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https://www.readbyqxmd.com/read/28803538/pharmacokinetics-of-tafamidis-a-transthyretin-amyloidosis-drug-in-rats
#1
Kyeong-Ryoon Lee, Jong-Woo Jeong, Hun-Chan Hyun, Jang Eunseo, Sunjoo Ahn Ahn, Sungwook Choi, Sang Hoon Joo, Sung-Sub Kim, Tae-Sung Koo
1. We characterized the pharmacokinetics of tafamidis, a novel drug to treat transthyretin-related amyloidosis, in rats after intravenous and oral administration at doses of 0.3-3 mg/kg. In vitro Caco-2 cell permeability and liver microsomal stability, as well as in vivo tissue distribution and plasma protein binding were also examined. 2. After intravenous injection, systemic clearance (CL), volumes of distribution at steady state (Vss), and half-life (T½) remained unaltered as a function of dose, with values in the ranges of 6...
August 14, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28776825/influence-of-food-on-the-gastric-motor-effect-of-the-kampo-medicine-rikkunshito-in-rat
#2
M Nahata, Y Mizuhara, C Sadakane, J Watanabe, N Fujitsuka, T Hattori
BACKGROUND: Rikkunshito, one of the Kampo medicines, is widely prescribed as a remedy for various upper gastrointestinal syndromes. The effect of rikkunshito is related to endogenous ghrelin and its active ingredient atractylodin enhances ghrelin receptor signaling. Kampo medicines are traditionally administered before or between meals; however, no definitive benefit of the timing of administration has been proven yet. To clarify the influence of food on the pharmacological action of rikkunshito, we investigated the gastric motor activity and pharmacokinetic profiles of atractylodin after the administration of rikkunshito in fasted and fed rats...
August 4, 2017: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/28774853/anti-alzheimer-s-potential-of-berberine-using-surface-decorated-multi-walled-carbon-nanotubes-a-preclinical-evidence
#3
Shikha Lohan, Kaisar Raza, S K Mehta, Gurjit Kaur Bhatti, Sumant Saini, Bhupinder Singh
Carbon nanotubes (CNTs), a sub-family of fullerenes, are nanosized seamless cylinders of graphene sheets with enormous drug loading potential. The current studies entail the systematic development of berberine (BRB)-loaded multiwalled carbon nanotubes (MWCNTs) with polysorbate and phospholipid coating for effective management of Alzheimer's Disease (AD). For systematic optimization using design of experiment (DoE), a central composite design (FCCD) was employed and the optimized formulation was choosen using numerical desirability function...
July 31, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28774678/determination-of-tranilast-in-bio-samples-by-lc-ms-ms-application-to-a-pharmacokinetic-and-brain-tissue-distribution-study-in-rats
#4
Wen Yang, Eboka Majolene B Sabi-Mouka, Lei Wang, Chang Shu, Yan Wang, Juefang Ding, Li Ding
As a potent drug used to improve the neurodegenerative conditions, there is few information about the brain tissue distribution of tranilast by now. In this study, a novel sensitive LC-MS/MS method has been developed and validated to determine tranilast in rat brain tissue samples. The calibration curve showed good linearity ranged from 2.140 to 428.0ng·mL(-1). The method was fully validated and successfully applied in the brain tissue distribution study of tranilast in rats, which had never been reported in detail by now...
June 20, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28747713/overcoming-blood-brain-barrier-with-a-dual-purpose-temozolomide-loaded-lactoferrin-nanoparticles-for-combating-glioma-serp-17-12433
#5
Sonali Kumari, Saad M Ahsan, Jerald M Kumar, Anand K Kondapi, Nalam M Rao
Targeted delivery of drugs to the brain is challenging due to the restricted permeability across the blood brain barrier (BBB). Gliomas are devastating cancers and their positive treatment outcome using Temozolomide (TMZ) is limited due to its short plasma half-life, systemic toxicity and limited access through the blood-brain barrier (BBB). Nanoparticles made of Lactoferrin (Lf) protein, have been shown to enhance the pharmacological properties of drugs. Here, we report the specific ability of Lf nanoparticles to cross BBB and target over-expressed Lf receptors on glioma for enhanced TMZ delivery...
July 26, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28745530/agomelatine-based-in-situ-gels-for-brain-targeting-via-the-nasal-route-statistical-optimization-in-vitro-and-in-vivo-evaluation
#6
Ahmed M Fatouh, Ahmed H Elshafeey, Ahmed Abdelbary
Agomelatine (AGM) is an antidepressant drug with a low absolute bioavailability due to the hepatic first pass metabolism. AGM-loaded solid lipid nanoparticles were formulated in the form of an in situ gel to prolong the intranasal retention time and subsequently to increase the absorbed amount of AGM. The optimized in situ gel formula had a sol-gel transition temperature of 31 °C ± 1.40, mucociliary transport time of 27 min ±1.41%, released after 1 and 8 h of 46.3% ± 0.85 and 70.90% ± 1...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28710563/an-observational-study-examining-the-effects-of-a-surgically-induced-inflammatory-response-on-the-distribution-of-morphine-and-its-metabolites-into-cerebrospinal-fluid
#7
Yan Wang, Kerry B Goralski, Derek J Roberts, Kathryn Landry, Mark E Issa, Lekha Sleno, Lisa C Julien, Jeremy Wood, Richard I Hall
PURPOSE: Morphine is administered intravenously for pain management in the perioperative period. The effect of the inflammatory response to surgery on morphine distribution across the blood-brain barrier (BBB) in humans was investigated. We hypothesized that a graded surgically induced, systemic inflammatory response alters cerebrospinal fluid (CSF) levels of morphine, morphine-3-glucuronide (M3G), and morphine-6-glucuronide (M6G) through a temporary reduction in BBB drug efflux transporter function...
July 14, 2017: Canadian Journal of Anaesthesia, Journal Canadien D'anesthésie
https://www.readbyqxmd.com/read/28705616/improvement-of-the-surface-hydrophilic-properties-of-naproxen-particles-with-addition-of-hydroxypropylmethyl-cellulose-and-sodium-dodecyl-sulphate-in-vitro-and-in-vivo-studies
#8
Víctor García-Herrero, Carlos Torrado, Juan José García-Rodríguez, Alicia López-Sánchez, Susana Torrado, Santiago Torrado-Santiago
In this study, a new surface-modified naproxen was developed to enhance brain concentration in acute migraine treatment. Fast-dissolving naproxen granules were made by mixing hydroxypropylmethylcellulose (HPMC) sodium dodecyl sulphate (SDS) and sodium croscarmellose with micronized naproxen particles. The aim of this study was to evaluate the effect of adding proportions of SDS to the HPMC film caused changes in the polymer chains of the HPMC, producing a new hydrophilic HPMC-SDS structure. These formulations with different HPMC/SDS ratios were characterised using electron microscopy (SEM), powder X-ray diffraction (PXRD), and differential scanning calorimetry (DSC)...
July 11, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28702763/pharmacokinetics-of-antifungal-drugs-practical-implications-for-optimized-treatment-of-patients
#9
REVIEW
Romuald Bellmann, Piotr Smuszkiewicz
INTRODUCTION: Because of the high mortality of invasive fungal infections (IFIs), appropriate exposure to antifungals appears to be crucial for therapeutic efficacy and safety. MATERIALS AND METHODS: This review summarises published pharmacokinetic data on systemically administered antifungals focusing on co-morbidities, target-site penetration, and combination antifungal therapy. CONCLUSIONS AND DISCUSSION: Amphotericin B is eliminated unchanged via urine and faeces...
July 12, 2017: Infection
https://www.readbyqxmd.com/read/28698254/mechanism-based-pharmacokinetic-pharmacodynamic-modeling-of-the-glucagon-like-peptide-1-receptor-agonist-exenatide-to-characterize-its-anti-obesity-effects-in-diet-induced-obese-mice
#10
Shinji Iwasaki, Teruki Hamada, Ikumi Chisaki, Tomohiro Andou, Noriyasu Sano, Atsutoshi Furuta, Nobuyuki Amano
Glucagon-like peptide-1 (GLP-1) analogs lower body weight in humans in addition to their potent anti-diabetic effects. Hence, agonistic targeting of the GLP-1 receptor could be a valid approach to target obesity. However, quantitative analyses of the pharmacokinetic/pharmacodynamic (PK/PD) relationship between GLP-1 analogs and their anti-obesity effect have not been reported in either animals or humans. Therefore, the present study was performed to establish a mechanism-based PK/PD model of GLP-1 receptor agonists using the GLP-1 analog, exenatide, for the development of promising new anti-obesity drugs...
July 11, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28694087/a-mathematical-model-of-a-recombinant-humanized-anti-cocaine-monoclonal-antibody-s-effects-on-cocaine-pharmacokinetics-in-mice
#11
Hanna N Wetzel, Tongli Zhang, Andrew B Norman
AIMS: A recombinant humanized anti-cocaine monoclonal antibody (mAb), h2E2, is at an advanced stage of pre-clinical development as an immunotherapy for cocaine abuse. It is hypothesized that h2E2 binds to and sequesters cocaine in the blood. MAIN METHODS: A three-compartment model of the effects of h2E2 on cocaine's distribution was constructed. The model assumes that h2E2 binds to cocaine and that the h2E2-cocaine complex does not enter the brain but distributes between the central and peripheral compartments...
July 7, 2017: Life Sciences
https://www.readbyqxmd.com/read/28688108/a-physiologically-based-pharmacokinetic-modeling-approach-to-predict-buprenorphine-pharmacokinetics-following-intravenous-sublingual-administration
#12
Hari V Kalluri, Hongfei Zhang, Steve N Caritis, Raman Venkataramanan
INTRODUCTION: Opioid dependence is associated with high morbidity and mortality. Buprenorphine(BUP) is approved by the FDA to treat opioid dependence. There is a lack of clear consensus on appropriate dosing of BUP due to inter-patient physiological differences in absorption/disposition, subjective response assessment and other patient comorbidities. The objective of this study is to build and validate robust physiologically-based-pharmacokinetic(PBPK) models for intravenous(IV) and Sublingual(SL) BUP as a first-step to optimize BUP pharmacotherapy...
July 8, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28684900/intranasal-agomelatine-solid-lipid-nanoparticles-to-enhance-brain-delivery-formulation-optimization-and-in-vivo-pharmacokinetics
#13
Ahmed M Fatouh, Ahmed H Elshafeey, Ahmed Abdelbary
PURPOSE: Agomelatine is a novel antidepressant drug suffering from an extensive first-pass metabolism leading to a diminished absolute bioavailability. The aim of the study is: first to enhance its absolute bioavailability, and second to increase its brain delivery. METHODS: To achieve these aims, the nasal route was adopted to exploit first its avoidance of the hepatic first-pass metabolism to increase the absolute bioavailability, and second the direct nose-to-brain pathway to enhance the brain drug delivery...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28682148/pharmacokinetics-of-an-intracerebroventricularly-administered-antibody-in-rats
#14
Yuki Noguchi, Motohiro Kato, Kazuhisa Ozeki, Masaki Ishigai
The pharmacokinetics (PK) of an antibody in the brain and the spinal cord is insufficiently understood, which is an obstacle to the discovery of antibody drugs that target diseases in the central nervous system. In this study, we focused on the elimination of IgG from cerebrospinal fluid (CSF) circulating in the brain and the spinal cord in rats, and, to evaluate the influence of CSF bulk flow on the clearance of IgG, also examined the PK of inulin in CSF. To monitor their concentrations in CSF, IgG and inulin were co-administered into the lateral ventricle via a catheter, and CSF was collected from the cisterna magna via another catheter time-sequentially...
July 6, 2017: MAbs
https://www.readbyqxmd.com/read/28679777/efficacy-of-onalespib-a-long-acting-second-generation-hsp90-inhibitor-as-a-single-agent-and-in-combination-with-temozolomide-against-malignant-gliomas
#15
Alessandro Canella, Alessandra M Welker, Ji Young Yoo, Jihong Xu, Fazly S Abbas, Divya Kesanakurti, Prabhakaran Nagarajan, Christine E Beattie, Erik P Sulman, Joseph L Liu, Joy Gumin, Frederick F Lang, Metin Gurcan, Balveen Kaur, Deepa Sampath, Vinay K Puduvalli
HSP90, a highly conserved molecular chaperone that regulates the function of several oncogenic client proteins is altered in glioblastoma. However, HSP90 inhibitors currently in clinical trials are short-acting, have unacceptable toxicities or are unable to cross the blood brain barrier (BBB). We examined the efficacy of onalespib, a potent, long-acting novel HSP90 inhibitor as a single agent and in combination with temozolomide (TMZ) against gliomas invitro and invivo<br /><br />Experimental Design: The effect of onalespib on HSP90, its client proteins, and on the biology of glioma cell lines and patient-derived glioma-initiating cells (GSC) was determined...
July 5, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28677844/enantioselective-analysis-of-ibuprofen-enantiomers-in-mice-plasma-and-tissues-by-high-performance-liquid-chromatography-with-fluorescence-detection-application-to-a-pharmacokinetic-study
#16
Katarzyna Przejczowska-Pomierny, Monika Włodyka, Agnieszka Cios, Elżbieta Wyska
A direct fluorometric high-performance liquid chromatography (HPLC) method was developed and validated for the analysis of ibuprofen enantiomers in mouse plasma (100 μl) and tissues (brain, liver, kidneys) using liquid-liquid extraction and 4-tertbutylphenoxyacetic acid as an internal standard. Separation of enantiomers was accomplished in a Chiracel OJ-H chiral column based on cellulose tris(4-methylbenzoate) coated on 5 μm silica-gel, 250 x 4.6 mm at 22 °C with a mobile phase composed of n-hexane, 2-propanol, and trifluoroacetic acid that were delivered in gradient elution at a flow rate of 1 ml min(-1) ...
July 5, 2017: Chirality
https://www.readbyqxmd.com/read/28664226/eribulin-shows-high-concentration-and-long-retention-in-xenograft-tumor-tissues
#17
Michiko Sugawara, Krista Condon, Earvin Liang, Christopher DesJardins, Edgar Schuck, Kazutomi Kusano, W George Lai
PURPOSE: Eribulin, a synthetic analog of the natural product halichondrin B, is a microtubule dynamics inhibitor. In this study, we report the pharmacokinetic profiles of eribulin in mice, rats, and dogs following intravenous administrations with optimized and validated bio-analytical methods. METHODS: Eribulin was administered at 0.5 and 2 mg/kg in mice, 0.5 and 1 mg/kg in rats, and 0.08 mg/kg in dogs. Tumor and brain penetration of eribulin was also evaluated in LOX human melanoma xenograft models...
August 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28662899/l-type-amino-acid-transporter-1-utilizing-prodrugs-how-to-achieve-effective-brain-delivery-and-low-systemic-exposure-of-drugs
#18
Elena Puris, Mikko Gynther, Johanna Huttunen, Aleksanteri Petsalo, Kristiina M Huttunen
L-type amino acid transporter 1 (LAT1) is selectively expressed in the blood-brain barrier (BBB) and brain parenchyma. This transporter can facilitate brain delivery of neuroprotective agents and additionally give opportunity to minimize systemic exposure. Here, we investigated structure-pharmacokinetics relationship of five newly synthesized LAT1-utilizing prodrugs of the cyclooxygenase inhibitor, ketoprofen, in order to identify beneficial structural features of prodrugs to achieve both targeted brain delivery and low peripheral distribution of the parent drug...
September 10, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28662343/effect-of-chronic-%C3%AE-hydroxybutyrate-ghb-administration-on-ghb-toxicokinetics-and-ghb-induced-respiratory-depression
#19
Bridget L Morse, Gurkishan S Chadha, Melanie A Felmlee, Kristin E Follman, Marilyn E Morris
BACKGROUND: γ-hydroxybutyrate (GHB) has a high potential for illicit use; overdose of this compound results in sedation, respiratory depression and death. Tolerance to the hypnotic/sedative and electroencephalogram effects of GHB occurs with chronic GHB administration; however, tolerance to respiratory depression has not been evaluated. GHB toxicodynamic effects are mediated predominantly by GABAB receptors. Chronic treatment may affect monocarboxylate transporters (MCTs) and alter the absorption, renal clearance and brain uptake of GHB...
June 29, 2017: American Journal of Drug and Alcohol Abuse
https://www.readbyqxmd.com/read/28656123/determination-of-epimedin-b-in-rat-plasma-and-tissue-by-lc-ms-ms-application-in-pharmacokinetic-and-tissue-distribution-studies
#20
Qianru Feng, Shunjun Xu, Jiejing Yu, Shuai Sun, Liu Yang
A simple, sensitive, and specific liquid chromatography tandem mass-spectrometric method was developed and validated for the determination of epimedin B in rat plasma and tissue samples. After being processed with a protein precipitation method, these samples were separated on an Agilent Eclipse XDB-C18 column with an isocratic mobile phase consisting of acetonitrile and 0.1% formic acid aqueous solution (32 : 68, v/v). The calibration curve of epimedin B was linear over the concentration range from 1 to 500 ng/mL in plasma and tissue homogenate...
2017: Journal of Analytical Methods in Chemistry
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