HPLC法测定恩普洛胶囊中丙磺舒的含量

目的　测定恩普洛胶囊中丙磺舒的含量。 方法 　高效液相色谱法 ;C8柱 (5μm.4.6× 15 0 mm) ;流动相为水 -乙腈 -1.0 mol· L- 1 磷酸二氢钾溶液 -1.0 mol· L- 1 醋酸溶液 (90 9∶ 690∶ 10∶ 1) ;流速 1.0 ml· min- 1 ;检测波长 2 5 4nm。结果 　丙磺舒在 2 5～ 2 0 0μg· ml- 1 范围内呈良好线性关系 (r=0 .99999) ,重现性良好 ,RSD=0 .1% (n=8) ,平均回收率 10 0 .0 % ,RSD=0 .5 % (n=9)。 结论 　本法操作简便 ,结果准确 ,重现性好     

RP-HPLC测定利福昔明的含量及有关物质

目的　建立测定利福昔明含量及有关物质的方法。方法　采用C18色谱柱 (5 μm ,15 0mm× 4.6mm) ,流动相为甲醇 -乙腈 - 0 .0 5mol·L-1磷酸二氢钾溶液 - 0 .5mol·L-1枸橼酸溶液 (5 0∶2 5∶2 0∶5 ) ,检测波长 2 5 4nm。结果　利福昔明在 5 0～ 2 0 0 μg·ml-1浓度范围内 ,峰面积与浓度呈良好的线性关系 (r=0 .9999) ,平均回收率为 99.9%。结论　所建方法简便 ,专属性及重复性好 ,可用于利福昔明的含量及有关物质的测定。     

高效液相色谱法测定土霉素及其盐酸盐的含量和有关物质

目的 :采用高效液相色谱法测定土霉素的含量及有关物质。方法 :SGEW5C18-AR柱为分析柱 ,流动相为 0 0 5mol·L-1草酸铵 -二甲基甲酰胺 - 0 2mol·L-1磷酸氢二铵 (75∶2 0∶5 ) ,用氨试液调节pH至 8 0± 0 2 ,柱温 35℃ ,流速 0 8mL·min-1,检测波长 2 80nm ,峰面积外标法。结果 :土霉素在 5～ 90 μg·mL-1范围内呈良好的线性关系 ,r=0 9994,平均回收率为 10 0 1% (n =7) ,RSD =0 87% (n =7)。结论 :本方法简便 ,快速 ,结果准确 ,可靠 ,重现性好。     

高效液相色谱法测定克拉霉素的含量

用高效液相色谱法 ,测定克拉霉素的含量。十八烷基硅烷键合硅胶 ( 5 um)为分析柱。流动相 :0 .1mol· L- 1 ,磷酸二氢铵溶液 (三乙胺调节 p H6.5 ) -乙腈 ( 70∶ 3 0 ) ;流速 :1.0 ml·m in- 1 ,检测波长 2 10 nm,进样量 2 0 μL。在进样量 2 .5～ 80 .0 μg的范围内 ,进样量与峰面积线性关系良好 r=0 .9999) ,重复进样 RSD=0 .2 9%。     

HPLC测定利福定胶囊的含量

目的　建立利福定胶囊的含量测定方法。方法　采用KromasilC18柱 (4 .6mm× 2 0 0mm ,5 μm) ,以甲醇 - 0 0 5mol·L-1乙酸铵溶液为流动相 ,进样 2 0 μl,检测波长 2 5 4nm。 结果　利福定在 0 0 5～ 0 5 4mg·ml-1范围内 ,呈良好的线性关系 (r =0 9999) ,平均回收率为 10 0 6 6 % ,RSD =0 82 %。结论　方法准确可靠 ,可用于测定利福定胶囊的含量     

HPLC法测定盐酸阿夫唑嗪片中盐酸阿夫唑嗪的含量

目的　建立用HPLC法测定盐酸阿夫唑嗪片中盐酸阿夫唑嗪含量。方法　以盐酸特拉唑嗪为内标,采用Alltima-CN柱,流动相为 0 0 5mol·L-1磷酸二氢钠溶液(0 5mol·L-1的氢氧化钠溶液调pH至 5 4 ) -乙腈(78∶2 2);检测波长:2 4 4nm。结果与结论　盐酸阿夫唑嗪在 5～ 5 0 μg·ml-1范围内呈良好的线性关系,回收率为 99 8%,RSD =0 9% (n =9)。     

高效液相色谱法测定诺氟沙星滴眼液的含量

目的 　采用高效液相色谱法测定诺氟沙星滴眼液的含量。方法 　C1 8柱 (15 0× 4.6mm,5 μm) ,流动相为 0 .0 2 5 mol·L- 1磷酸溶液 (用三乙胺调节 p H值至 3 .0± 0 .1) -乙腈 (87∶ 13 ) ;流速 1.0 ml· min- 1 ;检测波长 2 78nm。结果 　诺氟沙星在 0 .1～ 1.0μg呈良好线性 (r=0 .9998) ,平均回收率 10 0 .0 %,RSD为 0 .5 %。 结论 　本法简便、快捷 ,结果准确 ,重现性好     

HPLC测定土霉素片的含量

目的　测定土霉素片的含量。方法　采用HPLC法 ,C18色谱柱 ,以 0 0 5ml·L-1草酸铵溶液 -二甲基甲酰胺 - 0 2mol·L-1磷酸氢二铵溶液 (75∶2 0∶5 )为流动相 ,检测波长 2 80nm。结果　土霉素在 0 0 1～ 0 15mg·ml-1范围内呈良好的线性关系 ,回归方程为 :Y =2 5 4× 10 7X +2 15× 10 4(r =0 .9996 ,n =7)。平均加样回收率为 98 7% (RSD =1 13% ,n =5 )。结论　方法简便、快速、准确。     

反相离子对色谱法测定诺氟沙星滴眼液中的诺氟沙星和有关物质

目的 :建立了一种反相离子对色谱法测定诺氟沙星滴眼液中的诺氟沙星和有关物质。方法 :用SpherisorbC18ODS柱 ,甲醇 0 .0 5mol·L-1磷酸盐缓冲液 0 .0 5mol·L-1四丁基溴化铵 (2 5∶75∶4,pH =2 .75 )为流动相 ,紫外检测波长为 2 80nm。结果 :诺氟沙星线性范围 :0 .12～ 1.0 0 μg ,r =0 .9994,平均回收率为 98.0 % ,RSD为 1.0 % (n =5 )。结论 :该法准确、快速、简便 ,可用于诺氟沙星滴眼液中的诺氟沙星的含量测定。     

HPLC法测定麻咳糖浆中盐酸麻黄碱的含量

目的 :建立麻咳糖浆中盐酸麻黄碱含量测定的方法。方法 :HPLC法 ,色谱柱 :HypersilODS2 (5 μm ,4 .6mm× 2 0 0mm) ,流动相 :甲醇 - 0 .0 1mol·L-1磷酸二氢钾溶液 (磷酸调至pH 2 .5 ) (2 0∶80 ) ,检测波长 :2 10nm。结果 :盐酸麻黄碱在 4～12 μg范围内线性关系良好 (r =0 .9999,n =5 ) ,平均回收率为 99.1% ,RSD :1.2 %。结论 :本方法简便 ,结果准确 ,重现性好 ,可用于该制剂的质量控制指标之一。     

利福喷丁及其胶囊质量标准提高的研究

目的：提高利福喷丁及其胶囊的质量标准。方法：按照《中国药典》2015年版的相关规定,参考现行标准及研究文献,考察本品的性状、鉴别、有关物质及含量。结果：修订了溶解度、有关物质和含量测定色谱条件,增订了薄层色谱鉴别方法。结论：改进的标准可以更好地控制利福喷丁原料和胶囊的质量。     

Single-Dose Pharmacokinetics of Rifapentine in Women

Gender can be an important variable in the absorption and disposition of some drugs. In this open-label study, 15 healthy, nonsmoking women received a single 600-mg oral dose of rifapentine. Plasma samples were obtained at frequent intervals for up to 72 hr after the dose to determine the pharmacokinetic (PK) parameters of rifapentine and its active metabolite, 25-desacetyl-rifapentine. Peak plasma rifapentine concentrations (C_max ) were observed 5.9 hr after ingestion of the single dose. The mean area under the rifapentine plasma concentration–time curve [AUC(0 )] was 325 g · hr ml and the mean elimination half-life (t_1/2 ) was 16.3 hr. Plasma concentrations for the 25-desacetyl metabolite peaked at 15.4 hr after the rifapentine dose and declined with a terminal half-life of 17.3 hr. These rifapentine and 25-desacetyl-rifapentine PK data in women were compared to data generated previously in healthy men. Striking similarities in the PK profiles of parent drug and metabolite were found in the two populations. Mean differences in rifapentine CL/F (12%) and t_1/2 (2%) were small. The only adverse event reported in the female subjects was discoloration of the urine. Based on these PK and safety data, no dosage adjustments for rifapentine based on gender are recommended.     

A Novel Inhalable Form of Rifapentine

Recent murine studies found that rifapentine, dosed daily, at least halved tuberculosis treatment times compared with standard rifampicin and isoniazid-containing regimens. However, in humans, an inhalable form of rifapentine may be necessary to considerably shorten treatment duration because of the physiological barriers associated with oral therapy. The current study compares two inhalable rifapentine dry powders—a novel pure crystalline form and an amorphous form—by a series of in vitro tests. The crystalline and amorphous powders had a mass median aerodynamic size of 1.68 ± 0.03 and 1.92 ± 0.01 μm, respectively, associated with a fine particle fraction of 83.2 ± 1.2% and 68.8 ± 2.1%, respectively. A quinone degradation product was identified in the amorphous powder stored for 1 month, whereas the crystalline form remained chemically stable after storage at both 0% and 60% relative humidity, 25°C, for at least 3 months. Solubilized rifapentine was well tolerated by pulmonary tissue and macrophage cells up to approximately 50 μM. The accumulation of rifapentine within alveolar macrophage cells was significantly higher than for rifampicin, indicating enhanced delivery to infected macrophages. The novel inhalable crystalline form of rifapentine is suitable for targeted treatment of tuberculosis infection and may radically shorten treatment duration. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association.     

利福喷丁的溶解性与稳定性考察

目的:考察利福喷丁的溶解性及其稳定性,为开发其新剂型奠定基础。方法:采用紫外分光光度法测定利福喷丁在11种溶剂中的溶解度及研究4种增溶剂对其的增溶作用;考察其在正己烷和正辛醇中的表观油水分配系数及在高湿、高温、光照条件下的稳定性。结果:利福喷丁在三氯甲烷中溶解性较好,溶解度为13.076 mg.L-1,在水中溶解性较差,为3.046 mg.L-1;吐温-80对其增溶作用较强,溶解度达到823 mg.L-1;在正己烷和正辛醇中的表观油水分配系数分别为4.778±0.41、17.441 2±2.79;稳定性指标中色泽和主药含量在考察期内均有变化。结论:利福喷丁的脂溶性强、水溶性差,合适的增溶剂对其有一定的增溶作用,其在高温、高湿、光照条件下不太稳定。     

Single-dose Pharmacokinetics of Rifapentine in Elderly Men

Purpose. This study was undertaken to characterize the pharmacokinetic profiles of rifapentine and its active metabolite, 25-desacetyl-rifapentine, in elderly men. Methods. Fourteen healthy, nonsmoking male volunteers between the ages of 65 and 82 years received a single oral 600 mg dose of rifapentine. Plasma samples were collected at frequent intervals for up to 72 hours postdose. The control group consisted of 20 healthy, young (18–45 years) male volunteers from a previous, single-dose (600 mg) rifapentine pharmacokinetic study. Results. Plasma rifapentine concentrations above the minimum inhibitory concentration for M. tuberculosiswere observed at 2 hours after dosing. Disposition of rifapentine was monophasic with a mean terminal half-life of 19.6 hours. The peak plasma concentration of 25-desacetyl-rifapentine was found 21.7 hours, on average, after the rifapentine dose; the mean 25-desacetyl-rifapentine t_1/2was 22.9 hours. Compared to the younger subjects, apparent oral clearance of rifapentine (24%) was lower in the elderly male (p < 0.05), and Cmax (28%) was higher. The only adverse event reported in both the older and younger subjects in these single-dose studies was discoloration of the urine. Conclusions. Because the age-related changes in the pharmacokinetic profile of rifapentine observed in this study were modest and unlikely to be associated with toxicity, no dosage adjustments for this antibiotic are recommended in elderly patients.     

Rifapentine for the treatment of latent tuberculosis

Introduction: The goal of this article is to review the use of rifapentine in the treatment of latent tuberculosis infection (LTBI). Controlling LTBI is an important part of the global strategy to end the spread of tuberculosis. Rifapentine’s potent sterilizing effect against Mycobacterium tuberculosis combined with its long half-life make it an attractive LTBI treatment option.

Areas covered: A systematic literature search of Pubmed using the terms ‘rifapentine’ and ‘tuberculosis’ was performed. Articles identified were cross-referenced for other relevant publications. The mechanisms of action and resistance, pharmacokinetic and pharmacodynamics, potential drug interactions and side effects are discussed.

Expert commentary: Rifapentine in combination with isoniazid for twelve weeks is the best available option for treating latent TB in the majority of patients in the United States due to its favorable safety profile and the increased likelihood of completing therapy. Currently, rifapentine is not registered or available in other countries.     

HPLC法测定利福喷丁血药浓度的改进

本文就ＨＰＬＣ法测定利福喷丁的血药浓度进行了改进，以舒乐安定为内标，采用甲醇沉淀血浆中蛋白，离心后取上清液直接进样，方法简便、快速、灵敏度高，可推广使用。并应用该法测定了８例结核病患者不同时间的血药浓度，为临床合理用药提供了可靠依据。     

RP-HPLC法测定人血浆中利福喷丁的浓度

目的:建立反相HPLC法测定人血浆中利福喷丁的浓度.方法:以利福平为内标,采用ZORBAX SB-C18色谱柱(4.6mm×250 mm,5μm),以甲醇-0.02 mol·L-1磷酸缓冲液(67:33,v/v;pH 7.0)为流动相,流速1.0 ml·min-1,柱温40℃,340 nm处紫外检测.结果:日内平均回收率为97.5%,RSD=4.1%(n=5),日间平均回收率为95.6%,RSD=5.4%(n=5),线性范围为0.54～17.28μg·ml-1(r=0.999 5).结论:本法简便快速,灵敏度高,重现性好,适用于利福喷丁化疗方案的临床监测及其药动学研究.     

利福喷丁对氨茶碱药代动力学的影响

本文应用紫外分光光度法对两组家兔分别单服氨茶碱及氨茶碱加服利福喷丁后的药代动力学参数进行了对比。结果表明,按8mg/kg的剂量连服利福喷丁4d可使氨茶碱的消除速率常数(K)升高;半衰期(t_(1/2))下降;曲线下面积(AUC)减小。经统计学处理p<0.05。提示在临床上两药同服时,应加强对氨茶碱的血药浓度监测,进行个体化给药以控制氨茶碱的有效血药浓度。     

利福喷汀胶囊人体生物等效性研究

目的:评价两种利福喷汀胶囊的人体生物等效性.方法:20名男性健康志愿者随机交叉单剂量口服受试制剂或参比制剂利福喷汀胶囊600 mg后,采用高效液相色谱法测定血药浓度,用DAS软件计算药动学参数,并评价其生物等效性.结果:单剂量口服利福喷汀胶囊受试制剂和参比制剂的主要药动学参数分别为:t1/2(16.44 ±4.99)、(18.02±4.76)h;tmax(5.6±1.4)、(6.0±1.4)h; Cmax(8.41 ±1.71)、(8.96±1.76) μg· ml-1;AUC(0～72) (200.41 ±55.29)、(220.86±62.40)μg·h·ml-1;AUC0-∞(215.58±63.51)、(241.06±75.09)μg·h·m1-1.受试制剂的相对生物利用度为(92.3±14.3)％.结论:两种制剂具有生物等效性.