Tablet formulation studies on nimesulide and meloxicam-cyclodextrin binary systems

The objective of this work was to develop tablet formulations of nimesulide-β-cyclodextrin (NI-β-CD) and meloxicam-γ-cyclodextrin (ME-γ-CD) binary systems. In the case of nimesulide, 3 types of binary systems—physical mixtures, kneaded systems, and coevaporated systems—were studied. In the case of meloxicam, 2 types of binary systems—physical mixtures and kneaded systems—were investigated. Both drug-CD binary systems were prepared at 1∶1 and 1∶2 molar ratio (1∶1M and 1∶2M) and used in formulation studies. The tablet formulations containing drug-CD binary systems prepared by the wet granulation and direct compression methods showed superior dissolution properties when compared with the formulations of the corresponding pure drug formulations. Overall, the dissolution properties of tablet formulations prepared by the direct compression method were superior to those of tablets prepared by the wet granulation method. Selected tablet formulations showed good stability with regard to drug content, disintegration time, hardness, and in vitro dissolution properties over 6 months at 40°C±2°C and 75% relative humidity. Published: May 11, 2007     

酮洛芬缓释片人体药动学和生物等效性研究

目的:评价受试酮洛芬缓释片与参比酮洛芬片的生物等效性。方法:采用反相高效液相色谱法测定24名健康男性志愿受试者交叉单剂量口服受试酮洛芬缓释片与参比酮洛芬片150mg后血浆中酮洛芬的浓度,用3p97程序进行数据处理。结果:口服受试和参比酮洛芬制荆后的AUC_(0-(?))分别是38.94±9.15μg·h·ml~(-1)、38.04±6.90μg·h·ml~(-1);AUC_(0-(?))分别是44.50±8.09μg·h·ml~(-1)、42.99±8.36μg·h·ml~(-1);T_(max)分别是3.87±0.55 h、1.96±0.60h;C_(max)分别是5.78±1.11μg·ml~(-1)、11.62±2.10μg·ml~(-1);t_(1/2)(Ke)分别是5.88±1.16h、1.70±1.40h。结论:受试酮洛芬缓释片与参比酮洛芬片具有生物等效性。     

Hantzsch condensation reaction as a spectrofluorometric method for determination of alogliptin,an antidiabetic drug,in pure form,tablet form,and human and rat plasma

To analyze alogliptin in its pharmaceutical dosage forms and human plasma, a sensitive, inexpensive, simple, and precise spectrofluorimetric method was developed and tested. This method was also used to investigate the drug’s pharmacokinetic behaviour in the blood of rats. This was based on the Hantzsch reaction, which produces yellowish luminous products that can be detected spectrofluorometrically at 480 and 415 nm for emission and excitation, respectively, when the primary amine group in the examined drug reacts with acetylacetone and formaldehyde. Several experimental parameters that affect the reaction product's development and stability were explored and improved. The curve of fluorescence and concentration for alogliptin was linear in the concentration range 0.05–3.60 μg ml⁻¹. The proposed approach was validated according to International Council for Harmonization criteria. The method was successfully utilized to evaluate the examined drug in dose formulations and spiked human plasma with high accuracy.     

强力定眩片及联合他汀类对高脂血症小鼠的降脂作用

摘要 目的：探讨强力定眩片及联合他汀类药物的降脂作用,通过对上市药品再评价,指导临床合理用药。方法：采用60% kcal高脂饲料建立高脂血症小鼠模型,同时灌胃给予强力定眩片或瑞舒伐他汀钙片8周,于给药2、4、8周分别检测血清中血脂水平,8周给药结束后检测血清及肝脏中总胆固醇（TC）、甘油三酯（TG）、高密度脂蛋白（HDL-C）和低密度脂蛋白（LDL-C）含量,H&E染色和油红O染色观察肝脏脂肪病变情况。结果：给药2周、4周和8周,瑞舒伐他汀钙片组、强力定眩片高、中剂量组以及联合给药组TC、TG和LDL-C水平均低于模型组,差异具有统计学意义（P<0.05或P<0.01）,HDL-C高于模型组（P<0.05）,随着给药时间延长,药物的降脂作用更明显。H&E和油红O染色结果显示,模型组小鼠肝脏脂肪病变严重,出现脂肪空泡和红色脂滴,强力定眩片能成剂量依赖性改善肝脏脂肪病变,联合用药后肝脏脂肪病变改善最为显著,肝脏细胞基本恢复正常,肝脏细胞排列整齐,仅存在少量红色脂滴和脂肪空泡。结论：在观察的时间段（2周～8周）,随着用药时间的延长,除强力定眩片低剂量组外,各组对血脂指标改善明显,肝脏脂肪病变程度减轻,脂滴减少,强力定眩片呈现剂量依赖性,联合用药后强力定眩片和瑞舒伐他汀钙片具有协同降脂作用。本研究为临床合理用药提供了实验依据。     

坤复康片联合阿莫西林克拉维酸钾对慢性盆腔炎患者血液流变学、红细胞免疫功能和炎症因子的影响

摘要 目的：探讨坤复康片联合阿莫西林克拉维酸钾对慢性盆腔炎患者血液流变学、红细胞免疫功能和炎症因子的影响。方法：采用随机数字表法将我院2021年4月~2022年4月期间收治的98例慢性盆腔炎患者分为对照组（阿莫西林克拉维酸钾干混悬剂治疗,n=49）和研究组（坤复康片联合阿莫西林克拉维酸钾干混悬剂治疗,n=49）。对比两组症状好转时间、血液流变学、红细胞免疫功能和炎症因子水平,观察两种用药方案的安全性。结果：研究组的下腹疼痛、腰骶疼痛、白带量多、经期量多等临床症状好转时间均短于对照组（P<0.05）。研究组治疗14 d后全血高切黏度、全血低切黏度、血浆黏度、纤维蛋白原水平低于对照组（P<0.05）。研究组治疗14 d后血红细胞C3b受体花环率（RBC-C3bRR）高于对照组,免疫复合物花环率（RBC-ICR）低于对照组（P<0.05）。研究组治疗14 d后血清C反应蛋白（CRP）、白细胞介素-17（IL-17）、肿瘤坏死因子-α（TNF-α）、白细胞介素-6（IL-6）水平低于对照组（P<0.05）。两组不良反应发生率对比无差异（P>0.05）。结论：坤复康片联合阿莫西林克拉维酸钾可通过改善慢性盆腔炎患者的血液流变学、炎症因子、红细胞免疫功能来改善临床症状,具有较好的临床疗效。     

反相高效液相色谱法检测脂必妥片中洛伐他汀的含量

对脂必妥片样品进行预处理,得到的混合物用薄层色谱、反相高效液相色谱法进行定性、定量分析,建立检测其含量的方法。当色谱条件为色谱柱:Kromasil(C18250 mm×4.6 mm,5μm);流动相体积比:乙腈∶水为85∶15,;流速:1.0 ml.min-1;检测波长:420 nm;柱温:30℃;测定结果表明被测峰和其它峰可完全分离,在每毫升10.21~200.03μg内具有良好的线性关系,r=0.9997,测得其中洛伐他汀含量为0.25%,回收率:97.73%,RSD:0.56%。这种方法准确、可靠,可用于含洛伐他汀药品的质量控制。     

瘿瘤消散汤联合左甲腺素钠片治疗结节性甲状腺肿的疗效观察

目的:探讨瘿瘤消散汤联合左甲腺素钠片治疗结节性甲状腺肿的临床疗效。方法:选择2013年7月到2016年2月在我院门诊治疗的120例结节性甲状腺肿患者,随机分为对照组和试验组,各60例。对照组患者给予左甲腺素钠片治疗,试验组患者给予瘿瘤消散汤联合左甲腺素钠片治疗,两组患者均治疗6个月。评价并比较两组患者临床疗效。测量并比较两组患者治疗前后甲状腺结节最大横截面积和最大直径,检测并比较两组患者治疗前后血清促甲状腺激素(TSH)、促甲状腺素受体抗体(TRAb)、游离三碘甲状腺原氨酸(FT3)及游离甲状腺素(FT4)水平。结果:试验组患者的总有效率为86.67%,明显高于对照组的66.67%(P0.05)。治疗后,两组患者的甲状腺结节最大横截面积、最大直径均明显低于治疗前,并且试验组患者均明显低于对照组(P0.05)。治疗后,两组患者血清TSH、TRAb及FT3水平均明显低于治疗前,并且试验组患者均明显低于对照组,差异均具有统计学意义(P0.05);两组患者血清FT4水平治疗前后均无明显变化(P0.05)。结论:瘿瘤消散汤联合左甲腺素钠片治疗结节性甲状腺肿的临床疗效显著,能够明显缓解临床症状和体征,值得在临床上推广应用。     

Process analytical technology case study part I: Feasibility studies for quantitative near-infrared method development

This article is the first of a series of articles detailing the development of near-infrared (NIR) methods for solid-dosage form analysis. Experiments were conducted at the Duquesne University Center for Pharmaceutical Technology to qualify the capabilities of instrumentation and sample handling systems, evaluate the potential effect of one source of a process signature on calibration development, and compare the utility of reflection and transmission data collection methods. A database of 572 production-scale sample spectra was used to evaluate the interbatch spectral variability of samples produced under routine manufacturing conditions. A second database of 540 spectra from samples produced under various compression conditions was analyzed to determine the feasibility of pooling spectral data acquired from samples produced at diverse scales. Instrument qualification tests were performed, and appropriate limits for instrument performance were established. To evaluate the repeatability of the sample positioning system, multiple measurements of a single tablet were collected. With the application of appropriate spectral preprocessing techniques, sample repositioning error was found to be insignificant with respect to NIR analyses of product quality attributes. Sample shielding was demonstrated to be unnecessary for transmission analyses. A process signature was identified in the reflection data. Additional tests demonstrated that the process signature was largely orthogonal to spectral variation because of hardness. Principal component analysis of the compression sample set data demonstrated the potential for quantitative model development. For the data sets studied, reflection analysis was demonstrated to be more robust than transmission analysis. Published: October 6, 2005 The views presented in this article do not necessarily reflect those of the Food and Drug Administration.     

非洛地平缓释片对轻中度原发性高血压患者的降压疗效和对脉搏波 速度的影响

目的:探讨非洛地平缓释片对轻中度原发性高血压患者的降压疗效和对脉搏波速度的影响。方法:根据纳入标准选取我院260例原发性高血压患者,按计划方案给予非洛地平缓释片口服治疗。观察患者入院后、治疗2周末、14周末降压疗效及脉搏波传导速度的改变情况,并进行对比分析。结果:本组研究中接受治疗研究者共260例,其所有受检者在治疗2、6、10、14周后血压水平均有不同程度改善,与基线比较差异明显,有统计学意义(P<0.01)。脉搏波变化分析所有受试者脉搏波速度变化分析,基线脉搏波速度为(10.9±2.4)m/s,经过治疗后2周、14周基线脉搏波速度为(10.3±2.1)m/s,差异明显具有统计学意义(P<0.01);心率变化分析表明非洛地平缓释片在降压同时对心率影响不大,安全性评价表示,接受治疗期间曾有68例发生不良事件,占总数26.2%。笔者认为与药物无关,且均为轻度,经过适当处理后均缓解,对本研究无影响。结论:非洛地平缓释片降压效果良好,可同时降低颈动脉-股动脉脉搏波传导速度,改善大动脉僵硬度。     

百乐眠胶囊联合艾司西酞普兰片对失眠伴抑郁焦虑患者睡眠质量、不良情绪以及神经递质水平的影响

摘要 目的：探讨百乐眠胶囊联合艾司西酞普兰片对失眠伴抑郁焦虑患者睡眠质量、不良情绪以及神经递质水平的影响。方法：选取2017年7月~2019年12月期间我院收治的失眠伴抑郁焦虑患者117例,将上述患者根据随机数字表法分为对照组（n=58,艾司西酞普兰片治疗）和研究组（n=59,百乐眠胶囊联合艾司西酞普兰片治疗）,比较两组患者睡眠质量、不良情绪、多导睡眠图（PSG）参数、神经递质水平及不良反应。结果：研究组治疗2个月后的临床总有效率为93.22%（55/59）,高于对照组的79.31%（46/58）（P<0.05）。两组治疗2个月后汉密尔顿焦虑量表（HAMA）、汉密尔顿抑郁量表（HAMD）以及匹兹堡睡眠质量指数（PSQI）评分、睡眠潜伏期、P物质（SP）均较治疗前降低,且研究组低于对照组（P<0.05）。两组治疗2个月后睡眠总时间、睡眠效率、神经肽Y（NPY）、5-羟色胺（5-HT）升高,且研究组高于对照组（P<0.05）。治疗期间研究组不良反应发生率较对照组降低（P<0.05）。结论：失眠伴抑郁焦虑患者经百乐眠胶囊联合艾司西酞普兰片治疗后,睡眠质量、不良情绪得到显著改善,同时还可有效改善血清神经递质水平,减少不良反应,临床应用效果确切。