Cytological and cytogenetic effects of the fluoroquinolone ofloxacin on human periodontal ligament fibroblasts

The fluoroquinolone ofloxacin (OFLX) is one of the candidates of antibacterial agents to be topically used against periodontitis. To estimate the maximum concentration of OFLX which exerts little or no adverse effect on the periodontal ligament, cytological and cytogenetic effects of OFLX on human periodontal ligament fibroblasts (Pel cells) were examined. Treatment of Pel cells with < or =0.3 mM OFLX for 24 or 48 h had little inhibitory effect on cellular growth and survival. DNA, RNA and protein syntheses in Pel cells did not decrease in response to treatment with < or =0.3 mM OFLX. The constitutive level of alkaline phosphatase mRNA was retained in cells treated with < or = 0.03 mM OFLX for 24 or 48 h. The level of type I procollagen mRNA was not affected by treatment with < or = 0.003 mM OFLX for 24 or 48 h. Cytogenetic effects of OFLX were evaluated by the ability of OFLX to induce chromosome aberrations in Pel cells. Treatment with OFLX at 0.3-3.0 mM for 6, 24, or 48 h failed to induce chromosome aberrations in Pel cells. The failure of OFLX to induce chromosome aberrations was seen even in the presence of exogenous metabolic activation using a 5% rat liver post-mitochondrial supernatant mixture. These results indicate that treatment of Pel cells with < or =0.003 mM OFLX has few or no adverse effects on the cytological and cytogenetic endpoints examined, suggesting that there would be little adverse effect on growth and differentiation of the periodontal ligament, as well as little cytogenetic activity, if OFLX were to be topically administered to the gingival crevice at the minimal inhibitory concentration (MIC90) against periodontopathic bacteria (< or = 0.0027 mM). It is important to note, however, that extrapolation of these findings to in vivo conditions has yet to be undertaken.     

Topical chemotherapy in human periodontitis using a new controlled-release insert containing ofloxacin. I. Microbiological observation

The recognition that destructive periodontal diseases may be caused by specific microorganisms in periodontal pockets has led to an increased interest in and usage of antimicrobial agents in periodontal therapy. Recently, a new controlled-release insert containing ofloxacin, a synthetic antibiotic, has been developed. In this study, the controlled-release insert (PT-01) was microbiologically evaluated in combination with or without subgingival mechanical debridement. PT-01 was applied in the periodontal pockets of 27 patients with chronic periodontitis. Three sites with a deep probing pocket depth (greater than or equal to 5 mm) were randomly selected in different quadrants of each patient, and were assigned into three groups, i.e., PT-01 applied (T), placebo applied (P) and control sites (C). Periodontal treatments consisted of supragingival scaling with oral hygiene instruction for the first 2 weeks followed by root planing and subgingival scaling PT-01 was applied weekly on day 0 to 35, and the subgingival plaque samples from each site were collected on d 0, 14, 21 and 42. The dynamics of the subgingival microflora was investigated by dark field microscopy and by anaerobic and aerobic cultivation. In the supragingival scaling period, significant reduction in percentages of spirochetes and motile rods and significant increase of the percentage of coccoid cells were observed only at T sites. In addition, the total viable counts of bacteria, black-pigmented Bacteroides and Fusobacterium species were significantly reduced at T sites. After mechanical subgingival debridement, significant shifts in the proportion and reduction of the viable counts in the subgingival microflora were found at all sites.(ABSTRACT TRUNCATED AT 250 WORDS)     

Moxifloxacin versus ofloxacin plus metronidazole in uncomplicated pelvic inflammatory disease: results of a multicentre, double blind, randomised trial

OBJECTIVE: This multinational, multicentre, prospective, randomised, double blind, parallel group, non-inferiority study compared the efficacy and safety of moxifloxacin monotherapy with ofloxacin plus metronidazole in women with uncomplicated pelvic inflammatory disease. METHODS: Women from hospitals throughout 13 countries received a 14 day course of either oral moxifloxacin, 400 mg once daily (n = 384), or oral ofloxacin, 400 mg twice daily plus oral metronidazole, 500 mg twice daily (n = 365). RESULTS: Of the 741 patients in the intent to treat (ITT) population, 564 (74.2%) were valid for the per protocol (PP) analyses; 112 (19.9%) of these were included in the microbiologically valid population (MBV). Clinical resolution rates in the PP population at the test of cure visit (TOC, 5-24 days post-therapy, primary efficacy end point) were 90.2% (248/275) for moxifloxacin and 90.7% (262/289) for ofloxacin plus metronidazole (95% CI: -5.7% to 4.0%). At follow up (28-42 days post-therapy), resolution rates in the PP population were 85.8% (236/275) and 87.9% (254/289) for moxifloxacin and comparator, respectively (95% CI: -8.0% to 3.1%). Bacteriological success rates in the MBV population at TOC were 87.5% (49/56) for moxifloxacin and 82.1% (46/56) for comparator (95% CI: -8.3% to 18.8%). Against Chlamydia trachomatis and Neisseria gonorrhoeae, bacteriological success rates with moxifloxacin were 88.5% (23/26) and 100% (13/13) and for comparator 85.7% (18/21) and 81.8% (18/22), respectively. Drug related adverse events occurred less frequently with moxifloxacin (22.5% (85/378)) versus the comparator (30.9% (112/363)) (p = 0.01). CONCLUSION: In uncomplicated PID, once daily moxifloxacin monotherapy was clinically and bacteriologically as efficacious as twice daily ofloxacin plus metronidazole therapy and was associated with fewer drug related adverse events.     

反相高效液相色谱法测定泰麻滴鼻剂中主药的含量

目的：测定泰麻滴鼻剂中氧氟沙星和麻黄素的含量。方法：采用RP－HPLC法,用ODS柱,以甲醇－醋酸铵水溶液（1：1）用磷酸调节pH至6．0作为流动相,氯霉素为内标,检测波长淡256nm。结果：氧氟沙星和麻黄素平均回收率（n=5)分别为99．5％,101．5％;RSD分别为1．45％和1．57。结论：此法简便、快速、准确。     

司氟沙星注射液治疗急性细菌感染60例

目的：观察国产司氟沙星注射液（SPFX）治疗急性细菌感染的疗效和不良反应。方法：共治疗60例患者,随机分为试验,对照及开放组各20例,试验及开放组静脉滴注SPFX200mg.d^-1,qd;对照组静脉滴注氧氟沙星注射液（OFX）400mg.d^-1,bid;疗程均为5－14d。结果：试验及开放组共40例,总有效率和细菌清除率为95％和93．5％;对照组20例,总有效率和细菌清除率为80％和88．9％。用药中不良反应较轻,试验及开放组发生率5％,对照组发生率10％,结论：本药治疗临床常见的中重度急性细菌性感染疗效高,不良反应小。     

氧氟沙星三种给药途径的药代动力学研究

本文报道42例临床患者用经静脉、肌肉和口服三种途径给氧氟沙星后的药代动力学。其血清和尿浓度用 HPLC-离子对色谱荧光检测。结果经静脉和经肌肉为二房室模型,口服为一室。其主要药动学参数:半衰期(T1/2)5.96±1.26,5.05±1.04和4.96±0.69h;分布容积(V/F)57.5±15.6,67.9±26.9和94.1±24.6L;峰浓度(Cmax)3.88±1.05,2.77±0.86和1.94±0.74μg·ml~(-1);总清除率(CL_T)13.3±3.8,14.1±3.9和13.6±2.9 L·h~(-1)。     

氧氟沙星片剂的溶出度研究

本文采用转篮法对国产及进口几个厂家生产的盐酸氧氟沙星片剂进行了体外溶出度测定，并对其溶出参数（Td、T50、m）进行了统计处理。结果表明：不同厂家的产品之间，其溶出参数有显著性差别（p＜0．001）。     

氧氟沙星壳聚糖胶囊的研制及其急性毒性试验

目的研制氧氟沙星壳聚糖胶囊并对其质量标准及急性毒性进行研究。方法以氧氟沙星、壳聚糖、赤石脂为原料制备氧氟沙星壳聚糖胶囊 ,研究质量标准和急性毒性。结果该胶囊制备工艺可行 ,质量控制方法简便、可靠 ,含量测定平均回收率为 99.95 %。结论此品处方及制法可行 ,质量标准能够控制此品的质量 ,且小鼠急性毒性较低