What is Sarafloxacin | CAS# 98105-99-8
Sarafloxacin | CAS# 98105-99-8 is a broad-spectrum fluoroquinolone antibiotic effective against a variety of gram-negative and gram-positive organisms, especially Mycobacterium tuberculosis. Sarafloxacin HCl Trihydrate is water soluble.
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The main objective of this work was to quantify the lipophilicity of sarafloxacin | CAS# 98105-99-8 in the form of the apparent and true partition coefficient in an n-octanol/buffer system. For that purpose the ionization constants were determined by a spectrophotometric method, and the distribution profiles of microspecies in water as a function of pH for this fluoroquinolone were established.
The maximum concentration of the neutral species occurs at the sarafloxacin | CAS# 98105-99-8 isoelectric point, pH = 5.5. The apparent partition coefficient in the n-octanol/buffer system versus the pH profile of sarafloxacin | CAS# 98105-99-8 displayed a parabolic behavior that reached a maximum near the pH of the isoelectric point. The true partition coefficient was calculated from the log Papp and microconstant values and has the value of 0.846 ± 0.021.
Pharmacology and Biochemistry of Sarafloxacin | CAS# 98105-99-8
Absorption, Distribution and Excretion
Eggs were collected for 15 days after the initial drug treatment. Egg yolk and egg albumen were separated and assayed for total radioactive residues (TRR) using a combustion oxidizer and scintillation counting techniques. Radioactivity was detected in egg yolk and egg albumen on the second day of dosing and reached a maximum at 24 hr after drug withdrawal. Thereafter, the sarafloxacin | CAS# 98105-99-8 TRR levels in egg albumen declined rapidly and were undetectable 2 days after the last dose, whereas the levels in egg yolk declined at a much slower rate and were undetectable 7 days after drug withdrawal. In both the egg albumen and yolk, HPLC analysis indicated that the parent sarafloxacin | CAS# 98105-99-8 was the major component.
PMID:11141293 Chu PS et al; J Agric Food Chem 48 (12): 6409-11 (2000)
Pharmacokinetics of sarafloxacin | CAS# 98105-99-8, a fluoroquinolone antibiotic, was determined in pigs and broilers after intravenous (i.v.), intramuscular (i.m.), or oral (p.o.) administration at a single dose of 5 (pigs) or 10 mg/kg (broilers). Plasma concentration profiles were analysed by a noncompartmental pharmacokinetic method. Following i.v., i.m. and p.o. doses, the elimination half-lives were 3.37 +/- 0.46, 4.66 +/- 1.34, 7.20 +/- 1.92 (pigs) and 2.53 +/- 0.82, 6.81 +/- 2.04, 3.89 +/- 1.19 hR (broilers), respectively. After i.m. and p.o. doses, bioavailabilities (F) were 81.8 +/- 9.8 and 42.6 +/- 8.2% (pigs) and 72.1 +/- 8.1 and 59.6 +/- 13.8% (broilers), respectively. Steady-state distribution volumes (Vd(ss)) of 1.92 +/- 0.27 and 3.40 +/- 1.26 L/kg and total body clearances (ClB) of 0.51 +/- 0.03 and 1.20 +/- 0.20 L/kg/hr were determined in pigs and broilers, respectively. Areas under the curve (AUC), mean residence times (MRT), and mean absorption times (MAT) were also determined. Sarafloxacin | CAS# 98105-99-8 was demonstrated to be more rapidly absorbed, more extensively distributed, and more quickly eliminated in broilers than in pigs. Based on the single-dose pharmacokinetic parameters determined, multiple dosage regimens were recommended as: a dosage of 10 mg/kg given intramuscularly every 12 hr in pigs, or administered orally every 8 hr in broilers, can maintain effective plasma concentrations with bacteria infections, in which MIC90 are <0.25 ug/mL.
PMID:11696079 Ding HZ et al; J Vet Pharmacol Ther 24 (5): 303-8 (2001)
The absorption, metabolism, and excretion of (14)C-labelled sarafloxacin | CAS# 98105-99-8 was studied in three-month-old female New Zealand white rabbits. Two groups of three animals per group were treated orally by gavage with 10 mg/kg bw of (14)C-sarafloxacin base. A third group of three animals received the same dose by intravenous administration. Blood samples were collected 1, 3, 6, 12, and 24 hr after oral administration from animals in one of the groups, and urine and feces were collected daily for five days from animals in the other groups. ... Within five days of oral administration, about 11% of the dose was eliminated in the urine and about 79% in the feces. Urinary excretion after intravenous administration indicated that about 16% of the oral dose had been systemically absorbed.
WHO/FAO; Joint Meeting on Food Additives; Toxicological Evaluation of Certain Veterinary Drug Residues in Food, WHO Food Additive Series 41: Sarafloxacin (1998).
Five groups of 18 Sprague-Dawley rats of each sex were treated with sarafloxacin as follows: One group received a single intravenous dose of 20 mg/kg bw; three groups received a single oral dose of 20, 75, or 275 mg/kg bw; and animals in the fifth group received an oral dose of 1000 mg/kg bw daily for 14 consecutive days. Blood samples were collected from four rats in each group just before treatment and 0.5, 1, 2, 4, 6, 8, 12, and 24 hr after treatment on day 1 for the groups receiving the single dose and on days 1 and 14 for the 14-day treatment group. Plasma and urine samples were assayed for sarafloxacin | CAS# 98105-99-8 base by high-performance liquid chromatography. ... A comparison of the 0 to infinity area under the concentration time curve (AUC) after a single intravenous or oral dose of 20 mg/kg bw sarafloxacin indicated that its bioavailability was about 12%. A plot of the AUC against dose was linear up to 275 mg/kg bw but deviated from linearity at 1000 mg/kg bw.
Effect of Oral Sarafloxacin Dose and Dose Duration on Edwardsiella ictaluri-Infected Channel Catfish
Doses of 0, 2, 6, 10, and 14 mg sarafloxacin | CAS# 98105-99-8/kg of fish were administered for 5 or 10 d in feed given at a rate of 2% of total fish weight. Mean percent mortalities at the end of the 5-d trial of the different sarafloxacin | CAS# 98105-99-8 doses were as follows: 0 mg/kg, 86.1%; 2 mg/kg, 55.6%; 6 mg/kg, 44.4%; 10 mg/kg, 5.6%; and 14 mg/kg, 2.8%. After the 10-d trial doses, the mean percent mortalities were as follows: 0 mg/kg, 75.0%; 2 mg/kg, 71.5%; 6 mg/kg, 47.2%; 10 mg/kg, 0.0%; and 14 mg/kg, 2.8%.
Analysis of variance indicated no significant difference in efficacy between the 5- and 10-d treatments. Pairwise comparison of the combined 5- and 10-d dose responses indicated that the sarafloxacin | CAS# 98105-99-8 treatment at 2 mg/kg was not significantly different from no sarafloxacin | CAS# 98105-99-8 treatment, but that the sarafloxacin | CAS# 98105-99-8 dose of 6 mg/kg was significantly more effective (P < 0.01) than no sarafloxacin | CAS# 98105-99-8. Furthermore, the doses of 10 and 14 mg/kg were significantly more effective (P < 0.01) than the doses of 0, 2, and 6 mg/kg but were not significantly different from each other. Fifteen days after completion of the 10-d treatment, when survivors were analyzed, incidence of carriers was almost twice as great in groups that had received a 5-d treatment than in those that had received a l0-d treatment. However, low survival in the challenged groups that had received the lower doses precluded statistical analysis of the data.
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Huarong (Guangdong) Pharmaceutical Co., Ltd. is a pharmaceutical intermediate manufacturing and production company, based on the synthesis of DPP-4 inhibitor intermediates. It comprehensively constructs a production line for active ingredients of bisamide insecticides, as well as a multifunctional production line for chiral synthesis and enzymatic synthesis of compound intermediates. Build an advanced and green comprehensive production base for pharmaceutical and pesticide intermediates.
The company was established on November 8, 2023, with a type of other limited liability company and registered in Nanxiong City, Shaoguan City. The company's project plan covers an area of 53406.97 square meters. The main building includes 5 Class A multifunctional workshops, 1 Class C workshop, 1 comprehensive building, 1 quality inspection and research and development building, as well as supporting power and environmental protection facilities. The construction of the project covers an area of 19042 square meters, with a building area of 50137 square meters and a plot ratio of 0.94.
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