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https://www.readbyqxmd.com/read/27921260/development-of-oral-flexible-tablet-oft-formulation-for-pediatric-and-geriatric-patients-a-novel-age-appropriate-formulation-platform
#1
Prabagaran Chandrasekaran, Ruckmani Kandasamy
Development of palatable formulations for pediatric and geriatric patients involves various challenges. However, an innovative development with beneficial characteristics of marketed formulations in a single formulation platform was attempted. The goal of this research was to develop solid oral flexible tablets (OFTs) as a platform for pediatrics and geriatrics as oral delivery is the most convenient and widely used mode of drug administration. For this purpose, a flexible tablet formulation using cetirizine hydrochloride as model stability labile class 1 and 3 drug as per the Biopharmaceutical Classification System was developed...
December 5, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27921140/cocaine-administration-dose-dependently-increases-sexual-desire-and-decreases-condom-use-likelihood-the-role-of-delay-and-probability-discounting-in-connecting-cocaine-with-hiv
#2
Matthew W Johnson, Evan S Herrmann, Mary M Sweeney, Robert S LeComte, Patrick S Johnson
OBJECTIVES: Although cocaine use has been linked to sexual HIV risk behavior for decades, the direct effects of cocaine on sexual desire and sexual decision-making are unexamined. Research suggests delay discounting (devaluation of future outcomes) and probability discounting (devaluation of uncertain outcomes) play roles in condom use decisions. This study examined the effect of cocaine administration on sexual desire, hypothetical condom use, and discounting tasks. METHODS: This double-blind, within-subjects study compared the effects of 0, 125, and 250 mg/70 kg oral cocaine HCl in 12 cocaine users...
December 5, 2016: Psychopharmacology
https://www.readbyqxmd.com/read/27920831/assessment-of-drug-induced-proarrhythmias-due-to-pilsicainide-in-patients-with-atrial-tachyarrhythmias
#3
Hideki Koike, Tadashi Fujino, Makiko Koike, Shintaro Yao, Masaya Shinohara, Ken Kitahara, Toshio Kinoshita, Hitomi Yuzawa, Takeya Suzuki, Hideyuki Sato, Shunji Fukunaga, Kenzaburo Kobayashi, Takanori Ikeda
BACKGROUND: Pilsicainide, a pure Na(+) channel blocker, is a popular antiarrhythmic drug for the management of atrial tachyarrhythmias (AT), in Japan. However, serious drug-induced proarrhythmias (DIPs) may unexpectedly occur. We assessed the clinical background of AT patients presenting with DIPs caused by pilsicainide. METHODS: This study retrospectively enrolled 874 consecutive patients (543 men, 63.6±15.3 years old, and 57.9±16.5 kg of body weight), who were orally administered pilsicainide for AT management...
December 2016: Journal of Arrhythmia
https://www.readbyqxmd.com/read/27920809/rates-and-reasons-for-lack-of-persistence-with-anti-osteoporotic-drugs-analysis-of-the-campania-region-database
#4
Giovanni Iolascon, Francesca Gimigliano, Antimo Moretti, Ilaria Riccio, Massimo Di Gennaro, Maddalena Illario, Valeria Marina Monetti, Valentina Orlando, Enrica Menditto
Subjects with chronic diseases are more likely to be nonpersistent to pharmacological treatment. Lack of persistence is common among subjects using oral anti-osteoporotic drugs, and leads to increased risk of fragility fracture. The aim of our retrospective study is to analyze the rates and reasons for discontinuation of anti-osteoporotic drugs in the Campania Region. Subjects aged over 40 years were included if they had received at least one prescription for any anti-osteoporotic drugs. Data were obtained from an administrative database of regional data on outpatient drug prescriptions reimbursed by the National Health Service...
May 2016: Clinical Cases in Mineral and Bone Metabolism
https://www.readbyqxmd.com/read/27920684/worsening-of-lymphopenia-during-apremilast-treatment
#5
Antonios G A Kolios, Lars E French, Alexander A Navarini
Apremilast is an oral phosphodiesterase IV inhibitor recently registered for the treatment of psoriasis and psoriatic arthritis in Switzerland and other countries. Even though it offers only moderate efficacy compared to biologics, many patients prefer drugs given by the oral route. Apremilast is frequently used in private practice, as it showed no relevant safety signals in clinical trials and often, laboratory tests are omitted completely. Here we report a patient who developed acute lymphopenia and worsening of psoriasis during apremilast treatment, which resolved with discontinuation of apremilast...
September 2016: Case Reports in Dermatology
https://www.readbyqxmd.com/read/27920504/gender-and-age-related-treatment-compliance-in-patients-with-osteoporosis-in-germany
#6
Peyman Hadji, Louis Jacob, Karel Kostev
AIM: The purpose of this study was to analyze treatment compliance in osteoporotic patients treated with osteoporosis medications in Germany. METHODS: Patients included in the analysis had been diagnosed with osteoporosis with or without fractures and started anti-osteoporotic therapy (bisphosphonates, denosumab, or strontium ranelate) between 2011 and 2014 in a general (GP) or orthopedic practice (OP) setting in Germany. Data pertaining to 6,221 individuals followed in GP and 4,044 individuals followed in OP were analyzed retrospectively...
2016: Patient Preference and Adherence
https://www.readbyqxmd.com/read/27920499/smart-nanocrystals-of-artemether-fabrication-characterization-and-comparative-in-vitro-and-in-vivo-antimalarial-evaluation
#7
Syed Muhammad Hassan Shah, Farhat Ullah, Shahzeb Khan, Syed Muhammad Mukarram Shah, Marcel de Matas, Zahid Hussain, Muhammad Usman Minhas, Naser M AbdEl-Salam, Khaled Hafez Assi, Mohammad Isreb
Artemether (ARTM) is a very effective antimalarial drug with poor solubility and consequently low bioavailability. Smart nanocrystals of ARTM with particle size of 161±1.5 nm and polydispersity index of 0.172±0.01 were produced in <1 hour using a wet milling technology, Dena(®) DM-100. The crystallinity of the processed ARTM was confirmed using differential scanning calorimetry and powder X-ray diffraction. The saturation solubility of the ARTM nanocrystals was substantially increased to 900 µg/mL compared to the raw ARTM in water (145...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27920397/optimizing-combination-therapy-for-acute-lymphoblastic-leukemia-using-a-phenotypic-personalized-medicine-digital-health-platform-retrospective-optimization-individualizes-patient-regimens-to-maximize-efficacy-and-safety
#8
Dong-Keun Lee, Vivian Y Chang, Theodore Kee, Chih-Ming Ho, Dean Ho
Acute lymphoblastic leukemia (ALL) is a blood cancer that is characterized by the overproduction of lymphoblasts in the bone marrow. Treatment for pediatric ALL typically uses combination chemotherapy in phases, including a prolonged maintenance phase with oral methotrexate and 6-mercaptopurine, which often requires dose adjustment to balance side effects and efficacy. However, a major challenge confronting combination therapy for virtually every disease indication is the inability to pinpoint drug doses that are optimized for each patient, and the ability to adaptively and continuously optimize these doses to address comorbidities and other patient-specific physiological changes...
December 5, 2016: Journal of Laboratory Automation
https://www.readbyqxmd.com/read/27920312/dental-care-and-medicare-beneficiaries-access-gaps-cost-burdens-and-policy-options
#9
Amber Willink, Cathy Schoen, Karen Davis
Despite the wealth of evidence that oral health is related to physical health, Medicare explicitly excludes dental care from coverage, leaving beneficiaries at risk for tooth decay and periodontal disease and exposed to high out-of-pocket spending. To profile these risks, we examined access to dental care across income groups and types of insurance coverage in 2012. High-income beneficiaries were almost three times as likely to have received dental care in the previous twelve months, compared to low-income beneficiaries-74 percent of whom received no dental care...
December 1, 2016: Health Affairs
https://www.readbyqxmd.com/read/27919975/long-term-high-quality-survival-with-single-agent-mifepristone-treatment-despite-advanced-cancer
#10
Jerome H Check, Diane Check, Carrie Wilson, Patrice Lofberg
CASE REPORT: We show long-term high-quality survival following single-agent treatment with a progesterone receptor antagonist in two cases of advanced metastatic cancer. Because no biopsy was performed (patient refused) the exact type of lung cancer was not determined but the majority of oncologists who evaluated the patient thought that the rapid onset and syndrome of inappropriate anti-diuretic hormone was more consistent with small-cell lung cancer. The US Food and Drug Association granted a compassionate-use investigational new drug approval for use of single-agent 200 mg mifepristone orally/day to a moribund woman with never-treated metastatic lung cancer and a male with bilateral renal cell carcinoma who had undergone only a unilateral hemi-nephrectomy...
December 2016: Anticancer Research
https://www.readbyqxmd.com/read/27919957/simultaneous-administration-of-statins-and-pioglitazone-limits-tumor-growth-in-a-rat-model-of-malignant-glioma
#11
Jorge Humberto Tapia-Pérez, Robert Preininger, Elmar Kirches, Annegret Reinhold, Jana Butzmann, Sylvia Prilloff, Christian Mawrin, Thomas Schneider
BACKGROUND/AIM: Statins are cholesterol reducers with considerable dose-dependent effect against glioma cells. The apoptotic effect could be increased by combining statins or by adding pioglitazone (PGZ). The last one is an anti-diabetic drug, an agonist of the peroxisome proliferator-activated receptor-gamma (PPARG). We used an animal model to test the effect of such combination in vivo and we investigated the changes on immunological processes. MATERIALS AND METHODS: Thirty-three rats (F344/DuCrl) were anesthetized and glioblastoma (F98) cells were implanted stereotactically...
December 2016: Anticancer Research
https://www.readbyqxmd.com/read/27919699/identification-of-different-shapes-colors-and-sizes-of-standard-oral-dosage-forms-in-diabetes-type-2-patients-a-pilot-study
#12
Sven Stegemann, Regina Riedl, Harald Sourij
The clear identification of drug products by the patients is essential for a safe and effective medication management. In order to understand the impact of shape, size and color on medication identification a study was performed in subjects with type 2 diabetes mellitus (T2D). Ten model drugs differentiated by shape, size and color were evaluated using a mixed method of medication schedule preparation by the participants followed by a semi-structured interview. Detection times were fastest for the large round tablet shape and the bi-chromatic forms...
December 2, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27919660/a-comparison-of-vasodilation-mode-among-selexipag-ns-304-2-4-5-6-diphenylpyrazin-2-yl-isopropyl-amino-butoxy-n-methylsulfonyl-acetamide-its-active-metabolite-mre-269-and-various-prostacyclin-receptor-agonists-in-rat-porcine-and-human-pulmonary-arteries
#13
Chiaki Fuchikami, Kohji Murakami, Koyuki Tajima, Junko Homan, Keiji Kosugi, Kazuya Kuramoto, Michiko Oka, Keiichi Kuwano
Selexipag (NS-304; [2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}-N- (methylsulfonyl)acetamide]) is a novel, orally available non-prostanoid prostacyclin receptor (IP receptor) agonist that has recently been approved for the treatment of pulmonary arterial hypertension (PAH). We examined the effect of the active metabolite of selexipag, MRE-269, and IP receptor agonists that are currently available as PAH therapeutic drugs on the relaxation of rat, porcine and human pulmonary artery. cAMP formation in human pulmonary artery smooth muscle cells was induced by all test compounds (MRE-269, epoprostenol, iloprost, treprostinil and beraprost sodium) and suppressed by IP receptor antagonists (CAY10441 and 2-[4-(1H-indol-4-yloxymethyl)-benzyloxycarbonylamino]-3-phenyl-propionic acid)...
December 2, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27919497/comparative-efficacy-and-discontinuation-of-dimethyl-fumarate-and-fingolimod-in-clinical-practice-at-12-month-follow-up
#14
Carrie M Hersh, Thomas E Love, Samuel Cohn, Claire Hara-Cleaver, Robert A Bermel, Robert J Fox, Jeffrey A Cohen, Daniel Ontaneda
BACKGROUND: Dimethyl fumarate (DMF) and fingolimod (FTY) are approved oral disease modifying therapies (DMT) for relapsing multiple sclerosis (MS). Phase 3 trials established these agents as effective and generally well tolerated, though comparative efficacy and discontinuation remain unknown. OBJECTIVE: To assess real-world efficacy and discontinuation of DMF and FTY over 12 months in patients with MS. METHODS: We identified 458 DMF-treated and 317 FTY-treated patients in a large academic MS center...
November 2016: Multiple Sclerosis and related Disorders
https://www.readbyqxmd.com/read/27919469/dangerous-intoxication-after-oral-ingestion-of-poppers-alkyl-nitrites-two-case-reports
#15
Stéphanie Pain, François Chavant, Bernard Fauconneau, Jérémy Guenezan, Nicolas Marjanovic, Jean-Yves Lardeur, Bertrand Brunet, Marie-Christine Perault-Pochat
"Poppers" (alkyl nitrites) were made famous in the 1960s as a party drug and are still used today. They are highly volatile, sweet-smelling liquids commonly administered by inhalation. However, sometimes, they can be consumed by oral ingestion resulting in greater toxicity. They are used for their vasodilator effects but these volatile nitrites can also cause methemoglobinemia. Methemoglobinemia is a rare pathology that results from the oxidation of iron in the hemoglobin molecule. Oxidation of iron switches it from the ferrous to the ferric state and impedes the ability of hemoglobin to carry oxygen...
December 2, 2016: Thérapie
https://www.readbyqxmd.com/read/27919294/heantos-4-a-natural-plant-extract-used-in-the-treatment-of-drug-addiction-modulates-t-type-calcium-channels-and-thalamocortical-burst-firing
#16
Stuart M Cain, Soyon Ahn, Esperanza Garcia, Yiming Zhang, Zeina Waheed, John R Tyson, Yi Yang, Tran Van Sung, Anthony G Phillips, Terrance P Snutch
Heantos-4 is a refined combination of plant extracts currently approved to treat opiate addiction in Vietnam. In addition to its beneficial effects on withdrawal and prevention of relapse, reports of sedation during clinical treatment suggest that arousal networks in the brain may be recruited during Heantos administration. T-type calcium channels are implicated in the generation of sleep rhythms and in this study we examined whether a Heantos-4 extraction modulates T-type calcium channel currents generated by the Cav3...
December 5, 2016: Molecular Brain
https://www.readbyqxmd.com/read/27919212/investigating-drug-repositioning-approach-to-design-novel-prodrugs-for-colon-specific-release-of-fexofenadine-for-ulcerative-colitis
#17
Suneela S Dhaneshwar, Priyanka Singh
BACKGROUND: Recent immunologic data implicates involvement of mucosal immune cells of the intestine like eosinophils and mast cells to be functionally involved in the pathogenesis of UC. Mast cell activation is followed by increased secretion and elevated tissue concentration of histamine. Inhibition of mucosal histamine release in colon may be an effective therapeutic approach to treat UC. Some studies report that intestinal inflammation associated with acute and chronic colitis has been ameliorated by fexofenadine in mice...
December 5, 2016: Current Drug Delivery
https://www.readbyqxmd.com/read/27919207/safety-and-effectiveness-of-24-week-treatment-with-iguratimod-a-new-oral-disease-modifying-antirheumatic-drug-for-patients-with-rheumatoid-arthritis-interim-analysis-of-a-postmarketing-surveillance-study-of-2679-patients-in-japan
#18
Tsuneyo Mimori, Masayoshi Harigai, Tatsuya Atsumi, Takao Fujii, Masataka Kuwana, Hiroaki Matsuno, Shigeki Momohara, Syuji Takei, Naoto Tamura, Yoshinari Takasaki, Satoshi Ikeuchi, Satoru Kushimoto, Takao Koike
OBJECTIVE: To determine the real-world safety and effectiveness of iguratimod (IGU) for rheumatoid arthritis (RA), a 52-week, Japanese, postmarketing surveillance study was conducted. An interim analysis at week 24 was performed. METHODS: This study included all RA patients who received IGU following its introduction to the market. All adverse events (AEs) and adverse drug reactions (ADRs) were collected. Effectiveness was evaluated by the change in Disease Activity Score 28-C-reactive protein (DAS28-CRP) from baseline to week 24...
December 6, 2016: Modern Rheumatology
https://www.readbyqxmd.com/read/27919190/investigation-of-the-influence-of-glycyrrhizin-on-the-pharmacokinetics-of-celastrol-in-rats-using-lc-ms-and-its-potential-mechanism
#19
Guangkui Yan, Hanhua Zhang, Wei Wang, Yuan Li, Chenghuang Mao, Mingqiao Fang, Xianhong Yi, Jingdong Zhang
1. The aim of this study was to investigate the effects of glycyrrhizin on the pharmacokinetics of celastrol in rats. 2. Twelve male Sprague-Dawley rats were randomly assigned to two groups: control group and test group. Test group was pretreated with glycyrrhizin at a dose of 100 mg/kg/day for 10 days, and then the two groups were orally administered with celastrol at a dose of 1 mg/kg. The concentration of celastrol was determined using a sensitive and reliable LC-MS method. 3. The results showed that glycyrrhizin could significantly decrease the plasma concentration (from 64...
December 5, 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/27918966/development-of-novel-cilostazol-loaded-solid-snedds-using-a-spg-membrane-emulsification-technique-physicochemical-characterization-and-in-vivo-evaluation
#20
Omer Mustapha, Kyung Soo Kim, Shumaila Shafique, Dong Shik Kim, Sung Giu Jin, Youn Gee Seo, Yu Seok Youn, Kyung Taek Oh, Beom-Jin Lee, Young Joon Park, Chul Soon Yong, Jong Oh Kim, Han-Gon Choi
The objective of this study was to develop a novel solid self-nanoemulsifying drug delivery system (SNEDDS) using a membrane emulsification technique involving Shirasu porous glass (SPG) which produced very small and uniform emulsion droplets, resulting in enhanced solubility, dissolution and oral bioavailability of poorly water-soluble cilostazol. The effects of carriers on the drug solubility were assessed, and pseudo-ternary phase diagrams were plotted. Among the liquid SNEDDS formulations tested, the liquid SNEDDS composed of peceol (oil), Tween 20 (surfactant) and Labrasol (cosurfactant) at a weight ratio of 15/55/30, produced the smallest emulsion droplet size...
November 29, 2016: Colloids and Surfaces. B, Biointerfaces
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