A simple and sensitive liquid chromatographic method was developed for quantification of cefotetan disodium (CTT), a semi-synthetic cephamycin antibiotic, in human plasma. CTT and the internal standard chloramphenicol were extracted from plasma by a simple one-step protein precipitation with 35% (v/v) perchloric acid. Separation was carried out on a reverse-phase C18 column with a mobile phase of acetonitile-water containing 0.5% (v/v) phosphoric acids (20:80, v/v) at a flow rate of 1.0 mL/min. The column effluent was monitored by UV detection at 300 nm. The column temperature was maintained at 40°C. This method demonstrated good linearity in the range of 0.525-300.0 μg/mL, with correlation coefficients greater than 0.99. The limit of quantification (LOQ) was 0.525 μg/mL in human plasma. Intra- and inter-day precisions were less than 6.63% in terms of relative standard deviation (RSD). The accuracy, when expressed by the bias, ranged from 0.57% to 4.04%. The mean extraction recovery of CTT was higher than 40.94%. The method was found to be precise, accurate, and specific for CTT quantitative analysis, and was successfully applied for a pharmacokinetic study of CTT after a single intravenous dose of 1.0 g of CTT in healthy Chinese subjects.
Cefotetan ; blood ; pharmacokinetics ; Chromatography, Liquid ; methods ; Humans

OBJECTIVEAntibacteria activity of compounds from Puraboeo ruescens and Lysionotus pauciflorus was assayed.

METHODDisc diffusion was used to isolate compounds in vitro and berberine was positive control. The value of IC50 was assayed by the method of liquid culture. All kinds of chromatography were used to isolate the chemical constituent and structure was identified by MS and NMR spectroscopy.

RESULTEight compounds were isolated and identified as beta-sitosterol (1), E-3,4-dihydroxy cinnamic acid (2), barbinervic acid (3), 3beta,19alpha-dihydroxy12-en-28-ursolic acid (4), 28-O-beta-D-glucopyranosyl pomolic acid (5), 5,7-dihydroxy-6,8,4'-trimethoxy flavone (6), 5, 6, 4'-trihydroxy-7,8-dihydroxy flavone (7), 5-hydroxy-6,8,4'-trimethoxy flavone-7-O-beta-D-glucopyranosyl (8). Compound 3, 4 and 6 had activity against SA, MRSA and ESBLs respectively. Compound 3 showed (IC50 = 0.098 g x LU(-1), IC50 = 0.27 g x L(-1)) against SA and ESBLs-SA respectively. Compound 4 (IC50 = 0.130 g x L(-1)) was best to against MR SA.

CONCLUSIONCompound 1 - 5 were isolated from this plant for the first time. Compound 7 and 8 was isolated from Gesneriaceae for the first time.

Anti-Bacterial Agents ; isolation & purification ; pharmacology ; Bacteria ; drug effects ; Drugs, Chinese Herbal ; isolation & purification ; pharmacology ; Magnoliopsida ; chemistry