Asymmetrically Substituted Poly(diitaconates) Obtained by Reversible Addition‐Fragmentation Chain Transfer (RAFT) Polymerization: Synthesis,Copolymerization Parameters,and Antimicrobial Activity

Asymmetrically substituted poly(diitaconate) copolymers are synthesized from 1‐((N‐tert‐butoxycarbonyl)‐2‐aminoethyl)‐4‐propyl diitaconate (PrIA) and different comonomers (N,N‐dimethyl‐acrylamide, DMAA; acrylic acid; or ((N‐tert‐butoxycarbonyl)‐2‐aminoethyl)methacrylate) by reversible addition–fragmentation chain transfer polymerization (RAFT). The RAFT copolymerization parameters of PrIA and DMAA are r_DMAA = 0.49 and r_PrIA = 0.17, compared to r_DMAA = 0.52 and r_PrIA = 0.54 obtained by free radical copolymerization (FRP). Thus, the RAFT process has a stronger trend to alternating polymerization than the FRP process. The polydispersity index of the RAFT copolymers is around 1.2–1.8, compared to 2.8–2.9 for the corresponding FRP copolymers. After removal of the tert‐butoxycarbonyl protective groups, antimicrobially active synthetic mimics of antimicrobial peptides are obtained. The thus activated poly(PrIA‐co‐DMAA) copolymers (repeat unit ratio 1:1) have an increasing activity against Escherichia coli and Staphylococcus aureus with increasing molar mass. The RAFT copolymers are slightly more active and less toxic than comparable FRP polymers, leading to a higher selectivity for bacteria over mammalian cells. Higher molar fractions of PrIA in poly(PrIA‐co‐DMAA) copolymers (up to 80 mol%) do not increase their antimicrobial activity; reduction of the BuIA content in poly(BuIA‐DMAA) (down to 10 mol%) leads to a loss of activity against both E. coli and S. aureus.     

Iodinated curcumin bearing dermal cream augmented drug delivery,antimicrobial and antioxidant activities

Objectives: Curcumin (Cur) exhibits weak microbicidal activity owing to high lipophilicity and low cell permeability. Therefore, in the present investigation, Cur was iodinated using elemental iodine (I₂) to synthesise Cur–I₂ powder that was later formulated as Cur–I₂ dermal cream and characterised in vitro for antimicrobial and antioxidant activities.

Methods and results: Electrophilic addition of I₂ saturated the olefinic bonds of Cur, as confirmed by UV/visible spectroscopy, FT-IR, ¹H NMR and DSC techniques. In addition, in vitro skin permeation and retention analysis indicated that Cur–I₂ cream followed the first order and Higuchi model for drug release through the rat skin. The minimum inhibitory concentration (MIC) of Cur–I₂ powder was measured to be 60 and 90?µg/ml significantly (p?Staphylococcus aureus and Escherichia coli, respectively. Moreover, Cur–I₂ also exhibited strong antioxidant potential.

Conclusions: Cur–I₂ cream warrants further in vivo study to scale up the technology for clinical translation.     

新医改形势下药师参与住院药费控制成效分析

目的:通过对药师参与住院药费控制的成效分析,旨在为医改形式下药师参与药费控制提供参考借鉴。方法:在医院政策支持下,各部门密切协作,药师参与药费控制,采取系列措施:制定辅助用药目录与排他性药物目录、开展处方点评、利用信息手段实施事前干预、鼓励药师事前干预/在线干预、开展临床合理用药宣教等。统计分析药师参与住院药费控制前后西成药占比、医院自制药及中药占比、主要治疗药物及辅助用药占比、人均总费用及人均药费的变化。结果:住院西成药占比降低10.65%,达到医院预期目标。其中辅助用药下降幅度最大;零加成后主要治疗用药占比上升21.15%,医院自制药品及中药占比上升173.23%。人均药费及人均总费用较前减少不明显,符合医改总体目标。结论:新医改形式下药师参与住院药费控制成效显著,可发挥不可替代的职业价值。     

保健食品中新型二硫代卡地那非类似物的分析鉴定

目的 鉴定保健食品中非法添加的一个未知结构的二硫代卡地那非类似物。方法 采用高效液相色谱-二极管阵列检测器联用（HPLC-DAD）技术进行补肾壮阳类保健食品非法添加筛查时发现一个未知结构的二硫代卡地那非类似物,经过正相硅胶薄层色谱分离纯化得到目标化合物后,用超高效液相色谱-二级质谱联用（UPLC-MS/MS）技术获得其准分子离子和二级质谱图,用核磁共振得到碳谱和氢谱数据,结合文献分析,最终鉴定该化合物的结构。结果 在保健食品中发现了一个新型二硫代卡地那非类似物,结构为3,5-二甲基哌嗪基二硫代去甲卡地那非。结论 该化合物不在现有补肾壮阳类中成药检验标准的13种目标化合物范围内,是一种新的非法添加化学物质。     

基于网络搜索快速鉴定抗风湿类中成药和保健食品中非法添加的非那西丁及小檗碱

目的 鉴定抗风湿类中成药和保健食品中非法添加的2个未知成分。方法 采用高效液相色谱-二极管阵列检测器联用（HPLC-DAD）技术进行抗风湿类中成药和保健食品非法添加筛查时发现2个可疑色谱峰,采用UPLC-MS/MS技术获得其准分子离子和二级质谱图,然后通过网络搜索分析初步确定可疑成分,最后与对照品比较检测,最终确定2个非法添加化合物的结构。结果 在抗风湿类保健食品中检出盐酸小檗碱,中成药中检出非那西丁。结论 这2个化合物不在现有抗风湿类中成药和保健食品检验标准13种目标化合物范围内,容易逃脱标准监管范围。     

Gold-silver-palladium alloys for laser irradiation —Effects of gold addition—

The clasp arms are fatigued by wearing a denture, by taking it off, and by occlusion. We routinely use laser irradiation to harden only the surface layer of clasp arms consisting of gold-silver-palladium alloy partially hardened by laser irradiation to resist fatigue. Recently we tested laser irradiation on silver-palladium-copper alloys, and obtained the following results:

HPLC-MS/MS同时测定尿酸调节类中药及含中草药食品中22种非法添加药物

目的 采用高效液相色谱-串联质谱法同时测定尿酸调节类中药及含中草药食品中22种非法添加药物。方法 样品经含0.1%氨水的甲醇超声提取后,采用Agilent Poroshell 120 Bonus-RP(2.1 mm×100 mm,2.7μm)色谱柱进行分离,以甲醇-乙腈(1∶1)和0.005 mol·L^-1甲酸铵溶液为流动相梯度洗脱。采用电喷雾离子源正、负离子模式,以多反应监测扫描方式检测。结果 22种药物在10.0～200μg·L^-1内线性关系良好,相关系数r²均>0.99,检测限和定量限分别为0.125～0.750 mg·kg^-1和0.416～2.81 mg·kg^-1,平均回收率为80.2%～120.1%,RSD为1.1%～5.9%。收集的37批样品中均未检出非法添加的药物。结论 该方法操作简单、快速、灵敏度高,可实现同时检测尿酸调节类中药及含中草药食品中22种非法添加药物。     

Base Catalyzed Thiol–Ene Click Chemistry toward Inner ?CHCF? Bonds for Controlled Functionalization of Poly(vinylidene fluoride)

A facile and controlled base catalyzed thiol–ene click chemistry toward electron‐deficient ? CH?CF? double bonds in poly(vinylidene fluoride) PVDF (P(VDF‐DB)) is reported in present contribution for the first time. The addition reaction is carefully conducted under varied conditions including at the elevated temperature, in the different solvents, and with the altered catalysts and thiols. The addition reaction is well confirmed to follow the base catalyzed route and exhibits close dependence onto the reaction conditions. Besides the addition reaction, the other two side reactions catalyzed by alkylamines, including the further main chain degradation of P(VDF‐DB) substrates together with the nucleophilic substitution of thiols to ? CH?CF? units, can be completely avoided by choosing a catalyst with a proper pK_a value. With respect to the universality and well controlled feature of the reaction, the low cost and readily prepared P(VDF‐DB) substrate and the mild reaction conditions, this strategy may offer a robust tool for attaching various functional groups into PVDF side chain.     

Base Catalyzed Thiol–Ene Click Chemistry toward Inner CHCF Bonds for Controlled Functionalization of Poly(vinylidene fluoride)

A facile and controlled base catalyzed thiol–ene click chemistry toward electron‐deficient ?CH?CF? double bonds in poly(vinylidene fluoride) PVDF (P(VDF‐DB)) is reported in present contribution for the first time. The addition reaction is carefully conducted under varied conditions including at the elevated temperature, in the different solvents, and with the altered catalysts and thiols. The addition reaction is well confirmed to follow the base catalyzed route and exhibits close dependence onto the reaction conditions. Besides the addition reaction, the other two side reactions catalyzed by alkylamines, including the further main chain degradation of P(VDF‐DB) substrates together with the nucleophilic substitution of thiols to ?CH?CF? units, can be completely avoided by choosing a catalyst with a proper pK_a value. With respect to the universality and well controlled feature of the reaction, the low cost and readily prepared P(VDF‐DB) substrate and the mild reaction conditions, this strategy may offer a robust tool for attaching various functional groups into PVDF side chain.     

比马前列素用于睫毛增长的安全风险探讨

目的 探讨比马前列素用于睫毛增长的安全风险。方法 针对比马前列素的理化性质、药理作用和药动学、临床应用、不良反应、化妆品监管政策等方面进行梳理分析，为监管工作提供理论依据。结果 比马前列素是一种人工合成的前列腺素类似物——前列腺素F_2α类似物，可以有效降低眼压和促进毛发增长。其消除半衰期为45 min，主要通过尿液排泄。FDA孕期评级为C级，可能对胎儿有不利影响；上市后不良反应主要包括眼睛充血、眼睑红斑、眼刺激等，其安全性有必要进行进一步评估；不符合中国化妆品的定义和规定的功效宣称，欧盟和加拿大禁止比马前列素等药物成分用于化妆品，美国将其作为药品管理。结论 为了保证化妆品质量安全，规范和促进行业健康发展，建议中国监管部门跟踪关注比马前列素等前列腺素类似物的使用安全性，必要时调整管理措施。