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Development and validation of an LC-MS/MS method for tyrphostin A9

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Journal of Pharmaceutical Analysis 2019年第3期9卷 163-169页

作者： Lyndsey F.Meyer Dhaval k.shah Department of Pharmaceutical Sciences School of Pharmacy and Pharmaceutical SciencesThe State University of New York at Buffalo

Here we have presented a sensitive and selective LC-MS/MS method for the quantification of tyrphostin A9, which is a selective inhibitor for platelet derived growth factor receptor tyrosine kinase and has been investigated in vitro as a potent oxidative phosphorylation uncoupler. The murine analytical method was developed for three biological matrices: cell culture media, 3T3-L1 cell lysate, and murine plasma. For each matrix the limit of detection and the limit of quantification were found to be 0.5 ng/mL and 1.0 ng/ mL, respectively. The range of standard curve for each matrix was 1.0-100 ng/mL, linearity was >0.99, and the precision and accuracy were within 20%. 3-(3,5-di-tert-butyl-4-hydroxyphenyl) propanoic acid was found to be the most suitable internal standard. The validated LC-MS/MS method was used to investigate stability and in vitro pharmacokinetics of tyrphostin A9. It was found that tyrphostin A9 is susceptible to hydrolysis, and the degradation product was identified as 3,5-di-tert-butyl-4- hydroxybenzaldehyde. Tyrphostin A9 was not stable in biological matrices, and the rate of its degradation in murine plasma was faster than that in cell culture media. In vitro pharmacokinetic studies revealed that tyrphostin A9 concentrations in the cell culture media declined in a bi-exponential manner and the concentrations inside the adipocytes remained constant, suggesting tyrphostin A9 has an intracellular binding site and is retained within the cell. The LC-MS/MS method presented here paves the way for further quantitative investigations involving tyrphostin A9.

关键词： Tyrphostin 9/ A9/AG-9/Malonoben/SF6847 LC-MS/MS Stability Pharmacokinetics Tyrosine kinase inhibitor

A comparison of centrifugation and tangential flow filtration for nanoparticle purification: A case study on acetalated dextran nanoparticles

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Particuology 2020年第3期18卷 189-196页

作者： Nishan k.shah Ryan Ivone Jie Shen Samantha A.Meenach University of Rhode Island College of PharmacyDepartment of Biomedical and Pharmaceutical SciencesKingstonRI 02881USA University of Rhode Island College of EngineeringDepartment of Chemical EngineeringKingstonRI 02881USA

Tangential fiow filtration (TFF) is a purification method commonly used in a multitude of fields,including particle ***,there is still a lack of comprehensive understanding of the effects of key TFF parameters on nanoparticle (NP) characteristics (purification outcomes).The present study aimed to investigate the influence of various factors on the characteristics of TFF-purified *** most commonly used NP purification method,centrifugation,was studied as a control.A design of experiment approach was implemented to investigate the influence of transmembrane pressure,flow rate,and initial drug loading on NP characteristics using paclitaxel as a model small *** the determination of optimized TFF parameters,the two purification methods were assessed using other model small molecules (*** and resveratrol).The results indicated that the TFF parameters and initial loading of the drug played important roles in the purified NP *** with the centrifugation method,TFF resulted in smaller NP with higher drug *** was able to circumvent issues associated with conventional centrifugation,while yielding similar results,and can potentially serve as a suitable large-scale purification method for polymeric NP.

关键词： Tangential flow filtration Nanoparticle purification Box-Behnken design Acetalated dextran Drug delivery

Possible implications of animal models for the assessment of visceral pain

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Animal Models and Experimental Medicine 2020年第3期3卷 215-228页

作者： Bharata Regmi Manoj k.shah Department of Surgery and Pharmacology Agriculture and Forestry University(AFU)RampurChitwanNepal

Acute pain,provoked generally after the activation of peripheral nociceptors,is an adaptive sensory function that alerts the individual to avoid noxious ***,uncontrolled acute pain has a maladaptive role in sensory activity leading to development of a chronic pain state which persists even after the damage is resolved,or in some cases,in the absence of an initial local acute *** numbers of people suffer from visceral pain at least once during their life span,leading to substantial health care *** studies reporting on the mechanism of visceral pain are accumulating,it is still not precisely ***,this review aims to elucidate the mechanism of visceral pain through an evaluation of different animal models and their application to develop novel therapeutic approaches for treating visceral *** assess the nociceptive responses in viscera,several visceral pain models such as inflammatory,traction,stress and genetic models utilizing different methods of measurement have been *** them,the inflammatory and traction models are widely used for studying the visceral pain mechanism of different disease conditions and post-operative surgery in humans and animals.A hapten,2,4,6-trinitrobenzene sulfonic acid(TNBS),has been extensively used as an inflammatory agent to induce visceral *** traction model seems to cause a strong pain stimulation and autonomic reaction and could thus be the most appropriate model for studying the underlying visceral pain mechanism and for probing the therapeutic efficacies of various anesthetic and analgesics for the treatment of visceral pain and hyperalgesia.

关键词： animal model inflammation noxious stimuli traction visceral pain

Alternative Strategy for Development of Dielectric Calcium Copper Titanate‑Based Electrolytes for Low‑Temperature Solid Oxide Fuel Cells

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Nano-Micro Letters 2025年第1期17卷 310-332页

作者： Sajid Rauf Muhammad Bilal Hanif Zuhra Tayyab Matej Veis MAkYousaf shah Naveed Mushtaq Dmitry Medvedev Yibin Tian Chen Xia Martin Motola Bin Zhu College of Mechatronics and Control Engineering Shenzhen UniversityShenzhen 518060People’s Republic of China Department of Inorganic Chemistry Faculty of Natural SciencesComenius University BratislavaIlkovicova684215 BratislavaSlovakia Energy Storage Joint Research Center School of Energy and EnvironmentSoutheast UniversityNanjing 210096People’s Republic of China Hydrogen Energy Laboratory Ural Federal University620002 EkaterinburgRussia Laboratory of Electrochemical Devices Based on Solid Oxide Proton Electrolytes Institute of High Temperature Electrochemistry620066 EkaterinburgRussia School of Microelectronics Hubei UniversityWuhan 430062People’s Republic of China

The development of low-temperature solid oxide fuel cells(LT-SOFCs)is of significant importance for realizing the widespread application of *** has stimulated a substantial materials research effort in developing high oxide-ion conductivity in the electrolyte layer of *** this context,for the first time,a dielectric material,CaCu_(3)Ti_(4)O_(12)(CCTO)is designed for LT-SOFCs electrolyte application in this *** individual CCTO and its heterostructure materials with a p-type Ni_(0.8)Co_(0.15)Al_(0.05)LiO_(2−δ)(NCAL)semiconductor are evaluated as alternative electrolytes in LT-SOFC at 450–550℃.The single cell with the individual CCTO electrolyte exhibits a power output of approximately 263 mW cm^(-2) and an open-circuit voltage(OCV)of 0.95 V at 550℃,while the cell with the CCTO–NCAL heterostructure electrolyte capably delivers an improved power output of approximately 605 mW cm^(-2) along with a higher OCV over 1.0 V,which indicates the introduction of high hole-conducting NCAL into the CCTO could enhance the cell performance rather than inducing any potential short-circuiting *** is found that these promising outcomes are due to the interplay of the dielectric material,its structure,and overall properties that led to improve electrochemical mechanism in CCTO–***,density functional theory calculations provide the detailed information about the electronic and structural properties of the CCTO and NCAL and their heterostructure CCTO–*** study thus provides a new approach for developing new advanced electrolytes for LT-SOFCs.

关键词： LT-SOFCs Dielectric CaCu_(3)Ti_(4)O_(12) Semiconductor Ni_(0.8)Co_(0.15)Al_(0.05)LiO_(2−δ) Ionic conductivity Heterostructure electrolyte

Synthesis,characterization and antimicrobial activity of some new biquinoline derivatives containing a thiazole moiety

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Chinese Chemical Letters 2012年第4期23卷 454-457页

作者： Nirav k.shah Nimesh M.shah Manish P.Patel Ranjan G.Patel Department of Chemistry Sardar Patel UniversityVallabh Vidyanagar 388120GujaratIndia

A series of new biquinoline derivatives containing a thiazole moiety were synthesized by a one-pot,base-catalyzed cyclocondensation reaction of 2-chloro-3-formyl quinoline,malononitrile and *** the synthesized compounds were characterized by elemental analysis,FT-IR,~1H NMR and ^（13）C NMR *** the synthesized compounds were screened against three bacterial pathogens,namely Bacillus cereus,*** and Escherichia coli and for antifungal activity against three fungal pathogens,Aspergillus niger,Fusarium oxisporum and Rhizopus using the disc diffusion method.

关键词： Quinoline Multicomponent reaction Thiazole Antimicrobial activity

Is myopia a protective factor against central serous chorioretinopathy?

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International Journal of Ophthalmology(English edition) 2016年第2期9卷 266-270页

作者： George J.Manayath Saurabh Arora Hardik Parikh Parag k.shah Sarvesh Tiwari Venkatapathy Narendran Department of Retina and Ocular Oncology Aravind Eye Hospital

AIM： To evaluate if any association exists between central serous chorioretinopathy （CSCR） and the refractive status of the eye. METHODS： This retrospective, institutional, case control study included 499 patients, wherein 262 patients diagnosed as acute CSCR, were compared with an age and gender matched control group of 237 patients. All patients were evaluated with a detailed systemic and ocular history, objective and subjective refractions for both eyes and complete ocular examination by a retina specialist, at all visits. Optical coherence tomography confirmed the diagnosis of CSCR. ~ RESULTS： The mean age was found to be 40.7y in the study group （Group 1） compared to 38 10y in the control group （Group 2）. Most common refractive status in the study group, was emmetropia seen in 191 patients （72.9%）, followed by hypermetropia seen in 47 patients （17.9%） and astigmatism seen in 21 patients （8.0%）. Only 3 subjects （1.1%） had myopia, which was less than or equal to 1.0 D, compared to 70 subjects （29.5%） in the control group, suggesting a statistically significant lower incidence of CSCR among the myopic patients （P〈 0.0001）. With respect to the systemic factors, 26 （9.9%） patients were using systemic steroids in the study group （Group 1） compared to none in the control group （Group 2） suggesting a statistically significant association of CSCR with systemic steroid use （P〈0.05）. No other significant systemic risk factors were noted. CONCLUSION： Though CSCR is a multifactorial disease, myopia serves as a protective factor for CSCR. Thus, myopic eyes are less likely to develop CSCR. Since both retinal pigment epithelium （RPE） and choriocapillaris are postulated in the pathogenesis of CSCR, chorio-retinal thinning and atrophy seen in myopic eyes are less likely to cause CSCR.

关键词： central serous chorioretinopathy refractivestatus myopia

Outcomes of additional posterior to ridge diode laser versus conventional laser anterior to ridge in severe stage 3 retinopathy of prematurity-a randomized control trial

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Annals of Eye Science 2017年第1期2卷 255-259页

作者： Amrutha Sindhu Narendran Siddharth Parag k.shah Venkatapathy Narendran Narendran kalpana Department of Pediatric Retina&Ocular Oncology Aravind Eye Hospital&Postgraduate Institute of OphthalmologyCoimbatoreTamilnaduIndia

Background:Laser photocoagulation restricted to ablation of the avascular retina has been the conventional but not a completely effective treatment strategy in the management of threshold retinopathy of prematurity(ROP).The purpose of this study was to compare the structural outcomes of additional posterior to ridge diode laser compared to conventional diode laser to avascular retina alone in threshold stage III ***:This was a prospective,randomized study involving infants diagnosed with threshold stage III ROP in one or both the *** infants were randomized into control and study *** under the control group underwent conventional laser to avascular retina alone while infants under the study group received additional two rows of laser posterior to the ridge in the vascular *** infants were followed up at 2 weeks,1 month and up to 6 months after the laser ***:During the study period of 1 year,42 eyes of 24 infants were recruited into this study with 21 eyes in each *** mean birth weight was 1,310.48±400.92 g in the test group and 1,341.9±396.2 g in the control *** mean post conceptional age at the time of intervention was 36.43±2.79 weeks in test group and 36.29±2.55 weeks in the control *** 1-month post laser,19 eyes in the study group showed regression of neovascularization laser compared to 18 eyes in the control *** at the end of 3 and 6 months post laser,both groups had showed similar rates regression of neovascularization(19 of 21 eyes in both groups).Five eyes in the study group and six in the control group required additional laser *** eyes in the study group and one eye in the control group developed post laser vitreous ***:Posterior to ridge laser treatment for severe stage 3 ROP did not show any additional benefit compared to conventional laser.

关键词： Retinopathy of prematurity(ROP) diode laser posterior to ridge laser

Restless head syndrome:A retrospective study

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World Journal of Methodology 2025年第1期15卷 51-59页

作者： Sanjay Prakash Varoon Vadodaria Niraj Chawda Chetsi S shah Anurag Prakash Department of Neurology Smt.B.K.Shah Medical Institute and Research CentreSumandeep VidyapeethVadodara 391760GujarātIndia Department of Medicine Smt.B.K.Shah Medical Institute and Research CentreSumandeep VidyapeethVadodara 391760GujarātIndia Department of Medicine Parul Institute of Medical Sciences and Research CentreParul University WaghodiaVadodara 391760India

BACkGROUND Restless legs syndrome(RLS)is characterized by an urge to move with an unpleasant sensation in the lower *** typically affects the ***,it can also affect several other body regions,such as the arms,abdomen,face,neck,head,and genital *** are only a few reports of the RLS variant affecting the *** To assess the epidemiological,clinical,and other aspects of the RLS variant affecting the *** We conducted a retrospective study of 17 adult patients(>18 years)who met the RLS criteria and simultaneously experienced RLS-like symptoms in the *** The median age at which symptoms appeared was 41.6 *** and females were equally affected(1.1:1).All 17 patients had uncomfortable sensations in the lower *** or disturbed sleep was the most common comorbidity(n=16,88.2%).However,headache was the most common presenting or primary symptom(n=10,70.5%).Dizziness or an abnormal sensation in the head was the second most common presenting symptom(5 patients,29.4%).Other presenting features were leg pain,backache,and generalized body *** patients responded favorably to dopaminergic *** If RLS-related unpleasant sensations and pain are felt in the head,they may be misinterpreted as headache,dizziness,or psychosomatic *** and headaches in a subset of patients may be two phenotypic manifestations of the same disorder.

关键词： Restless legs syndrome Restless head syndrome Dopamine Headache Migraine Tension-type headache

Leveraging real-time data to drive quality improvement in a pediatric health system

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Pediatric Investigation 2018年第3期2卷 184-187页

作者： Sopnil Bhattarai Rahul k.shah Children's National Health System WashingtonDCUSA Division of Otolaryngology Children's National Health SystemWashingtonDCUSA

We are inundated by data;healthcare is no *** electronic medical record,the numerous patient care monitors,and the thousands of medications to be reconciled with specific dosing parameters are a few examples of the omnipresent and intimidating nature of data in *** the world,healthcare without data does not *** data represent many forms but are quickly moving towards electronic *** ubiquitous as data are the near universal finding that such data are *** is an urgent need for real-time data in improving processes and ultimately outcomes in *** data lag by four to eight weeks,if not longer,then true change cannot occur and harm continues in that *** review article discusses the urgent need for real-time data and demonstrates examples of how Children's National Medical Center in Washington,DC uses real-time data to drive outcomes.

关键词： Hospital acquired conditions (HAC) Joint Commission Preventable harm index Quality improvement Real-time data Tracer

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