Formoterol inhaled as dry powder or via pressurized metered-dose inhaler in a cumulative dose-response study

Formoterol administered by a dry-powder (DP) capsule inhaler was compared with a pressurized metered-dose inhaler (pMDI) with regard to bronchodilating and systemic effects. The study used a double-blind, crossover, double-dummy technique. Twelve patients with moderate reversible asthma in a stable phase were examined on two separate study days, and the inhalers were given in randomized order. After baseline measurements, increasing doses of formoterol were given at intervals of 75 min. FEV₁ and heart rate and tremor measurements were repeated after each dose, and the doses were 12 + 12 + 24 + 48 μg, giving a total dose of 96 μg. The peak expiratory flow rate (PEFR) was recorded in the morning before the first dose, after the last dose, and then repeatedly at home until 19 h after the last dose. There was an equal increase in ventilatory capacity at each dose level, independent of inhaler device. Repeated PEFR measurements after the last dose did not reveal any differences in duration of effect. There was a slight but statistically significant increase in heart rate and tremor after the highest doses of the DP formulation compared to the pMDI. These systemic effects can probably be explained by the reduced oral deposition of the aerosol caused by using a spacer. This study indicates that the DP and pMDI formulations of formoterol are equipotent in bronchodilation.     

Comparison of Bricanyl® Turbuhaler and Berotec® dry powder inhaler

Terbutaline (Bricanyl) 0.5 mg t.i.d. administered via Turbuhaler was compared with fenoterol (Berotec) 0.2 mg t.i.d. administered via Inhalator Ingelheim in 36 asthmatic children aged 7-12 years. The study was of an open crossover design with two randomly allocated treatment periods, each lasting 2 weeks. Forced expiratory volume in 1 s (FEV1) and forced vital capacity (FVC) were measured at clinic visits before study start and at the end of each treatment period. The patients recorded peak expiratory flow (PEF) before and after inhaler use, morning and evening. They also recorded asthma symptoms and number of extra inhalations. At the end of the study, children and parents were asked for inhaler preference. No differences between the treatments were found concerning the results of the lung function measurements at the clinic or at the PEF measurements at home. No differences were found between the treatments as regards asthma symptoms or number of extra inhalations. Two patients experienced mild side effects during fenoterol treatment, none during terbutaline treatment. Treatment with terbutaline in Turbuhaler was preferred by a majority of children and parents. In conclusion, in this group of asthmatic children, treatment with terbutaline administered via Turbuhaler was as efficacious as treatment with fenoterol administered via Inhalator Ingelheim. There was a clear preference in favour of the Turbuhaler.     

山药配方颗粒溶化性差的原因分析与解决策略

山药配方颗粒由山药饮片经水煎煮提取、分离、浓缩、干燥、制粒而成,具有调剂简单、使用方便、免煎易服等优势。然而,因山药富含淀粉与黏液质类成分,其提取物粉末与配方颗粒溶化性差,在5 min内难以完全溶化或分散,不溶物即使在水中静置24 h也难以完全溶散,影响了配方颗粒的质量评价与患者的服药心理。因此,通过研究山药提取物及其配方颗粒的溶化过程与机制,发现山药特殊的化学组成、高温提取过程中淀粉的变性及其与蛋白质等物质的复合、喷雾干燥过程中“衣膜”的收缩形成等因素综合叠加,最终形成“衣膜”包覆淀粉粒的特殊微观结构,是山药配方颗粒溶化性差的根本原因。基于课题组前期对粉体结构-性质-功能的研究,笔者提出采用粉体改性工艺改善山药配方颗粒溶化性的技术策略,并通过实验证明改性处理后的山药配方颗粒能在2 min内实现全部溶散,解决了该技术难题,可为其他类似品种的溶化性改善提供借鉴,推动中药配方颗粒产业的高质量发展。     

制备工艺对ATO超细粉体导电性能的影响

采用化学共沉淀法制备锑掺杂二氧化锡（ATO）超细导电粉体,研究了反应温度,滴定终点pH值,掺锑量及锻炼温度对粉体导电性的影响,并对实验结果进行了讨论。     

Topical Vancomycin Powder and Dilute Povidone-Iodine Lavage Reduce the Rate of Early Periprosthetic Joint Infection After Primary Total Knee Arthroplasty

BackgroundVancomycin powder and dilute povidone-iodine lavage (VIP) was introduced to reduce the incidence of periprosthetic joint infection (PJI) in high-risk total knee arthroplasty (TKA) patients. We hypothesize that VIP can reduce the incidence of early PJI in all primary TKA patients, regardless of preoperative risk.MethodsAn infection database of primary TKAs performed before a VIP protocol was implemented (January 2012-December 2013), during a time when only high-risk TKAs received VIP (January 2014-December 2015), and when all TKAs received VIP (January 2016-September 2019) at an urban, university-affiliated, not-for-profit orthopedic hospital was retrospectively reviewed to identify patients with PJI. Criteria used for diagnosis of PJI were the National Healthcare Safety Network and Musculoskeletal Infection Society guidelines.ResultsVIP reduced early primary TKA PJI incidence in both the high-risk and all-risk cohorts compared with the pre-VIP cohort by 44.6% and 56.4%, respectively (1.01% vs 0.56% vs 0.44%, P = .0088). In addition, after introducing VIP to all-risk TKA patients, compared with high-risk TKA patients, the relative risk of PJI dropped an additional 21.4%, but this finding did not reach statistical significance (0.56% vs 0.44%, P = .4212). There were no demographic differences between the 3 VIP PJI cohorts.ConclusionVIP is associated with a reduced early PJI incidence after primary TKA, regardless of preoperative risk. With the literature supporting its safety and cost-effectiveness, VIP is a value-based intervention, but given the nature of this historical cohort study, a multicenter randomized controlled trial is underway to definitively confirm its efficacy.     

基于“药辅合一”理念的Pickering乳技术提升儿科用药羚珠散中石菖蒲挥发油热稳定性的研究

目的 在“药辅合一”理念下导入Pickering乳技术,提升儿科用药羚珠散中石菖蒲挥发油的稳定性。方法 对羚珠散各饮片粉末进行初步表征,确定稳定剂。通过成乳量、包油量和乳剂形态筛选出最佳稳定剂质量浓度、油水比和制备方法。并使用近红外光谱（nearinfraredspectroscopy,NIRS）分析石菖蒲油在Pickering乳中的包裹状态。比较不同时间下各组别挥发油的保有量、丙二醛和过氧化物的含量。再通过GC-MS分析其中成分的变化趋势。结果 筛选出珍珠粉作为Pickering乳的稳定剂,珍珠粉质量浓度为65 mg/mL,油水比9∶11为最优成乳条件,高压均质法为最优的制备方法,NIRS分析可知石菖蒲挥发油被珍珠粉包裹,Pickering乳液中没有形成新的化学键。对比各组在不同时间段下石菖蒲油的保有率和其中丙二醛和过氧化物含量,可知40℃放置1、3、8 h的Pickering乳剂相比于石菖蒲挥发油组有更高的保有率和更低的氧化程度。GC-MS分析结果表明,相比于石菖蒲挥发油组,Pickering乳组挥发性成分的稳定性显著提高。结论 在“药辅合一”理念下Pickering乳可用于含油固...     

水提干法制粒的中药配方颗粒溶化性与粉体物理属性相关性研究

目的 为加快实现中药生产过程中对中药配方颗粒的质量控制,从粉体物料属性出发,探究其对水提工艺下干法制粒的中药配方颗粒溶化性影响机制。方法 以60种中药配方颗粒及中间体混合粉为研究对象,通过对各品种混合粉粉体属性进行测定,建立粉体物性参数与颗粒溶化性关联模型。采用二维矩阵热点图对各品种间及物性指标间相似性进行分析,结合系统聚类分析对其进行归类,并运用多元统计方法初步筛选影响水提工艺下中药配方颗粒溶化性的关键因素。结果 各品种间粉体物性参数相关系数在-0.951～1.000,并按照各品种物理属性大致可以分为5类,结合变量投影响应值（variable importance for the projection,VIP）、自变量回归系数与方差膨胀因子（variance inflation factor,VIF）分析,最终筛选出其休止角（α）、含水量（HR）、吸湿性（H）与比表面积（SSA）4个指标为影响中药配方颗粒溶化性的关键物料属性（critical material attributes,CMAs）。结论 基于中药粉体物料属性与数据分析初步探寻影响水提条件下干法制粒的中药配方颗粒的溶化性机...     

金银花颗粒在旋风分离器中的流场数值模拟分析

目的 针对金银花颗粒在旋风分离器中的运动行为过程进行研究,考察不同设计参数和操作工艺条件下,颗粒在设备内部的运动过程变化规律。方法 基于仿真模拟技术,考察受不同设备长径比、入口进气雷诺数、颗粒质量流量3个因素影响的金银花颗粒在分离器内的运动规律,并以金银花颗粒得粉率为验证指标参数,对模型可靠性进行了分析。结果 通过仿真模拟得到了各个不同工艺条件下的金银花颗粒运动轨迹分布,计算出了对应设备的颗粒得粉率。提出金银花颗粒分离的最佳工艺建议为设备长径比5∶1,入口进气雷诺数3.23×10⁴,颗粒质量流量80.1 mg/s,得到的金银花颗粒得粉率为96.30%。结论 为旋风分离器内金银花颗粒的有关研究提供指导,同时改善旋风分离器在控制和设计上的不足。     

青黛表面改性对口腔溃疡双层膜质量与药效的影响

目的 采用溶剂浇铸法制备口腔溃疡双层膜剂,研究青黛表面改性前后对膜剂质量与药效的影响。方法 通过单因素实验设计和响应面优化法优选膜剂最佳处方,并对膜剂表面形貌、黏附时间、抗拉强度、含量测定以及体外药物释放等性能进行评估。进一步采用化学灼烧法建立大鼠口腔溃疡模型,考察膜剂对溃疡组织肿瘤坏死因子-α（tumor necrosis factor-α,TNF-α）、白细胞介素-1β（interleukin-1β,IL-1β）、IL-6以及口腔溃疡组织形态的影响。结果 空白隔离层确定为25 mg/mL的乙基纤维素乙醇溶液,载药膜最佳处方为63 mg/mL PVA17-88、55 mg/mL PVP K30、3.0 mg/mL明胶与0.047 mL/mL甘油。青黛表面改性后,双层膜剂比未改性双层膜剂具有更加光滑均一的外观、更高的含量均匀性和有效成分靛蓝释放率。药效学结果表明,与模型组相比,阳性组与青黛改性膜剂组显著降低了溃疡组织TNF-α、IL-1β、IL-6的含量（P＜0.05）,并减少了炎症细胞的浸润,溃疡组织愈合程度较高。结论 青黛改性之后的口腔溃疡双层膜剂具有更好的质量与更佳的疗效,具有较好的应用前景。     

饮片细粉对肠炎宁半浸膏片压缩成型的影响研究

目的 研究半浸膏颗粒中饮片细粉含量对其物理性质和压缩性能的影响。方法 以肠炎宁片为模型药物,测定含不同饮片细粉比例的肠炎宁颗粒的粉体学性质、压缩过程参数、抗张强度等指标,采用不同压缩方程对片剂抗张强度-压力、孔隙率-压力、抗张强度-孔隙率的变化规律进行拟合,阐明肠炎宁半浸膏片的成型机制,并用主成分分析对粉体学性质、压缩过程参数及拟合系数之间的相关性进行分析。结果 当肠炎宁颗粒中的饮片细粉含量小于6%时,随着饮片细粉含量的增加,粒子间的结合力增强,粉体的成型性增强;当含量超过6%后,饮片细粉弹性作用增强,粒子间结合力减弱,抑制成型。结论 从压缩成型角度说明了肠炎宁半浸膏片中饮片细粉含量的临界值为6%,可为半浸膏片的处方工艺优化提供较好的理论和实验依据。