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Oral liquid drug

Clizia Guccione, Maria Camilla Bergonzi, Khaled M Awada, Vieri Piazzini, Anna Rita Bilia
The aim of this study was the development and characterization of lipid nanocarriers using food grade components for oral delivery of Serenoa repens CO2 extract, namely microemulsions (MEs) and self-microemulsifying drug delivery systems (SMEDDSs) to improve the oral absorption. A commercial blend (CB) containing 320 of S. repens CO2 extract plus the aqueous soluble extracts of nettle root and pineapple stem was formulated in two MEs and two SMEDDSs. The optimized ME loaded with the CB (CBM2) had a very low content of water (only 17...
March 15, 2018: Planta Medica
Evelina Cardoso, Thomas Mercier, Anna Dorothea Wagner, Krisztian Homicsko, Olivier Michielin, Kim Ellefsen-Lavoie, Laurène Cagnon, Manuel Diezi, Thierry Buclin, Nicolas Widmer, Chantal Csajka, Laurent Decosterd
A sensitive and selective method of high performance liquid chromatography (HPLC) coupled to tandem mass spectrometry (MS/MS) has been developed for the simultaneous quantification of six anticancer protein kinase inhibitors (PKIs), dabrafenib, trametinib, vemurafenib, cobimetinib, pazopanib, regorafenib, and two active metabolites (regorafenib-M2 and regorafenib-M5) in human plasma. Plasma protein precipitation with methanol enables the sample extraction of 100 μL aliquot of plasma. Analytes are detected by electrospray triple-stage quadrupole mass spectrometry and quantified using the calibration curves with stable isotope-labeled internal standards...
February 8, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Kelly R Hume, Skylar R Sylvester, Lucia Borlle, Cheryl E Balkman, Angela L McCleary-Wheeler, Mary Pulvino, Carla Casulo, Jiyong Zhao
Doxycycline has antiproliferative effects in human lymphoma cells and in murine xenografts. We hypothesized that doxycycline would decrease canine lymphoma cell viability and prospectively evaluated its clinical tolerability in client-owned dogs with spontaneous, nodal, multicentric, substage a, B-cell lymphoma, not previously treated with chemotherapy. Treatment duration ranged from 1 to 8 weeks (median and mean, 3 weeks). Dogs were treated with either 10 ( n  = 6) or 7.5 ( n  = 7) mg/kg by mouth twice daily...
2018: Frontiers in Veterinary Science
Sanyog Jain, Pooja Yadav, Rajan Swami, Nitin Kumar Swarnakar, Varun Kushwah, Sameer S Katiyar
Implication of different dietary specific lipids such as phytantriol (PT) and glyceryl monooleate (GMO) on enhancing the oral bioavailability of amphotericin B (AmB) was examined. Liquid crystalline nanoparticles (LCNPs) were prepared using hydrotrope method, followed by in vitro characterization, Caco-2 cell monolayer uptake, and in vivo pharmacokinetic and toxicity evaluation. Optimized AmB-LCNPs displayed small particle size (< 210 nm) with a narrow distribution (~ 0.2), sustained drug release and high gastrointestinal stability, and reduced hemolytic toxicity...
March 12, 2018: AAPS PharmSciTech
Jasna Neumann, Olof Beck, Norbert Dahmen, Michael Böttcher
BACKGROUND: Oral fluid (OF) is being developed as a specimen for the determination of drug intake as an alternative to serum and plasma. It is generally considered as an attractive specimen due to the noninvasive nature of the sampling procedure and the relation to the free fraction of drug in the blood. These features are of particular value in drug treatment of psychiatric disorders. To establish OF for the purpose of monitoring drug therapy, the relationship between concentrations in OF and serum/plasma must be documented...
April 2018: Therapeutic Drug Monitoring
Huu H Huynh, Clara Roessle, Hélène Sauvageon, Alain Plé, Isabelle Madelaine, Catherine Thieblemont, Samia Mourah, Lauriane Goldwirt
BACKGROUND: Idelalisib is the first orally active selective phosphatidylinositol 3-kinase delta inhibitor approved by Food and Drug Administration and European Medicines Agency in 2014 for the treatment of several types of blood cancer. Idelalisib is widely used as a monotherapy or in combination with rituximab, bendamustine, or ofatumumab with a significant efficacy. However, idelalisib has shown increased risk of infection and a higher frequency of serious adverse events. It may be useful to determine idelalisib concentration in human plasma to adjust dose and to manage adverse effects in clinical practice...
April 2018: Therapeutic Drug Monitoring
Quoc-Ky Truong, Xuan-Lan Mai, Jae-Yong Lee, Jongsook Rhee, Dinh Vinh, Jongki Hong, Kyeong Ho Kim
A simple, sensitive, and rapid assay based on hydrophilic interaction liquid chromatography (HILIC) with tandem mass spectrometry was developed and validated for the simultaneous determination of metformin and 13 other oral antihyperglycaemic drugs in human urine using metoprolol as an internal standard. A simple sample clean-up procedure using the "dilute and shoot" approach enabled fast and reliable analysis. Chromatographic separation was performed on a HILIC column using an elution gradient of mobile phase A, composed of 1 mM ammonium formate (pH 5), and mobile phase B, composed of acetonitrile, at a flow rate of 0...
March 9, 2018: Archives of Pharmacal Research
Sufeng Zhou, Mingxue Tao, Yuanyuan Wang, Lu Wang, Lijun Xie, Juan Chen, Yuqing Zhao, Yun Liu, Hongwen Zhang, Ning Ou, Guangji Wang, Feng Shao, Jiye Aa
1. The aim of this analysis was to explore the influence of CYP3A4*1G and CYP3A5*3 polymorphisms on the pharmacokinetics of tylerdipine in healthy Chinese subjects. 2. A total of 64 and 63 healthy Chinese subjects were included and identified as the genotypes of CYP3A4*1G and CYP3A5*3, respectively. Plasma samples were collected for up to 24 h post-dose to characterize the pharmacokinetic profile following single oral dose of the drug (5, 15, 20, 25, 30 mg). Plasma levels were measured by a high-performance liquid chromatography-mass spectrometry (LC-MS/MS)...
March 9, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Hisanao Izumi, Yasuharu Shinoda, Takashi Saito, Takaomi Saido, Keita Sato, Yasushi Yabuki, Yotaro Matsumoto, Yoshitomi Kanemitsu, Yoshihisa Tomioka, Nona Abolhassani, Yusaku Nakabeppu, Kohji Fukunaga
Alzheimer's disease (AD) is a progressive neurodegenerative disease and the most common form of elderly dementia in the world. At present, acetylcholine inhibitors, such as donepezil, galantamine and rivastigmine, are used for AD therapy, but the therapeutic efficacy is limited. We recently proposed T-type voltage gated Ca2+ channels (T-VGCCs) enhancer as a new therapeutic candidate for AD. In the current study, we confirmed the pharmacokinetics of SAK3 in the plasma and brain of mice using ultra performance liquid chromatography-tandem mass spectrometry...
March 3, 2018: Neuroscience
Machiko Watanabe, Chisato Yamada, Yoshinori Komagata, Hirotoshi Kikuchi, Hiroyuki Hosono, Fumio Itagaki
Background: Patients with Sjögren's syndrome (SS) typically present clinically with xerostomia (dry mouth) because of progressive damage to the exocrine glands. We developed a new, low-dose pilocarpine/sodium alginate (LPA) solution with pilocarpine hydrochloride to inhibit systemic adverse effects by administering via the oral mucosa. The purpose of this study was to assess its stability, safety, and efficacy. Methods: The pilocarpine concentration in an LPA liquid formulation was measured 3, 7, 14, and 28 days after preparation to assess its stability...
2018: Journal of Pharmaceutical Health Care and Sciences
C Rehn, E Odouard, F Poncet, P Cochat, V Breant, X Dode
BACKGROUND AND GOAL OF THIS STUDY: Few available galenic formulations of drugs have pediatric doses, so that many of them are used off label in children. The influence of such pharmaceutical formulation on therapeutic adherence was evaluated in a systematic review of the literature. MATERIALS AND METHODS: This search was performed in 4 data bases: Medline, the Cochrane Library, Web of Science and Science Direct. Included articles were in French or English and focused on therapeutic adherence and route of administration...
March 1, 2018: Annales Pharmaceutiques Françaises
Athena K Petrides, Stacy E F Melanson, Michalis Kantartjis, Rachel D Le, Christiana A Demetriou, James G Flood
BACKGROUND: Oral fluid (OF) has become an increasingly popular matrix to assess compliance in pain management and addiction settings as it reduces the likelihood of adulteration. However, drug concentrations and windows of detection are not as well studied in OF as in urine (UR). We compared the clinical utility and analytical performance of OF and UR as matrices for detecting common benzodiazepines and opioids. METHODS: OF and UR concentrations of 5 benzodiazepines and 7 opioids were measured by liquid chromatography-tandem mass spectrometry (LC-MS/MS) in 263 paired OF and UR specimens...
February 27, 2018: Clinica Chimica Acta; International Journal of Clinical Chemistry
Yu Chen, Lin Chen, Hong Zhang, Shibo Huang, Yuqing Xiong, Chunhua Xia
Sulfonylureas (SUs) such as glibenclamide, gliclazide, glimepiride, glipizide and gliquidone are one of the first oral medicines available for the treatment of type 2 diabetes, and are widely used for the treatment of hyperglycaemia. The hepatic transporters, organic anion transporting polypeptide 1B1 (OATP1B1) and organic anion transporting polypeptide 1B3 (OATP1B3), play an important role in the disposition of a variety of drugs by mediating their uptake from blood into hepatocytes. Drug-drug interactions mediated by OATP1B1/1B3 may result in the hepatic transporting change for drug substrates...
March 2, 2018: Basic & Clinical Pharmacology & Toxicology
Yu Kyong Kim, Kwang-Hee Shin, Jeffrey Alderman, Kyung-Sang Yu, In-Jin Jang, SeungHwan Lee
Background: Migraine is one of the most common headache disorders that greatly affect the quality of life. Selective serotonin (5-HT) receptor agonists such as triptamine-based drugs called triptans are used for treatment of migraine. Purpose: This study aimed to evaluate the pharmacokinetic (PK) and tolerability profiles of eletriptan hydrobromide (eletriptan HBr), a selective 5-hydroxytryptamine (also known as serotonin) 1B/1D receptor agonist, in Koreans and compare the results to those observed in non-Koreans in a previously published study...
2018: Drug Design, Development and Therapy
Bozena Kociszewska-Najman, Natalia Mazanowska, Bronislawa Pietrzak, Leszek Paczek, Monika Szpotanska-Sikorska, Joanna Schreiber-Zamora, Ewa Hryniewiecka, Dorota Zochowska, Emilia Samborowska, Michal Dadlez, Miroslaw Wielgos
Currently, the majority of neonates born to organ recipient mothers on chronic immunosuppressive therapy are formula fed. However, over the past few years, evidence has grown, suggesting that breastfeeding might be possible and beneficial. We designed a study assessing the transfer of tacrolimus into the colostrum of posttransplant mothers. We assessed the amount of tacrolimus and its metabolites, M-1 and M-3, that would be ingested by the breastfed neonates. Concentrations of tacrolimus and its metabolites were measured in colostrum from 14 posttransplant mothers as well as in venous cord blood and venous blood of the neonates...
February 27, 2018: Nutrients
Yong-Mei Guan, Wei-Feng Zhu, Xue-Jing Guan, Zheng-Gen Liao, Guo-Wei Zhao, Wei Dong, Xin-Li Liang
The study was aimed to establish a liquid chromatography-tandem mass spectrometric method for the determination of the docetaxel concentration in rat plasma, and study the effect of coumarin constituents (imperatorin, isoimperatorin and oxypeucedanin) in Angelica dahurica on pharmacokinetics of docetaxel.Plasma was precipitated with acetonitrile and determined by LC-MS method with Paclitaxel as an internal standard. The specificity, linearity, range, accuracy, precision and stability of the method were suitable for the determination of docetaxel in plasma...
December 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
Seong Eun Jin, Hyekyung Ha, Chang-Seob Seo, Hyeun-Kyoo Shin, Soo-Jin Jeong
Objective: The aim of this study was to investigate the possible herb-drug interactions between the traditional herbal formula Guibi-tang (GBT; Guipi-tang , Kihi-to ) and conventional drugs. Materials and Methods: GBT was orally administered to either male or female Sprague Dawley (SD) rats once daily at doses of 1000, 2000, or 5000 mg/kg/day for 13 weeks. The messenger ribonucleic acid (mRNA) expression of drug-metabolizing enzyme cytochrome P450 isozymes (cytochrome P450s; CYP1A1, 1A2, 2B1/2, 2C11, 2E1, 3A1, 3A2, and 4A1) was analyzed in hepatic tissues by reverse transcription-polymerase chain reaction...
January 2018: Pharmacognosy Magazine
Elusa Scheibler, Renata Medina da Silva, Carlos Eduardo Leite, Maria Martha Campos, Maria Antonia Figueiredo, Fernanda Gonçalves Salum, Karen Cherubini
OBJECTIVE: Nystatin and chlorhexidine are extensively used in oral medicine; however, there is some controversy about the possibility of these drugs showing antagonism. To clarify this issue, this study investigated the efficacy and stability of nystatin and chlorhexidine in combination. DESIGN: An in vitro study was conducted to analyze the effect of nystatin and chlorhexidine combined on Candida albicans ATCC 18804, using the drugs mixed as a single formulation and as independent formulations used sequentially with different time intervals between them...
February 15, 2018: Archives of Oral Biology
Lauriane Goldwirt, Kevin Beccaria, Alain Ple, Hélène Sauvageon, Samia Mourah
PURPOSE: Central nervous system (CNS) dissemination occurs in 4.1% of mantle cell lymphoma (MCL) patients and clinically significant CNS involvement in chronic lymphocytic leukemia (CLL) patients reaches 4%. Ibrutinib, an orally administered Bruton's tyrosine kinase (BTK) inhibitor, has shown substantial activity in CLL or MCL patients with CNS localization, and in primary central nervous system lymphoma (PCNSL). The drug efficacy to treat primary or secondary CNS impairments relies on its brain distribution through the blood-brain barrier (BBB), the aim of the present work was to study the brain distribution of ibrutinib using an in vivo mice model...
February 23, 2018: Cancer Chemotherapy and Pharmacology
Agnieszka Karbownik, Edyta Szałek, Katarzyna Sobańska, Agnieszka Klupczynska, Szymon Plewa, Tomasz Grabowski, Anna Wolc, Marta Moch, Zenon J Kokot, Edmund Grześkowiak
BACKGROUND: Diabetes mellitus (DM) is a complex metabolic disorder which affects the function of numerous tissues and alters the pharmacokinetic parameters of many drugs. As many oncological patients are diabetics, it is important to determine the influence of this chronic disease on the pharmacokinetics (PK) of anticancer drugs. Lapatinib is a tyrosine kinase inhibitor (TKI), approved for the treatment of human epidermal growth factor receptor 2 (HER2)-positive metastatic breast cancer...
September 18, 2017: Pharmacological Reports: PR
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