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Hplc pharmacokinetics

Zhijun Wang, Steven Yeung, Shang Chen, Yasmin Moatazedi, Moses S S Chow
Wilforlide A (WA), an active compound in Tripterygium wilfordii Hook F (TW) which is a traditional Chinese medicine for treatment of autoimmune diseases, is a quality control marker for TW product. At present, the bioavailability/pharmacokinetics of WA is not known. Such information is not only essential to evaluate the relevance of WA as a quality control maker, but also important for future clinical efficacy studies. Therefore, a high-performance liquid chromatography-atmospheric pressure chemical ionization tandem mass spectrometric method (HPLC-APCI-MS/MS) was developed and applied to a bioavailability/pharmacokinetic study of WA...
May 16, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Dalyara Mendonça de Matos, Milainy Rocha Viana, Marcela Cristina de Oliveira Alvim, Lara Soares Aleixo de Carvalho, Laura Hora Rios Leite, Ademar Alves da Silva Filho, Jorge Willian Leandro Nascimento
Kaurenoic acid (KA) is a kaurane diterpene found in several medicinal plants that displays biological activities, such as anti-inflammatory, smooth muscle relaxant and hypotensive response. However, there are no pharmacokinetic data available about this molecule. The purpose of the study was to determine the pharmacokinetics profile and the oral bioavailability of KA in rats. Wistar rats submitted to jugular vein cannulation received 50 mg/kg of KA by intravenous or oral route. The implanted cannula allowed intravenous administration and serial blood collection along 10 h...
May 14, 2018: Fitoterapia
Bruno L Abbadi, Valnês da Silva Rodrigues-Junior, Adilio da Silva Dadda, Kenia Pissinate, Anne D Villela, Maria M Campos, Luiz G de França Lopes, Cristiano V Bizarro, Pablo Machado, Eduardo H S Sousa, Luiz A Basso
The emergence of strains of Mycobacterium tuberculosis resistant to isoniazid (INH) has underscored the need for the development of new anti-tuberculosis agents. INH is activated by the mycobacterial katG -encoded catalase-peroxidase, forming an acylpyridine fragment that is covalently attached to the C4 of NADH. This isonicotinyl-NAD adduct inhibits the activity of 2- trans -enoyl-ACP(CoA) reductase (InhA), which plays a role in mycolic acid biosynthesis. A metal-based INH analog, Na3 [FeII (CN)5 (INH)]·4H2 O, IQG-607, was designed to have an electronic redistribution on INH moiety that would lead to an intramolecular electron transfer to bypass KatG activation...
2018: Frontiers in Microbiology
B Pastina, P J Early, R L Bergman, J Nettifee, A Maller, K Y Bray, R J Waldron, A M Castel, K R Munana, M G Papich, K M Messenger
The objective of this study was to describe the pharmacokinetics (PK) of cytarabine (CA) after subcutaneous (SC) administration to dogs with meningoencephalomyelitis of unknown etiology (MUE). Twelve dogs received a single SC dose of CA at 50 mg/m2 as part of treatment of MUE. A sparse sampling technique was used to collect four blood samples from each dog from 0 to 360 min after administration. All dogs were concurrently receiving prednisone (0.5-2 mg kg-1 day-1 ). Plasma CA concentrations were measured by HPLC, and pharmacokinetic parameters were estimated using nonlinear mixed-effects modeling (NLME)...
May 15, 2018: Journal of Veterinary Pharmacology and Therapeutics
John D Sheppard, Paul C Cockrum, Angela Justice, Mark C Jasek
INTRODUCTION: Little is known of the ocular distribution characteristics of currently branded non-steroidal anti-inflammatory drugs (NSAIDs) in the United States. This study was designed to predict the ocular bioavailability characteristics in humans using Dutch Belted rabbits as a surrogate. Commercially available, topically-applied NSAIDs containing bromfenac or nepafenac/amfenac were evaluated. METHODS: 126 healthy adult Dutch Belted rabbits were randomly assigned to three treatment cohorts (BromSite® twice daily [BID] in the right eye, BromSite® once daily [QD] in the right eye, Prolensa® QD in the right eye and Ilevro™ QD in the left eye) and 7 post-dosing time points (0...
May 14, 2018: Ophthalmology and Therapy
Lei Zhang, Fei Li, Wang-Jun Qin, Chao Fu, Xiang-Lin Zhang
Ginsenoside Re, an active ingredient in Panax ginseng, is widely used as a therapeutic and nutriment. Intestinal microbiota plays crucial roles in modulating the pharmacokinetics and pharmacological actions of ginsenoside Re. The aim of this study was to explore the relationship between bacterial community variety and the metabolic profiles of ginsenoside Re. We developed two models with intestinal dysbacteriosis: a pseudo-germ-free model induced by a non-absorbable antimicrobial mixture (ATM), and Qi-deficiency model established via over-fatigue and acute cold stress (OACS)...
May 10, 2018: Biomedical Chromatography: BMC
Elias David-Neto, Ana Heloisa Triboni, Fernanda Ramos, Fabiana Agena, Paschoalina Romano
BACKGROUND: Enteric-coated mycophenolate sodium (EC-MPS) is frequently used in renal transplantation. The pharmacokinetic profile of mycophenolic acid (MPA) shows a broad range of time-to-maximum-concentration (Tmax) that limits the use of a single MPA concentration to calculate the area under the time-concentration curve (AUC). For both research and clinical MPA monitoring, measuring a complete AUC is troublesome to the center and patients. METHODS: We obtained 171 complete MPA-AUC12h (0, 20,40,60,90,120, 180, 240, 360, 480, 600, 720 min) from 59 adult (54±16 years) patients (29 male, 43 whites) who have been receiving stable doses of Tacrolimus/EC-MPS and steroids...
May 4, 2018: Therapeutic Drug Monitoring
Jagdish Mahale, Lynne M Howells, Rajinder Singh, Robert G Britton, Hong Cai, Karen Brown
Curcumin, derived from turmeric, has been extensively investigated for its broad spectrum of biological activities. Previously reported HPLC-UV methods have focussed on analysis of the parent compound. Here, a sensitive HPLC-UV method was developed and partially validated, then used for the simultaneous determination of curcumin and its glucuronide and sulfate metabolites in plasma and lung tissue from mice. The assay was applied to an in vivo pharmacokinetic study comparing formulated curcumin (Meriva™) with standard curcumin...
May 9, 2018: Biomedical Chromatography: BMC
Jin Xiang, Qin Yu, Mao-Zhi Liang, Yong-Ping Qin, Feng Nan
OBJECTIVE: To develop a high performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method for the determination of voriconazole in human plasma and its bioequivalence. METHODS: 48 healthy male volunteers received a single dose of 200 mg voriconazole tablets in a two period (with two preparations) and randomized crossover bioequivalence study. Their plasma voriconazole was determined using HPLC-MS/MS. The pharmacokinetic parameters and bioequivalence of the two preparations were calculated with WinNonlin® 6...
January 2018: Sichuan da Xue Xue Bao. Yi Xue Ban, Journal of Sichuan University. Medical Science Edition
Guoping Yang, Qi Pei, Chengxiao Fu, Jie Huang, Jun Chen, Shuang Yang, Yuxia Xiang, Jing Wang, Hongyi Tan, Xiaolei Liu
Pyragrel is a novel thromboxane A2-synthetase inhibitor for the treatment of cerebral infarction, and it is currently being investigated in phase I clinical trials. This paper reports the first reliable LC-MS/MS method for the simultaneous determination of Pyragrel and its two main metabolites, M1 and M2, in human plasma. All analytes were extracted from human serum using liquid-phase extraction and separated on a Zorbax EcLipse XDB C18 column using isocratic elution with a mobile phase composed of methanol, water and formic acid (65:35:0...
April 14, 2018: Journal of Pharmaceutical and Biomedical Analysis
Jian Gao, Rui Zhen, Hai Liao, Wenquan Zhuang, Wenbo Guo
Numerous studies concerning hepatic arterial infusion chemotherapy (HAIC) have been conducted by adopting regimens containing 5-fluorouracil (FU), with a favourable efficacy compared with conventional transcatheter arterial chemoembolisation (TACE) treatment; however, the detailed mechanism of HAIC remains unclear. The present study aimed to evaluate peripheral concentration time curves of 5-FU administered through the hepatic artery, which may additionally explain the mechanism of action of HAIC. A total of 10 eligible patients underwent transcatheter arterial embolization and a 2-day HAIC treatment regimen using a folinic acid, fluorouracil and oxaliplatin regimen...
May 2018: Oncology Letters
Qaiser Iqbal, Sajid Bashir, Syed Umer Jan, Muhammad Zubair Malik, Iftikhar Afzal, Ayesha Khalid
A new high performance liquid chromatography (HPLC) method for the quantitative determination of sitagliptin in human plasma was developed and validated for pharmacokinetics study. The plasma was spiked with the internal standard (Salbutamol, IS), extracted with trichloro acetic acid. The extracted analyte was injected into a Symmetry® ODS C18 column (250mm×4.5mm, 5m) and the flourometric detector was operated at 267nm for excitation and 575nm for emission. The mobile phase consisting of Potassium dihydrogen phosphate buffer pH (4...
May 2018: Pakistan Journal of Pharmaceutical Sciences
Bing-Jun Qian, Chong-Chong Tian, Xiao-Hong Ling, Li-Li Yu, Feng-Yun Ding, Jiang-Hua Huo, Liu-Cun Zhu, Yao-Lin Wen, Jiang-Hua Zhang, Pu Jing
AIMS: The antihypertensive mechanism (s) of the epigallocatechin-3-gallate (EGCG), a major effective component in green tea, might associate with microRNAs (miRNAs). Here, we aimed to investigate which microRNA in aorta of spontaneously hypertensive rats (SHRs) were modulated by administration of EGCG and its mechanism. MAIN METHODS: The pharmacokinetic behaviors of EGCG and epigallocatechin (EGC) in Sprague-Dawley rats were analyzed by HPLC and DRUG AND STATISTICS software...
April 26, 2018: Life Sciences
Hui-Fei Wu, Xiang-Yu Wang, Ji-Feng Deng, Shi-Jian Quan, Qi Wang, Wei-Rong Li
BACKGROUND AND OBJECTIVE: Danggui-Shaoyao-San (DSS), a famous Chinese formula, has been widely used to treat gynecological disorders since ancient times and has recently showed efficacy in treating Alzheimer's disease. Butylidenephthalide (BDPH) and alisol B (ALI) are recognized as the primary active ingredients of DSS. The objectives of the present study were to evaluate the pharmacokinetic comparative study of BDPH and ALI in herbal extracts and their purified forms. METHOD: A sensitive and specific high-performance liquid chromatography tandem mass spectrometry (HPLC-MS/MS) methodology was developed to determine the concentration level of BDPH and ALI in rat plasma...
April 27, 2018: European Journal of Drug Metabolism and Pharmacokinetics
Pu Li, Min-Ji Wei, Zhi-Yuan Zhang, Sheng-Ju Yin, Xin Wang, Ya-Qing Lou, Zi-Sheng Kang, Yuan Lu, Xuan Wei, Suo-Di Zhai, Guo-Liang Zhang
Mizolastine is a selective histamine H1 receptor antagonist for chronic urticaria or allergic rhinitis. We investigated whether the variant genotypes of metabolic enzymes UGT1A1, CYP3A5 and transporter ABCB1 influence pharmacokinetic phenotype of substrate mizolastine in Chinese volunteers. Genotyping of single nucleotide polymorphisms (SNPs) in UGT1A1*6 (G211A), CYP3A5*3 (A6986G) and ABCB1 (C3435T) were determined by the pyrosequencing method. After a single oral dose of 10 mg mizolastine, the plasma concentrations were measured using validated high performance liquid chromatography (HPLC) in 24 Chinese healthy volunteers...
April 27, 2018: Basic & Clinical Pharmacology & Toxicology
Wenji Li, Hilly Yang, Brian Buckley, Lujing Wang, Ah-Ng Kong
Even through more sensitive methods for quantifying trace levels of curcumin in plasma were urgently needed, beyond tandem mass spectrometry, the Paul trap MS/MS/MS has never been tested for curcumin quantification. Because of its unique trap function to accumulate target compounds selectively by optimizing multiple stage MS experiments, it showed great potential to remove background issues reported at low concentration ranges. A novel Triple stage Ion Trap Mass Spectrometry coupled with High Performance Liquid Chromatography (HPLC-ITMS/MS/MS) method has been developed and validated as a curcumin quantification method, for the first time...
April 17, 2018: Journal of Pharmaceutical and Biomedical Analysis
Samaa Alrushaid, Neal M Davies, Judy E Anderson, Tyson Le, Jaime A Yáñez, Zaid H Maayah, Ayman O S El-Kadi, Ousama Rachid, Casey L Sayre, Raimar Löbenberg, Frank J Burczynski
PURPOSE: MyoNovin is a novel skeletal muscle-regenerating compound developed through synthesis of two nitro groups onto a guaifenesin backbone to deliver nitric oxide to skeletal muscle with a potential to treat muscle atrophy. The purpose of this study was to utilize in silico, in vitro, and in vivo approaches to characterize MyoNovin and examine its safety, biodistribution, and feasibility for drug delivery. METHODS: In silico software packages were used to predict the physicochemical and biopharmaceutical properties of MyoNovin...
2018: Journal of Pharmacy & Pharmaceutical Sciences: a Publication of the Canadian Society for Pharmaceutical Sciences
Fugeng Zhang, Yu Zhang, Xiaofeng Li, Shaoqiang Zhang, Mingdan Zhu, Wuxun Du, Xuefeng Xiao
BACKGROUND: Qiliqiangxin capsule (QLQX), composed of 11 herbs, is an effective traditional Chinese medicine (TCM) that has been widely used for treatment of chronic heart failure (CHF) in China. In the Chinese pharmacopoeia (Ch.P.) only astragaloside was described as the marker component to control the quality of QLQX, which could not reflect the overall effectiveness. PURPOSE: The aim of this work was to investigate the quality markers (Q-markers) of QLQX based on the association of the pharmacodynamics (PD) of inhibitory effect on activated renin-angiotensin-aldosterone system (RAAS) and the pharmacokinetics (PK) of bioactive compounds according to the Q-marker theory...
March 21, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
Baohai Liu, Shuangdi Li, Xiaodan Sui, Lianyi Guo, Xingmei Liu, Hongmei Li, Leming Gao, Shusheng Cai, Yanrong Li, Tingting Wang, Xuehua Piao
Background: Polygonum cuspidatum Siebold & Zucc. (PCS) has antibacterial properties and may prevent Ulcerative colitis (UC) but related molecular mechanism remains unknown. NF-κB signaling pathway is associated with inflammatory responses and its inactivation may be critical for effective therapy of UC. Methods: UC mouse (C57BL/6J) model was established by using dextran sulfate sodium (DSS). The extract of PCS (PCSE) was prepared by using ethanol and its main ingredients were measured by HPLC. Thirty-two UC mice were evenly assigned into DG (received vehicle control), LG (0...
2018: Frontiers in Pharmacology
Pawel Zbyszynski, Bianca R Tomasini-Johansson, Donna M Peters, Glen S Kwon
PURPOSE: To develop PEGylated variants of pUR4/FUD (FUD), a fibronectin assembly inhibitor, using 10 kDa, 20 kDa, and 40 kDa PEGs to evaluate their binding affinity and inhibitory potency. METHODS: The FUD peptide was recombinantly expressed, purified, and PEGylated at the N-terminus using 10 kDa, 20 kDa, and 40 kDa methoxy-PEG aldehyde. The PEGylates were purified and fractionated using ion-exchange chromatography. The molecular weight and degree of PEGylation of each conjugate was verified using MALDI-TOF...
April 24, 2018: Pharmaceutical Research
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