新兵心理应激反应与积极心理品质及特质应对方式的关系

目的 探讨新兵的心理应激反应与积极心理品质及特质应对方式的关系,为新兵训练时的心理指导和干预提供理论依据.方法 以曾经完成过训练任务的新兵作为研究对象.采用事件影响量表修订版(IES-R)、新兵积极心理品质评估问卷(PMCS-R)和特质应对方式问卷(TCSQ)对某部队男性新兵进行问卷调查.结果 其调查1 322名新兵,其心理应激反应程度与特质消极应对呈正相关(r=0.544,P＜0.05),与特质积极应对、积极心理品质呈负相关(r=-0.280,-0.201,均P＜0.05).以应激事件影响总分为因变量,积极心理品质各维度分和特质应对方式各维度分为预测变量进行多元逐步分析,消极应对、积极应对、智慧和自控4个因子进入回归方程,可解释应激反应总分变异的32.4％.结论 积极心理品质和特质应对方式可影响新兵的心理应激反应水平.     

流动与非流动初中生积极心理品质的比较

目的对流动与非流动初中生积极心理品质:自立人格、心理韧性、正性-负性情绪进行比较,为推动流动初中生心理健康发展提供依据。方法采用青少年自立人格量表、青少年心理韧性量表、正性-负性情绪量表对深圳某中学658名初中1～3年级的学生进行抽样调查,以筛选出的392名流动初中生为研究组,其他学生为对照组。利用SPSS16.0统计软件对调查结果进行统计分析。结果①流动与非流动初中生在自立人格各因子及正性-负性情绪上无显著差异;②流动初中生在心理韧性的积极认知上得分显著高于非流动初中生(F=4.078,P<0.05),其它因子无显著差异。结论流动对流动初中生积极心理品质发展的影响并不明显,可通过教育发挥流动的积极意义。     

Antimicrobial and physicochemical characterization of endodontic sealers after exposure to chlorhexidine digluconate

ObjectivesAssess the antibacterial, physical and chemical properties of AH Plus, BioRoot RCS and Pulp Canal Sealer (PCS) in contact with 2% chlorhexidine digluconate (CHX) used as final irrigant prior to root canal obturation.MethodsThe antimicrobial properties were investigated by direct contact tests for planktonic and biofilm growth of E. faecalis, S. mutans, S.epidermidis and S.aureus in vitro. The setting time, wettability, microhardness and surface roughness were also assessed. The sealers were studied in no contact, 1-minute (short-term) and continuous contact (long-term) with CHX. Chemical characterization of sealers was performed by scanning electron microscopy, X-ray diffraction analysis and Fourier-transform infrared spectroscopy after CHX or saline used as the last irrigant in an ex vivo tooth model and in endo training blocks.ResultsCHX increased the antibacterial activity of all the sealers investigated against planktonic bacteria and biofilms with PCS exerting the highest antimicrobial activity with and without the presence of CHX. The setting of AH Plus and BioRoot RCS was retarded, while for PCS accelerated in the presence of CHX. AH Plus and PCS were more hydrophilic after contact with CHX, whilst BioRoot RCS was hydrophobic in a time-dependent manner. The microhardness of sealers was compromised and the surface roughness increased after CHX exposure for AH Plus and BioRoot RCS, and decreased for PCS. CHX did not affect the sealers’ chemistry, but PCS that exhibited two extra phases.SignificanceCHX improved the antibacterial efficacy of endodontic sealers but further evidence is needed to confirm its suitability as a final irrigant prior to root canal obturation.     

Overcoming Poor Tabletability of Bulky Absorption Enhancers by Spray Drying Technology

Absorption enhancers are often a major component of solid oral peptide formulations as compared to the active pharmaceutical ingredient and excipients. This commonly results in poor tabletability that is hard to mitigate in direct compaction by addition of small amounts of excipients. To improve the tabletability of bulky absorption enhancers, the model absorption enhancers, sodium cholate and deoxycholic acid, were co–spray-dried with hydroxypropyl methylcellulose E5, where the percentage of absorption enhancers was not lower than 90% (w/w). The physicochemical properties of the resulting powders were assessed by laser diffraction, scanning electron microscopy, X-ray powder diffraction, thermogravimetric analysis, and differential scanning calorimetry. The powders were compressed into tablets, and the tabletability was evaluated. Co–spray drying with 10% of hydroxypropyl methylcellulose significantly improved the tabletability of the both absorption enhancers. Moreover, it was demonstrated that small particle size and amorphous state rather than high moisture content contributed to the improved tabletability of the spray-dried powders. The study suggests that spray drying technology can be promising to overcome the poor tabletability of oral peptide formulation consisting of large amounts of absorption enhancers.     

中药小包装饮片的历史源流及其调剂规范化操作的思考

目的传承历代中药调剂操作经验,规范现代中药小包装饮片调剂操作技术。方法通过查阅历代古籍和现代文献,系统整理和分析中药饮片小包装的历史渊源、使用利弊、包装选择、使用现状及调剂规程等五方面情况,回顾小包装饮片的发展历程,总结调剂操作经验,编排现代调剂操作规程。结果中药小包装饮片调剂具有独特的优势,"审、摆、看、对、拿、掂、分、核、包、发"的"十字口诀"是其主要操作要点。结论中药小包装饮片调剂"十字口诀"易记、易懂、易操作,提高临床调剂质量、规范调剂技能具有指导意义。     

The influence of physicochemical properties on the reactivity and stability of acyl glucuronides†

1.?Formation of 1-O-acyl-β-d-glucuronide conjugates is a significant pathway in the metabolism of drugs containing a carboxylic acid group. The formation of acyl glucuronides results in an increase in both the aqueous solubility and molecular mass of the conjugate in comparison to the parent drug and thus facilitates excretion in both urine and bile.

2.?Acyl glucuronides are effectively esters, which undergo first order decomposition by both hydrolysis and the intra-migration of the acyl group around the glucuronide ring to yield 2-, 3- and 4-O-glucuronic acid esters which, unlike the metabolically formed 1-O-acyl-β-d-glucuronides, are not substrates for β-glucuronidase. The first order degradation half-life is therefore a composite value of these two reactions and a useful indicator of chemical reactivity and potential toxicity.

3.?Intra-molecular migration is expected to be the predominant pathway due to entropic considerations.

4.?Such conjugates, together with their isomeric ester derivatives, react with nucleophilic sites on proteins and small endogenous molecules, such as glutathione, which potentially contributes to the observed toxicity and adverse drug reactions associated with some drugs.

5.?Examination of the stability of the 1-O-acyl-β-d-glucuronides of aryl acetic acid, α-carbon substituted aryl acetic acid, aliphatic and aromatic acids, as determined by their first order degradation half-lives, indicates the significance of electronic and steric features that contribute to conjugate stability under physiological conditions.

6.?Examination of the of the electronic properties of the carbonyl carbon atom in acyl glucuronides, as measured by the pKa of the parent acid, together with the steric substituents about the acyl carbonyl provides insight into the reactivity of these conjugates.

7.?The investigations reported herein on a large number of 1-O-acyl-β-d-glucuronides has allowed rationalisation of their physicochemical properties in relation to the structure of the parent drug and has the potential to contribute to the design of carboxylic acid containing drug molecules with increased stability of a major metabolite with potential reduction in toxicity and adverse drug reactions.     

纳米制剂在心肌缺血区域的靶向机制及应用

缺血性心脏病是严重威胁人类健康的疾病。至今为止,药物预处理和治疗依旧是心肌缺血预防和治疗的重要手段。但大多数抗心肌缺血药物缺乏组织特异性,同时由于缺血区域血液循环受阻,导致药物在缺血部位的分布往往不甚理想。靶向纳米制剂是一种治疗心血管疾病的新型给药策略。纳米制剂在体内主要可以通过"被动靶向"、"主动靶向"和"物理化学靶向"作用将药物递送至病变部位,提高药物在缺血区域的靶向性和释放率,从而改善药物治疗效果。本文对应用靶向纳米制剂治疗心肌缺血的疗效及机制研究作一综述。     

Can we estimate the critical micelle concentration of amphiphilic drug bases from molecular connectivity indices?

Self-aggregation of drugs is since many years an important topic in the pharmaceutical sciences. Drugs can aggregate similar to surfactants and thereby exhibit a critical micelle concentration (CMC). The present work focused on amphiphilic drug bases and it was aimed to predict log(CMC) based on chemical structure alone. A dataset of 35 compounds was gathered mostly form the literature and complemented with own measurements based on ultrasonic resonator technology. The hydrophilic–lipophilic balance (HLB) values of the protonated bases were calculated and provided a range of 22.9–27.4. Based on a hypothesis from surfactant sciences, it was tried to predict log(CMC) with connectivity and shape indices as well as molecular dipole moment. A fairly good model was obtained using the Randix index (RI), 3?D Wiener number (WN) and molecular dipole moment (DM) (R²?=?0.824). Interestingly, a simple linear regression of log(CMC) with the Randic index alone, resulted in an acceptable model (R²?=?0.755). The present work should help with early identification of drug bases that exhibit surfactant-like behavior and an estimation of log(CMC) values is proposed. An improved understanding of drug aggregation and prediction of log(CMC) helps to better cope with physical consequences like, for example, “anomalous” drug solubility in drug discovery and development.