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        Pharmacokinetic, metabolic stability, plasma protein binding and CYP450s inhibition/induction assessment studies of N-(2-pyridylmethyl)-2- hydroxiymethyl-1-pyrrolidinyl-4-(3-chloro-4-methoxy-benzylamino)-5- pyrimidine-carboxamide as potential type 5 phos

        Haijun Qu,Xiaoxiao Hu,Xiaoli Shi,Chuan Wang,Longyuan Wang,Guoping Wang 한국통합생물학회 2019 Animal cells and systems Vol.23 No.3

        N-(2-pyridylmethyl)-2-hydroxiymethyl-1-pyrrolidinyl-4-(3-chloro-4-methoxy-benzylamino)-5- pyrimidine-carboxamide (NHPPC) is a new potential of type 5 phosphodiesterase (PDE5) inhibitors, synthesized from the avanafil analogue for the treatment of erectile dysfunction. The targets of this article were to assess plasma protein binding, liver microsomal metabolic stability, inhibition and induction on cytochrome P450 isozymes and the pharmacokinetics of NHPPC. Equilibrium dialysis technique was applied to determine Plasma protein binding (PPB) and NHPPC was evaluated in male Sprague–Dawley rats and Beagle dogs in vivo pharmacokinetic. The NHPPC was highly bound to plasma proteins in rats, dogs and human tested and the mean values for PPB rate were 96.2%, 99.6% and 99.4%, respectively. After in vitro liver microsomes incubated for 60 min, the percent remaining of NHPPC was 42.8%, 0.8% and 42.0% in rats, dogs and human, respectively. In vitro intrinsic clearance was found to be 0.0233, 0.1204 and 0.0214 mL/min/mg protein in rat, dog and human liver microsomes of NHPPC, respectively. NHPPC showed no significant inhibitory effects on major CYP450 enzymes, and had no significant induction potential on CYP1A2 and CYP3A4. Following oral administration in rats and dogs, tmax was 6 and 0.5 h, respectively. The clearance for NHPPC was 1.19 and 1.46 L/h/kg in rats and dogs, respectively. And absolute bioavailability in rat and dog were approximately 34.5% and 53.1%, respectively. These results showed that NHPPC has a good development prospect.

      • Reconfigurable Flight Control System Design for Blended Wing Body UAV Based on Control Allocation

        Xiaobo Qu,Jingping Shi,Haijun Zhou,Ling Zuo,Yongxi Lyu 제어로봇시스템학회 2018 제어로봇시스템학회 국제학술대회 논문집 Vol.2018 No.10

        The aircraft control surface fault reconfigurable scheme based on control allocation is an active approach to achieve fault-tolerant in flight control. It has obvious advantages such as the structure and parameters of the control law does not need to be redesigned as deflector failures occurs. The attainable moment subset and allocation efficiency with typical control allocation algorithms are evaluated. A modular scheme reconfigurable flight control system (FCS) of a miniature tailless Blended Wing Body UAV is studied by utilizing weighted pseudo-inverse, direct control, and fixed-point control allocation methods. The performance of the reconfigurable FCS is tested and verified with the simulation including typical failure modes such as deflector floating, loss-of-effectiveness and lock-in-place. Results validate that the reconfigurable FCS based on control allocation has preferable ability to handle deflector failures, improve the safety and reliability of aircraft. And the modular scheme proposed in the article demonstrates a good application prospect in the field of aviation and aerospace engineering.

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        Research on the explosion release method and damage mechanism of titanium alloy fan blade

        Yanan Zhang,Zekan He,Chuang Liu,Meng Wang,Haijun Xuan,Mingmin Qu,Zehui Fang 대한기계학회 2023 JOURNAL OF MECHANICAL SCIENCE AND TECHNOLOGY Vol.37 No.8

        The current advanced aero-engine fan rotors are usually integrally-bladed rotor discs, and the root of the fan blade has irregular curved surface, which brings technical difficulties and challenges to achieve the blade releasing. In this paper, the dynamic response and energy dissipation process of the titanium alloy blade under shaped charge jet explosion were analyzed by numerical model, and the explosion damage mechanism of titanium alloy fan blades was clarified. Finally, a FBO test was conducted to verify the blade explosion release method in rotating state. Through the energy dissipation analysis of the whole explosion process, it can be seen that the overall residual kinetic energy of the blade is about 15.7 J, which is only 0.02 % of the initial kinetic energy of the releasing blade in rotating. It is indicated that the explosion separation method will not generate additional kinetic energy to the released blade.

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