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https://www.readbyqxmd.com/read/29643323/effects-of-linagliptin-versus-voglibose-on-treatment-related-quality-of-life-in-patients-with-type-2-diabetes-sub-analysis-of-the-l-step-study
#1
Hiromasa Goto, Tomoya Mita, Yoshio Fujitani, Shimpei Fujimoto, Kiyohito Takahashi, Hiroaki Satoh, Takahisa Hirose, Toru Hiyoshi, Masumi Ai, Yosuke Okada, Hideki Nishimura, Hisamoto Kuroda, Toshiki Matsubara, Masahiko Gosho, Hitoshi Ishii, Hirotaka Watada
Treatment-related quality of life (QOL) is an important aspect of diabetes management. However, no studies have compared the influence of dipeptidyl peptidase-4 inhibitors versus alpha-glucosidase inhibitors on treatment-related QOL. This prespecified sub-analysis of the Linagliptin Study of Effects on Postprandial blood glucose (L-STEP) compared the effects of linagliptin (5 mg once daily) and voglibose (0.2 mg/meal thrice daily) on treatment-related QOL in Japanese patients with type 2 diabetes (T2DM) inadequately controlled with diet and exercise therapy...
April 10, 2018: Endocrine Journal
https://www.readbyqxmd.com/read/29518717/synthesis-molecular-modeling-and-evaluation-of-%C3%AE-glucosidase-inhibition-activity-of-3-4-dihydroxy-piperidines
#2
Siva Prasad Kasturi, Sujatha Surarapu, Srinivas Uppalanchi, Shubham Dwivedi, Perumal Yogeeswari, Dilep Kumar Sigalapalli, Nagendra Babu Bathini, Krishna S Ethiraj, Jaya Shree Anireddy
Biological evaluation of 3,4-dihydroxy piperidines as α-glucosidase inhibitors is being reported for the first time. Forty-five derivatives (amides, di-amides and sulfonamides) were made using cis and trans 3,4-dihydroxy piperidines to evaluate their α-glucosidase inhibition activity. Polar groups (-OH, -NH2 ) on phenyl ring having derivatives 5i, 5l, 7g, 7i &12j showed excellent activity compared to standard references. Acarbose, Voglibose and Miglitol were used as standard references. Molecular docking simulations were done for compounds to identify important binding modes responsible for inhibition activity of α-glucosidase...
February 26, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29503428/-effect-of-food-thickeners-on-the-disintegration-dissolution-and-drug-activity-of-rapid-oral-disintegrating-tablets
#3
REVIEW
Takashi Tomita, Yukinao Kohda, Kenzo Kudo
 For patients with dysphagia in medical facilities and nursing homes, food thickeners are routinely used to aid the ingestion of medicines such as tablets. However, some types of thickeners affect the disintegration and dissolution of tablets, such as rapidly-disintegrating magnesium oxide tablets and donepezil hydrochloride orally disintegrating tablets. Additionally, delayed disintegration and dissolution of tablets affect a drug's efficacy. As an example, with Voglibose orally disintegrating tablets, marked differences are observed in changes in glucose levels during glucose tolerance testing...
2018: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
https://www.readbyqxmd.com/read/29501171/preparation-of-carbon-functionalized-magnetic-graphene-mesoporous-silica-composites-for-selective-extraction-of-miglitol-and-voglibose-in-rat-plasma
#4
Xiaodan Liu, Jianan Feng, Yan Li
In this work, magnetic graphene/mesoporous silica composites with carbon-functionalized pore-walls (denoted as MG@mSiO2 -C composites) were synthesized and applied as restricted access matrix solid phase extraction (RAM-SPE) adsorbents for the determination of miglitol and voglibose in rat plasma by LC-MS/MS. The MG@mSiO2 -C composites were synthesized by using the template (Cetyltrimethyl Ammonium Bromide, CTAB) as carbon source with sulfuric acid pretreated. The obtained nano-composites were proven to have many unique properties such as large specific surface area of 277...
May 15, 2018: Talanta
https://www.readbyqxmd.com/read/29495953/voglibose-mediated-alterations-in-neurometabolomic-profiles-in-the-hypothalamus-of-high-fat-diet-fed-mice
#5
Soo Jin Yang, Hyun Ju Do, Youngae Jung, Geum-Sook Hwang, Min-Jeong Shin
The alpha-glucosidase inhibitor voglibose (VO) was recently reported to have a protective effect against weight gain as well as affect various metabolic changes related to food intake and gut-brain signaling. We hypothesized that VO prevents weight gain by altering neurometabolome profiles in the hypothalamus to reduce food intake. To test this hypothesis, we assessed metabolite profiles in the hypothalamus of standard diet- or high-fat (HF) diet-fed mice in the absence or presence of VO. In total, 29 male C57BL/6 mice were divided into 3 groups: (1) lean control, (2) HF, and (3) HF + VO...
March 1, 2018: Nutritional Neuroscience
https://www.readbyqxmd.com/read/29493100/glucose-excursions-and-hypoglycemia-in-patients-with-type-2-diabetes-treated-with-mitiglinide-voglibose-versus-glimepiride-a-randomized-cross-over-trial
#6
Kanta Fujimoto, Yui Shibayama, Eriko Yamaguchi, Sachiko Honjo, Akihiro Hamasaki, Yoshiyuki Hamamoto
BACKGROUND: Glucose excursions and hypoglycemia are associated with cardiovascular complications. However, no studies have evaluated glucose excursions and the frequency of hypoglycemia in patients treated with mitiglinide/voglibose versus glimepiride as add-on to dipeptidyl peptidase-4 inhibitor therapy. METHODS: This cross-over trial included 20 patients with type 2 diabetes. After initiating vildagliptin 100 mg, patients were randomly assigned to receive mitiglinide/voglibose 10 mg/0...
March 1, 2018: Journal of Diabetes
https://www.readbyqxmd.com/read/29427024/comparison-of-the-effects-of-linagliptin-and-voglibose-on-endothelial-function-in-patients-with-type-2-diabetes-and-coronary-artery-disease-a-prospective-randomized-pilot-study-effort
#7
Taku Koyama, Atsushi Tanaka, Hisako Yoshida, Jun-Ichi Oyama, Shigeru Toyoda, Masashi Sakuma, Teruo Inoue, Yoritaka Otsuka, Koichi Node
Endothelial dysfunction contributes to poor cardiovascular prognosis in patients with type 2 diabetes mellitus (T2DM) and coronary artery disease (CAD). The effect of dipeptidyl peptidase-4 inhibitors on endothelial function remains controversial. We sought to compare the effects of linagliptin and voglibose on endothelial function, as assessed by reactive hyperemia-peripheral arterial tonometry (RH-PAT). Sixteen patients with newly diagnosed T2DM and CAD were randomized 1:1 to linagliptin (5 mg, once-daily) or voglibose (0...
February 9, 2018: Heart and Vessels
https://www.readbyqxmd.com/read/29367471/effects-of-linagliptin-monotherapy-compared-with-voglibose-on-postprandial-lipid-profiles-in-japanese-patients-with-type-2-diabetes-linagliptin-study-of-effects-on-postprandial-blood-glucose-l-step-sub-study-1
#8
Akira Kurozumi, Yosuke Okada, Hiroaki Satoh, Ikuo Inoue, Hiroko Chimori, Etsuko Akita, Toshihiko Shiraiwa, Yoshio Fujitani, Tomoya Mita, Masahiko Gosho, Hirotaka Watada
Recently, we reported that linagliptin had equivalent efficacy to voglibose in reducing postprandial blood glucose levels in drug-naïve patients with type 2 diabetes (L-STEP Study). As a sub-study of the L-STEP Study we examined the effect of linagliptin on postprandial lipids profile. Between October 2012 and April 2014, the study enrolled patients with type 2 diabetes mellitus who had inadequate glycemic control. Patients were randomly assigned to either the linagliptin group (5 mg once daily, n = 85) or the voglibose group (0...
January 25, 2018: Endocrine Journal
https://www.readbyqxmd.com/read/29189010/diastereoselective-synthesis-of-salacinol-type-%C3%AE-glucosidase-inhibitors
#9
Fumihiro Ishikawa, Kazumi Jinno, Eri Kinouchi, Kiyofumi Ninomiya, Shinsuke Marumoto, Weijia Xie, Osamu Muraoka, Toshio Morikawa, Genzoh Tanabe
A facile and highly diastereoselective approach toward the synthesis of potent salacinol-type α-glucosidase inhibitors, originally isolated from plants of the genus "Salacia", was developed using the S-alkylation of thiosugars with epoxides in HFIP (∼90%, dr, α/β = ∼ 26/1). The dr ratio of the product was significantly improved by the protocol as compared to that of the conventional S-alkylation of thiosugars (dr, α/β = ∼ 8/1). The protocol could be used for gram scale synthesis of the desired compounds...
January 5, 2018: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/29151501/the-efficacy-of-corticosteroid-therapy-in-a-patient-with-nonalcoholic-steatohepatitis-overlapping-autoimmune-hepatitis-a-case-report
#10
Takuya Komura, Hajime Ohta, Takuya Seike, Yoshiaki Shimizu, Ryotaro Nakai, Hitoshi Omura, Takashi Kagaya, Satomi Kasashima, Atsuhiro Kawashima, Sakae Oba, Kennichi Harada, Shuichi Kaneko, Masashi Unoura
The overlap of multiple liver diseases can cause the disease activity and severity to worsen rapidly in some cases. We rarely see patients with non-alcoholic steatohepatitis (NASH) with overlapping autoimmune hepatitis (AIH). A 64-year-old woman who had been prescribed oral drugs to treat diabetes and hypertension (metformin 500 mg/day and voglibose 0.9 mg/day, and termisartan 40 mg/day and amlodipine 5 mg/day, respectively) was diagnosed with NASH with histological confirmation. At 68 years of age, her liver injury worsened with an IgG of 2,871 mg/dL and a high serum anti-nuclear antibody (ANA) level of 2,560...
November 20, 2017: Internal Medicine
https://www.readbyqxmd.com/read/29123848/a-case-of-type-2-diabetes-mellitus-with-metformin-associated-lactic-acidosis-initially-presenting-the-appearance-of-a-sulfonylurea-related-hypoglycemic-attack
#11
Kota Nishihama, Kanako Maki, Yuko Okano, Rei Hashimoto, Yasuhiro Hotta, Mei Uemura, Taro Yasuma, Toshinari Suzuki, Toyomi Hayashi, Eiji Ishikawa, Yutaka Yano, Esteban C Gabazza, Masaaki Ito, Yoshiyuki Takei
Case: A 64-year-old Japanese woman with diabetes mellitus was admitted for hypoglycemia. Her diabetes had been under good control with glimepiride, voglibose, exenatide, and metformin for a few years. Although overt proteinuria was observed, the serum creatinine values were within normal range during the routine outpatient follow-up. Hypoglycemic attack caused by glimepiride and loss of appetite by urinary tract infection were diagnosed. Then, metformin-associated lactic acidosis with acute renal failure caused by dehydration was detected...
January 2017: Acute Medicine & Surgery
https://www.readbyqxmd.com/read/29080007/rapid-analysis-of-pharmaceutical-drugs-using-libs-coupled-with-multivariate-analysis
#12
P K Tiwari, S Awasthi, R Kumar, R K Anand, P K Rai, A K Rai
Type 2 diabetes drug tablets containing voglibose having dose strengths of 0.2 and 0.3 mg of various brands have been examined, using laser-induced breakdown spectroscopy (LIBS) technique. The statistical methods such as the principal component analysis (PCA) and the partial least square regression analysis (PLSR) have been employed on LIBS spectral data for classifying and developing the calibration models of drug samples. We have developed the ratio-based calibration model applying PLSR in which relative spectral intensity ratios H/C, H/N and O/N are used...
October 27, 2017: Lasers in Medical Science
https://www.readbyqxmd.com/read/29058089/evidence-based-treatment-of-neurogenic-orthostatic-hypotension-and-related-symptoms
#13
REVIEW
Sabine Eschlböck, Gregor Wenning, Alessandra Fanciulli
Neurogenic orthostatic hypotension, postprandial hypotension and exercise-induced hypotension are common features of cardiovascular autonomic failure. Despite the serious impact on patient's quality of life, evidence-based guidelines for non-pharmacological and pharmacological management are lacking at present. Here, we provide a systematic review of the literature on therapeutic options for neurogenic orthostatic hypotension and related symptoms with evidence-based recommendations according to the Grading of Recommendations Assessment, Development and Evaluation (GRADE)...
December 2017: Journal of Neural Transmission
https://www.readbyqxmd.com/read/28978579/nocturnal-reactive-hypoglycaemia-well-treated-subjectively-and-objectively-with-voglibose
#14
Hiroyuki Koyama, Hideomi Ohguchi, Takashi Yagi, Kenro Imaeda
Clinicians sometimes encounter difficulty in diagnosing hypoglycaemia. Here, we present a case report of a 53-year-old woman with recurrent nocturnal hypoglycaemia. A continuous glucose monitoring system (CGMS) revealed postprandial hyperglycaemia and subsequent hypoglycaemia, and an oral glucose tolerance test showed an impaired glycaemic and delayed hyperinsulinaemic pattern. On the basis of these clinical findings, we diagnosed her unexplained hypoglycaemia as reactive hypoglycaemia. CGMS showed a sharp contrast of diurnal variation in blood glucose levels including hypoglycaemia between before and after treatment with an alpha-glucosidase inhibitor, voglibose...
October 4, 2017: BMJ Case Reports
https://www.readbyqxmd.com/read/28931726/impaired-insulin-igf-1-is-responsible-for-diabetic-gastroparesis-by-damaging-myenteric-cholinergic-neurones-and-interstitial-cells-of-cajal
#15
Shu Yang, Bo Wu, Haimei Sun, Tingyi Sun, Kai Han, Dandan Li, Fengqing Ji, Guoquan Zhang, Deshan Zhou
Diabetic gastroparesis is a common complication of diabetes mellitus (DM) that is characterized by decreased serum insulin and insulin-like growth factor-1 (IGF-1). Despite the fact that insulin treatment not glycemic control potently accelerated gastric emptying in type 1 DM patients, the role of insulin/InsR and IGF-1/IGF-1R signaling in diabetic gastroparesis remains incompletely elucidated. In the present study, type 1 DM mice were established and treated with insulin or Voglibose for 8 weeks. The gastric emptying was delayed from DM week 4 when the gastric InsR and IGF-1R were declined...
October 31, 2017: Bioscience Reports
https://www.readbyqxmd.com/read/28792171/glycemic-pentad
#16
Glycemic Pentad Forum
BACKGROUND: Conventionally, diabetes management involved targeting the triad of FPG, PPG, and HbA1c. However, several studies have suggested the quintessential need for a paradigm shift to incorporate glycemic variability and quality of life in the holistic diabetes control regimen. AIM: To generate a consensus and ratify the position of Glycemic Variability (GV) and Quality of Life (QOL), along with the traditional triad, in diabetes management in India. To evaluate whether the triple fixed dose combination of metformin, glimepiride, and voglibose can accomplish the goals of glycemic pentad...
July 2017: Journal of the Association of Physicians of India
https://www.readbyqxmd.com/read/28743290/pneumatosis-intestinalis-with-a-benign-clinical-course-a-report-of-two-cases
#17
Aya Takase, Nobuhiro Akuzawa, Hiroshi Naitoh, Jun Aoki
BACKGROUND: Pneumatosis intestinalis (PI) is a rare condition characterized by the presence of gas within the gastrointestinal tract wall. Most cases of PI have a benign clinical course, although some have serious outcomes. Mechanical stress on or bacterial infection of the gastrointestinal tract wall may be responsible for the onset of PI, but the detailed mechanism of PI pathogenesis is still unclear. Here, we describe two Japanese patients presenting with benign PI. CASE PRESENTATION: Case 1, a 37-year-old previously healthy male patient, had a 1-week history of abdominal pain, and case 2, a 78-year-old female diabetic patient, had a 2-week history of voglibose treatment and abdominal pain...
July 25, 2017: BMC Research Notes
https://www.readbyqxmd.com/read/28672278/hydrazinyl-arylthiazole-based-pyridine-scaffolds-synthesis-structural-characterization-in%C3%A2-vitro-%C3%AE-glucosidase-inhibitory-activity-and-in-silico-studies
#18
Farman Ali, Khalid Mohammed Khan, Uzma Salar, Muhammad Taha, Nor Hadiani Ismail, Abdul Wadood, Muhammad Riaz, Shahnaz Perveen
Acarbose, miglitol, and voglibose are the inhibitors of α-glucosidase enzyme and being clinically used for the management of type-II diabetes mellitus. However, many adverse effects are also associated with them. So, the development of new therapeutic agents is an utmost interest in medicinal chemistry research. Current study is based on the identification of new α-glucosidase inhibitors. For that purpose, hydrazinyl arylthiazole based pyridine derivatives 1-39 were synthesized via two step reaction and fully characterized by spectroscopic techniques EI-MS, HREI-MS, (1)H-, and (13)C NMR...
September 29, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28584404/the-%C3%AE-glucosidase-inhibitor-voglibose-stimulates-delayed-gastric-emptying-in-healthy-subjects-a-crossover-study-with-a-13-c-breath-test
#19
Kenji Kanoshima, Mizue Matsuura, Megumi Kaai, Yumi Inoh, Kanji Ohkuma, Hiroshi Iida, Takashi Nonaka, Koji Fujita, Tomonori Ida, Akihiko Kusakabe, Atsushi Nakajima, Masahiko Inamori
The gastrointestinal effects of α-glucosidase inhibitors have not been sufficiently investigated. The aim of this study was to determine whether a single dose of pre-prandial voglibose might affect the rate of gastric emptying, determined using the (13)C breath test. Ten healthy male volunteers participated in this randomized, two-way crossover study. The subjects fasted overnight and received 0.2 mg voglibose or a placebo 2 h before a test meal. They were then served a liquid test meal consisting of 200 kcal per 200 ml that contained 100 mg (13)C-acetate...
May 2017: Journal of Clinical Biochemistry and Nutrition
https://www.readbyqxmd.com/read/28495082/synthesis-and-%C3%AE-glucosidase-inhibition-activity-of-dihydroxy-pyrrolidines
#20
Sivaprasad Kasturi, Sujatha Surarapu, Srinivas Uppalanchi, Jaya Shree Anireddy, Shubham Dwivedi, Hasitha Shilpa Anantaraju, Yogeeswari Perumal, Dilep Kumar Sigalapalli, Bathini Nagendra Babu, Krishna S Ethiraj
A new series of Deacetylsarmentamide A and B derivatives, amides and sulfonamides of 3,4-dihydroxypyrrolidines as α-glucosidase inhibitors were designed and synthesized. The biological screening test against α-glucosidase showed that some of these compounds have the positive inhibitory activity against α-glucosidase. Saturated aliphatic amides were more potent than the olefinic amides. Among all the compounds, 5o/6o having polar -NH2 group, 10f/11f having polar -OH group on phenyl ring displayed 3-4-fold more potent than the standard drugs...
June 15, 2017: Bioorganic & Medicinal Chemistry Letters
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