetic β-lactam antibiotic

Ticarcillin disodium (Ticarcillin disodium salt) Chemical Structure

Cas No.:4697-14-7

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10mM (in 1mL Water)
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100mg
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产品描述

Ticarcillin is a semisynthetic β-lactam antibiotic.1,2 It is active against P. aeruginosa, E. coli, P. mirabilis, P. rettgeri, and K. aerogenes (MICs = 4-125 μg/ml).2 Topical administration of ticarcillin (2.5 mg per eye) reduces P. aeruginosa colony count in rabbit eye.1 Formulations containing ticarcillin have been used in the treatment of a variety of bacterial infections.

1.Ahmad, A., Smolin, G., Okumoto, M., et al.Ticarcillin in the treatment of experimental pseudomonas keratitisBr. J. Ophthalmol.61(2)92-95(1977) 2.Comber, K.R., Basker, M.J., Osborne, C.D., et al.Synergy between ticarcillin and tobramycin against Pseudomonas aeruginosa and Enterobacteriaceae in vitro and in vivoAntimicrob. Agents Chemother.11(6)956-964(1977)

Chemical Properties

Cas No. 4697-14-7 SDF
别名 替卡西林二钠
Canonical SMILES O=C([C@@H](C(C)(C)S[C@]1([H])[C@@H]2NC(C(C([O-])=O)C3=CSC=C3)=O)N1C2=O)[O-].[Na+].[Na+]
分子式 C15H14N2Na2O6S2 分子量 428.39
溶解度 DMSO: 125 mg/mL (291.79 mM); Water: ≥ 100 mg/mL (233.43 mM) 储存条件 4°C, protect from light
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1 mg 5 mg 10 mg
1 mM 2.3343 mL 11.6716 mL 23.3432 mL
5 mM 0.4669 mL 2.3343 mL 4.6686 mL
10 mM 0.2334 mL 1.1672 mL 2.3343 mL
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Research Update

Antibacterial activity of ticarcillin in the presence of clavulanate potassium

Am J Med 1985 Nov 29;79(5B):13-24.PMID:3878080DOI:10.1016/0002-9343(85)90124-x.

The antibacterial effects produced by Ticarcillin disodium plus clavulanate potassium, a combination of the broad-spectrum penicillin ticarcillin, and the beta-lactamase inhibitor clavulanic acid as the potassium salt, have been measured in vitro and in experimental infection studies. The presence of clavulanic acid resulted in a significant enhancement of the activity of ticarcillin against a wide range of beta-lactamase-producing bacteria. These included ticarcillin-resistant strains of Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, P. vulgaris, Yersinia enterocolitica, and the anaerobe Bacteroides fragilis. In addition, beta-lactamase-producing isolates of Hemophilus influenzae, Branhamella catarrhalis, Neisseria gonorrhoeae, and Staphylococcus aureus were susceptible to ticarcillin and clavulanate. Clavulanic acid did not influence the activity of ticarcillin against ticarcillin-susceptible bacteria. The bactericidal effects of the antibiotic combination were measured in an in vitro kinetic model in which the drug concentrations were varied to simulate those measured in humans after intravenous dosing with ticarcillin (3.0 g) and clavulanate potassium (100 mg clavulanic acid). In these tests, ticarcillin plus clavulanic acid had pronounced bactericidal activity against ticarcillin-resistant bacteria. The protection of ticarcillin by clavulanic acid from inactivation by bacterial beta-lactamases in vivo was demonstrated in experimental infection models in which the efficacy of the ticarcillin plus clavulanic acid combination against infections caused by beta-lactamase-producing bacteria was correlated with the presence of effective concentrations of both antibiotic and inhibitor at the site of infection.

Osmolality of small-volume i.v. admixtures for pediatric patients

Am J Hosp Pharm 1990 Jun;47(6):1359-64.PMID:2368732doi

The osmolalities of pediatric i.v. admixtures were measured to identify drug concentrations in selected vehicles that would conserve fluid while maintaining osmolality values of 400 mOsm/kg or less. Test solutions were prepared by diluting appropriate volumes of freshly reconstituted powdered drug products or commercially diluted drug products with 5% dextrose injection, 0.9% sodium chloride injection, or both to provide 5 mL of each admixture at desired drug concentrations. To reduce their osmolalities, trimethoprim-sulfamethoxazole and ampicillin sodium were also diluted in 0.45% sodium chloride injection; Ticarcillin disodium was diluted only in 0.45% sodium chloride injection. A vapor pressure osmometer was used to measure osmolalities in triplicate for three solutions prepared for each admixture. Of the 63 different admixtures prepared with 5% dextrose injection or 0.9% sodium chloride injection or both, 47 (75%) had osmolalities of 400 mOsm/kg or less. At least one concentration of each selected drug diluted in these vehicles had an osmolality of less than 425 mOsm/kg, except for trimethoprim-sulfamethoxazole and ampicillin sodium. Selected concentrations of the latter two drugs and Ticarcillin disodium in 0.45% sodium chloride injection resulted in acceptable osmolalities. For most drugs diluted to the same concentration in 5% dextrose injection and 0.9% sodium chloride injection, osmolalities were lower in the dextrose solutions. Selection of an appropriate vehicle and drug concentration can control the osmolality of i.v. admixtures when the volume of fluid must be minimized, as for pediatric patients.

Stability and compatibility of topotecan hydrochloride with selected drugs

Am J Health Syst Pharm 1999 May 1;56(9):875-81.PMID:10344611DOI:10.1093/ajhp/56.9.875.

The physical and chemical compatibility of topotecan 56 microg/mL (as the hydrochloride) with 18 other drugs during simulated Y-site injection was studied. A vial of topotecan hydrochloride was reconstituted under aseptic conditions with sterile water for injection to yield a solution containing 1 mg of topotecan base per milliliter and further mixed with 0.9% sodium chloride injection or 5% dextrose injection. Equal volumes of topotecan solution and each secondary drug, also prepared in 0.9% sodium chloride injection or 5% dextrose injection, were mixed in sterile vials. All mixtures were stored at 20-23 degrees C under normal fluorescent light. Samples were taken initially and at four hours for analysis by high-performance liquid chromatography, visual inspection, and pH measurement. With a few exceptions, the drug combinations exhibited no visible change in color or clarity initially or after four hours, and the concentration of topotecan hydrochloride and of the secondary drugs was 95% or more of the initial concentration. The concentration of topotecan hydrochloride dropped to 88.7% of the initial concentration after four hours when the drug was mixed with Ticarcillin disodium and with clavulanate potassium in 5% dextrose injection. An intense yellow color and a slight haze developed immediately after topotecan hydrochloride was mixed with dexamethasone sodium phosphate or with fluorouracil in 0.9% sodium chloride injection. The topotecan-mitomycin combination in both diluents became pale purple immediately and turned dark pink-lavender within four hours, after which analysis showed 15-20% degradation of mitomycin. During simulated Y-site injection, topotecan hydrochloride was physically and chemically compatible with 15 of 18 drug products.

Stability and compatibility of admixtures of intravenous ciprofloxacin and selected drugs

Clin Ther 1996 Mar-Apr;18(2):246-55.PMID:8733985DOI:10.1016/s0149-2918(96)80005-1.

The stability and compatibility of ciprofloxacin with selected drugs in intravenous admixtures were studied. Ciprofloxacin 2 mg/mL in 5% dextrose was combined with each of 22 other drugs at concentrations commonly used in clinical practice. Each combination was maintained at room temperature (approximately 22 degrees C) in constant fluorescent light. Immediately after preparation and at 6 and 24 hours, each admixture was examined visually in normal fluorescent room light and the pH value was determined. For samples lacking visible precipitates or having pH changes of not more than 1 unit, ciprofloxacin concentration was assayed by using high-performance liquid chromatography. When combined with ciprofloxacin, 14 of the study drugs did not alter the concentration of ciprofloxacin, including amikacin sulfate, atracurium besylate, aztreonam, cimetidine hydrochloride, dobutamine hydrochloride, fluconazole, gentamicin sulfate, metronidazole (intravenous, ready to use), midazolam hydrochloride, norepinephrine bitartrate, pancuronium bromide, potassium chloride, tobramycin sulfate, and vecuronium bromide. There were five drugs that were determined to be incompatible with ciprofloxacin because of precipitate formation (amphotericin B, ampicillin sodium/sulbactam sodium, cefuroxime sodium, piperacillin sodium, and sodium bicarbonate). Incompatibility with ciprofloxacin based on pH changes of more than 1 unit was found with four drugs: ampicillin sodium/sulbactam sodium, ceftazidime, metronidazole hydrochloride (powder only), and Ticarcillin disodium/clavulanate potassium. Intravenous ciprofloxacin 2 mg/mL admixed in 5% dextrose was stable and compatible with 14 of the 22 test drugs for up to 24 hours at room temperature. The other eight drugs should not be combined with ciprofloxacin.

Effect of freezing and microwave thawing on the stability of six antibiotic admixtures in plastic bags

Am J Hosp Pharm 1982 Jan;39(1):104-8.PMID:6798865doi

The stability of six antibiotics in intravenous fluids in polyvinyl chloride containers after freezing and microwave-thawing is reported. Tobramycin sulfate 160 mg, amikacin sulfate 1 g, Ticarcillin disodium 3 g, clindamycin phosphate 300 mg, nafcillin sodium 1 g, and ampicillin sodium was also diluted in plastic bags of 0.9% sodium chloride injection 50 ml. For each antibiotic except ampicillin sodium, three bags were prepared and assayed immediately for antibiotic content. Two of the bags were frozen at -20 degrees C for 30 days and then thawed, one by exposure to room-temperature air and the other by microwave radiation. Each was assayed immediately and after 8 and 24 hours storage at room temperature. The third bag was not frozen, but was stored at room temperature and assayed at 8 and 24 hours. Five bags of ampicillin sodium were prepared-three in 0.9% sodium chloride, which were frozen at -20, -30, and -70 degrees C, and two in 5% dextrose, which were frozen at -30 and -70 degrees C. All ampicillin solutions were stored 30 days, assayed, microwave-thawed, and assayed again. All antibiotics except ampicillin retained 90% or more potency when microwave-thawed after storage at -20 degrees C for 30 days, and after subsequent storage at room temperature for 24 hours. Ampicillin sodium was stable in 0.9% sodium chloride when stored at -30 or -70 degrees C, microwave-thawed, and stored up to eight hours at room temperature. Ampicillin sodium was stable in 5% dextrose when stored at -70 degrees C and microwaved-thawed, but its potency declined to 70.5% after eight hours storage at room temperature.