Effects of chronic tramadol exposure on the zebrafish brain: a proteomic study

Tramadol hydrochloride (TH), has become the most prescribed opioid worldwide. However, its neurotoxicity and abuse potential are not well documented. In the present study, TH administration induced abnormal behavior and body and brain mean weight loss. Two principal metabolites O- and N-desmethyltramadol were detected in the brain tissue, and N-desmethyltramadol was the main metabolite produced. A total of 30 differential protein spots were identified using semi-quantitative 2D-PAGE and proteomic analyses, and classified into 13 categories, in which subtypes of 14-3-3 proteins, creatine kinase, ATP synthase beta chain, and tubulin were identified at the separated location on the gels 3, 3, 4, and 11 times respectively. Many TH responsive proteins have functions related to oxidative stress, including 14-3-3 proteins, creatine kinase BB, ubiquitin carboxy-terminal hydrolase L-1, ATP synthase, synaptosome-associated protein, tubulin and actin. Irrespective of oxidative damage, other pathways affected include apoptosis, energy metabolism, signal disorders, and cytoskeletal structure. Ultrastructural observation of mitochondria showed a series of morphological changes in the case of TH exposure.     

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。     

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。     

藤茶保健含片的研制

以藤茶浓缩汁、麦芽糖醇、山梨糖醇和低聚异麦芽糖为主要原料,经混合、造粒、干燥、压片等工序,制成了低热量、具有保健功能的藤茶含片.     

Enantioselective retardation of rac-propranolol from matrices containing cellulose derivatives

The dissolution characteristics of propranolol enantiomers from tablet formulations containing cellulose, or one of eight cellulose derivatives, were determined under a range of conditions. The derivatives examined were: cellulose tris(phenylcarbamate) (1), cellulose tris(2,3-dichlorophenylcarbamate) (2), cellulose tris 2,4-dichlorophenylcarbamate (3), cellulose tris(2,6-dichlorophenylcarbamate) (4), cellulose tris(2,3-dimethylphenylcarbamate) (5), cellulose tris(3,4-dichlorophenylcarbamate) (6), cellulose tris (3,5-dichlorophenylcarbamate) (7), cellulose tris(3,5-dimethylphenylcarbamate) (8). In water at 25°C, the release rates of (-)R-propranolol were generally greater than those of (-)-S-propranolol, although these differences were not always statistically significant; only compounds 5 and 8 demonstrated significant enantioselectivity. Using compound 8 in further experiments, statistically significant stereoselective dissolution of propranolol HCl was observed in buffer pH 7.4 at 25°C (intrinsic dissolution rates: 0.41 ± 0.01 mgcm²min⁻¹ for R-propranolol and 0.30 ± 0.02 mgcm²min⁻¹ for S-propranolol; P = 0.003). The cumulative amounts of enantiomers released at every time point were also found to be statistically significant (mean ratio R:S 1.25 ± 0.05). The observed low stereoselectivity of 8 with propranolol base was probably attributable to low solubility in pH 7.4 buffer, although stereoselective release did increase with time. This suggested that there is a relationship between stereoselectivity and contact time in an aqueous environment. Results also suggested that increased temperature may affect the release process as well as stereoselective interactions of 8 with individual enantiomers. To conclude, differential release of rac-propranolol from cellulose derivative matrices has been demonstrated, which supports the principle of stereoselective retardation as a potential means of stereoselective drug delivery for solid dosage forms. Chirality 9:307–312, 1997. © 1997 Wiley-Liss, Inc.     

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。     

氯雷他定片剂一致性评价研究方法

为改善我国部分仿制药质量与国际先进水平还存在一定差距的现状,《国家药品安全“十二五”规划》中明确提出了开展仿制药一 致性评价,全面提高仿制药质量的任务。氯雷他定片作为抗过敏药物的主要品种之一,需在 2018 年底前完成一致性评价。基于现有质量和 疗效一致性评价指导原则与相关研究报道,针对氯雷他定原料药的晶型研究、原辅料杂质的比较研究、片剂溶出曲线的比较方法以及生物 等效性试验研究等进行了总结和概括,并对有待解决的共性问题进行了讨论。     

Effect of lipid lowering tablet on blood lipid in hyperlipidemia model rats

Observe the effect of lipid-lowering tablets on body weight, liver index and serum biochemical indexes of hyperlipidemia rats. The hyperlipidemia rat model was replicated successfully. Compared with the model group, high, medium and low dose lipid-lowering tablets group could significantly increase the body weight of rats with hyperlipidemia (P?<?0.01, P?<?0.05); High and middle dose lipid-lowering tablets group could significantly reduce the liver index of high fat rat (P?<?0.01); High, medium and low dose lipid-lowering tablets group could significantly decrease levels of TC, TG, LDL-C, AST, ALT, ALP, Y-GT in serum (P?<?0.01, P?<?0.05), and significantly increase the level of HDL-C (P?<?0.01). Lipid-lowering tablets can effectively regulate the body lipid metabolism of rats, and have a certain therapeutic effect on hyperlipidemia.     

甲磺酸多沙唑嗪控释片联合中药坐浴治疗老年非细菌性前列腺炎的临床疗效

目的:探讨甲磺酸多沙唑嗪控释片联合中药坐浴治疗老年非细菌性前列腺炎的临床疗效。方法:选取我院泌尿男科收治的老年非细菌性前列腺炎患者60例,随机分配为实验组和对照组,每组各30例,对照组患者使用甲磺酸多沙唑嗪控释片进行治疗,实验组患者在对照组的治疗基础上加用中药坐浴进行治疗,两组患者均治疗1个月。治疗结束后对患者前列腺液中的WBC水平进行检测,并应用美国国家卫生研究院慢性前列腺炎症状指数(NIH-CPSI)表对患者的前列腺功能进行评分,同时比较治疗结束后两组患者临床总有效率。结果:与治疗前相比,两组患者WBC计数及NIH-CPSI评分均有所降低(P0.05);与对照组相比,实验组患者治疗后WBC计数及NIH-CPSI评分较低(P0.05);临床总有效率较高(P0.05)。结论:甲磺酸多沙唑嗪控释片联合中药坐浴能够提高老年非细菌性前列腺炎患者的前列腺功能,降低炎症反应,临床疗效更好。     

酪酸梭菌活菌片联合 马来酸曲美布汀、谷维素对IBS患者的疗效

目的探讨酪酸梭菌活菌片联合马来酸曲美布汀、谷维素对肠易激综合征患者的临床疗效。方法选择80例肠易激综合征患者,随机分为治疗组(n=40)和对照组(n=40)。治疗组患者采用酪酸梭菌活菌片联合马来酸曲美布汀、谷维素进行治疗,对照组患者采用马来酸曲美布汀和谷维素进行治疗。结果治疗组患者有效率高于对照组,两组疗效比较差异有统计学意义(P0.05)。结论酪酸梭菌活菌片联合马来酸曲美布汀、谷维素对肠易激综合征患者疗效显著。