π-Extended donor–acceptor (D–A)-type molecules, which bear both electron-donor and electron-acceptor substituents on the backbone, exhibit unique optical properties, such as bathochromic shifts in absorption and emission, large Stokes shifts, solvatochromic behavior, and fluorescence quenching in polar solvents. These unique properties are attributed to intramolecular charge transfer (ICT) or twisted intramolecular charge transfer (TICT) in the ground and excited states. This review article introduces three types of D–A-type molecules that are used as detection reagents for (1) methanol, (2) amino acids during solid-phase peptide synthesis (SPPS), and (3) amines present in the biological environment. For methanol detection, D–A-type fluorophores with basic guanidine moieties were developed to differentiate between methanol (MeOH) and ethanol (EtOH) based on the small difference in their pKa values (ΔpKa=0.4). Selective protonation of the guanidine moiety in methanol disrupts the D–A structure, allowing emission in the resultant polar environment. Similarly, an acid-base reaction between the hydrogen chloride (HCl) salts of the D–A-type molecules and amines is applied to detect amines during SPPS. In this method, a colorless solution of an HCl salt of the D–A-type molecule is deprotonated by amines, forming a yellow solution. This is the first reported quantitative and non-destructive colorimetric method for detecting amines. Finally, a turn-on-type amine-labeling reagent was developed for the nucleophilic aromatic substitution (S_NAr) reaction. This new reagent enables protein staining of living cells with a large Stokes shift and without solvent-polarity-dependent fluorescence quenching.

The aim of our study was to develop a solventless drug pelletization and polymer coating technique for pharmaceutical manufacturing. This review describes a dry coating technique using a mechanical powder processor and a V-shaped blender to produce coated pellets or tablets by mechanically mixing polymer particles and core materials (such as drug pellets and uncoated tablets) without the need for a solvent. First, aqueous latexes comprising colloidal polymethacrylates and ethylcellulose were solidified by freeze drying to produce polymer particles for the dry coating process. These particles and the cores were then subjected to mechanical powder processing or V-shaped blending to provide coated formulations with controlled-release characteristics. Polymer coating was achieved by using agglomerates comprising assembled colloidal polymer. The agglomerated polymer was easily pulverized during the mixing treatments due to its loose structure (the lack of close contacts between the colloidal particles), and the resulting fine polymer with high adhesiveness was deposited on the cores. Colloidal polymer dispersed in aqueous latex tends to coagulate in the freeze-drying process due to condensation of the dispersion, yielding dense agglomerates with poor coating characteristics. The presence of surfactants (such as sodium lauryl sulfate) in the latex can prevent adhesion between colloidal particles in the freeze-drying process, providing loosely structured agglomerates suitable for dry coating. Dry coating with a V-shaped blender could thus be achieved with these polymer particles instead of having to use a mechanical powder processor.

Oligonucleotides, including DNA and RNA, can be functionalized by chemical modification based on synthetic organic chemistry. For example, ligand–oligonucleotide conjugates have a wide variety of applications. Conjugates of functional ligands and oligonucleotides have attracted attention in recent years as a drug delivery system (DDS) for improving the efficacy of oligonucleotide therapeutics. In addition, oligonucleotide conjugates with drug candidate compounds as ligands have been applied to drug screening using DNA-encoded libraries (DELs). Against this background, we have focused on the development of practical synthetic methods for ligand–oligonucleotide conjugates. Recently, we have developed a new synthetic method to construct oligonucleotides conjugated with coumarins and dipeptides, which are expected to have bioactivity, for application to DDS research of oligonucleotide therapeutics and drug discovery research using DEL. In this review, we will discuss the details, including how to construct a coumarin scaffold on oligonucleotides based on Knoevenagel condensation.

The pharmacokinetic (PK)/pharmacodynamic (PD) approach has been widely used in clinical practice to optimize antimicrobial treatment. To promote the appropriate use of antimicrobial agents, it is important to consider certain factors, such as patient (e.g., age, physique, medical history, comorbidities, and organ dysfunction), site of infection (the target site where many causative bacteria are present), and microorganism (causative bacteria and susceptibility), and the dosing regimen should be selected based on the PK/PD approach. However, for renally excreted antibiotics, dosing regimens based on only renal function, such as creatinine clearance, are mainly used. Therefore, other factors such as patient pathological factors, antibiotic penetration of target sites, susceptibility of the causative bacteria to antibiotic, and clinical evaluation (efficacy and toxicity) should be considered simultaneously. These studies aimed to tailor the dosing of antimicrobial agents to individual patients by considering these factors. Multifaceted PK/PD evaluation may improve antimicrobial efficacy and safety, thereby contributing to the successful treatment of infectious diseases. Furthermore, improved treatment success rates may help manage the prevalence of antimicrobial-resistant bacteria, which is expected to become a significant problem in the future.

Prescribing direct oral anticoagulants (DOACs) with off-label dosage and administration is discouraged due to concerns about their effectiveness and safety. Consequently, our hospital pharmacist established a formulary with physicians for oral anticoagulants. Our study aimed to assess the adherence to this formulary by investigating the rate of appropriate DOAC prescribing. We included patients who were newly prescribed or continued on DOACs (dabigatran, rivaroxaban, apixaban, and edoxaban) at our hospital. We calculated the percentage of patients prescribed the correct dosage and administration according to the package insert and compared this across three time periods: pre-intervention (period A; April–September 2019), post-intervention phase 1 (period B; August 2021–January 2022), and post-intervention phase 2 (period C; November 2022–April 2023). We also examined the number of inquiries and consultation requests made by hospital pharmacists regarding DOAC dosage and administration. A total of 782 patients were surveyed (191 in period A, 263 in period B, and 328 in period C). The appropriate prescribing rates for DOACs were 79.1% in period A, 84.4% in period B, and 86.6% in period C. The proportion of cases where hospital pharmacists questioned or consulted doctors about DOAC dosage and administration was 3.7% in period A, 6.1% in period B, and 10.1% in period C. These findings indicate that active intervention by hospital pharmacists using the formulary regarding oral anticoagulant formularies may promote appropriate DOAC use.

Budesonide Rectal Foam (BF) was introduced in 2017 and changed in November 2022 upon request, addressing the challenges encountered with liquid rectal formulations indicated for ulcerative colitis (UC). This formulation is an important agent in the treatment of rectal to sigmoid colon lesions in moderate UC. As the characteristics of the formulation of the rectal formulation are thought to influence patient satisfaction, a survey was conducted on the formulation and patient satisfaction among patients who used BF before and after the change. The survey spanned from January 2023 to May 2023. As the primary endpoint, the same patients were evaluated on the Visual Analogue Scale (VAS) for patient satisfaction. Significant variations in formulation usability and patient satisfaction were observed in 20 eligible patients before and after the change (p<0.05). Patient satisfaction with the formulation was strongly correlated with formulation usability, ease of pushing the head, and ease of insertion (r>0.7). The change in packaging was thought to improve the usability of the formulation and patient satisfaction. The formulation’s usability and ease of insertion had a clear influence on satisfaction with the rectal formulation.

This survey aimed to reveal the actual preventing exposure for handling of clothing and sweat of patients treated with anticancer drugs, following the publication of “Guideline for Preventing Occupational Exposure in Cancer Chemotherapy Drugs, 2019 Edition” (Guideline 2019). A survey was conducted among nurses working at 95 hematopoietic stem cell transplantation promotion base hospitals from September 1, 2023 to October 31, 2023. The response rate was 84.2% (80 facilities). Of the respondents, 45% wore gloves when touching patients’ skin to administer anticancer drugs. Almost the nurses identified “urine” and “feces” as fluids on contaminated linen, while 14.1% also identified “sweat.” For new staff, the results for preventing exposure education on “if touching the patients’ skin” and “if handling clothing and linen” were 23.8% and 34.9%, respectively. This survey shows that nurses may not be following the Guideline 2019 for use of personal protective equipment and handling of clothes. Medical institutions handling anticancer drugs need to educate their staff for preventing occupational exposure.

Blood purification therapy with cytokine-adsorbing hemofilters has been used to treat sepsis-associated hypercytokinemia. Polymethylmethacrylate (PMMA) hemofilters are frequently used for this purpose; however, adsorption and removal of teicoplanin, a therapeutic agent, have been reported. Similar concerns have been shared regarding daptomycin because its structure resembles that of teicoplanin; nevertheless, there have been no reported effects associated with daptomycin in this context. We studied the adsorption of daptomycin onto a PMMA hemofilter in vitro and investigated its adsorption onto hollow fiber membranes by adding cut PMMA membranes to a daptomycin solution. Additionally, the daptomycin solution was circulated in a dialysis circuit connected to a PMMA hemofilter, and changes in daptomycin content were examined. The daptomycin content decreased immediately after adding the hollow fiber membranes, similar to that observed for teicoplanin. The daptomycin content was lower than that of the standard reagent in the dialysis circuit model, reaching values below the measurement limit after 20 min. These results suggested that daptomycin was adsorbed and removed by the PMMA hemofilter. Encountering this effect during clinical use is plausible; therefore, daptomycin administration via a PMMA hemofilter should be avoided during blood purification therapy.