Tablet formulation containing meloxicam and β-cyclodextrin: Mechanical characterization and bioavailability evaluation

The purpose of this research was to evaluate β-cyclodextrin (β-CD) as a vehicle, either singly or in blends with lactose (spray-dried or monohydrate), for preparing a meloxicam tablet. Aqueous solubility of meloxicam in presence of β-CD was investigated. The tablets were prepared by direct compression and wet granulation techniques. The powder blends and the granules were evaluated for angle of repose, bulk density, compressibility index, total porosity, and drug content. The tablets were subjected to thickness, diameter, weight variation test, drug content, hardness, friability, disintegration time, and in vitro dissolution studies. The effect of β-CD on the bioavailability of meloxicam was also investigated in human volunteers using a balanced 2-way crossover study. Phase-solubility studies indicated an A_L-type diagram with inclusion complex of 1∶1 molar ratio. The powder blends and granules of all formulations showed satisfactory flow properties, compressibility, and drug content. All tablet formations prepared by direct compression or wet granulation showed acceptable mechanical properties. The dissolution rate of meloxicam was significantly enhanced by inclusion of β-CD in the formulations up to 30%. The mean pharmacokinetic parameters (C_max, K_e, and area under the curve [AUC]_0−∞) were significantly increased in presence of β-CD. These results suggest that β-CD would facilitate the preparation of meloxicam tablets with acceptable mechanical properties using the direct compression technique as there is no important difference between tablets prepared by direct compression and those prepared by wet granulation. Also, β-CD is particularly useful for improving the oral bioavailablity of meloxicam.     

芪丹通脉片促进骨髓间充质干细胞向缺血心肌趋化迁移

目的:研究芪丹通脉片对骨髓间充质干细胞向缺血心肌趋化迁移的作用。方法:SD大鼠,随机分为单纯移植组,益气组,活血组。芪丹通脉片组,各组大鼠灌服中药14天后,采用冠状动脉左前降支结扎法建立心肌梗死模型。经尾静脉注入DIO标记的骨髓间充质干细胞,3天后取缺血部位的心肌,应用流式细胞仪分析计算出每克心肌所含有的DIO阳性细胞数;行冰冻切片,采用荧光显微镜观察DIO阳性细胞;4周后采用多导生理记录仪记录大鼠平均动脉压(MAP)、左心室收缩峰压(LVPSP)、左心室内压最大上升变化速率(+LVdp/dtmax)和最大下降速率(-LVdp/dtmax)。结果:芪丹通脉片组较益气组、活血组、单纯移植组,每克心肌所含有的DIO阳性细胞数增多,其差异有统计学意义;冰冻切片镜下观察,芪丹通脉片组阳性细胞数较益气组、活血组、单纯移植组增多,其差异有统计学意义;心功能检测示:芪丹通脉片组MAP、LVPSP、+LVdp/dtmax、-LVdp/dtmax较益气组、活血组、单纯移植组改善明显,差异有统计学意义。结论:芪丹通脉片具有促进骨髓间充质干细胞向缺血心肌趋化迁移的作用,益气与活血中药配伍应用优于单纯益气药或活血药。     

义齿清洁片对义齿菌斑细菌构成的影响

目的 比较义齿清洁片对义齿菌斑细菌构成的影响。方法 义齿清洁片保丽净和雅克菱连续2 d浸泡义齿过夜,白天带入,采集义齿黏膜面菌斑标本,PCR扩增细菌16S rDNA基因V4-V5区,Miseq Illumina高通量测序。结果 保丽净在科水平韦荣球菌科减少,增加链球菌科,在属水平韦荣球菌属减少,链球菌属增加。相反地,雅克菱在科水平链球菌科减少,韦荣球菌科增加,在属水平链球菌属减少,同时韦荣球菌属细菌增加。结论 根据保丽净和雅克菱对义齿菌斑不同的清洁效果,可以考虑保丽净和雅克菱交替使用以获得更好的义齿清洁效果。     

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。     

心血管领域复方创新药的范例：缬沙坦沙库比曲片与依那普利叶酸片——给我国新药创制带来的启示

缬沙坦沙库比曲片与依那普利叶酸片均属于复方创新药,即其中单药在组成复方后的疗效或适应证发生新的变化。针对临床需求、疗效以及循证依据,详细剖析这两种复方创新药的组方特点,重点探讨复方创新药与一般复方药的区别,为以临床价值为导向和基于患者人群特点的重大新药创制提供借鉴。     

胃复春片联合兰索拉唑肠溶片对慢性萎缩性胃炎患者血清胃肠激素、炎症因子及免疫功能的影响

摘要 目的：胃复春片联合兰索拉唑肠溶片对慢性萎缩性胃炎（CAG）患者血清胃肠激素、炎症因子及免疫功能的影响。方法：选取62例CAG患者,根据门诊挂号奇偶性分为对照组（n=31,兰索拉唑肠溶片治疗）和研究组（n=31,胃复春片联合兰索拉唑肠溶片治疗）。比较两组患者疗效、胃肠激素[胃泌素(GAS)、胃动素(MTL)]、炎症因子[超敏C反应蛋白（hs-CRP）、肿瘤坏死因子-α（TNF-α）、白介素-6（IL-6）]、免疫功能及不良反应。结果：研究组治疗2个月后的总有效率为87.10%（27/31）,高于对照组的64.52%（20/31）,差异有统计学意义（P<0.05）。治疗2个月后,研究组hs-CRP、TNF-α、IL-6、GAS、CD8P低于对照组,MTL、CD4P、CD4⁺/CD8⁺高于对照组（P<0.05）。两组不良反应发生率对比未见明显差异（P>0.05）。结论：胃复春片联合兰索拉唑肠溶片治疗CAG疗效确切,可有效改善机体胃肠激素、炎症因子水平及免疫功能,且安全可靠,具有一定应用价值。     

Process analytical technology case study,part III: Calibration monitoring and transfer

This is the third of a series of articles detailing the development of near-infrared spectroscopy methods for solid dosage form analysis. Experiments were conducted at the Duquesne University Center for Pharmaceutical Technology to develop a system for continuous calibration monitoring and formulate an appropriate strategy for calibration transfer. Indcators of high-flux noise (noise factor level) and wave-length uncertainty were developed. These measurements, in combination with Hotelling’s T² and Q residual, are used to continuously monitor instrument performance and model relevance. Four calibration transfer techniques were compared. Three established techniques, finite impulse response filtering, generalized least squares weighting, and piecewise direct standardization were evaluated. A fourth technique, baseline subtraction, was the most effective for calibration transfer. Using as few as 15 transfer samples, predictive capability of the analytical method was maintained across multiple instruments and major instrument maintenance.     

桂枝茯苓丸联合妇乐片对子宫内膜异位症的临床疗效

目的:探讨桂枝茯苓丸联合妇乐片对子宫内膜异位症患者血清甲胎蛋白(AFP)、血清脂质结合唾液酸(LSA)及临床疗效的影响。方法:选取我院确诊并治疗的子宫内膜异位症患者68例,按随机数字表法进行分组,每组34例。对照组患者予以妇乐片口服治疗;研究组患者在对照组用药基础上予以桂枝茯苓丸联合治疗,所有患者连续服药6个月。观察两组患者治疗前后血清甲胎蛋白(AFP)、血清LSA、肿瘤坏死因子-α(TNF-α)及血管内皮生长因子(VEGF)水平的变化情况、临床疗效及不良反应发生率。结果:研究组治疗后临床有效率91.18%,高于对照组治疗后临床有效率70.59%,差异具有统计学意义(P0.05);与对照组比较,研究组治疗后血清AFP、LSA、TNF-α、VEGF水平降低,差异具有统计学意义(P0.05);对照组不良反应发生率为8.24%,研究组不良反应发生率为5.88%,两组间不良反应发生率无统计学意义(P0.05)。结论:采用桂枝茯苓丸联合妇乐片治疗子宫内膜异位症,能有效提高患者的临床疗效,推测其机制与降低血清AFP、LSA、TNF-α、VEGF水平有关。