Dry powder inhalations containing thymopentin and its immunomodulating effects in Wistar rats

Thymopentin (TP5), a synthetic pentapeptide, has been used in clinic as a modulator for immunodeficiences through intramuscular administration. The purpose of this study was to design and evaluate dry powder inhalations (DPIs) for pulmonary delivery of TP5. Dry powder inhalations containing leucine (a dispersibility enhancer), mannitol, and lactose (bulking agents) were prepared by spray-drying from aqueous formulations. The formulation components on the aerosolisation characteristics of spray-dried powders were investigated through the use of various amount of leucine, lactose and mannitol. Following spray-drying, resultant powders were characterized using scanning electron microscopy, laser diffraction and tapped density measurements, and the aerosolisation performance was determined using Twin Stage Impinger. The immunosuppression Wistar rats model was constructed to evaluate the immunomodulating effects of TP5 DPIs in vivo. The results of T-lymphocyte subsets (CD3+, CD4+, CD8+, CD4+/CD8+ ratio) analyses suggest that TP5 DPIs have modulating effects. On an overall evaluation, TP5 pulmonary delivery DPIs may be feasible for the future clinical application.     

沙美特罗替卡松粉复合吸入剂联合孟鲁司特治疗咳嗽变异性哮喘的疗效观察

目的探讨沙美特罗替卡松粉复合吸入剂联合孟鲁司特对咳嗽变异性哮喘（CVA）患者的临床疗效。方法100例CVA患者完全随机分为孟鲁司特组和联合治疗组各50例,孟鲁司特组给予孟鲁司特（默沙东公司,商品名：顺尔宁）10mg,每晚1次,疗程8周;联合治疗组吸人沙美特罗替卡松粉复合吸入剂（葛兰素史克公司,商品名：舒利迭）50μg／250μg,2次／d,口服孟鲁司特10mg,每晚1次,疗程均为8周。观察2组治疗前后临床症状、肺功能以及诱导痰中炎性细胞的变化。结果2组药物治疗后临床咳嗽症状改善明显,孟鲁司特组总有效率82％,联合治疗组总有效率94％,二者比较,差异有统计学意义（P〈0．01）;与孟鲁司特组比较,联合治疗组诱导痰中相关炎症细胞总数和嗜酸粒细胞百分比较治疗前减少明显（2．76±0．61vs3．02±0．55;10．2±2．9vs14．8±3．5,P〈0．05）,肺通气功能（FEV1,FEV1预计值和FEV1／FVC）改善明显（P〈0．05）,联合治疗组疗效优于孟鲁司特组。结论沙美特罗替卡松粉复合吸入剂联合孟鲁司特治疗CVA具有较好的疗效。     

湿感头痛散联合针灸康复治疗发作期紧张性头痛的临床疗效观察

目的：探讨湿感头痛散联合针灸康复治疗发作期紧张性头痛的临床疗效。方法选取我院120例急紧张性头痛患者,通过随机数字表法分为联合组和针灸组各60例,联合组采用湿感头痛散联合针灸治疗,针灸组单用针灸治疗,观察比较两组患者临床疗效。结果两组患者治疗后,联合组的临床疗效总有效率高于针灸组,差异有统计学意义（P＜0．05）;联合组的HAMD、HAMA评分优于针灸组（P均＜0．05）;联合组的头痛发作频率、持续时间（h）少于针灸组（P均＜0．05）;联合组的VAS（分）低于针灸组（P＜0．05）。结论采用湿感头痛散联合针灸治疗紧张性头痛有助于缓解患者的抑郁,减少发作次数,减少持续时间以及疼痛感,疗效显著,值得临床推广。     

八宝眼粉质量标准的研究

目的:建立八宝眼粉的质量控制方法.方法:采用化学反应和薄层色谱法(TLC)鉴别方中炉甘石、人工牛黄、冰片;采用气相色谱法(GC)测定冰片的含量.结果:鉴别效果满意;冰片在0.09808～0.78464 μg范围内呈良好的线性关系,平均加样回收率为101.5%,RSD=1.40%(n=5).结论:本方法简便、快速准确,可作为该制剂质量控制方法.     

Multi-walled carbon nanotube-induced inhalation toxicity: Recognizing nano bis-demethoxy curcumin analog as an ameliorating candidate

Human beings and ecosystems are being possibly exposed to CNTs, as there is a rise in global production rate of carbon nanotubes (CNTs). This may affect the health of humans and increases the environmental risk. We have already reported the pulmonary toxicity due to the inhalation of MWCNTs. We claim that a compound with anti-inflammatory and antioxidant activity may ameliorate the CNT-induced toxic effect. With this view, we have investigated the ameliorative effect of intravenously-administered nano bis-demethoxy curcumin analog (NBDMCA) against MWCNTs-induced inhalation toxicity by examining the lung histopathology for inflammatory cell dynamics, pulmonary remodeling and estimating the inflammatory biomarkers in the broncho-alveolar lavage fluid. We observed that NBDMCA could ameliorate the injury as evidenced by the decline in the levels of markers of inflammation, cell damage, and the histopathological changes induced by MWCNTs. We conclude that NBDMCA may be used to reduce the risk of MWCNTs-induced inhalation toxicity.     

高效液相色谱法同时测定三七伤药片中新北美圣草苷和柚皮苷的含量

目的 建立三七伤药片中同时测定新北美圣草苷和柚皮苷含量的方法.方法 以甲醇为溶剂,进行超声提取;色谱柱:Agilent C18(250 mm×4.6 mm,5 μm);流动相:乙腈-0.1%磷酸溶液(17:83),流速:1 mL·min-1,检测波长:283 nm,柱温35 ℃.结果 新北美圣草苷在87.55~1 313.25 ng范围内线性关系良好(r=0.999 4),平均回收率为99.13%,RSD=1.21% (n =6),柚皮苷在80.4~1 206 ng范围内线性关系良好(r=0.999 6),平均回收率为96.78%,RSD=3.34%(n=6).结论 高效液相色谱法(HPLC)可以同时测定新北美圣草苷和柚皮苷的含量,方法简便、准确、灵敏度高、重现性好,可用于三七伤药片中骨碎补的质量控制.     

Computational fluid dynamics (CFD) assisted performance evaluation of the Twincer™ disposable high-dose dry powder inhaler

Objectives To use computational fluid dynamics (CFD) for evaluating and understanding the performance of the high‐dose disposable Twincer? dry powder inhaler, as well as to learn the effect of design modifications on dose entrainment, powder dispersion and retention behaviour. Methods Comparison of predicted flow and particle behaviour from CFD computations with experimental data obtained with cascade impactor and laser diffraction analysis. Key findings Inhaler resistance, flow split, particle trajectories and particle residence times can well be predicted with CFD for a multiple classifier based inhaler like the Twincer?. CFD computations showed that the flow split of the Twincer? is independent of the pressure drop across the inhaler and that the total flow rate can be decreased without affecting the dispersion efficacy or retention behaviour. They also showed that classifier symmetry can be improved by reducing the resistance of one of the classifier bypass channels, which for the current concept does not contribute to the swirl in the classifier chamber. Conclusions CFD is a highly valuable tool for development and optimisation of dry powder inhalers. CFD can assist adapting the inhaler design to specific physico‐chemical properties of the drug formulation with respect to dispersion and retention behaviour.     

硫酸特布他林干粉吸入剂制备工艺的优化研究

目的:优化硫酸特布他林干粉吸入剂的制备工艺。方法:采用喷雾干燥技术制备硫酸特布他林干粉吸入剂,采用双层液体碰撞器测定其体外肺沉积率,扫描电镜观察干粉的表观形貌,热重分析仪测定干粉的水分含量,激光粒度测定仪测定粒径大小,以产品收率、水分含量、粉末的空气动力学粒径及体外肺沉积率为考察指标,通过正交设计结合多指标综合评价法优化最佳制备工艺。结果:通过正交试验-多指标综合评价,最佳制备工艺为:喷雾压力190 kPa,干燥风速0.7 m3.min-1,供液速度7.0 mL.min-1,入口温度120℃。结论:按最佳制备工艺制得的干粉收率为50.54%,水分含量为0.467%,空气动力学粒径为1.80μm,体外肺沉积率为55.19%。正交试验结合多指标综合评价法用于硫酸特布他林干粉吸入剂制备工艺的优化有效可用。     

通痹胶囊对佐剂关节炎大鼠的继发关节病变及免疫功能的影响

目的初步探讨复方中药通痹胶囊对类风湿关节炎(RA)的治疗作用及机制。方法取Wistar雄性大鼠,制成佐剂关节炎(AA)模型,设正常组、模型组、雷公藤多甙对照组、通痹胶囊治疗组,观察不同处理因素对各组实验鼠继发关节肿胀度,继发病变分级,胸腺、脾脏重量及白细胞介素(IL)-1β的影响。结果治疗后通痹胶囊组、雷公藤组的继发关节肿胀,继发病变分级以及对实验鼠的胸腺、脾脏重量、IL-1β的影响与模型组相比差异均有显著性(P<0.05);通痹胶囊组与雷公藤组相比差异无显著性(P<0.05)。结论通痹胶囊对佐剂关节炎大鼠继发病变有明显的治疗作用;对模型大鼠胸腺、脾脏重量及IL-1β的抑制说明该方有一定的免疫抑制作用,这可能是该方治疗RA的机制之一。     

生脉散超微粉的显微特征和溶出度研究

目的 研究生脉散超微粉的显微特征和溶出度差异,为生脉超微粉应用提供实验依据.方法 采用光学显微镜观察颗粒显微结构;电镜扫描观察微观形貌;以五味子甲素和五味子乙素为指标,采用HPLC法测定生脉散细粉和超微粉在不同时间溶出的量,计算累积溶出度.结果 生脉散经超微粉碎后,基本无完整细胞存在,粒度均匀;生脉散超微粉中五味子甲素和五味子乙素溶出速率高于细粉,但是180 min后累积溶出量没有明显差异.结论 超微粉碎可使生脉散显微特征变化明显,化学成分五味子甲素和五味子乙素溶出速率加快.