Synthesis and Biological Evaluation of Umifenovir Analogues as Anti-SARS-CoV-2 Agents.

The unprecedented novel coronavirus disease 2019 (COVID-19) pandemic is a threat to global health and the economy. Since the outbreak of COVID-19, great effort has been made to reposition existing drugs to shorten development timelines, in addition to vaccine development and drug discovery campaigns. Umifenovir is a broad-spectrum antiviral agent used to treat influenza in China and Russia and is currently undergoing clinical trials for the treatment of COVID-19. In this article, the synthesis of umifenovir analogues and their biological evaluation are reported. The inhibitory activities of analogues against the binding of the spike glycoprotein (S-protein) of the novel severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) to the ACE2 receptor, which is a possible mode of action for umifenovir to inhibit viral infection, were investigated.

[Evaluation of the Usefulness of Postoperative Analgesic Solution Preparation by Pharmacists in the Surgical Department].

Pharmacists began preparing drug solutions intraoperatively for postoperative analgesia in the Department of Surgery at Chiba University Hospital from May 2014. To verify the usefulness of pharmacists preparing these drug solutions, we conducted a questionnaire survey among 51 anesthesiologists and received 44 responses (recovery rate 86.3%). Burden on the anesthesiologists was significantly reduced both temporally and mentally when the pharmacists prepared the drug solutions compared with when the anesthesiologists did (p<0.01). The anesthesiologists' degree of anxiety about sometimes having to prepare drug solutions alone without any confirmation was also significantly reduced when pharmacists prepared them (p<0.01), which implies the need for a double-check system. In addition, 88.6% of anesthesiologists said that they were reassured with preparations done by the pharmacists under a sterile environment using a clean bench. Overall, 88.6% of anesthesiologists responded that they were satisfied with the preparation of drug solutions by pharmacists. Based on the results of this survey, pharmacists' preparation of drug solutions for postoperative analgesia is considered to be useful in ensuring the quality and safety of medical care because it reduced anesthesiologists' work to prepare the drug solutions, allowing them to concentrate on anesthesia and related work, it established a double-check system between the two staff teams, and it was done under a sterile environment.

Benchmarking Protocols for Evaluating Small Parts Robotic Assembly Systems.

This paper presents a set of performance metrics, test methods, and associated artifacts to help progress the development and deployment of robotic assembly systems. The designs for three task board artifacts that replicate small part insertion and fastening operations such as threading, snap fitting, and meshing with standard screws, nuts, washers, gears, electrical connectors, belt drives, and wiring are presented. To support the evaluation of robotic assembly and disassembly operations, benchmarking protocols and performance metrics are presented that leverage these task boards. Finally, robot competitions are discussed as use cases for these task boards.

Effect of particle size on skin permeation and retention of piroxicam in aqueous suspension.

The effects of particle size on the skin permeation and retention of piroxicam (PXC) in an aqueous suspension were investigated. PXC particles of about 23 nm, 173 nm, and 2.1 microm in size were prepared by the cogrinding of PXC/polyvinylpyrrolidone (PVP) K12/sodium dodecyl sulfate physical mixture (mean particle size, 9.6 microm) using a vibrational rod and ball mills. Particles were stable after storage in 0.1 m acetate buffer (pH 4.5) for 24 h. The amount of PXC that permeated and was retained in hairless mouse skin increased with the reduction of particle size up to 23 nm. Amorphous PXC was formed when PXC was coground with PVP, though the amorphous formation did not affect the amount of PXC permeated. Reduction of particle size to less than 50 nm, and the subsequent increase in surface area of PXC nanocrystals appeared to affect skin permeation and retention behavior.

[The interchange between hospital pharmacists and pharmacists: evaluation of practical classes "chozaigijutsu-konwakai" from the participants].

We have held practical classes called chozaigijutsu-konwakai(Konwakai) for pharmacists working in drugstores every month since December 1994. Konwakai is composed of lectures and practice. The practice is carried out for pharmacists to obtain a better understanding of prescriptions and compounding them in exercises. In this study, we analyzed the answers to questionnaires distributed at the end of each konwakai to all participants. It was found that the age of participants as well as the length of compounding experience varied markedly, indicating that pharmacists of various generations are interested in konwakai. Regarding the contents of lectures and practice, the answers indicated that the practice was particularly useful, suggesting the importance of exercise for learning techniques in compounding. Since there were many requests for consultations on routine work, frequent communications between pharmacists in the hospital and drugstores appears necessary. In conclusion, regular meetings including practical classes such as konwakai are very important for pharmacists in drugstores that receive prescriptions from hospitals. Further efforts to improve the konwakai should be maid in the future.