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Sulfasymazine Sale

(Synonyms: 磺胺均三嗪) 目录号 : GC32304

Sulfasymazine是一种磺酰胺类药物,表现出抗菌特性。

Sulfasymazine Chemical Structure

Cas No.:1984-94-7

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实验参考方法

Animal experiment:

Carworth Farms CF-1 mice, 4 to 6 weeks of age, weighing 19 to 22 g are used in this study. The mice are infected by intraperitoneal injection of the several bacteria strains. Sulfasymazine is administered either in the diet or in a single dose by gavage. With the drug-diet method, each group of 10 mice is permitted to feed at will from 1 day before infection to 6 days after infection from a common hopper containing Sulfasymazine uniformly mixed with ground Wayne Mouse Blox. The mice are kept under conditions of alternating 3 h periods of light and dark, in order to encourage eating at more or less regular intervals throughout each 24-h period. Drug intakes, as mg per kg of body weight per day, are determined by calculations based on the initial average weight of the mice, the total diet consumed during the treatment period, and the concentration of drug in the diet[1].

References:

[1]. Redin GS, et al. An evaluation of sulfasymazine in infections in mice. Chemotherapy. 1966;11(6):309-14.

产品描述

Sulfasymazine is a sulfonamide drug and displays antibacterial properties.

Sulfasymazine is a sulfonamide drug and displays antibacterial properties. On a dosage basis, Sulfasymazine is from 2 to 10 times more potent than sulfisoxazole; on a blood level basis, Sulfasymazine potency ranges from 0.3 to 1. In acute toxicity studies in mice, the sodium salt of Sulfasymazine is tolerated at 2000 mg/kg orally, and at 1000 mg/kg intraperitoneally[1].

[1]. Redin GS, et al. An evaluation of sulfasymazine in infections in mice. Chemotherapy. 1966;11(6):309-14.

Chemical Properties

Cas No. 1984-94-7 SDF
别名 磺胺均三嗪
Canonical SMILES O=S(C1=CC=C(N)C=C1)(NC2=NC(CC)=NC(CC)=N2)=O
分子式 C13H17N5O2S 分子量 307.37
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 3.2534 mL 16.267 mL 32.5341 mL
5 mM 0.6507 mL 3.2534 mL 6.5068 mL
10 mM 0.3253 mL 1.6267 mL 3.2534 mL
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Research Update

[Clinical chronopharmacokinetics]

J Pharmacol 1984;15 Suppl 1:95-124.PMID:6374299doi

Circadian (approximately or equal to 24 hours) and other endogenous biological rhythms, detectable at all levels of organisation, constitute a temporal structure in all species, including man. Circadian, circannual, and other rhythmic changes in biological susceptibility and response of organisms to a large variety of physical and chemical agents, including medications and foods, are rather common phenomena. A better understanding of periodic and thus predictable changes in drug effects can be attained through consideration of three complementary concepts: the chronopharmacokinetics of a drug (rhythmic changes in its pharmacokinetics), the chronesthesy (rhythmic changes in susceptibility of target biosystems to the drug), and the chronergy (the drug-integrated overall effects). The chronopharmacokinetics of many drugs have been evaluated in man (tables I-IV) including sodium salicylate, aspirin, indomethacin (fig. 1), sustained-release indomethacin, paracetamol (acetaminophen), phenacetin, amidopyrine, theophylline sustained-release theophylline (fig. 2), aminophylline, sustained-release aminophylline, digitalis, propranolol, clorazepate, hexobarbitone (hexobarbital), diazepam, midazolam, lithium, phenytoin (diphenylhydantoin), nortriptyline, ethanol, erythromycine , ampicillin, Sulfasymazine , sulphanilamide, cis-diammine-dichloroplatinum (fig. 3), mequitazine (fig. 4), d-xylose, ferrous sulphate, potassium chloride, hydrocortisone and prednisolone, among others. The roles presumably played by circadium rhythms in drug metabolizing liver enzymes (fig. 5), and kidney function are summarized, and the practical implications of chronopharmacokinetics, aiming both to improve in a quantitative manner the metabolic fate of a drug and its effectiveness, are discussed.

Circadian changes of drug disposition in man

Clin Pharmacokinet 1982 Sep-Oct;7(5):401-20.PMID:6754207DOI:10.2165/00003088-198207050-00002.

Circadian (approximately equal to 24 hours) and other endogenous biological rhythms, detectable at all levels of organisation, constitute a temporal structure in all animal species, including man. Circadian, circannual, and other rhythmic changes in biological susceptibility and response of organisms to a large variety of physical and chemical agents, including medications and foods, are rather common phenomena. A better understanding of periodic and thus predictable changes in drug effects can be attained through consideration of three complementary concepts: the chronopharmacokinetics of a drug (rhythmic changes in its pharmacokinetics), the chronesthesy (rhythmic changes in susceptibility of target biosystems to the drug), and the chronergy (the drug-integrated overall effects). The chronopharmacokinetics of many drugs have been evaluated in man including sodium salicylate, aspirin, indomethacin, paracetamol (acetaminophen), phenacetin, amidopyrine, theophylline, digitalis, propranolol, clorazepate, hexobarbitone (hexobarbital), lithium, phenytoin (diphenylhydantoin), nortriptyline, ethanol, erythromycin, ampicillin, Sulfasymazine, sulphanilamide, cisplatin (cis-diammine dichloroplatinum), d-xylose, ferrous sulphate, potassium chloride, hydrocortisone and prednisolone, among others. The roles presumably played by circadian rhythms in drug metabolising liver enzymes and kidney function are summarized, and the practical implications of chronopharmacokinetics, aiming both to improve in a quantitative manner the metabolic fate of a drug and its effectiveness, are discussed.

Similar sulfonamides with different crystal structures: Sulfasymazine and sulfatriazine

Acta Crystallogr C 2008 Jun;64(Pt 6):o309-12.PMID:18535336DOI:10.1107/S0108270108011888.

The crystal structures of 4-amino-N-(4,6-diethyl-1,3,5-triazin-2-yl)benzenesulfonamide, C13H17N5O2S, and 4-amino-N-(4,6-dimethoxy-1,3,5-triazin-2-yl)benzenesulfonamide, C11H13N5O4S, also known as Sulfasymazine and sulfatriazine, respectively, are dominated by hydrogen-bond interactions. All three potential hydrogen-bond donors are employed in each case, resulting in a three-dimensional network for Sulfasymazine, while an entirely different hydrogen-bonded layer structure is obtained for sulfatriazine. This study demonstrates the versatile nature of the hydrogen-bonding capabilities in sulfonamides, even in structurally very similar molecules.

Rapid gas-liquid chromatographic method for determination of sulfathiazole in swine feed

J Assoc Off Anal Chem 1983 Mar;66(2):287-90.PMID:6853414doi

A gas-liquid chromatographic (GLC) method for determining residues of sulfathiazole (STZ) in swine feed has been developed. Feed is extracted first with acetone and then with ammonia-acetone. STZ is isolated from other feed extractives on a Sephadex LH-20 column with methanol-toluene. The sulfa residues are methylated with diazomethane, and the eluate is evaporated to dryness. A solution containing an internal standard of methyl Sulfasymazine is used to dilute the sample before injection onto an OV-25 GLC column. The precision of the method was determined by assaying 10 sets of feed spiked at 0.5, 1, 2, and 5 ppm STZ. The mean recoveries and coefficients of variation were 90.2 (5.90), 89.5 (4.67), 87.4 (5.62), and 87.7% (4.29), respectively. The critical steps of the method, including the stability of STZ, were also determined.

Rapid gas-liquid chromatographic method for determination of sulfamethazine in swine feed

J Assoc Off Anal Chem 1982 Sep;65(5):1048-53.PMID:7130074doi

A gas-liquid chromatographic method is described for the quantitative determination of trace amounts of sulfamethazine in swine feed. Sulfamethazine is extracted in ammoniated acetone and isolated from other extractants on a Sephadex LH-20 column. The eluate is methylated with diazomethane and evaporated to dryness. The residue is dissolved in a solvent containing an internal standard of methyl Sulfasymazine before being injected onto an OV-25 GLC column. An estimation of precision was established by assaying 10 sets of swine feed fortified with 0.5, 1,2, and 5 ppm SMZ. Mean recoveries were 96.0, 94.3, 93.5, and 94.0%, respectively, with an average coefficient of variation of 3.07%. The critical steps and ruggedness of the method were also determined.