Evaluation of Solubility and Membrane Permeability of Middle-Molecule Compounds Using Artificial Membranes and Living Cells
Yakugaku Zasshi. 2024;144(5):529-537. doi: 10.1248/yakushi.23-00191-1.ABSTRACTIn contrast to small molecules, middle molecules present a promising therapeutic modality owing to their elevated specificity, minimal adverse effects, capacity to target protein-protein interactions, and, unlike antibody-based drugs, their suitability for oral administration and intracellular target engagement. Post-oral administration, the paramount considerations encompass solubility and membrane permeability during the initial phase until the drug attains systemic circulation. Furthermore, penetration of the cell membrane is essential to acce...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - May 1, 2024 Category: Drugs & Pharmacology Authors: Kayoko Kanamitsu Mayumi Ishii Eri Watanabe Hiroyuki Miyachi Source Type: research

Development of Integrated Database for Experiments and Simulations
Yakugaku Zasshi. 2024;144(5):539-543. doi: 10.1248/yakushi.23-00191-2.ABSTRACTResearchers collect data and use various methods to organize it. Ensuring the reliability and reproducibility of data is crucial, and collaboration across different research fields is on the rise. However, when there is geographical distance, sharing data becomes a challenging task. Therefore, there is a need for the development of a mechanism for sharing data on the web. We have developed an integrated database to facilitate the sharing and management of research data, particularly focusing on small molecules. The integrated database serves as a...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - May 1, 2024 Category: Drugs & Pharmacology Authors: Issaku Yamada Naoki Kimura Takao Nomura Satoko Otsuguro Hiroyuki Miyachi Yasuteru Shigeta Katsumi Maenaka Source Type: research

Development of Membrane Permeability Coefficient by Means of Novel Molecular Dynamics Methods
Yakugaku Zasshi. 2024;144(5):545-551. doi: 10.1248/yakushi.23-00191-3.ABSTRACTThe membrane permeability, and its evaluation, is crucial factor in the process of uptake of compounds from outside to inside the cell and in the inhibition of the activity of disease-causing target proteins. Although molecular dynamics (MD) simulations have been shown to be able to reproduce the conformational changes of compounds occurring during membrane permeation, it is still challenging to extract the membrane permeability at an affordable computational workload solely by conventional MD. Indeed, the time scale accessible by MD is far below...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - May 1, 2024 Category: Drugs & Pharmacology Authors: Ryuhei Harada Yuki Mitsuta Yasuteru Shigeta Source Type: research

Syntheses and Structure-Activity Relationship Studies of Antitumor Bicyclic Hexapeptide RA-VII Analogues
Yakugaku Zasshi. 2024;144(5):553-565. doi: 10.1248/yakushi.23-00208.ABSTRACTA series of antitumor bicyclic hexapeptide RA-VII analogues modified at residue 2, 3, or 6 were prepared by the chemical transformation of the hydroxy, methoxy, or carboxy groups or the aromatic rings of natural peptides RA-II, III, V, VII, and X. Analogues with modified side chains or peptide backbones, which cannot be prepared by the chemical transformation of their natural peptides, and newly isolated peptides from Rubia cordifolia roots were synthesized by using protected cycloisodityrosines prepared by the degradation of bis(thioamide) obtaine...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - May 1, 2024 Category: Drugs & Pharmacology Authors: Yukio Hitotsuyanagi Source Type: research

Evaluation of Pharmacy Students' Understanding of Clinical Trials and Research through Questionnaires Before and After the Hospital Practical Training
Yakugaku Zasshi. 2024;144(5):567-576. doi: 10.1248/yakushi.23-00202.ABSTRACTA questionnaire survey was conducted to evaluate practical training and improve education on clinical trial and research. This survey was based on the results of questionnaire before and after the practical training undertaken by 240 pharmaceutical students (Kanto region; 1 university, Tokai region; 2 university, Kinki region; 9 university) at Mie University Hospital between 2011 and 2022. In the questionnaire before practical training, lectures in university (n=219, 91%) were the main source of information on clinical trials and research. Fifty-tw...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - May 1, 2024 Category: Drugs & Pharmacology Authors: Chihiro Shiraishi Mayumi Kotera Yasuyuki Ota Eiko Takeshige Chisato Minamide Rie Kurimoto Aki Sato Miho Inamori Misaki Kataoka Toru Ogura Satoshi Tamaru Takuya Iwamoto Source Type: research

A Questionnaire Survey of Nurses on Pharmacist Services in the Emergency Rooms at Tokushukai Medical Group
Yakugaku Zasshi. 2024;144(5):577-584. doi: 10.1248/yakushi.23-00205.ABSTRACTWe conducted a multicenter survey of emergency room nurses to obtain information that would be useful for the establishment of pharmacist services in emergency rooms. Notably, 199 valid responses were obtained from 12 hospitals. The most common expectation from pharmacists in the emergency room was "drug management" (70.9%), followed by "providing information to physicians regarding the patient's medication history" (59.3%), and "auditing of dosage and interaction" (57.3%). The working arrangements that the survey respondents wanted regarding pharm...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - May 1, 2024 Category: Drugs & Pharmacology Authors: Hiroki Tateishi Yasuhiro Saito Yuichi Miyata Yuto Sakaguchi Kojiro Yamamoto Eiji Takeda Riku Iwasaki Yuji Miyazaki Daisuke Maekawa Maiki Yoshikawa Yosuke Takeuchi Yohei Yano Takao Goto Hiroyuki Watanabe Source Type: research

Mechanistic Analysis of Oxidative Stress-related Diseases Using Nitroxyl Radicals and Electron Spin Resonance
Yakugaku Zasshi. 2024;144(4):339-344. doi: 10.1248/yakushi.23-00141.ABSTRACTExcessive production of reactive oxygen species (ROS) causes oxidative stress and is involved in the development and progression of a wide variety of diseases. Therefore, techniques for measuring oxidative stress are indispensable for analysis of the mechanisms of various diseases. The method involving ESR and the durable nitroxyl radical (ESR/spin probe method) is useful for this purpose, because the ESR signal intensity of the spin probe changes on reacting with ROS and other unstable radicals. In this review, the author's research applying the E...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - March 31, 2024 Category: Drugs & Pharmacology Authors: Shoko Okazaki Source Type: research

Implementation and Future of Quantitative NMR in the Pharmaceutical and Food Fields
Yakugaku Zasshi. 2024;144(4):345-346. doi: 10.1248/yakushi.23-00151-F.NO ABSTRACTPMID:38556305 | DOI:10.1248/yakushi.23-00151-F (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - March 31, 2024 Category: Drugs & Pharmacology Authors: Nahoko Uchiyama Naoki Sugimoto Source Type: research

Route to the Adoption of Quantitative NMR in the Japanese Pharmacopoeia
This report outlines how and why qNMR has been adopted as an official method in the JP and introduces its progression from JP16 to JP18. The results of a survey of companies in the Japan Pharmaceutical Manufacturers' Association regarding how and when to use qNMR from development to manufacturing stages are introduced. The issues involved in the expansion of the use of qNMR in the field of chemical pharmaceuticals in 2017 are discussed and how these were resolved.PMID:38556306 | DOI:10.1248/yakushi.23-00151-1 (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - March 31, 2024 Category: Drugs & Pharmacology Authors: Yukihiro Goda Source Type: research

Standardization and Practical Application of Quantitative NMR (qNMR)
Yakugaku Zasshi. 2024;144(4):353-357. doi: 10.1248/yakushi.23-00151-2.ABSTRACTIn Japan, quantitative NMR (qNMR) has already been recognized as a standard method for determining the purity of quantitative samples not only in the Japanese Pharmacopoeia and the Japanese Standards and Specifications for Food Additives but also in the Japanese Industrial Standard (JIS K 0138: 2018). However, since there was no consensus on the establishment of a standard method, the international standardization of qNMR was initiated based on a proposal from Japan. After three years of discussion among experts, International Organization for St...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - March 31, 2024 Category: Drugs & Pharmacology Authors: Naoki Sugimoto Source Type: research

Quantitative < sup > 31 < /sup > P-NMR for Purity Determination of Organophosphorus Compounds (Pharmaceuticals)
Yakugaku Zasshi. 2024;144(4):359-365. doi: 10.1248/yakushi.23-00151-3.ABSTRACTQuantitative NMR (qNMR), particularly 1H-qNMR, is useful for determining the absolute purity of organic molecules. However, identifying the target signal(s) for quantification is difficult, because of the overlap and complexity of organic molecules. Therefore, we focused on the 31P nucleus, owing to the simplicity of its signals, and investigated the 31P-qNMR absolute determination method by using organophosphorus drugs, water-soluble cyclophosphamide hydrate (CP), and water-insoluble sofosbuvir (SOF). The optimized and reproducible 31P-qNMR cond...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - March 31, 2024 Category: Drugs & Pharmacology Authors: Nahoko Uchiyama Source Type: research

High Purity Solvents for qNMR Measurement
In this study, we investigated the influence of solvent quality on qNMR accuracy focusing on organic impurities, water content, and deuteration ratio. If signals from organic impurities and signals from the analyte overlap, the duplication of signal integration will directly affect the qNMR analytical result. To examine overlapping, we performed blank solvent tests. Additionally, a high water content and low deuteration ratio affect the detection sensitivity, thus reducing the signal-to-noise (S/N) ratio of the target. Thus, these factors must be considered to obtain accurate qNMR results.PMID:38556309 | DOI:10.1248/yakush...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - March 31, 2024 Category: Drugs & Pharmacology Authors: Yasuhiro Muto Toru Miura Yoshiaki Iwamoto Source Type: research

Application of qNMR in Standard Materials Used for the Crude Drugs
Yakugaku Zasshi. 2024;144(4):373-380. doi: 10.1248/yakushi.23-00151-5.ABSTRACTCrude drugs and Kampo formulations derived from natural materials such as plants, animals, and minerals are multicomponent medicines that contain numerous chemical constituents. Quantitative determination of characteristic constituents for quality control is crucial for the standardization and quality assurance of natural medicines. Quantitative assays to determine marker compound contents are commonly performed using HPLC systems. In order to achieve accurate quantitative determination, it is essential to use standard materials with well-defined...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - March 31, 2024 Category: Drugs & Pharmacology Authors: Azusa Suzuki Source Type: research

The Applications of qNMR in Drug Quality Control
Yakugaku Zasshi. 2024;144(4):381-385. doi: 10.1248/yakushi.23-00151-6.ABSTRACTNMR is well known as one of the most important methods for elucidating the structure of organic compounds. Furthermore, it has recently been recognized as a powerful tool for quantitative analysis. The quantitative NMR (qNMR) has become an official analytical method described in detail in the Japanese Pharmacopoeia. And today, it is widely applied in drug development. The qNMR method offers many new advantages over traditional and conventional quantitative analysis methods. For example, this method requires only a few milligrams of the analyte an...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - March 31, 2024 Category: Drugs & Pharmacology Authors: Eri Ena Yumi Asai Takashi Hasebe Hiroshi Oe Shuichi Hirose Yoshimasa Takahashi Source Type: research

Mechanisms of Aging and Age-related Diseases and Their Regulation: Dispatch of Information from Basic Research
Yakugaku Zasshi. 2024;144(4):387. doi: 10.1248/yakushi.23-00165-F.NO ABSTRACTPMID:38556312 | DOI:10.1248/yakushi.23-00165-F (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - March 31, 2024 Category: Drugs & Pharmacology Authors: Ryoya Takahashi Yoshikazu Higami Source Type: research