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Exploring the potential of porous silicas as a carrier system for dissolution rate enhancement of artemether

Asian Journal of Pharmaceutical Sciences 2016年第6期11卷 760-770页

作者： jaywant n.pawar Harita R.Desai Kailas K.Moravkar Deepak K.Khanna Purnima D.Amin Department of Pharmaceutical Sciences and Technology Institute of Chemical Technology(Elite Status)N.P.MargMatunga(E)Mumbai 400019India Applied Technology Inorganic MaterialsEvonik Degussa India Pvt.Ltd.Krislon HouseSakivihar RoadSakinakaAndheri(East)Mumbai 400069India

Malaria is a parasitic and vector determined blood-conceived infectious disease transmitted through infected mosquitoes. Anti-malarial drug resistance is a major health problem, which hinders the control of malaria. A Results of a survey of drug-resistant malaria demonstrated safe proclivity to nearby all anti-malarial regimes accessible except from artemisinin and its derivatives. Artemether is a BCS class IV drug effective against acute and severe falciparum malaria;hence there is a strong need to improve its solubility. Silica is one of the most widely studied excipients. Silica can be used in solubility enhancement by preparing its solid solution/dispersion with the drug. The objective of this research was to improve dissolution rate of Artemether using non-precipitated porous silica(Aeroperl 300 Pharma) and precipitated silica like EXP. 9555, EXP. 9560, and EXP. 9565. Specific surface area calculated from BET method of porous silicas viz. APL 300(A), Exp. 9555(B), Exp. 9560(C), Exp. 9565(D) was found to be 294.13 m^2/g(A), 256.02 m^2/g(B), 213.62 m^2/g(C) and 207.22 m^2/g(D) *** drug release from the developed formulation was found to be significantly higher as compared to neat ARM. This improved solubility and release kinetics of ARM may be attributed to high surface area, improved wettability and decreased crystallinity. Solid-state characterization of the developed optimized formulation F3 was carried out with respect to FTIR chemical imaging, XRD,SEM, and DSC. All the porous silicas which we have explored in the present context showed a significant capability as a carrier for solubility enhancement of ARM.

关键词： Artemether Solubility Solid dispersion Porous silica Aeropearl 300

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Development of amorphous dispersions of artemether with hydrophilic polymers via spray drying: Physicochemical and in silico studies

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Asian Journal of Pharmaceutical Sciences 2016年第3期11卷 385-395页

作者： jaywant n.pawar Rahul T.Shete Avinash B.Gangurde Kailas K.Moravkar Sharadchandra D.Javeer Divakar R.Jaiswar Purnima D.Amin Department of Pharmaceutical Sciences and Technology Institute of Chemical Technology Nathalal Parekh Marg

Artemether(ARM) is a poorly water soluble and poorly permeable drug effective against acute and severe falciparum malaria, hence there is a strong need to improve its solubility. The objective of the study was to enhance the solubility and dissolution rate of ARM by preparation of solid dispersions using spray-drying technique. Solid dispersions of ARM were prepared with Soluplus, Kollidon VA 64, HPMC and Eudragit EPO at weight ratios of 1:1, 1:2,1:3 using spray drying technology, and characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry(DSC), and X-ray powder diffraction(XRD) to identify the physicochemical interaction between drug and carrier, as well as effect on *** prepared solid dispersion of ARM with polymers showed reduced crystallinity as compared to neat ARM, which was confirmed by DSC and XRD. Drug/polymer interactions were studied in-silico by docking and molecular dynamics which indicated formation of van der Waals type of interactions of ARM with the polymers. Based on solubility studies, the optimum drug/Soluplus ratio was found to be 1:3. The dissolution studies of formulation SD3 showed highest drug release up to 82% compared to neat ARM giving only 20% at 60 minutes. The spray-dried products were free of crystalline ARM; possessed higher dissolution rates, and were stable over a period according to ICH guidelines. These findings suggest that an amorphous solid dispersion of ARM could be a viable option for enhancing the dissolution rate of ARM.

关键词： Artemether Docking In silico study Solid dispersion Spray drying

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Study of boundary layer characteristics during the landfalling of a nisarga cyclone

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TROPICAL CYCLOnE RESEARCH AnD REVIEW 2024年第2期13卷 55-71页

作者： pawar, Rani P. Priyadarshini, Prajna Dharmaraj, T. nade, Dada P. Patil, Mahendra n. Patil, Omkar M. Victor, n. Jeni pawar, Sambhaji M. Kanase, D. G. pawar, Sunil D. Indian Inst Trop Meteorol Minist Earth Sci Pune Maharashtra India Bharati Vidyapeeths Dr Patangrao Kadam Mahavidya Dept Phys Sangli India IIG KSK Geomagnet Res Lab Allahabad Uttar Pradesh India Sanjay Ghodawat Univ Kolhapur Dept Phys Kolhapur India

One of the most important parameters in meteorology is the mean wind pro fi le in the tropical cyclone boundary layer. The vertical pro fi le of wind speed and wind direction were measured during the period of the nisarga cyclone from May 31st, 2020, to June 5th, 2020, using the newly installed Phased Array Doppler Sodar system at the Center for Space and Atmospheric Science (CSAS), Sanjay Ghodawat University, Kolhapur (16.74 degrees n, 74.37 degrees E; near India ' s western coast). Our analysis revealed that the maximum mean wind speed was 17 m/s on June 3, 2020, at 10:00 IST. It also shows the change in wind direction from southwest to southeast on June 2 and 3, 2020. Daily high-resolution reanalysis data in the domain, 0 - 25 degrees n, 65 - 110 degrees E, during the period from May 31st to June 5th, 2020, revealed the variation of the atmospheric pressure of the nisarga cyclone from 1000 to 1008 hPa, sea surface temperature (SST) between 30 degrees C and 31 degrees C, outgoing longwave radiation (OLR) between 100 and 240 Wm-2 , wind speed between 3 and 15 m/s, and low values of vertical wind shear (VWS) were observed to the north of nisarga track. These observations may provide more insights for the study of boundary layer turbulence during cyclonic activities. (c) 2024 The Shanghai Typhoon Institute of China Meteorological Administration. Publishing services by Elsevier B.V. on behalf of KeAi Communication Co. Ltd. This is an open access article under the CC BY license (http://***/licenses/by/4.0/).

关键词： Phased Array Doppler Sodar Tropical cyclone Atmospheric boundary layer Vertical turbulence intensity VERTICAL WInD SHEAR TROPICAL CYCLOnES SODAR OBSERVATIOnS GRAVITY-WAVES PERSPECTIVES TEMPERATURE InTEnSITY MOnSOOn BEnGAL BAY

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Characterization of early maturing elite genotypes based on MTSI and MGIDI indexes:an illustration in upland cotton(Gossypium hirsutum L.)

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Journal of Cotton Research 2024年第3期7卷 253-265页

作者： D S RAJ Supritha PATIL Rajesh S. PATIL Bhuvaneshwara R. nAYAK Spurthi n. pawar Kasu n. Department of Genetics and Plant Breeding College of AgricultureUniversity of Agricultural SciencesDharwad 580005India Agricultural Research Station Dharwad 580005India Department of Biotechnology College of AgricultureUniversity of Agricultural SciencesDharwad 580005India Department of Crop Physiology College of AgricultureUniversity of Agricultural SciencesDharwad 580005India

Background Globally,the cultivation of cotton is constrained by its tendency for extended periods of *** maturity plays a potential role in rainfed-based multiple cropping system especially in the current era of climate *** the current study,a set of 20 diverse Gossypium hirsutum genotypes were evaluated in two crop seasons with three planting densities and assessed for 11 morphological traits related to early *** study aimed to identify genotype(s)that mature rapidly and accomplish well under diverse environmental conditions based on the two robust multivariate techniques called multi-trait stability index(MTSI)and multi-trait genotype-ideotype distance index(MGIDI).Results MTSI analysis revealed that out of the 20 genotypes,three genotypes,viz.,nnDC-30,A-2,and S-32 accomplished well in terms of early maturity traits in two ***,three genotypes were selected using MGIDI method for each planting densities with a selection intensity of 15%.The strengths and weaknesses of the genotypes selected based on MGIDI method highlighted that the breeders could focus on developing early-maturing genotypes with specific traits such as days to first flower and boll *** selected genotypes exhibited positive genetic gains for traits related to earliness and a successful harvest during the first and second ***,there were negative gains for traits related to flowering and boll *** The study identified three genotypes exhibiting early maturity and accomplished well under different planting *** multivariate methods(MTSI and MGIDI)serve as novel approaches for selecting desired genotypes in plant breeding programs,especially across various growing *** methods offer exclusive benefits and can easily construe and minimize multicollinearity issues.

关键词： Cotton MTSI MGIDI Genotype environment interaction Early maturity Multi-trait Multi-environment

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Water Resource Management in the Intermountain Izeh Plain,Southwest of Iran

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Journal of Mountain Science 2009年第1期6卷 25-41页

作者： Kalantari.n.pawar.n.J Keshavarzi.M.R Geology Department Shahid Chamran UniversityAhvazIran Geology Department University of PunePune-411 007India

Ever growing demand for water for agricultural activities in the Izeh Plain has enhanced the use of groundwater. Due to enormous groundwater abstraction since 1985, the overall static water level has receded by more than 5 meters reflecting that the aquifer is under stress condition. As a result, interest is focused on application of artificial recharge as an option for groundwater management to augment water supply in this area. Therefore, in the present investigations, suitable sites for artificial recharge were selected by an integrated surface and sub-surface assessment of the area. On the basis of the data collected from four target points, it was realized that the selected sites for artificial recharge could not meet water demand of the area. In this study attention was also paid to utilization of the existing Miangran Lake water as an alternative to combat water shortage for irrigation. The study further indicated that the available Miangran Lake water could be used for irrigation of the reclaimed agricultural land and enabling to convert 20o0 hectares of rain-fed land into irrigation. The total cost to utilize lake water is US$ 2,756,729 and it was estimated that the project could recoup the investment within 5 years which is quite reasonable in this water scarcity prone area.

关键词： Artificial recharge stream MiangranLake groundwater Izeh Plain

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novel,efficient,and green procedure for the synthesis of 1,5-benzodiazepines catalyzed by MgBr_2 in aqueous media

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Chinese Chemical Letters 2009年第1期20卷 32-36页

作者： Shivaji S.pawar Murlidhar S.Shingare Shivaji n.Thore Department of Chemistry Vinyakrao Patil Mahavidyala Vaijapur Department of Chemistry Dr.Babasaheb Ambedkar Marathwada University

MgBr2 performs as a novel catalyst for the synthesis of various 1,5-benzodiazepine derivatives from wide range of substituted o- phenylenediamines and various ketones in good to excellent isolated yields （93-98%） using water as solvent at ambient temperature. Several solvents were examined for this reaction; however, in terms of reaction yield and time, water was found to be the optimum solvent. The remarkable advantages offered by this method are easily and inexpensive available catalyst, simple procedure, mild conditions, much faster （40-60 man） reactions and good to excellent yields of products.

关键词： MgBr2 o-Phenylenediamines Ketones Aqueous media 1,5-Benzodiazepine

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Glyoxylic acid as catalyst:A simple selective synthesis of 1,2-disubstituted benzimidazoles in aqueous media

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Chinese Chemical Letters 2008年第9期19卷 1055-1058页

作者： Shivaji S.pawar Deepak V.Dekhane Murlidhar S.Shingare Shivaji n.Thore Department of Chemistry Vinyakrao Patil Mahavidyala VaijapurAurangabad 423701(M.S.)India Department of Chemistry Dr.Babasaheb Ambedkar Marathwada UniversityAurangabad 431004(M.S.)India

Glyoxylic acid （5 mol%） performs as a novel highly water-soluble catalyst for the synthesis of 2-aryl-l-arylmethyl-lH- benzimidazoles from a wide range of substituted o-phenylenediamines and various substituted aldehydes in good to excellent isolated yields （85-95%） using water as solvent at ambient temperature. The remarkable advantages offered by this method are easily and inexpensive available catalyst, simple procedure, mild conditions, much faster （20--40 rain） reactions and excellent yields of products.

关键词： Glyoxylic acid Benzimidazoles Aqueous media 2-Aryl-l-arylmethyl-lH-benzimidazoles o-Phenylenediamines and aldehydes

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Central nervous system activity of Illicium verum fruit extracts

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Asian Pacific Journal of Tropical Medicine 2013年第11期6卷 869-875页

作者： Divya Chouksey neeraj Upmanyu RS pawar Phytochemistry and Pharmacognosy Division VNS Institute of PharmacyNeelbudBHOPALM.P.India R.K.D.F.College of Pharmacy Hoshangabad RoadBhopalM.P.-462047.India

Objective:To research the acute toxicity of Illicium verum(***)fruit extracts and its action on central nervous ***:The TLC and HPTLC techniques were used as fingerprints to determine the chemical components present in *** albino rats and mice were utilized for *** powdered material was successively extracted with n-hexane,ethyl acetate and methanol using a Soxhlet *** toxicity studies were performed as per OECD *** CnS activity was evaluated on parameters of general behavior,sleeping pattern,locomotor activity,anxicty and myocoordination *** animals were trained for seven days prior to experiments and the divided into five groups with six animals in *** drug was administered by intraperitoneal route according to body *** dosing was done as prescribed in each ***:Toxicity studies reported 2 000 mg/kg as toxicological dose and 1/10 of the same dose was taken as therapeutic dose Intraperitoneal injection of all extracts at dose of 200 mg prolonged phenobarbitone induced sleeping time,produced alteration in general behavior pattern,reduced locomotor activity and produced anxiolytic effects but the extracts do not significantly alter muscles coordination *** three extracts of *** at the dose of 200 mg,methanol extract was found to produce more prominent effects,then hexane and ethylacetate ***:The observation suggested that the extracts of I. verum possess potent CnS depressant action and anxiolytic effect without interfering with motor coordination.

关键词： Illicium verum TLC HPTLC Anxiolytic CnS depressant

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Differently synthesized gold nanoparticles respond differently to functionalization with L-amino acids

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Particuology 2020年第5期18卷 97-104页

作者： Darshana V.Havaldar Reshma V.Patil Disha n.Moholkar Priyanka S.Magdum Akash P.Vadrale Kiran D.pawar School of nanoscience and Biotechnology Shivaji UniversityKolhapurMaharashtraIndia

The potential utility of gold nanoparticles(AunPs)synthesized via different methods for biomedical applications vary greatly due to inherent differences in their surface *** the present study,we investigated the functionalization of AunPs synthesized by chemical reduction,plant extract,and bacteria-mediated methods with 22 L-amino *** produced by bacteria-mediated(B_AunPs)and plant-mediated(P_AunPs)methods showed good potential,as they were able to be functionalized with six(histidine,lysine,methionine,phenylalanine,tryptophan,and tyrosine)and four(cystine,tryptophan,tyrosine,and valine)amino acids,*** contrast,AunPs produced by chemical reduction(C_AunPs)were not found to be suitable for *** functionalization conditions were found to be amino acid concentration of 20-25 mM and neutral pH(7)for P_AunPs,whereas B_AunPs tolerated more variable *** electrophoretic mobility of P_AunPs after functionalization indicated that these nanoparticles were less sensitive than B_AunPs to the deviations from optimal conditions.A significant change in mobility was observed when B_AunPs were functionalized with either methionine or ***,the results of this study suggest that the suitability of the three differently synthesized AunPs with amino acids is in the following order:B_AunPs>P_AunPs>C_AunPs.

关键词： Gold nanoparticles Biogenic synthesis Amino acids Functionalization Electrophoretic mobility

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Lithium bromide catalyzed solvent free method for synthesis of 2-substituted benzimidazoles and imidazopyridines

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Chinese Chemical Letters 2010年第5期21卷 519-523页

作者： Deepak V.Dekhane Shivaji S.pawar Sunil V.Gupta Murlidhar S.Shingare Shivaji n.Thore Department of Chemistry Vinyakrao Patil Mahavidyala VaijapurAurangabad 423701MSIndia Department of Chemistry Dr.Babasaheb Ambedkar Marathwada UniversityAurangabad 431004MSIndia

The first successful lithium bromide mediated solvent free condensation of arylenediamine and esters to obtain 2-substituted benzimidazole and imidazopyridine in good to excellent yields is described.

关键词： Benzimidazoles Arylenediamine Aliphatic esters Lithium bromide Imidazopyridines

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