Development of an LC‐MS/MS method for determining the pharmacokinetics of clonidine following oral administration of Zhenju antihypertensive compound

Zhenju antihypertensive compound (ZJAHC) is a combined Chinese–Western medicine formula including clonidine (CLO), hydrochlorothiazide (HCT), rutin, Chrysanthemum indicum extract and pearl powder. Compared with CLO preparations, ZJAHC shows improved activities and decreased adverse effects. It is believed that the side effects of CLO are caused by its high peak plasma concentration. Hence, study of the influence of ZJAHC on the pharmacokinetic behaviors of clonidine seems essential. In present study, the plasma concentrations of CLO were determined with a liquid chromatography–tandem mass spectrometry (LC‐MS/MS) method. The MS/MS transitions monitored for clonidine and internal standard were 230.2 → 213.1 and 152.2 → 110.2, respectively. The analyte was quantified in a single run within 3 min. The pharmacokinetic study showed that the area under the plasma concentration–time curve of CLO in ZJAHC (60 µg/kg CLO) was similar to that of CLO‐HCT‐high (120 µg/kg CLO) but the peak concentration was much lower than that in CLO‐HCT‐high. ZJAHC could enhance the bioavailability without greatly increasing peak concentration of clonidine. This comprehensive effect of enhancing the bioavailability and avoiding the high peak plasma concentration for CLO might mainly result from the co‐contribution of Western medicine and traditional Chinese medicine (TCM), while the effect of TCM was stronger than that of Western medicine. Copyright © 2014 John Wiley & Sons, Ltd.     

Directing-Group-Free C7-Alkylations of N-Alkylindoles Mediated by Cationic Zirconium Complexes: Role of Brønsted Acid for Catalytic Manifold

Highly position selective alkylations of N-alkylindoles at C7-positions have been enabled by cationic zirconium complexes. The strategy provides a straightforward access to install alkyl groups at C7-positions of indoles without a complex directing group. Mechanistic studies provided support for the importance of Brønsted acids in the catalytic manifold.     

Unlocking the Drug Potential of the Bryostatin Family: Recent Advances in Product Synthesis and Biomedical Applications

Bryostatins are a class of naturally occurring macrocyclic lactones with a unique fast developing portfolio of clinical applications, including treatment of AIDS, Alzheimer's disease, and cancer. This comprehensive account summarizes the recent progress (2014–present) in the development of bryostatins, including their total synthesis and biomedical applications. An emphasis is placed on the discussion of bryostatin 1 , the most-studied analogue to date. This review highlights the synthetic and biological challenges of bryostatins and provides an outlook on their future development.     

Dynamic effect of constant inertial acceleration on vibration isolation system with high-order stiffness and Bouc–Wen hysteresis

Nonlinear Dynamics - Nonlinear vibration isolation provides with an effective way for vibration reduction with broad band and high efficiency. This investigation focuses on the dynamic effects of a...     

General Formation of Macro-/Mesoporous Nanoshells from Interfacial Assembly of Irregular Mesostructured Nanounits

Mesoporous core–shell nanostructures with controllable ultra-large open channels in their nanoshells are of great interest. However, soft template-directed cooperative assembly to mesoporous nanoshells with highly accessible pores larger than 30 nm, or even above 50 nm into macroporous range, remains a significant challenge. Herein we report a general approach for precisely tailored coating of hierarchically macro-/mesoporous polymer and carbon shells, possessing highly accessible radial channels with extremely wide pore size distribution from ca. 10 nm to ca. 200 nm, on diverse functional materials. This strategy creates opportunities to tailor the interfacial assembly of irregular mesostructured nanounits on core materials and generate various core–shell nanomaterials with controllable pore architectures. The obtained Fe,N-doped macro-/mesoporous carbon nanoshells show enhanced electrochemical performance for the oxygen reduction reaction in alkaline condition.     

DISPERSION COMPENSATION CFBG IN100km 10Gbit／s RECIRCULATING SYSTEMS

A 10Gbit/s recirculating system is configured with Chirped Fiber Bragg Grating (CFBG) for the dispersion compensation. For the first time, the transmission distance in the loop reaches 1000km with bit error rate of 10-9. The effect of the group delay ripple of the fiber grating is also investigated in the recirculating systems, and it is shown that the transmission distance is limited to 4 cycles (4×167.1km ) in the loop with the power penalty fluctuation below 1.0dB. Thus the group delay ripple should be reduced to allow for the wavelength drift of±5GHz. At the end of this letter, the principles are given for designing long haul recirculating systems with dispersion compensation CFBG.     

Numerical Evaluation of a Two-Loop Diagram in the Cutoff Regularization

The sunset diagram of λφ4 theory is evaluated numerically in cutoff scheme and a nonzero finite term(in accordance with dimensional regularization (DR) result) is found in contrast to published calculations. This findingdramatically reduces the critical couplings for symmetry breaking in the two-loop effective potential discussed in ourprevious work.     

Analysis and architecture design of variable block-size motion estimation for H.264/AVC

Variable block-size motion estimation (VBSME) has become an important video coding technique, but it increases the difficulty of hardware design. In this paper, we use inter-/intra-level classification and various data flows to analyze the impact of supporting VBSME in different hardware architectures. Furthermore, we propose two hardware architectures that can support traditional fixed block-size motion estimation as well as VBSME with less chip area overhead compared to previous approaches. By broadcasting reference pixel rows and propagating partial sums of absolute differences (SADs), the first design has the fewer reference pixel registers and a shorter critical path. The second design utilizes a two-dimensional distortion array and one adder tree with the reference buffer that can maximize the data reuse between successive searching candidates. The first design is suitable for low resolution or a small search range, and the second design has advantages of supporting a high degree of parallelism and VBSME. Finally, we propose an eight-parallel SAD tree with a shared reference buffer for H.264/AVC integer motion estimation (IME). Its processing ability is eight times of the single SAD tree, but the reference buffer size is only doubled. Moreover, the most critical issue of H.264 IME, which is huge memory bandwidth, is overcome. We are able to save 99.9% off-chip memory bandwidth and 99.22% on-chip memory bandwidth. We demonstrate a 720-p, 30-fps solution at 108 MHz with 330.2k gate count and 208k bits on-chip memory.     

H.264/AVC技术进展及其务实发展策略思考

结合NGN及3G演进的固定、移动视频业务实际需求状况，论述H．264／AVC的重要技术进展及其务实发展策略。