[Analysis of Risk Factors for Side Effects and the Establishment of Supportive Therapy during Cancer Chemotherapy].
Abstract Cancer chemotherapy has a high frequency of side effects, and patients often experience adverse health effects. This review focuses on risk factors and supportive care for the prevention of chemotherapy side effects. 1) Drug-induced interstitial lung disease (DILD) is one of the serious adverse events associated with chemotherapy, and this retrospective study investigated the risk of DILD in Japanese patients with lung cancer. Among the 459 patients who received lung cancer chemotherapy from April 2007 to March 2013, 33 (7.2%) developed chemotherapy-associated DILD. Preexisting interstitial lung disease w...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - November 3, 2018 Category: Drugs & Pharmacology Authors: Sakurada T Tags: Yakugaku Zasshi Source Type: research

[Asymmetric Synthesis of Unnatural Amino Acid-containing Peptides via Direct Asymmetric Reaction of Peptidyl Compounds].
Abstract Unnatural amino acids and the peptides bearing such units have gathered much attention due to their interesting biological activities and synthetic utility as chiral building blocks for the synthesis of complex molecules. This paper descibes an asymmetric synthesis of unnatural amino acid derivatives and their subsequent application to the preparation of unnatural amino acid-containing peptides. The α-imino carboxylic acid derivatives, which are common substrates for the synthesis of unnatural amino acids, could be readily prepared by MnO2-mediated oxidation of N-PMP-protected glycine derivatives. T...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - November 3, 2018 Category: Drugs & Pharmacology Authors: Inokuma T Tags: Yakugaku Zasshi Source Type: research

[Safety Evaluation of Cellular-type Artificial Blood Based on Pharmacokinetic Analysis and Its Use in Medical Gas Delivery].
Abstract Hemoglobin vesicles (HbVs) in which human hemoglobin is encapsulated in a phospholipid bilayer membrane (liposome) have been developed as artificial red blood cells. Although the effectiveness of HbVs, including their physicochemical characteristics and pharmacological effects, has been reported, data on the pharmacokinetic properties of HbVs are limited. Previously, we developed two kinds of radiolabeled HbV, 125I-HbV and 3H-HbV, in which the internal hemoglobin and lipid membranes were labeled with 125I and 3H, respectively. Using these isotope-labeled HbVs, we clarified the detailed pharmacokinetic pro...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - November 3, 2018 Category: Drugs & Pharmacology Authors: Taguchi K Tags: Yakugaku Zasshi Source Type: research

[Epigenetic Regulation of Pharmacokinetic-related Genes in Human Tissues].
Abstract The translocation of drugs across biological membranes not only occurs via passive diffusion but also by transporter-mediated processes. Knowledge of tissue-specific drug transporter expression, as well as characterization of substrate drugs of individual transporters, leads to a better understanding of the role of these transporters in the pharmacokinetics of drugs. The ATP-binding cassette transporter family member breast cancer resistance protein (BCRP) is one of the most important intestinal efflux transporters involved in the intestinal absorption or permeability of drugs. A genetic variant in the BC...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - November 3, 2018 Category: Drugs & Pharmacology Authors: Hirota T Tags: Yakugaku Zasshi Source Type: research

[A Cost-effectiveness Analysis of Sunitinib vs. Interferon-alpha in Patient with Advanced Renal Cell Carcinoma in Japan].
This study focused on the perspective of public healthcare payer, as only direct medical costs were estimated from the treatment schedule for metastatic renal cell cancer. In the cost-effectiveness analysis, outcomes were valued in terms of life years (LYs) and quality-adjusted life years (QALYs). We calculated the incremental cost-effectiveness ratio (ICER) during the cost-effectiveness analysis. The results were tested using Monte Carlo simulations. Sunitinib and IFN-α treatment resulted in LYs of 2.40 years and 2.03 years, QALYs of 1.58 and 1.25, and expected costs of 13,572,629 yen and 6,083,002 yen, respectively...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - November 3, 2018 Category: Drugs & Pharmacology Authors: Tomura K, Naito Y, Sunaga T, Kurihara T, Usuda M, Nagatani A, Ogawa Y, Akiyama N, Sasaki H, Murata T, Sakamaki H, Kogo M, Sasaki T Tags: Yakugaku Zasshi Source Type: research

[Survey of the Efficacy of Long-term and Successive Pharmaceutical Care in Outpatient Chemotherapy by Oncology Pharmacy Specialists].
In conclusion, long-term and successive pharmaceutical care by oncology pharmacy specialists in outpatient chemotherapy contributes to a safe and less onerous chemotherapy implementation, as it has been highly adopted, is effective in many cases, and has been proven to be important for risk management in chemotherapy. PMID: 30381649 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - November 3, 2018 Category: Drugs & Pharmacology Authors: Saito Y, Harada S, Kobayashi M, Ueda K, Yamazaki K, Kumai M, Miyamoto T, Kasashi K, Yamada T, Komatsu Y, Iseki K Tags: Yakugaku Zasshi Source Type: research

[Influence of Bases for External Medicines with Different Coatability and Water Retentivity on Wound Healing].
In conclusion, these results imply an important role of the bases of external medicines in the treatment of skin diseases. PMID: 30381650 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - November 3, 2018 Category: Drugs & Pharmacology Authors: Yamada Y, Ueda Y, Ashizuka Y, Hashimoto K, Tabara K, Kitano T, Fujikawa M, Kumagai Y, Matsumoto T Tags: Yakugaku Zasshi Source Type: research

[Influence of Storage Conditions after One-dose Packaging on Stability of Magnesium Oxide Tablets].
Abstract The intestinal motor function declines in the elderly. Many patients have constipation and ingest magnesium oxide for a prolonged period. One-dose packaging of drugs is adopted for many elderly patients to help them to avoid forgetting to take an increase in the number of oral drugs to be taken and improve convenience. Several studies on differences in stability among magnesium oxide preparations including generic drugs have been reported, but no study on the influence of the storage conditions after one-dose packaging on the properties of magnesium oxide tablets has been reported. Three types of magnesiu...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - November 3, 2018 Category: Drugs & Pharmacology Authors: Sato K, Inaoka N, Kodama Y, Muro T, Nakamura T, Sasaki H, Kitahara T Tags: Yakugaku Zasshi Source Type: research

[Neurotoxicity Mechanism of Environmental Chemicals and Its Evaluation System].
Abstract  It is pivotal to assess the toxicity and safety of chemicals, including medicines, in the research field of environmental health science. Here we introduce neurotoxic mechanisms in mammals of environmental organotin and Parkinson's disease-related chemicals. We clarified that low concentrations of tributyltin decrease α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)-type glutamate receptor subunit GluA2 (GluR2) expression, leading to the vulnerability of cultured neurons. That is, tributyltin reduces GluA2 prior to neuronal death. This GluA2 decrease can be used as a sensitive evaluati...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - October 4, 2018 Category: Drugs & Pharmacology Authors: Kotake Y Tags: Yakugaku Zasshi Source Type: research

[Behavioral and Molecular Pharmacological Study of the Role of Angiotensin II in Spinal Pain Transmission].
In conclusion, our findings suggest that Ang II may act as a neurotransmitter and/or neuromodulator in spinal pain transmission. This review describes our recent efforts regarding the role of spinal Ang II in spinal pain transmission. PMID: 30270265 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - October 4, 2018 Category: Drugs & Pharmacology Authors: Nemoto W Tags: Yakugaku Zasshi Source Type: research

[Development of an In Vitro System for Evaluating Intestinal Drug Disposition Using Human Induced Pluripotent Stem Cell-Derived Intestinal Epithelial Cells].
Abstract  Tissues of the small intestine are crucial to understanding drug disposition because these tissues regulate the bioavailability of drugs. However, no evaluation system is currently available for precise and comprehensive analysis of intestinal pharmacokinetics. To address this, functional intestinal epithelial cells were generated from human induced pluripotent stem (iPS) cells for use in pharmacokinetic studies. An improved intestinal differentiation method was established by screening a variety of small molecule compounds against cells during differentiation. The mRNA expression levels of intestinal ...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - October 4, 2018 Category: Drugs & Pharmacology Authors: Iwao T Tags: Yakugaku Zasshi Source Type: research

[Host Defense against Bacterial Infection and Bacterial Toxin-induced Impairment of Innate Immunity].
Abstract  Whereas granulopoiesis during Gram-negative bacterial infection is accelerated through activation of toll-like receptor 4 (TLR4), it has not been elucidated whether Gram-positive bacterial infection can stimulate granulopoiesis. Using the well-known TLR2 agonist peptidoglycan (PGN), it was shown that neutrophils in bone marrow and spleen and plasma granulocyte colony-stimulating factor were increased in mice that had received intraperitoneal administration of PGN. Incorporation of bromodeoxyuridine into bone marrow neutrophils increased in mice administered PGN, demonstrating that PGN promotes granulop...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - October 4, 2018 Category: Drugs & Pharmacology Authors: Takehara M Tags: Yakugaku Zasshi Source Type: research

[Lifestyle Inspires Future Pharmacotherapy and Drug Discovery].
PMID: 30270268 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - October 4, 2018 Category: Drugs & Pharmacology Authors: Miyamoto L, Nishida M Tags: Yakugaku Zasshi Source Type: research

[New Strategies for Exercise-Mimetic Medication].
Abstract  Moderate exercise has been reported to combat several diseases, including cardiovascular diseases and depressants. However, many patients do not have ability to undergo exercise therapy due to aging and severity of the symptoms. Therefore development of new drugs that can imitate exercise therapy is desired and actually studied worldwide. The heart is one of the physical load-responsive target organs such as skeletal muscles and vascular smooth muscles. The heart can adapt from environmental stress by changing its structure and morphology (i.e., remodeling). Physiological remodeling, caused by exercise...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - October 4, 2018 Category: Drugs & Pharmacology Authors: Oda S, Numaga-Tomita T, Nishida M Tags: Yakugaku Zasshi Source Type: research

[Noble Heart Failure Therapy Using Food Compositions].
Abstract  Hemodynamic stresses, including hypertension and myocardial infarction, activate neurohumoral factors such as the sympathetic nervous system and the renin-angiotensin system, and can lead to the progression of heart failure. Established pharmacological agents such as angiotensin II receptor blockers (ARBs), angiotensin-converting enzyme (ACE) inhibitors, and β-blockers target extra-cellular molecules and receptors on the cell membrane. These agents have shown some efficacy for the treatment of heart failure, but the long-term survival rate of patients with heart failure remains low. Additional eff...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - October 4, 2018 Category: Drugs & Pharmacology Authors: Morimoto T, Funamoto M, Sunagawa Y, Katanasaka Y, Miyazaki Y, Hasegawa K Tags: Yakugaku Zasshi Source Type: research

[A Cellular Pharmacological Approach to the Development of Drugs to Treat Muscle Wasting].
Abstract  Skeletal muscle atrophy reduces quality of life and increases mortality. However, there are few available drugs for the treatment of muscle atrophy. Recently, cell signaling pathways involved in skeletal muscle atrophy or hypertrophy have been determined. To develop drugs for skeletal muscle atrophy, we have studied compounds which modulate pathways of myogenic differentiation, a pivotal step for the maintenance of skeletal muscle mass. First, we examined a K+ channel opener on myogenic differentiation, since hyperpolarization is a trigger for skeletal muscle differentiation. 5,6-Dichloro-1-ethyl-1,3-d...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - October 4, 2018 Category: Drugs & Pharmacology Authors: Sakamoto K Tags: Yakugaku Zasshi Source Type: research

[Amino Acid Nutrition in the Prevention and Treatment of Sarcopenia].
Abstract  Sarcopenia is the decrease in skeletal muscle mass and muscular function that occurs with aging. The underlying mechanisms of sarcopenia include anabolic resistance, which is defined as a poor muscle protein synthetic response to previously effective stimuli such as nutrients and exercise. Among the nutrients that humans ingest, amino acids directly trigger the synthesis of muscle proteins. The essential amino acid leucine, in particular, functions as a stimulatory signal. Leucine-enriched essential amino acids help overcome anabolic resistance in elderly individuals to effectively stimulate muscle pro...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - October 4, 2018 Category: Drugs & Pharmacology Authors: Kobayashi H Tags: Yakugaku Zasshi Source Type: research

[Do Myokines Have Potential as Exercise Mimetics?]
Abstract  Exercise is generally considered to have health benefits for the body, although its beneficial mechanisms have not been fully elucidated. Recent progressive research suggests that myokines, bioactive substances secreted from skeletal muscle, play an important role in mediating the benefits of exercise. There are three types of myokines in terms of the muscular secretion mechanism: those in which the secretion is promoted by stimulation, such as irisin, interleukin (IL)-6, and IL-15; those whose secretion is constitutive, such as thioredoxin, glutaredoxin, and peroxiredoxin; and those whose secretion is...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - October 4, 2018 Category: Drugs & Pharmacology Authors: Manabe Y Tags: Yakugaku Zasshi Source Type: research

[AMPK as a Metabolic Intersection between Diet and Physical Exercise].
Abstract  Physical exercise is well known to be beneficial to our health. Therapeutic exercise is widely applicable to metabolic disorders, including obesity and diabetes. In addition, recent studies have suggested its potential benefit in the treatment of more various diseases such as mental disorders and cancer. 5'AMP-activated protein kinase (AMPK), which is an intracellular central metabolic sensor as well as a regulator, has been demonstrated to play significant roles in the contracting skeletal muscles, suggesting that AMPK should be one of the key molecules mediating metabolic effects during physical exer...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - October 4, 2018 Category: Drugs & Pharmacology Authors: Miyamoto L Tags: Yakugaku Zasshi Source Type: research

[Modification of Energy Metabolism and Higher Brain Function by Feeding Rhythm].
Abstract  A molecular clock exists within almost all organizations in a living body, and these clocks influence the periodicity of many physiological phenomena such as eating behaviors, the sleep-wake cycle, and hormone secretion. Especially, a living body's energy metabolism is involved with the molecular clocks genetically driven in peripheral tissues, which act in strong relation to eating rhythms. However, the possibility that rhythms may also have an inverse influence has recently been pointed out. In this manuscript, we review the outline of circadian rhythms, then refer to the possibility that a clock gen...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - October 4, 2018 Category: Drugs & Pharmacology Authors: Otsuka A, Shiuchi T Tags: Yakugaku Zasshi Source Type: research

[Questionnaire Survey for Pharmacists to Identify Factors Associated with Confusion Errors Involving Similar-appearing Press-through Package (Blister Pack)].
Abstract  Similar-appearing press-through package (PTP) sheets (also known as blister packs) that contain different medicines may result in incorrect medication due to confusion errors. To evaluate the significance of this problem and to identify the factors that may lead to such errors, we conducted a questionnaire survey for pharmacists. Three hundred and eighty-two pairs of PTP sheets with similar appearance were included in the questionnaire. Factors related to color (sheet color at the front of the sheet 90.9%, color of tablet/capsule 57.1%, print color at the front of the sheet 45.9%) were most frequently ...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - October 4, 2018 Category: Drugs & Pharmacology Authors: Tamaki H, Satoh H, Hori S, Sawada Y Tags: Yakugaku Zasshi Source Type: research

[Assessing the Effects of Prescription Adjustment and Medication Non-adherence Associated with Medication Efficacy Classifications from Leftover Drugs through the SETSUYAKU-BAG Campaign].
Abstract  The increase in medical expenditure has been worsening and poses a serious social problem. Commonly, leftover drugs are retained by patients. We estimated the possible reduction in prescription rates by appropriately reusing leftover drugs, and investigated the medication efficacy classifications that render leftover drugs due to the medication non-adherence. A retrospective cross-sectional survey of prescription data was performed at community pharmacies engaged in the appropriate reuse of leftover drugs through the SETSUYAKU-BAG campaign. We evaluated the drug costs and number of drugs originally pre...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - October 4, 2018 Category: Drugs & Pharmacology Authors: Kobayashi D, Koyanagi K, Kubota T, Sakamoto Y, Kihara T, Miisho T, Kasaki T, Kunitake M, Takeshita F, Ando E, Baba T, Seo T, Tanaka T, Shimazoe T Tags: Yakugaku Zasshi Source Type: research

[The Beneficial Effects of Switching from Dipeptidyl Peptidase-4 Inhibitors to Dulaglutide on Plasma Glucose and Hemoglobin A1c Levels: A Case Report of Four Patients with Type 2 Diabetes].
Abstract  Incretin-based therapy consists of dipeptidyl peptidase-4 (DPP-4) inhibitors and glucagon-like peptide-1 (GLP-1) receptor agonists. Whether switching from DPP-4 inhibitors to one of the GLP-1 receptor agonists, dulaglutide, has greater beneficial effects remains unknown. Therefore, this study aimed to investigate the effectiveness of switching from DPP-4 inhibitors to dulaglutide in four patients with type 2 diabetes. All four patients with hyperglycemia who switched from DPP-4 inhibitors to dulaglutide demonstrated noticeable decreased plasma glucose levels on the next day after switching. Two of the ...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - October 4, 2018 Category: Drugs & Pharmacology Authors: Shimoda K, Hoshino T, Morisaki T, Shiotsu K, Mizuno Y Tags: Yakugaku Zasshi Source Type: research

[Applications of Raman Spectroscopy on Quality Control of Hospital Formulations].
Abstract   Hospital formulation has several advantages, including the flexibility of customization as per the disease state or the patients' precise requirements. However, compared with commercial formulations, hospital formulations are usually not under the same level of quality check. In the present study, we tested mixed powder formulations prepared in a hospital pharmacy using Raman spectroscopy to investigate the feasibility of applying Raman spectroscopy as a quality-control tool of hospital formulations. For this purpose, we first established a numerical evaluation method to determine the uniformi...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - September 12, 2018 Category: Drugs & Pharmacology Authors: Moriyama K, Yakushige A, Yamamoto M, Ogura Y, Fukushima S, Kamei T, Akagi S, Tokuda H, Takayanagi K, Takami Y Tags: Yakugaku Zasshi Source Type: research

[Contribution to the Development of Pharmaceutical Education in Six-year and Four-year Programs].
Abstract  I joined efforts to promote the pharmaceutical education system by participating in committees for developing a model core curriculum for pharmaceutical sciences (core curriculum), in pharmacist educator workshops, in the development of a pharmaceutical common achievement test, evaluation of pharmaceutical education programs, and the creation of a national examination for pharmacists. This review outlines the efforts to reform these pharmaceutical education systems. The core curriculum was prepared under the initiative of the Pharmaceutical Society of Japan. Pharmacist educator workshops were frequentl...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - September 5, 2018 Category: Drugs & Pharmacology Authors: Akaike A Tags: Yakugaku Zasshi Source Type: research

[Development of Protein Knockdown Technology as Emerging Drug Discovery Strategy].
Abstract  Protein knockdown technologies based on small molecules are attracting considerable attention in the pharmaceutical industry as a strategy for novel drug discovery. We and others have developed such compounds, designated as Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Erasers (SNIPERs), proteolysis-targeting chimeras (PROTACs), and Degronimids, which induce selective degradation of target proteins. These compounds contain two different ligands, specific for an ubiquitin E3 ligase and for a target protein, respectively, connected by a linker. SNIPERs, PROTACs, and Degro...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - September 5, 2018 Category: Drugs & Pharmacology Authors: Ohoka N Tags: Yakugaku Zasshi Source Type: research

[Use of Pharmacogenetic Information for Therapeutic Drug Monitoring of an Antiarrhythmic Drug].
Abstract  Antiarrhythmic drugs require therapeutic drug monitoring (TDM) to avoid adverse effects such as proarrhythmia. However, TDM is not necessarily used to adjust the dosage of antiarrhythmic drugs because there is a lack of information regarding the therapeutic range of the serum concentration and the selection of patients who require TDM. The aim of this review was to provide an overview of the pharmacogenetic information on the pharmacokinetics and drug response of flecainide, a class Ic antiarrhythmic drug with a sodium channel-blocking effect. A population pharmacokinetic analysis revealed that the CYP...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - September 5, 2018 Category: Drugs & Pharmacology Authors: Doki K Tags: Yakugaku Zasshi Source Type: research

[Development of Novel Preparations for Nitrogen Heterocycles Based on Cascade Reactions].
Abstract  Nitrogen heterocycles are important skeletons in biologically active compounds such as medicines and natural alkaloids. However, in terms of the efficiency of the synthetic process, the many synthetic steps required to achieve the target compounds with complex architectures pose a significant problem. To overcome this challenge, novel approaches were developed to afford biologically active heterocycles, 1,2-diazepines, pyrroloisoquinolines, and pyrrolizidines utilizing cascade reactions that enable multiple bond formation in a one-pot process. This review discusses three one-pot reactions: 1) 1,2-diaze...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - September 5, 2018 Category: Drugs & Pharmacology Authors: Sugimoto K Tags: Yakugaku Zasshi Source Type: research

[Design of Spray-dried Porous Particles for Sugar-based Dry Powder Inhaler Formulation].
Abstract  For efficient and deeper drug delivery into the lungs via dry powder inhalers (DPIs), we designed porous spray-dried particles (SDPs) containing anti-tuberculosis drugs and sugar-based excipients. The SDPs were prepared by spray-drying ethanol solutions containing isoniazid and/or rifampicin and sucrose, maltose, or highly branched cyclic dextrin (HBCD). Solid-state fluorescence emission spectroscopy showed that 1-naphthoic acid (1-NPA), a model drug, was dispersed in a molecular dispersion/solid solution, suggesting high potential of HBCD as an excipient in DPIs. 1-NPA was dispersed not only as active...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - September 5, 2018 Category: Drugs & Pharmacology Authors: Kadota K Tags: Yakugaku Zasshi Source Type: research

[Pharmaceutical Properties of Rikkunshito Extract Suppository and Bioequivalence by Pharmacokinetic Parameters and Effectiveness against Nausea and Vomiting and Anorexia in Rats].
In this study, RK suppository was prepared by using RK formulation (A, B, and C) and Witepsol (H and S) (AH, BH, CH, AS, BS, and CS). Pharmaceutical properties, namely, hardness, dispersibility, long-term stability, and drug (hesperidin and glycyrrhizic acid) release were measured for AH, BH, AH, and AS. The pharmacokinetic parameters, effectiveness of substance P against NV and anorexia, and serotonin-activated ghrelin levels were assessed for BH only. AH, BH, AS, and AS demonstrated uniform and sufficient hardness. The release rate of oleaginous components, such as glycyrrhizic acid, did not change significantly, while t...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - September 5, 2018 Category: Drugs & Pharmacology Authors: Murata I, Nishiyama T, Kawasaki H, Naito C, Kamata T, Furukawa Y, Iwata M, Sugino M, Inoue Y, Kanamoto I Tags: Yakugaku Zasshi Source Type: research

[Possibility of Poor Outcomes after Treatment Using Teicoplanin at the Minimum Inhibitory Concentration of > 2 μg/mL in Methicillin-resistant Staphylococcus aureus Bacteremia].
[Possibility of Poor Outcomes after Treatment Using Teicoplanin at the Minimum Inhibitory Concentration of>2 μg/mL in Methicillin-resistant Staphylococcus aureus Bacteremia]. Yakugaku Zasshi. 2018;138(9):1181-1189 Authors: Kagami K, Imai S, Tazawa Y, Iwasaki S, Fukumoto T, Akizawa K, Yamada T, Ishiguro N, Iseki K Abstract  Only minimal information exists regarding the treatment outcomes of patients suffering from methicillin-resistant Staphylococcus aureus (MRSA) bacteremia treated with teicoplanin (TEIC) when the TEIC minimum inhibitory concentration (MIC) is close to the upper limit of the &...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - September 5, 2018 Category: Drugs & Pharmacology Authors: Kagami K, Imai S, Tazawa Y, Iwasaki S, Fukumoto T, Akizawa K, Yamada T, Ishiguro N, Iseki K Tags: Yakugaku Zasshi Source Type: research

[Characterization of Surface Interaction between Chitosan-modified Liposomes and Mucin Layer by Using CNT Probe AFM Method].
Abstract  In order to characterize the adhesion and deformation behavior between chitosan-modified liposomes and the mucin layer of the small intestine, mucin was coated on hydrophobic surface-modified carbon nanotube (CNT) probe of an atomic force microscope. The interaction between this mucin layer and the liposomes with or without chitosan modification in phosphoric acid buffer solution was determined by atomic force microscopy. The pH of the buffer solution was controlled at 2.8 and 7.0. The chitosan modification increased the attractive force between the liposomes and mucin layer during the separation proce...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - September 5, 2018 Category: Drugs & Pharmacology Authors: Yamamoto M, Tsuchiya T, Iijima M, Takeuchi H, Kamiya H Tags: Yakugaku Zasshi Source Type: research

[Outcomes of Pharmacists' Involvement with Residents of Special Nursing Homes for the Elderly].
Abstract  The current study aimed to examine the outcomes of pharmacists' involvement with elderly people in special nursing homes. We analyzed 58 cases involving regular visits by community pharmacists to 41 residents. The residents' mean age was 87.8±6.9 years, and 68.3% were prescribed 6 or more types of medication. Antipsychotic and insomnia medication was taken by 24.4% and 31.8% of residents, respectively. Pharmaceutical consultation following medication use accounted for 60.3% of pharmacists' involvement with residents. The outcomes of these consultations included improvements in prescription conte...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - September 5, 2018 Category: Drugs & Pharmacology Authors: Hashimoto R, Fujii K, Yoshida K, Shimoji S, Masaki H, Kadoyama K, Nakamura T, Onda M Tags: Yakugaku Zasshi Source Type: research

[Comparison of Adhesive Properties of Transdermal Patches Distributing in Japan - Tack and Peel Strength].
In this study, measurements of the adhesive properties of 38 transdermal patches of ten different APIs were performed using several unified testing methods (180˚ peel test, 90˚ peel test, self-adhesion test, and probe tack test) under unified experimental conditions. The adhesive properties were found to be quite different among the patches, even for the same API, dose, and size. For example, the ratios of the maximum to minimum measured values of tack and 180˚ peel strength for tulobuterol patches were 5 and 29, respectively. In the case of generic products for which the bioequivalence to a brand-name product is assure...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - August 24, 2018 Category: Drugs & Pharmacology Authors: Miyazaki T, Kanno H, Aso Y, Goda Y Tags: Yakugaku Zasshi Source Type: research

[Taste and Health: Current Status of Nutrient Sensor Research].
PMID: 30068838 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - August 8, 2018 Category: Drugs & Pharmacology Authors: Uneyama H, Takeuchi K Tags: Yakugaku Zasshi Source Type: research

[Gastrointestinal Spice Sensors and Their Functions].
Abstract  Capsaicin is a constituent of chili pepper, and induces the burning sensation on the tongue. The site of action for capsaicin has been discovered as transient receptor potential vanilloid receptor subtype 1 (TRPV1) that resides on the membranes of pain- and heat-sensing primary afferent nerves. The immunohistochemical study on the stomach revealed that nerve fibers expressing TRPV1 exist along gastric glands in the mucosa, around blood vessels in the submucosa, in the myenteric plexus, and in the smooth muscle layers. High numbers of TRPV1-immunoreactive axons were observed in the rectum and distal ...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - August 8, 2018 Category: Drugs & Pharmacology Authors: Horie S, Tashima K, Matsumoto K Tags: Yakugaku Zasshi Source Type: research

[Clarification of the Mechanism Involved in Orexigenic Action by Oral Zinc Ingestion].
This study showed the first evidence that gastrointestinal zinc signal is indispensable for the food appetite induction in the experimentally anorexigenic rat. However, since it has not yet been clarified the mechanism involved in zinc sensing by the epithelial membrane of the gastrointestinal tract, further detailed investigations are necessary. PMID: 30068840 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - August 8, 2018 Category: Drugs & Pharmacology Authors: Komai M, Goto T, Ohinata K, Kambe T, Mayanagi Y, Shirakawa H Tags: Yakugaku Zasshi Source Type: research

[Nutrient Sensing and Anorexia via Neuropeptides].
Abstract  Various neuropeptides play an essential role in the nutrient sensing mechanism and related homeostasis. Nesfatin-1 is a newly identified neuropeptide having anorectic activity, and nesfatin-1-containing neurons are widely distributed in the brain, including the hypothalamus and brain stem. Our previous study showed that dehydration-induced anorectic effects are mediated via the central nesfatin-1 pathway in rats. Our recent studies have also shown that peripheral anorectic peptides (cholecystokinin-8, glucagon-like peptide-1, and leptin) and an antineoplastic agent (cisplatin) caused inhibition of f...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - August 8, 2018 Category: Drugs & Pharmacology Authors: Ueta Y Tags: Yakugaku Zasshi Source Type: research

[Young Innovators Driving the Next Generation of Academic Drug Discovery].
PMID: 30068842 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - August 8, 2018 Category: Drugs & Pharmacology Authors: Matsumaru T, Yasuda D Tags: Yakugaku Zasshi Source Type: research

[Green Pharma: A New Strategy for Drug Discovery in Academia by Targeting Glial Cells and ATP Receptors].
Abstract  Neuropathic pain associated with cancer, diabetic neuropathy, and postherpetic neuralgia is a type of intractable chronic pain characterized by mechanical allodynia and abnormal pain hypersensitivity evoked by innocuous stimuli. However, this disorder has no specific treatment. We previously showed that the purinergic receptor P2X4 (P2X4R), a subtype of ATP-gated nonselective cation channels, is highly upregulated in spinal microglia after peripheral nerve injury, and blocking the function of P2X4R reverses mechanical allodynia. In the present study, we screened a chemical library of 1979 clinically...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - August 8, 2018 Category: Drugs & Pharmacology Authors: Yamashita T, Tsuda M, Tozaki-Saitoh H, Inoue K Tags: Yakugaku Zasshi Source Type: research

[Biophysical Analysis of the Protein-Small Molecule Interactions to Develop Small Molecule Drug Discovery].
Abstract  In small molecule drug discovery, researchers must find specific binders that interact with a target protein and inhibit its function in connection with human diseases. It is of critical importance to know the binding mode of compounds interacting with a target protein to assure hit validation and optimization. Biophysical analysis is a powerful quantitative approach to evaluate the binding modes of such candidates. Since the level of sensitivity of biophysical analysis is suitable to quantitatively detect the binding of fragment compounds, and because of the remarkable success of compound libraries...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - August 8, 2018 Category: Drugs & Pharmacology Authors: Nagatoishi S, Caaveiro JMM, Tsumoto K Tags: Yakugaku Zasshi Source Type: research

[Exploration of Insect Growth Regulators Targeting Noppera-bo, an Enzyme Involved in Ecdysteroid Biosynthesis].
Abstract  Insect growth regulators (IGRs) are chemicals that adversely affect the physiological processes associated with insect development and cause abnormalities that impair insect survival. Ecdysone, an insect steroid hormone originally identified as a molting hormone, plays an essential role in developmental transition, such as during molting and metamorphosis. Recently, a member of the epsilon class of glutathione S-transferases (GST), GSTe14, also called Noppera-bo (Nobo), has been identified as essential for regulating the biosynthesis of ecdysone. Knockout or knockdown of the nobo gene causes ecdyson...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - August 8, 2018 Category: Drugs & Pharmacology Authors: Fujikawa Y, Inoue H Tags: Yakugaku Zasshi Source Type: research

[Molecular Conjugation for the "Diazido Probe" Method].
[Molecular Conjugation for the "Diazido Probe" Method]. Yakugaku Zasshi. 2018;138(8):1049-1058 Authors: Yoshida S Abstract  Target identification of screening hit compounds with unknown mechanisms of action obtained from chemical libraries by phenotypic assays has played an important role in the development of innovative drugs that work based on novel mechanisms. To improve the usability of the target identification based on the photoaffinity labeling method, we have studied the "diazido probe" method, wherein a photoreactive aromatic azido and relatively photostable aliphatic...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - August 8, 2018 Category: Drugs & Pharmacology Authors: Yoshida S Tags: Yakugaku Zasshi Source Type: research

[Hit-to-Lead in Academia: Discovery of a Protein-Protein Interaction Inhibitor of Keap1-Nrf2].
Abstract  In the process of recent hit-to-lead studies, not only in industry but also in academia, early evaluation of metabolic properties has been one of the key aspects supporting a higher probability of success in drug discovery. In this review, we introduce the development of chemical seeds targeting the Kelch-like ECH-associated protein-1 (Keap1) as an example of an academic hit-to-lead study considering metabolic stability. Keap1 regulates the function of nuclear factor erythroid 2-related factor 2 (Nrf2), which induces various antioxidative or detoxification proteins. An inhibitor of protein-protein i...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - August 8, 2018 Category: Drugs & Pharmacology Authors: Yasuda D, Obata R, Takahashi K, Ohe T, Mashino T Tags: Yakugaku Zasshi Source Type: research

[Biogenesis, the Function of Peroxisomes, and Their Role in Genetic Disease: With a Focus on the ABC Transporter].
Abstract  Peroxisomes are organelles that are present in almost all eukaryotic cells. These organelles were first described in 1954, in the cytoplasm of the proximal tubule cells in the mouse kidney, using electron microscopy by Rhodin and referred to as "microbodies". Then, de Duve and Baudhuin isolated microbodies from rat liver using density gradient centrifugation, defined the microbodies as membrane-bound organelles containing several H2O2-producing oxidases and H2O2-degrading catalase, and named them peroxisomes. At present, the biogenesis of peroxisomes in mammals involves three different pro...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - August 8, 2018 Category: Drugs & Pharmacology Authors: Imanaka T Tags: Yakugaku Zasshi Source Type: research

[Questionnaire Survey to Pharmacists after a Workshop on the Chemical Structural Formula of Drugs].
Abstract  Recently, it has been reported that only a small number of sixth-year students who had undergone a long-term pre-clinical training in the fifth year found organic chemistry useful. To explain this, we hypothesized that pharmacists are unable to utilize the knowledge of organic chemistry to solve clinical problems. With the aim of addressing this problem, we conducted a workshop consisting of a series of lectures and exercises on structural similarity, solubility, absorption, and metabolism of drugs based on a chemical structural formula. Then, we administered a questionnaire survey to 253 participan...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - August 8, 2018 Category: Drugs & Pharmacology Authors: Shimizu T, Nishimura K, Ueda M Tags: Yakugaku Zasshi Source Type: research

[Effects of Serum Sodium Concentrations on Nausea and Vomiting after Moderately Emetogenic Chemotherapy].
Abstract  Chemotherapy-induced nausea and vomiting (CINV) is the most unbearable adverse effect of chemotherapy. The antiemesis guidelines of the National Comprehensive Cancer Network indicate that hyponatremia is a risk factor for CINV, although the relationship between the incidence of CINV and hyponatremia has not been sufficiently studied. This two-center prospective observational study evaluated whether low serum sodium concentrations were a risk factor for CINV. The study included 34 patients who were scheduled to receive first-line carboplatin- or oxaliplatin-based chemotherapy for gynecological or col...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - August 8, 2018 Category: Drugs & Pharmacology Authors: Hatakeyama S, Suzuki N, Abe K, Konno N, Kaneko T, Toyoguchi T, Shiraishi T Tags: Yakugaku Zasshi Source Type: research

[Study of Child-resistant Packaging Technologies to Prevent Children from Accidental Ingestion of Drugs in Japan].
In this study, we investigated pediatric characteristics such as literacy ability and finger function in Japanese subjects and examined the usefulness of child-resistant (CR) packaging technologies used in the U.S. when given to children in Japan. The survey covered 104 Japanese children aged 37-84 months. The results of the survey revealed that of the five types of CR packaging technologies, that which leveraged the differences in hand size and muscle mass between children and adults was effective against children aged 3-6 years. However, the CR packaging styles that rely on literacy, the ability to use tools, and the abi...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - August 8, 2018 Category: Drugs & Pharmacology Authors: Mizoguchi M, Miura G, Ojima F Tags: Yakugaku Zasshi Source Type: research

[Design of Microdialysis-CLC Method for Measurement of Drug Behavior in Lacrimal Fluid after Instillation].
In conclusion, we showed that the microdialysis-CLC method was suitable to measure the drug behavior in lacrimal fluid after instillation. These findings provide significant information that can be used in the design and evaluation of ophthalmic formulation. PMID: 30068852 [PubMed - in process] (Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan)
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - August 8, 2018 Category: Drugs & Pharmacology Authors: Nagai N, Ueno A, Ishii M, Fukuoka Y, Otake H Tags: Yakugaku Zasshi Source Type: research

[ αCGRP Transgenic Mice Display Typical Physiologic Features].
[αCGRP Transgenic Mice Display Typical Physiologic Features]. Yakugaku Zasshi. 2018;138(8):1119-1126 Authors: Mishima S, Otsuka A, Matsuuchi S, Hashikawa N, Inoue K, Hashikawa N Abstract  Calcitonin gene-related peptide (CGRP) plays an important role in several physiological processes such as vasodilation, cardiovascular homeostasis and transmission of pain. Here we report the generation of a transgenic mouse overexpressing αCGRP and the impact of this on baseline physiological responses. αCGRP transgenic mice displayed significantly increased αCGRP mRNA levels in the kidn...
Source: Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan - August 8, 2018 Category: Drugs & Pharmacology Authors: Mishima S, Otsuka A, Matsuuchi S, Hashikawa N, Inoue K, Hashikawa N Tags: Yakugaku Zasshi Source Type: research