Pharmacokinetic study of single and multiple oral dose administration of antofloxacin hydrochloride in healthy male volunteers / 中华医学杂志(英文版)

<p><b>BACKGROUND</b>A new fluroquinolone antibacterial agent, antofloxacin hydrochloride, developed in China, is an 8-NH(2) derivant of levofloxacin. The purpose of the study was to evaluate the pharmacokinetic characteristics of single and multiple oral doses of antofloxacin hydrochloride in Chinese healthy male volunteers.</p><p><b>METHODS</b>An open-label, non-randomized, single and multiple dose clinical trial was conducted. In single dose study, 12 subjects took 200 mg antofloxacin hydrochloride. In multiple dose study, 12 subjects took antofloxacin hydrochloride 400 mg once on day 1 and 200 mg once daily from day 2 to day 7. HPLC was used to assay the serum and urinary concentrations of antofloxacin.</p><p><b>RESULTS</b>In single dose study, the maximum concentration of drug in serum (C(max)), the time to reach C(max) (T(max)), and the area under the serum concentration-time curve (AUC (0-∞)) of antofloxacin were (1.89 ± 0.65) mg/L, (1.29 ± 0.26) hours, and (25.24 ± 7.26) mg×h(-1)×L(-1), respectively. Accumulating elimination rate of antoflocaxin from urine within 120 hours was 39.1%. In multiple dose study, blood concentration of antofloxiacin achieved stable state on day 2 after dosing. The minimum concentration drug in serum (C(min)), AUCss, mean concentration of drug in serum (C(av)), and degree of fluctuation (DF) were (0.73 ± 0.18) mg/L, (47.59 ± 7.85) mg×h(-1)×L(-1), (1.98 ± 0.33) mg/L, and 1.74 ± 0.60, respectively. On day 7 after dosing, T(max), C(max), and AUC (0-∞) was (1.14 ± 0.50) hours, (2.52 ± 0.38) mg/L, and (48.77 ± 8.44) mg×h(-1)×L(-1), respectively. Accumulating elimination rate of antofloxaxin from urine within 120 hours after the last dosing was 60.06%.</p><p><b>CONCLUSIONS</b>The regimen of 400 mg loading dose given on the first treatment day and then 200 mg dose once daily results in satisfactory serum drug concentration.</p>

Study on drug resistance and molecular epidemiology of Streptococcus pneumoniae isolated in Chongqing / 中华流行病学杂志

<p><b>OBJECTIVE</b>To investigate the prevalence and drug resistance of Streptococcus (S.) pneumoniae in patients infected in communities and molecular epidemiology with BOX-polymerase chain reaction (PCR) in Chongqing areas.</p><p><b>METHODS</b>A total of 680 clinical specimens from sputum and throat/nasal swabs were collected from patients seen from September 2000 to March 2001. Antibiotic susceptibility was determined by agar dilution test. BOX-PCR was used for molecular typing of S. pneumoniae.</p><p><b>RESULTS</b>A total of 39 isolates of S. pneumoniae were collected with the isolation rate of 5.7%. Of the 34 S. pneumoniae strains, two showed low-level resistance to penicillin (MIC 0.125 mg/L), one to levofloxacin, but many to macrolide and clindamycin (nearly 70%). All the strains were susceptible to beta-lactams and vancomycin. BOX-PCR typing demonstrated a high discriminatory potential and easy to be accurately analysed. 35 S. pneumoniae strains (include ATCC49619) were divided into 25 distinct types, representing 29 subtypes with A (n = 3) as the predominant type. 2 penicillin-resistant strains were shown to be different types.</p><p><b>CONCLUSION</b>Penicillin resistant rate of S. pneumoniae was low in Chongqing, but macrolide and clindamycin resistant strains were common while BOX-PCR typing was a suitable technique to type S. pneumoniae. No dominant antibiotic resistant strains were found in Chongqing.</p>

A study on the clinical and pathological efficacy of lamivudine in the treatment of chronic hepatitis B / 中华肝脏病杂志

<p><b>OBJECTIVE</b>To investigate clinical effect, liver pathohistological changes (including pathology, HBV markers in liver tissue) in patients with chronic hepatitis B.</p><p><b>METHODS</b>70 patients of chronic hepatitis B were administered 100 mg Lamivudine orally daily for 1 year. The serum HBV-DNA, HBeAg/anti-HBe, hepatic chemistry and the hepatic fibrosis markers were studied. The needle biopsy of liver were performed in 35 patients before and after treatment and Knodell pathological score were done, HBsAg, HBcAg, alpha-SMA in liver tissue were examined by immunohistochemistry method.</p><p><b>RESULTS</b>After 1 year treatment the full response rate, partial response rate and no response rate were 23.72%, 69.49% and 6.78%, the patients in whom HBeAg seroconversion had higher base-line Alanine aminotransferase levels than the patients without seroconversion. Activity index of hepatic histology in 41.18% patients had a significant decrease. Histological assessment revealed that necrosis in portal area, pylenphlebitis and fibrosis were obviously alleviated. The liver immunohistochemistry examination showed HBcAg and alpha-SMA in liver decreased significantly in the patients with HBeAg seroconversion, no obvious alteration was observed in HBsAg expression. Lamivudine seems an effective compound with high safety and low side effect.</p><p><b>CONCLUSION</b>These results suggested that lamivudine (100mg/d) could suppress HBV-DNA replication, promote ALT normalization, accelerate HBeAg/anti-HBe seroconversion, improve the liver pathological changes, slow down the development of liver fibrosis</p>