螺旋霉素高产株的推理选育和工业生产

产二素链霉菌SIPI9004经自发或诱发的突变和推理选育，得到若干耐药性变种。第六代一株变种10-29，产生螺旋霉素比原始菌株SIPI9004增产约6倍。该变种应用于工业生产(30m^3发酵罐)，发酵效价、总单位和指数三项指标比原来生产菌株F-16分别提高26．1％、33．3％和26．8％。     

一阶导数紫外分光光度法测定乙酰螺旋霉素片剂含量

 采用一阶导数光谱法测定乙酰螺旋霉素片剂的含量，平均回收率为100．63％，RSD为0．47％（n＝6），方法简便、快速，可消除赋形剂干扰，适用于乙酰螺旋霉素的片剂测定。     

酰基激酶和酰基CoA合成酶对螺旋霉素合成的影响

螺旋霉素链霉菌生物合成螺旋霉素的过程受许多酶的调控作用，酰基激酶和酰基CoA合成酶是螺旋霉素内酯环合成的重要酶，实验测定了它们的酶活趋势和酶的影响因子，结果表明，酰基激酶和酰基CoA合成酶都有两个活力峰，前者活性集中在发酵中前期，后者活性集中在发酵中后期，实验发现Co2 ,Mn2 对酰基激酶和酰基CoA合成酶有较强的激活作用，Cu2 对酰基激酶有抑制作用，但对酰基CoA合成酶有很强的激活作用，在发酵中期向摇瓶中补加二阶阳离子比在发酵初期加入有更明显的激活作用，平均效价最高提高了31％。     

不同培养基对乙酰螺旋霉素片含量测定的影响

目的研究不同培养基对乙酰螺旋霉素含量的影响。方法按照《中国药典》2010年版(二部)乙酰螺旋霉素含量测定项下的抗生素微生物检定法(管碟法),采用不同厂家或同一厂家不同批号的抗生素检定培养基Ⅱ号(7.8～8.0)对乙酰螺旋霉素片进行含量测定,比较分析测定结果。结果不同生产厂家或同一生产厂家不同批号的抗生素检定培养基检测结果有较明显差异。结论建议制定用于含量测定的培养基质量控制的国家标准。     

不同检定菌对乙酰螺旋霉素量-效关系的影响

采用二种不同检定菌（枯草芽孢杆菌、藤黄八叠球菌），对乙酰螺旋霉素进行标准曲线回归系数（斜率）测定，结果表明：藤黄八叠球菌对乙酰螺旋霉素各组分的敏感度比枯草芽孢杆菌高。     

螺旋霉素对牙周炎活动破坏发生率的影响

本文对7例牙周炎患者的170颗牙、970个部位于治疗结束后作为纵向观察时的基线。以后每隔2个月定点复查1次，共观察了6～12个月、以2次检查之间新出现≥2mm的附着丧失作为活动期的诊断标准，比较了口服螺旋霉素和服药结合牙周刮治治疗后牙周炎活动破坏的发生率。结果表明：牙周炎活动破坏的估计年发生率为2．8％，单纯口服螺旋霉素和服药结合牙周刮治的两组牙齿，其活动破坏的发生率无显著差异（P＞0．1）。说明螺旋霉素治疗牙周炎的远期效果仍较好。提示螺旋霉素可以作为牙周炎患者有效的辅助用药。     

乙酰螺旋霉素生产中间体质量控制的探讨

用ＨＰＬＣ检测并探明了乙酰螺旋霉素合成中各步中间体组份的变化情况，从而建立了质量控制。     

Simultaneous determination of metronidazole and spiramycin in bulk powder and in tablets using different spectrophotometric techniques

Metronidazole (MZ) is an anti-infective drug used in the treatment of anaerobic bacterial and protozoa infections in humans. It is also used as a veterinary antiparasitic drug. Spiramycin (SP) is a medium-spectrum antibiotic with high effectiveness against Gram-positive bacteria. Three simple, sensitive, selective and precise spectrophotometric methods were developed and validated for the simultaneous determination of MZ and SP in their pure form and in pharmaceutical formulations. In methods A and B, MZ was determined by the application of direct spectrophotometry and by measuring its zero-order (D(0)) absorption spectra at its λ(max) = 311 nm. In method A, SP was determined by the application of first derivative spectrophotometry (D(1)) and by measuring the amplitude at 218.3 nm. In method B, the first derivative of the ratio spectra (DD(1)) was applied, and SP was determined by measuring the peak amplitude at 245.6 nm. Method C entailed mean centering of the ratio spectra (MCR), which allows the determination of both MZ and SP. The methods developed were used for the determination of MZ and SP over a concentration range of 5-25 μg ml(-1). The proposed methods were used to determine both drugs in their pure, powdered forms with mean percentage recoveries of 100.16 ± 0.73 for MZ in methods A and B, 101.10 ± 0.90 in method C, 100.09 ± 0.70, 100.02 ± 0.88 and 100.49 ± 1.26 for SP in methods A, B and C, respectively. The proposed methods were proved using laboratory-prepared mixtures of the two drugs and were successfully applied to the analysis of MZ and SP in tablet formulation without any interference from each other or from the excipients. The results obtained by applying the proposed methods were compared statistically with a reported HPLC method and no significant difference was observed between these methods regarding both accuracy and precision.     

Macrolide antibiotics in food-animal health

Several 14- and 16-membered-ring macrolide antibiotics have acquired important roles in the modern production of food animals. Macrolide antibiotics exhibit many similar antimicrobial properties whether used in veterinary or human medicine. In addition to their direct inhibitory action on micro-organisms, macrolides exert a variety of subinhibitory concentration (sub-MIC) effects that are being increasingly recognised as important factors in the explanation of therapeutic results. Macrolides achieve wide tissue distribution and high intracellular concentrations that contribute prominently to their efficacy. Another important factor governing efficacy is the complex interaction between macrolides, micro-organisms, and phagocytes that may enable the host defence system to enhance the antibiotic’s inhibitory action. A potential role for macrolides in modulating inflammatory processes has also been recognised. In both sub-MIC effects and interactions with the host immune system, different macrolides exert different responses that may reinforce or oppose each other. This complexity of responses requires additional studies in appropriate disease states and animal species in order to elucidate a more comprehensive understanding and explanation of in vivo outcomes.