紫外分光光度法测定盐酸沙拉沙星原料的含量

建立紫外分光光度法测定盐酸沙拉沙星原料的含量。用0.1mol/L NaOH溶液为溶剂,在274nm波长处测定吸收度。结果沙拉沙星对照品质量浓度在2.4～12.0μg/mL范围内与吸收度呈良好的线性关系,线性回归方程A=0.089C+0.05,r=0.9999(n=5);平均回收率为99.74%,RSD=0.40%(n=5)。本方法操作简便、快捷、经济、结果准确,可用于盐酸沙拉沙星原料的含量测定。     

紫外分光光度法测定硫酸链霉素的含量

采用紫外分光光度法测定硫酸链霉素的含量,检测波长323 nm.硫酸链霉素在12～48 mg/L的浓度范围内,其紫外吸收值与浓度呈线性关系,回归方程为A=0.012 1 C 0.000 5,r=0.999 9;平均回收率为99.82%,RSD为0.62%.     

紫外分光光度法和高效液相色谱法测定盐酸土霉素可溶性粉的含量

采用紫外分光光度法和高效液相色谱法测定盐酸土霉素可溶性粉中土霉素的含量。紫外分光光度法试验表明,用0.01 mol/L盐酸溶液作参比液,以268 nm为测定波长,土霉素在4~32μg/mL范围内吸光度与浓度呈良好的线性关系,相关系数r=0.9999,平均回收率(n=5)为101.04%,RSD=1.02%。高效液相色谱法试验表明,以0.05 mol/L草酸铵溶液-二甲基甲酰胺-0.2 mol/L磷酸氢二铵溶液(75∶20∶5)为流动相,以280 nm为检测波长,土霉素在0.02~0.14mg/mL范围内浓度与峰面积线性关系良好,相关系数r=0.9999,平均回收率(n=5)为100.52%,RSD=0.25%。紫外分光光度法、高效液相色谱法与抗生素微生物检定法比较,结果基本一致。     

紫外分光光度法测定泰乐菌素注射液含量方法的建立

以0.1 mol/L盐酸溶液为参比液,采用紫外分光光度法在290 nm波长处测定泰乐菌素注射液中泰乐菌素的含量.结果表明,泰乐菌素在5 U/mL～50 U/mL浓度范围内,其吸光度与浓度呈良好的线性关系,相关系数r=0.999 2,平均回收率为99.6%,RSD为0.4(n=6).该方法操作简便、快速、准确,适于作为生产企业中问产品的质量控制方法.     

紫外分光光度法测定替米考星注射液含量

以稀磷酸液为稀释溶剂,采用紫外分光光度法测定替米考星注射液含量,检测波长为291nm.结果表明,线性范围为10.0～30.0μg·mL-1时,紫外吸收值与供试液质量浓度线性关系良好(r=0.999 7),平均回收率为102.5%(RSD=0.30%).本方法操作简便,快速准确,适用于替米考星注射液含量快速测定.     

盐酸林可霉素紫外分光光度测定方法的建立

以0.02 mol/L氯化钯溶液为参比液,采用紫外分光光度法在380 nm±1 nm波长处测定盐酸林可霉素注射液中林可霉素的含量.结果表明,林可霉素在50 μg/mL～250 μg/mL范围内,其吸光度与浓度呈良好的线性关系,相关系数r=0.999 9,平均回收率为99.5%,RSD为0.9%(n=5).该方法操作简便、快速,结果准确,适于作为生产企业中间产品的质量控制方法.     

紫外分光光度法测定氧氟沙星油剂注射液的含量

采用紫外分光光度法测定氧氟沙星油剂注射液的含量,选择氯仿与无水甲醇作溶剂,于220～400 nm间扫描,在299 nm波长处有最大吸收峰,辅料无干扰.实验结果表明,氧氟沙星浓度在0.5～2.5 μg/mL范围内,其吸收度与浓度呈良好的线性关系.线性方程为A=-0.86×10-2 4.75×10-1 C,r=0.999 9,平均回收率为100.3%,RSD=0.36%(n=5).     

原子吸收分光光度法测定右旋糖酐铁注射液的含量

建立了原子吸收分光光度法测定右旋糖酐铁注射液含量的方法,以盐酸溶液(1→100)为溶剂,检测波长248.3 nm,在5～20 μg/mL范围内吸收度与浓度呈良好的线性关系,r=0.999 5,回收率98.8%,RSD为1.5%(n=5),稳定性好.本方法与碘量法相比,操作简便、快速,结果准确.     

紫外分光光度法测定细叶十大功劳叶中总生物碱含量

为了建立细叶十大功劳叶中总生物碱的提取及含量测定方法,试验以盐酸-甲醇(1∶100)为溶剂,采用回流提取法提取细叶十大功劳叶中总生物碱,并以盐酸小檗碱为对照品,紫外分光光度法测定其含量,选定波长为345 nm。结果表明:细叶十大功劳叶中总生物碱含量以盐酸小檗碱计为3.825%,线性回归方程为A=0.063 58C-0.004 48(r=1.000 0),平均回收率为100.7%,相对标准偏差(RSD)=0.45%(n=6)。说明该含量测定方法操作简便、结果准确,可用于细叶十大功劳叶中总生物碱含量的测定。     

紫外分光度法测定硫酸庆大霉素含量

应用紫外分光光度法测定硫酸庆大霉素含量。以紫外分光光度法在232nm波长处测定。结果是硫酸庆大霉素浓度在20～60U/ml范围内线性关系良好r=0.9990。平均回收率为98.83%，RSD为0.26%，本法与旧中国兽药典规定方法比较更具简单，易操作，适用于硫酸庆大霉素含量的快速测定。     

旋光法测定甲磺酸达氟沙星的含量

采用旋光法测定甲磺酸达氟沙星的含量,结果表明,在6～14 mg/mL浓度范围内,甲磺酸达氟沙星的旋光度与浓度呈良好的线性关系(r=0.999 8).与电位滴定法相比,本法具有简单、快速、易操作等优点.     

Safety of masitinib mesylate in healthy cats

Background: Masitinib mesylate is a PO‐administered tyrosine kinase inhibitor developed both for human and animal diseases with activity against both mutated and wild type forms of the c‐kit receptor and platelet‐derived growth factor receptors α and β, and is currently registered in Europe for the treatment of mast cell tumors in dogs. Hypothesis/Objectives: The objective of this study was to determine if healthy cats can tolerate administration of masitinib without clinically relevant adverse effects. Animals: Twenty healthy research colony‐specific pathogen‐free cats. Methods: This study was a prospective, randomized phase 1 clinical trial. Masitinib was administered PO to 20 healthy cats. Ten cats received 50 mg masitinib every other day for 4 weeks, and 10 cats received 50 mg masitinib daily for 4 weeks. Results: Clinically relevant proteinuria was noted in 2/20 (10%) cats (both treated daily), and neutropenia was noted in 3/20 (15%) (seen in both treatment groups). An increase in serum creatinine concentration and adverse gastrointestinal effects were noted in some cats. Conclusions and Clinical Importance: Masitinib mesylate was tolerated in the majority of cats. Long‐term administration and pharmacokinetic studies are needed to further assess the use of masitinib in cats.     

单诺沙星脂质体在蛋雏鸡血浆的药代动力学

分别采用静脉注射和内服两种给药途径给予健康蛋雏鸡甲磺酸单诺沙星溶液和甲磺酸单诺沙星脂质体混悬液(剂量为5 mg/kg).结果显示,两种剂型静注给药的药时数据均符合无吸收二室开放模型,主要药动学参数分别为T1/2α 0.349 6、0.351 8 h;T1/2β6.411 4、8.193 2 h;AUC3.799 7、5.066 0 mg/(L·h);CLβ1.723 2、1.131 7 L/(kg·h).两种剂型内服给药的药时数据均符合一级吸收一室开放模型,主要药动学参数分别为T1/2 Ka0.301 7、0.524 4 h;T1/2K 4.479 2、5.021 7 h;AUC 3.284 4、4.610 6 mg/(L·h);Cmax 0.483 8、1.054 8 mg/L;Tp 1.287 3、1.936 2 h;生物利用度分别为86.44%、91.01%.可见这两种剂型的静注与内服给药的体内药动学特征不同.与甲磺酸单诺沙星溶液相比,甲磺酸单诺沙星脂质体血浆半衰期延长,达峰浓度高,有效浓度维持时间持久,内服生物利用度提高.     

Single-dose oral pharmacokinetics of pergolide mesylate in healthy adult mares

This pilot study evaluated protection of an equine autogenous bacterin-toxoid vaccine against Corynebacterium pseudotuberculosis infection. Twenty-four BALB/c mice were inoculated with two doses of bacterin-toxoid vaccine or two injections of a placebo. Clinical, microbiologic, and pathologic outcomes were assessed after intradermal infection with one of two equine-origin C. pseudotuberculosis strains. Mice receiving bacterin-toxoid from fast-growing C. pseudotuberculosis showed significant protection from challenge infection, as evidenced by a higher survival rate, fewer gross and histopathologic lesions, and lower bacterial levels on culture. Successful protection via a vaccine against equine internal abscesses might provide supplementary management options against an important, potentially fatal disease.     

Use of prostaglandins and bromocriptine mesylate for pregnancy termination in bitches

OBJECTIVE: To assess the efficacy and safety of 2 protocols using bromocriptine mesylate and prostaglandins to terminate unwanted pregnancy in bitches. DESIGN: Prospective randomized single-blind controlled study. ANIMALS: 34 crossbred and purebred bitches referred for possible pregnancy termination. Seven additional pregnant bitches were used as controls. PROCEDURE: Pregnancy was assessed by ultrasonographic examination from day 25 after mating in all bitches. Of the 34 bitches, 25 were pregnant and were randomly allocated to a treatment group. Group-1 dogs (n = 12) received a combination of increasing amounts of bromocriptine mesylate (15 to 30 microg/kg [6.8 to 13.6 microg/lb], p.o., q 12 h) and dinoprost tromethamine (0.1 to 0.2 mg/kg [0.045 to 0.09 mg/lb], s.c., q 24 h). Group-2 dogs (n =13) received a combination of increasing amounts of bromocriptine mesylate (the same schedule as group-1 dogs) and cloprostenol sodium (1 microg/kg [0.45 microg/lb], s.c., q 48 h). Both groups were treated until pregnancy termination. Results-Treatment success was 100% in both groups. Days of treatment required for pregnancy termination did not significantly differ between groups (5.0 +/- 0.6 vs 3.7 +/- 0.6 days, group-1 and group-2 dogs, respectively) although adverse effects only developed in group-1 dogs. At the end of the protocols, pseudopregnancy was observed in 3 of 12 and 6 of 13 group-1 and group-2 dogs, respectively. Pregnancy termination was followed by a mucoid sanguineous vulvar discharge for 3 to 10 days. CONCLUSIONS AND CLINICAL RELEVANCE: Results of this study indicate that protocols that combine the use of bromocriptine mesylate and prostaglandins for the termination of unwanted pregnancy in bitches are efficient and safe. The use of bromocriptine mesylate and cloprostenol had the best results and could be easily used on an outpatient basis.     

达氟沙星脂质体在蛋雏鸡体内的组织动力学及靶向性研究

将260只28日龄试验鸡(体质量215~230 g)随机分成5组:健康对照组20只,甲磺酸达氟沙星溶液静注给药组和内服给药组、甲磺酸达氟沙星脂质体静注给药组和内服给药组,每组60只。以5 mg/kg体质量剂量分别采用静脉注射和内服2种给药途径给予健康蛋雏鸡甲磺酸达氟沙星溶液和脂质体混悬液,于给药后0.167、0.333、0.5、0.75、1、1.5、2、4、6、9、12、24 h各剖杀5只鸡,取血液、肝脏、肾脏、肺脏和肌肉样品。采用反相HPLC色谱内标法测定各组织中达氟沙星浓度。应用MCPKP分析软件处理血浆药物浓度-时间数据,比较2种剂型的组织药动学参数。结果显示,与溶液组相比,甲磺酸达氟沙星脂质体组肝脏、肺脏中的药物分布明显提高,肾脏中的分布降低;通过相对摄取率、靶向效率和峰浓度比3个靶向指标的对比,脂质体组明显提高了肺部靶向性,且在肺部有一定的缓释作用。     

Preparation and evaluation of danofloxacin mesylate microspheres and its pharmacokinetics in pigs

Danofloxacin mesylate gelatin microspheres (DFM-GMS) were prepared by an emulsion chemical crosslinking technique. Distribution of particle size, morphologic characteristics, drug content, and drug stability were evaluated. In-vitro study showed that the release of danofloxacin mesylate (DFM) from microspheres was much slower than from the raw material (DFM) in the release medium. Pharmacokinetic characteristics were evaluated following intramuscular injection of DFM-GMS or DFM in pigs at dosage of 2.5 mg/kg body weight. Elimination half-life (t_1/2β) of the drug was 24.32 h for DFM-GMS, and 6.61 h for DFM (P?<?0.01). Overall, DFM-GMS could be applied as a long-acting and lung targeting dosage form of DFM for clinical application.

     

Clinical efficacy of tirilazad mesylate for treatment of endotoxemia in neonatal calves.

The clinical efficacy of the lazaroid, tirilazad mesylate, a new therapeutic agent for prophylaxis and treatment of endotoxemia, was evaluated in 24 neonatal Holstein calves. Endotoxemia was induced by IV infusion of commercial Escherichia coli lipopolysaccharide (3.25 micrograms/kg of body weight) over 3 hours. Group-1 calves were given endotoxin alone; group-2 calves were given an infusion of 0.9% sterile saline solution, then were treated with tirilazad mesylate (1.5 mg/kg) 1 hour after the infusion was started. Group-3 calves were treated with tirilazad mesylate 1 hour after the start of the endotoxin infusion, and group-4 calves were given tirilazad mesylate 1 hour before the start of the endotoxin infusion. Clinical signs of endotoxemia were mitigated by tirilazad mesylate. In addition, tirilazad mesylate protected calves from endotoxin-induced hyperglycemia; treatment after endotoxin infusion decreased the severity of hypoglycemia and prevented lactic acidosis. Treatment with tirilazad mesylate after initiation of endotoxin infusion was as protective as was pretreatment.     

A phase I clinical trial evaluating imatinib mesylate (Gleevec) in tumor-bearing cats

A phase I clinical trial evaluating the toxicity of orally-administered imatinib mesylate was performed in 9 tumor-bearing cats. Imatinib is a small molecule, tyrosine kinase inhibitor, which selectively blocks the function of overexpressed proteins associated with various malignancies. Cats included in the study had diagnoses of fibrosarcoma, squamous cell carcinoma, and mast cell tumor, and each cat was staged using CBC and serum biochemistry; urinalysis, thoracic radiographs, and abdominal ultrasonography were performed in some cats. Most cats were treated previously by surgery, radiation therapy, chemotherapy, or some combination of these treatments. None of the cats received any concurrent chemotherapy. Six cats were treated with imatinib mesylate at 1-2 mg/kg PO q24h. Dose escalations were made to 2, 4, and 10 mg/kg PO q24h in 5 cats. Two cats started therapy at 10 mg/kg PO q24h, and 1 cat started therapy at 15 mg/kg PO q24h; all 3 cats remained at these dosages. No signs of toxicity, as evaluated by CBC and serum biochemistry, were noted in 8 of the 9 cats, and minimal gastrointestinal toxicity was observed. Due to the low frequency of adverse effects, further evaluation of imatinib is ongoing at a dosage of 10 mg/kg PO q24h.     

The effects of deferoxamine mesylate on iron elimination after blood transfusion in neonatal foals

Background: Hepatic failure is one of the more common complications in foals requiring blood transfusion to treat neonatal isoerythrolysis. Iron intoxication is likely the cause of hepatic injury. Objectives: To determine the effects of deferoxamine on iron elimination in normal foals. Animals: Thirteen neonatal foals. Methods: Randomized‐controlled trial. At 1–3 days of age, foals received either 3 L of washed packed dam's red blood cells (RBC) or 3 L of saline IV once. Foals were treated with deferoxamine (1 g) or saline (5 mL) SC twice daily for 14 days. Foals were randomly assigned to 1 of 3 groups: RBC/deferoxamine (deferoxamine), RBC/saline (placebo), or saline/saline (control). Blood and urine samples and liver biopsy specimens were collected for measurement of hematological, biochemical, and iron metabolism variables. Results: There was a significant (P < .05) increase in hematocrit, RBC count, and hemoglobin in the groups transfused with packed RBC as compared with controls at all times. Biochemical variables and liver biopsy scores were not significantly different between groups at any time. Urine iron concentrations and fractional excretion of iron were significantly higher in deferoxamine treated foals. By 14 days after transfusion, liver iron concentrations in foals treated with deferoxamine (79.9 ± 30.9 ppm) were significantly lower than that of foals receiving placebo (145 ± 53.0 ppm) and similar to that of controls (44.8 ± 4.09 ppm). Conclusions and Clinical Importance: Deferoxamine enhances urinary iron elimination and decreases hepatic iron accumulation after blood transfusion in foals.