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Pharmacokinetic aspects and in vitro–in vivo correlation potential for lipid-based formulations

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Acta Pharmaceutica Sinica B 2014年第5期4卷 333-349页

作者： Sivacharan Kollipara rajesh kumar Gandhi Formulations Department Pharmaceutical&Analytical DevelopmentTechnical R&DNovartis Healthcare Pvt.Ltd.Hyderabad 500078Andhra PradeshIndia

Lipid-based formulations have been an attractive choice among novel drug delivery systems for enhancing the solubility and bioavailability of poorly soluble drugs due to their ability to keep the drug in solubilized state in the gastrointestinal *** formulations offer multiple advantages such as reduction in food effect and inter-individual variability,ease of preparation,and the possibility of manufacturing using common excipients available in the *** these advantages,very few products are available in the present market,perhaps due to limited knowledge in the in vitro tests(for prediction of in vivo fate)and lack of understanding of the mechanisms behind pharmacokinetic and biopharmaceutical aspects of lipid formulations after oral *** current review aims to provide a detailed understanding of the in vivo processing steps involved after oral administration of lipid formulations,their pharmacokinetic aspects and in vitro in vivo correlation(IVIVC)*** pharmacokinetic and biopharmaceutical aspects such as formulation dispersion and lipid digestion,bioavailability enhancement mechanisms,impact of excipients on efflux transporters,and lymphatic transport are discussed with *** addition,various IVIVC approaches towards predicting in vivo data from in vitro dispersion/precipitation,in vitro lipolysis and ex vivo permeation studies are also discussed in detail with help of case studies.

关键词： Pharmacokinetics Lipolysis IVIVC Efflux transporters Lymphatic delivery Food effect

Distributed resource scheduling in smart grid with electric vehicle deployment using fireworks algorithm

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Journal of Modern Power Systems and Clean Energy 2016年第2期4卷 188-199页

作者： K.Srikanth REDDY Lokesh kumar PANWAR rajesh kumar Bijaya Ketan PANIGRAHI IIT Delhi New DelhiIndia MNIT Jaipur JaipurRajasthanIndia

Global warming and climate change are two key probing issues in the present *** electricity sector and transportation sector are two principle entities propelling both these *** from these two sectors can be offset by switching to greener ways of transportation through the electric vehicle (EV) and renewable energy technologies (RET).Thus,effective scheduling of both resources holds the key to sustainable *** paper presents a scheduling scenario-based approach in the smart *** formulation with dual objective function including both emissions and cost is developed for conventional unit commitment with EV and RET *** this work,the scheduling and commitment problem is solved using the fireworks algorithm which mimics explosion of fireworks in the sky to define search space and the distance between associated sparks to evaluate global ***,binary coded fireworks algorithm is developed for the proposed scheduling problem in the smart ***,possible scenarios inconventional as well as smart grid are put *** that,the proposed methodology is simulated using a test system with thermal generators.

关键词： Unit commitment problem(UCP) Binary fireworks algorithm(BFWA) Constrained optimization Renewable energy technologies(RETs) Plug-in electric vehicle(PEV)

Perturbing tumor cell metabolism with a Ru(Ⅱ)photo-redox catalyst to reverse the multidrug resistance of lung cancer

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Science China Chemistry 2023年第5期66卷 1482-1488页

作者： Siqi Wei Hui Liang Anyi Dao Yuzhen Xie Fengshu Cao Qingyan Ren Ashish kumar yadav rajesh Kushwaha Arif Ali Mandal Samya Banerjee Pingyu Zhang Shaomin Ji Huaiyi Huang School of Pharmaceutical Science(Shenzhen)Shen Zhen Campus of Sun Yat-sen University Shenzhen 518107China Light Industry and Chemical Engineering College Guangdong University of TechnologyGuangzhou 510006China College of Chemistry and Environmental Engineering Shenzhen UniversityShenzhen 518060China Department of Chemistry Indian Institute of Technology(BHU)Varanasi UP-221005India

The novel concept of enzyme photocatalysis has recently attracted much attention in developing anticancer ***,the relationship between coenzyme depletion and cellular metabolomic changes has rarely been ***,we report the rational design of a deep-red light-triggered bis-tridentate Ru(Ⅱ)photocatalyst(Ru3),which induces cell metabolism disorder to combat multidrug ***3 exhibits promising multiple triplet excited states,a long lifetime,and high photocatalytic activity toward the ***,Ru3 shows high phototherapeutic activity(photo index=191–833)against diverse resistant(cisplatin,5-fluorouracil,or paclitaxel)lung cancer cells by inhibiting cellular peptide,lipid,and glycerophospholipid *** believe that cell metabolism inhibition by photo-redox catalysts is an effective form of therapeutics for drug-resistant cancer cells.

关键词： drug resistance photocatalytic therapy Ru(Ⅱ)photocatalyst NADPH cell metabonomic

Optimization of Cognitive Femtocell Network via Oppositional Beetle Swarm Optimization Algorithm

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Intelligent Automation & Soft Computing 2023年第4期36卷 819-832页

作者： K.rajesh kumar M.Vijayakumar Department of ECE Adhiyamaan College of EngineeringHosurTamilnaduIndia Department of EEE K.S.R.College of EngineeringTiruchengodeTamilnaduIndia

In past decades,cellular networks have raised the usage of spectrum resources due to the victory of mobile broadband *** devices create massive data than ever before,facing the way cellular networks are installed pre-sently for satisfying the increased trafﬁc *** development of a new exclusive spectrum offered to meet up the trafﬁc requirements is challenging as spectrum resources are limited,hence *** radio technology is pre-sented to increase the pool of existing spectrum resources for mobile users via Femtocells,placed on the top of the available macrocell network for sharing the same ***,the concurrent reuse of spectrum resources from Femto networks poses destructive interference on macro *** resolve this issue,this paper introduces an optimal channel allocation model using the Oppo-sitional Beetle Swarm Optimization Algorithm(OBSOA)to allocate the channel with interference avoidance.A new OBSOA is derived in this paper by the inclu-sion of opposition-based learning(OBL)in *** algorithm allocates the channels used by PUs(PUs)to the secondary users(SUs)in such a way that inter-ference is *** proposed approach is implemented in the MATrix LABoratory(MATLAB)*** performance of this proposed approach is evaluated in terms of several measures and the experimental outcome veriﬁed the superior nature of the OBSOA-based channel allocation *** mod-el has resulted in a maximum signal-to-interference-plus-noise ratio value of 86.42 dB.

关键词： Femto networks channel allocation spectrum reuse cognitive network

Pharmacokinetic, pharmacodynamic, and neurochemical investigations of lamotrigine-pentylenetetrazole kindled mice to ascertain it as a reliable model for clinical drug-resistant epilepsy

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Animal Models and Experimental Medicine 2020年第3期3卷 245-255页

作者： Sandeep kumar rajesh K.Goel Department of Pharmaceutical Sciences&Drug Research Punjabi UniversityPatialaPunjabIndia

Background:Pentylenetetrazole kindling has long been used for the screening of investigational antiseizure *** presence of lamotrigine,at a very low dose,does not hamper kindling in mice;rather it modifies this epileptogenesis process into drug-resistant *** lamotrigine-pentylenetetrazole kindled mice show resistance to lamotrigine,phenytoin,and *** may also be possible that other licensed antiseizure drugs,like the mentioned drugs,remain ineffective in this model;therefore,this was the subject of this ***:Swiss albino mice were kindled with pentylenetetrazole for 35 days in the presence of either methylcellulose vehicle or lamotrigine(subtherapeutic dose,ie,5 mg/kg).Vehicle vs lamotrigine-kindled mice were compared in terms of(a)resistance/response toward nine antiseizure drugs applied as monotherapies and two drug combinations;(b)lamotrigine bioavailability in blood and brain;(c)blood-brain barrier integrity;and(d)amino acids and monoamines in the cerebral cortex and ***:Lamotrigine vs vehicle-kindled mice are similar(or not significantly different P>.05 from each other)in terms of(a)response toward drug combinations;(b)lamotrigine bioavailability;and(c)blood-brain barrier integrity except for,significantly(P<.05)reduced taurine and increased glutamate in the cerebral cortex and *** from these,lamotrigine-kindled mice show significant(P<.05)resistant to lamotrigine(15 mg/kg),levetiracetam(40 mg/kg);carbamazepine(40 mg/kg),zonisamide(100 mg/kg),gabapentin(224 mg/kg),pregabalin(30 mg/kg),phenytoin(35 mg/kg),and topiramate(300 mg/kg).Conclusion:Lamotrigine-pentylenetetrazole kindling takes longer to develop(~5 weeks)in comparison to lamotrigine-amygdale(~4 weeks)and lamotriginecorneal(~2 weeks)kindling ***,drug screening through this model may yield superior drugs with novel antiseizure mechanisms.

关键词： animal models drug-resistant epilepsy kindling lamotrigine refractory epilepsy

Adaptive sensitive frequency band selection for VMD to identify defective components of an axial piston pump

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Chinese Journal of Aeronautics 2022年第1期35卷 250-265页

作者： Anil kumar C.P.GANDHI Hesheng TANG Govind VASHISHTHA rajesh kumar Yuqing ZHOU Jiawei XIANG College of Mechanical and Eilectrical Engineering Wenzhou UniversityWenzhou 325035China Amity University Uttar Pradesh Noida 201313India Ray at Bahru University Mohali 140104India Sant Longowal Institute of Engineering and Technology Longowal 148106India

The underlying study investigates single valued neutrosophic entropy based adaptive sensitive frequency band selection for variational mode decomposition(VMD)for the purpose of identifying defective components in an axial *** proposed methodology is applied in the following ***,VMD is applied for decomposing vibration signals into various frequency bands,called as *** computing energy of each VMD,the lower(minimum)and upper(maximum)bounds from these energy readings are extracted for defect conditions,such as outer race,inner race,worn piston,faulty cylinder and valve plate,and blocked hole of the ***,energy interval ranges are obtained and further converted into the form of single valued neutrosophic sets(SVNSs).Then,the proposed neutrosophic entropy measure is deployed for quantifying the non-linear connection between each bearing defect conditions and various frequency *** mode having maximum neutrosophic entropy value is designated to the“most sensitive”frequency ***,envelope demodulation is applied to the most sensitive selected frequency band for finding defective *** proposed neutrosophic entropy and VMD based methodology is effective in providing a better insight for selecting suitable frequency band for carrying out envelope demodulation in comparison to existing methods.

关键词： Axial piston pump Frequency band selection Reciprocating machinery Rotating machinery Trigonometric neutrosophic entropy Variational mode decomposition Vibration

Effect of stacking sequence on physical, mechanical and tribological properties of glass-carbon hybrid composites

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Friction 2014年第4期2卷 354-364页

作者： Gaurav AGARWAL Amar PATNAIK rajesh kumar SHARMA Jyoti AGARWAL Department of Mechanical Engineering Invertis UniversityBareillyIndia Department of Mechanical Engineering National Institute of Technology(NIT)HamirpurIndia Department of Computer Engineering Rajshree Institute of Management&Technology(RIMT)BareillyIndia

A study was done to determine the effect of best stacking sequence(position and orientation)on the mechanical properties,friction and wear response of hybrid *** main purpose of the study was to determine the best available stacking sequence for which the physical,mechanical and three body abrasive wear rate is *** for mechanical properties(tensile strength,flexural strength,inter laminar shear strength,impact strength and hardness)was done on glass-carbon hybrid *** composites were then subjected to test for three body abrasive wear on a designed experimental *** different factors(sliding velocity,fabric weight percentage,normal load,sliding distance and abrasive particle size)varied in steps to evaluate the friction and three body abrasive wear response of the *** design of experiment using Taguchi’s orthogonal array and analysis of variance(ANOVA)was applied to find out minimum specific wear *** results revealed the significance in arrangement of two different layers of fabric(glass and carbon)and the difference in properties obtained by *** Taguchi experimental analysis it has been observed that three body abrasive wear rate is minimum at 72 cm/s sliding velocity,30 wt.%fabric content,80 N normal load,90 m sliding distance and 125μm abrasive particle *** scanning electron microscope(SEM)studies revealed the dynamics of three‐body abrasive wear and underlying micro‐mechanisms that result in the analysis of three body abrasive wear.

关键词： hybrid composite stacking sequence Taguchi’s method wear mechanism

Proteomic analysis of differentially abundant proteins in the embryo and endosperm of Givotia moluccana (L.) Sreem

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Journal of Forestry Research 2020年第6期31卷 2097-2109页

作者： Durgeshwar Pullaiahgari rajesh kumar Meena Swaroopa Rani Tirupaati Padmaja Gudipalli Department of Plant Sciences School of Life SciencesUniversity of HyderabadHyderabadTelangana 500046India

Proteome analysis of embryo and endosperm of Givotia moluccana,a promising angiosperm tree species was carried out using two-dimensional electrophoresis combined with matrix-assisted laser desorption/ionization time of flight to identify differentially abundant proteins and their possible *** study revealed the presence of 492 protein spots in the embryo and 432 in the endosperm,and the relative abundance of 44 spots varied significantly between the *** the 21 functionally characterized protein spots,14.3%were involved in metabolism and energy,28.6%in protein destination and storage,14.3%in defense and stress and 19%in cell growth and *** embryo-specific protein ATPdependent zinc metalloprotease FtsH is predicted to be involved in chloroplast biogenesis and the endospermspecific protein hydroxyacyl-ACP dehydratase in fatty acid *** results suggested that the seeds have proteins required for germination and for stress responses.

关键词： Proteome Embryo Endosperm Euphorbiaceae Givotia moluccana Forest tree 2-DE

Effects of in ovo delivered xylo-and mannan-oligosaccharides on growth performance,intestinal immunity,cecal short-chain fatty acids,and cecal microbiota of broilers

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Journal of Animal Science and Biotechnology 2022年第4期13卷 1099-1114页

作者： Amit kumar Singh Utsav Prakash Tiwari Birendra Mishra rajesh Jha Department of Human Nutrition Food and Animal SciencesUniversity of Hawaii at Manoa1955 East-West RdHonoluluHI 96822USA

Background:This study investigated a novel in ovo feeding strategy to determine the prebiotic effects of xylo-and mannan-oligosaccharides(XOS and MOS)differing in the degree of polymerization.A total of 192 fertilized eggs were divided into 6 treatment groups:i)normal saline control(NSC),ii)xylotriose(XOS3),iii)xylotetraose(XOS4),iv)mannotriose(MOS3),v)mannotetraose(MOS4),and vi)no injection control(NIC),each containing 4 replicate trays with 8 eggs per *** d 17 of incubation,3 mg of oligosaccharides(except for controls)dissolved in 0.5 mL of 0.85%normal saline were injected into the amnion of Cobb 500 broilers *** hatch,the chicks were raised for 28 d under standard husbandry practices and were fed a commercial broilers diet ad libitum,and samples were collected ***:The hatchability,growth performance,and relative weights of breast,drumstick,liver,and proventriculus were not different among the treatments(P>0.05).The XOS3 injection increased the total short-chain fatty acid production at d 28 compared with both control groups(P0.05).On the hatch day,the expression level of the CD3 gene(a T cell marker)was increased by XOS3,while the IL-10 gene(a marker of anti-inflammatory cytokine)was reduced by MOS4(P0.05),except XOS4 increased IL-4 compared with NSC(P<0.05).The broilers in the MOS4 group had higher operational taxonomic units(OTUs)and had more differentially abundant taxa,including order Lactobacillales and family Leuconostocaceae(P<0.05)than both controls on d *** predictive functional profiling indicated that the linoleic acid metabolism pathway w

关键词： Broilers Gut health Immunity in ovo Mannanoligosaccharides Microbiota Oligosaccharides Prebiotics Xylooligosaccharides