交沙霉素的抗菌作用及临床治疗各种细菌感染34例

本文测定了交沙霉素的体外抗菌作用。43株表皮葡萄球菌(表葡菌)和金黄色葡萄球菌(金葡菌)对交沙霉素和红霉素敏感率分别为81％和54％。交沙霉素对26株厌氧葡萄球菌(消化球菌)、消化链球菌和28株类杆菌的MIC_(50)分别为0.5和2mg/L。交沙霉素对34例口腔、五官及皮肤的感染全部有效,其中显效(痊愈)占88％。31例获细菌33株,细菌转阴率为97％。治疗中仅3例出现头晕和轻度消化道反应。     

反相高效液相色谱法测定交沙霉素片的含量

目的：建立反相高效液相色谱（RP—HPLC）法测定交沙霉素片含量的方法。方法：色谱柱为汉邦C18柱（150mm×4．6mm，5μm），流动相为乙腈-0.1mol／L醋酸铵溶液（60：40），检测波长为232nm。结果：交沙霉素浓度线性范围为0．1～1．0mg／mL（r=0．9998），平均回收率为96．3％（n=6），RSD=1.69％。结论：RP—HPLC法测定交沙霉素片含量准确、灵敏、简便。     

(S)-(-)-9-氟-2,3-二氢-3-甲基-10-[4-(2-吡啶)-1-基哌嗪]-7-氧代-7H-吡啶[1,2,3-de][1,4]苯并噁嗪-6-羧酸(YH-6)与其它抗微生物药体外抗支原体活性的比较(英文)

目的:测定新喹诺酮YH-6对支原体的抑制活性并与其它抗微生物药剂作比较。方法:MIC的测定采用微量稀释法。结果:YH-6对解脲支原体(Uu),人型支原体(Mh),口腔支原体(Mo),唾液支原体(Ms)的MIC分别为250μg·L~(-1),500μg·L~(-1),125μg·L~(-1),125μg·L~(-1),它的抑制活性与红霉素,柱晶白霉素相当,是氧氟沙星的2-8倍。Uu,Mh对YH-6及交沙霉素和泰洛星不易产生诱导耐药性,而对红霉素和四环素易产生诱导耐药性和多重耐药性,而对YH-6,交沙霉素和泰洛星无多重耐药性。结论:YH-6对支原体有很强的抑制活性,且不易形成诱导耐药性。Uu和Mh的红霉素或四环素抗性菌株对YH-6无多重耐药性。     

Effects of josamycin on carbamazepine kinetics

Summary The steady state pharmacokinetics of oral carbamazepine in epileptic patients (n=8) was compared before and after one week of treatment with josamycin (2 g/day). There was a small but statistically significant decrease in oral clearance of total (17%) and unbound (21.5%) drug. In spite of an unchanged AUC of 10,11-epoxide carbamazepine the ratio of metabolite to parent drug AUC was significantly decreased (20.2%). The plasma protein binding of carbamazepine and its 10,11-epoxide metabolite did not vary. The results demonstrate impairment by josamycin of the apparent clearance of carbamazepine. Care should be taken in patient receiving both carbamazepine and josamycin.     

不同pH介质中交沙霉素溶出度比较

本文采用紫外分光光度法测定了交沙霉素片在不同ＰＨ介质中的溶出度，结果表明随着ＰＨ值的升高，Ｔ５０，Ｔｄ均增加，具有一定的相关性。     

Josamycin Concentration in Human Ejaculate and its Influence on Sperm Motility/Josamycinkonzentrationsbestimmung in menschlichem Ejakulat und deren Einfluß auf die Spermienmotilität

The concentration of josamycin was determined in the split ejaculate of 5 volunteers after oral administration for several days. One aim of this investigation was to examine the penetration of the macrolide antibiotic into the prostate and the seminal vesicles. 2.23 +/- 1.8 micrograms/ml josamycin was found in fraction I of the ejaculate, consisting mostly of prostatic secretion, and 1.56 +/- 1.37 micrograms/ml josamycin in fraction II comprising mainly secretions from the seminal vesicles. The concentrations of josamycin found in both fractions of the ejaculate are clearly comparable with serum levels of the antibiotic. Josamycin thus attains concentrations in the prostate and seminal vesicles which are effective against Mycoplasma and Chlamydia, pathogens of increasing importance in infections of the urogenital tract. In vitro studies on samples from 30 andrological patients showed that josamycin (0.5 micrograms/ml) did not impair, but even increased the motility of spermatozoa (p less than or equal to 0.01). On the basis of these results josamycin is recommended for the treatment of andrological patients. In particular, the specific antibacterial spectrum also indicates the use of this antibiotic for treatment of the partner when children are desired. The usual precautionary measures for pregnancy must then be adhered to.     

交沙霉素及其片剂效价的比浊法测定

建立了比浊法测定交沙霉素及其片剂的效价.以金黄色葡萄球菌为试验菌,加菌量3.0%～5.0%,(37±0.5)℃培养4h,于530nm在线测定.交沙霉素浓度在1～3u/ml范围内,吸光度与其浓度对数成良好的线性关系.交沙霉素及其片剂的平均回收率为100.2%(RSD 1.8%)和99.9%(RSD 2.1%).     

荷移比色法测定交沙霉素

目的:建立测定交沙霉素制剂含量的方法。方法:利用交沙霉素与茜素红在水-醇介质中发生电荷转移反应,形成电荷转移络合物,采用可见分光光度法测定。结果:荷移反应生成的荷移络合物在530nm处有最大吸收,表观摩尔吸光系数是5.92×103L.mol-1.cm-1,药物浓度在0~120mg/L范围内服从比耳定律,平均回收率在98.0%以上,RSD为1.0%(n=6)。结论:方法稳定、准确、灵敏、快速,对样品的测定结果令人满意。     

Synthesis and antibacterial activities of some novel 17, 18-unsaturated carbonyl compounds derivated from josamycin

Some novel josamycin derivatives bearing an arylalkyl-type side chain were designed and synthesized. By HWE or Wittig reaction, 16-aldehyde group of josamycin analogs were converted into unsaturated carbonyl compounds. They were evaluated for their in vitro antibacterial activities against a panel of respiratory pathogens. 8b and 8e exhibited comparable activities against a panel of respiratory pathogens, especially to resistant ones in the series of desmycarosyl josamycin analogs. Among of all the target molecules, 21 showed the best antibacterial activities.