Volume 41,
Issue 12,
2013
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扉・目次
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Source:
薬理と治療 41巻12号, 1079-1080 (2013);
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DRUG PROFILE SERIES
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Source:
薬理と治療 41巻12号, 1083-1102 (2013);
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REVIEW
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Source:
薬理と治療 41巻12号, 1109-1119 (2013);
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Na+/glucose co-transporter 2(SGLT-2)inhibitors represent a new strategy in the treatment of diabetes. These drugs inhibit glucose reabsorption from renal tubules, thereby promoting urinary glucose excretion and decreasing plasma glucose levels. Furthermore, the effect to induce glycosuria is dependent on the plasma glucose level, which may be associated with a low risk of hypoglycemia. This unique mechanism of action is independent of pancreatic β-cell function. Thus, they have the potential to be used as combination therapy with other oralanti-diabetic drugs. Animal studies and clinical trials have revealed that, by causing glycosuria, SGLT-2 inhibitors not only reduce plasma glucose levels, but also cause weight losses, and improve insulin resistance or insulin secreting capacity. SGLT-2 inhibitors may benefit the diabetic state by decreasing glucotoxicity and visceral fat accumulation. To understand the characteristics of SGLT-2 inhibitors, this article reviews the role of kidney or SGLTs in glucose homeostasis, and benefit and risk of these drugs based on previous reports.
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ORIGINAL ARTICLES
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Source:
薬理と治療 41巻12号, 1121-1127 (2013);
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Objectives The objective is to investigate pig ear skin as a alternative for human skin in the prediction of drug concentration profiles in order to optimize the developmental formulation. Methods In vitro tape-stripping were conducted on pig ear skin. Three approved test(generic)lipophilic drugs and their corresponding reference drugs were applied to the skin for 4 hr. These drug profiles across the stratum corneum(SC)were determined to compare the drug concentrations of test to that of reference. In order to determine the drug concentration profile, Lulicon cream 1% was applied to the skin for 4, 12, and 24 hr. The formulation of Luliconazole 1% ointment was optimized with the determined drug concentration profile of the cream and assessed cutaneous bioequivalence to the cream by human dermatopharmacokinetics(DPK)study. Results The in vitro test:reference ratios for drug concentration in SC 4 hr after application of commercially available topical formulations were close to one. Whether the dosage forms were same or different, these drug concentrations and test:reference ratios were inagreement with reported human DPK data. Evaluated drug concentration profile of Lulicon cream 1% showed that the average concentration of Luliconazole in the pig ear SC reached to steady state at 4 hr after application. We developed Luliconazole 1% ointment optimized by the drug concentration profile of the cream. As a result of human DPK study, bioequivalence of the two Luliconazole formulation was confirmed. Conclutions Thease data suggested that pig ear skin DPK model has promise as a tool for topical formulation evaluation and optimization to predict the drug concentration profile in human SC. Especially among lipophilic drugs as like Luliconazole.
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Source:
薬理と治療 41巻12号, 1129-1137 (2013);
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Objectives The purpose of the study was to determine whether its regular intake of the reduced form of CoQ10 was useful in managing workers’stress. Methods Nineteen nurses working at a university hospital received soft capsule containing100 mg of the reduced form of CoQ10 for 4 weeks. Based on test food intake during the study, the subjects were divided into two groups:a“good intake group”composed of those who took the test food every day, and“poor intake group”composed of the remaining subjects. The basic attributes, lifestyle, working conditions, job stress level, and work engagement of the groups were analyzed. Job stress level and work engagement were investigated using Brief Job Stress Questionnaire(BJSQ)and Utrecht Work Engagement Scale Japan(UWES-J), and levels of cortisol, VMA and 8-0HdG, respectively. Intragroup and intergroup comparison of the variables was performed. Results In the good intake group, a significant increase in“job satisfaction”in the BJSQ(P=0.009), a significant decrease in“physical complaint”(P=0.024), and a significant increase in the UWES-J score(P=0.017)were observed, although poor intake group showed no significant difference at either time point. No adverse events or clinically significant changes in the physical examination and blood test were observed in either group. Conclusion The results suggest that regular intake of the reduced form of CoQ10 may reduce physical symptoms due to job stress and thereby enhance work engagement, indicating usefulness for stress management for workers.