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Research and application of fluorescence system on norfloxacin-terbium-phen-sDbs

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Journal of Rare Earths 2012年第8期30卷 842-846页

作者：吕玉光李烨赵悦辉杨立滨江欣王莹吴兴华 college of pharmacy Jiamusi University Provincial Key Laboratory of biological Agents College of PharmacyJiamusi University Institute for Drug Control of Jiamusi

Fluorescence characteristics of complex system of rare earth terbium （Tb3＋）, norfloxacin, 1,10-phenanthroline（1,10-phen） and sur- factant sodium dodecyl benzene sulfonate （sDbs） had been studied by using fluorescence spectroscopy. In a buffer solution （pH=6.3）, the fluorescence intensity of the norfloxacin-Tb3＋（NFLX-Tb3＋） system had been remarkably enhanced by sDbs and 1,10-Phen. When excited at 335 nm, a good linear relationship between fluorescence intensity of NFLX-Tb3＋ system and NFLX concentration was obtained in the range of 8× 10-8-4× 10-6 mol/L, and the linear equation was F=2× 10^8 CNFLX＋22.7 with correlation coefficient of 0.9959. In addition, this method was compared with some previous literatures, the proposed method had relatively higher sensitivity and lower detect limit. The method was sim- ple, rapid, sensitive, practical and suitable for direct analysis of pharmaceutical preparation. It was successfully applied to determine the cap- sules, human serum and urine in real pharmaceutical samples.

关键词： norfloxacin terbium 1,10-phenanthroline sodium dodecyl benzene sulfonate fluorescence spectra pharmaceutical analysis rare earths

17β-Estradiol up-regulates UDP-glucuronosyltransferase 1A9 expression via estrogen receptor α

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Acta Pharmaceutica sinica b 2016年第5期6卷 504-509页

作者： sung-joon Cho Miaoran Ning Yanyan Zhang Leah H.Rubin Hyunyoung Jeong Department of biopharmaceutical sciences College of PharmacyUniversity of Illinois at Chicago Department of pharmacy Practice College of PharmacyUniversity of Illinois at Chicago Department of Psychiatry University of Illinois at Chicago

UDP-glucuronosyltransferase 1A9(UGT1A9) is a major phase II enzyme responsible for elimination of drugs and endogenous *** data have shown increased elimination of UGT1A9 substrates in pregnant women or oral contraceptive users,but the role of estrogen in the regulation of UGT1A9 expression remains *** this study,we investigated the effect of 17β-estradiol(E2) on UGT1A9 expression and the role of ERα in the transcriptional regulation of UGT1A9.E2 significantly increased UGT1A9 promoter activity in Hep G2 cells in the presence of ERα.UGT1A9 induction by E2 was abrogated by antiestrogen ICI182,780 in Hep G2 cells that constitutively express ERα.Results from transient transfection of ERα mutants into Hep G2 cells demonstrated that mutation at DNA-binding domain of ERα abrogates increased UGT1A9 promoter activity by *** and mutation assays of UGT1A9 promoter revealed a putative ERE located within -2262/-1987 *** of healthy human liver tissues revealed significantly higher UGT1A9 expression in women as compared to ***,these findings provide a mechanistic basis for the previous clinical reports and may shed a light on identifying sources for inter-individual variability in UGT1A9-mediated drug metabolism.

关键词： UGT1A9 17β-Estradiol Estrogen receptor Drug metabolism sex difference

Complex formulations, simple techniques: Can 3D printing technology be the Midas touch in pharmaceutical industry?

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Asian Journal of Pharmaceutical sciences 2019年第5期14卷 465-479页

作者： shrawani Lamichhane santosh bashyal Taekwang Keum Gyubin Noh Jo Eun seo Rakesh bastola Jaewoong Choi Dong Hwan sohn sangkil Lee college of pharmacy Keimyung University

3 D printing is a method of rapid prototyping and manufacturing in which materials are deposited onto one another in layers to produce a three-dimensional object. Although 3 D printing was developed in the 1980 s and the technology has found widespread industrial applications for production from automotive parts to machine tools,its application in pharmaceutical area is still limited. However,the potential of 3 D printing in the pharmaceutical industry is now being recognized. The ability of 3 D printing to produce medications to exact specifications tailored to the needs of individual patients has indicated the possibility of developing personalized medicines. The technology allows dosage forms to be precisely printed in various shapes,sizes and textures that are difficult to produce using traditional techniques. However,there are various challenges associated with the proper application of3 D printing in the pharmaceutical sector which should be overcome to exploit the scope of this technology. In this review,an overview is provided on the various 3 D printing technologies used in fabrication of complex dosage forms along with their feasibility and limitations.

关键词： Three-dimensional printing Personalized medicine Fused deposition modeling Inkjet printing Complex formulations

Coleus forskohlii shows anti-psoriatic activity in imiquimod-induced psoriasis rats

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Asian Pacific Journal of Tropical biomedicine 2024年第9期14卷 382-390,I0002-I0007页

作者： sagarika Majhi Iti Chauhan Deepak Kumar Md.Niyaz Alam Md.sarfaraj Hussain Muzaffar Iqbal Faculty of pharmacy I.T.S College of PharmacyMuradnagarGhaziabadU.P.India Lord buddha Koshi pharmacy college of pharmacy BaijanathpurNH 107Saharsa(Bihar)852201India Department of Pharmaceutical Chemistry College of PharmacyKing Saud UniversityP.O.Box 2457Riyadh 11451Saudi Arabia

Objective:To evaluate anti-psoriatic activity of Coleus forskohlii in rats with imiquimod-induced ***:Imiquimod was used to induce psoriasis in *** weight,skin thickness,erythema,scaling,spleen weight,and histological alternations were measured to assess the effect of Coleus ***,an emulgel formulation containing Coleus forskohlii 10%was prepared and characterized along with its ex vivo permeation ***:The emulgel formulation containing Coleus forskohlii 10%had a pH of 5.40±0.36,with optimum spreadability of(31.67±2.08)g/(cm·s)and viscosity of(15966.67±1274.10)cps,and enhanced both the rate and the extent of drug permeation through psoriatic *** an ex vivo study,the quantity of drug permeated(19.18%),deposited(52.38%),and drug remaining in the donor compartments(28.31%)was *** forskohlii significantly alleviated imiquimod-induced psoriasis by increasing glutathione and superoxide dismutase activity,decreasing malondialdehyde and nitric oxide levels,and alleviating histological alternations in rat ***:Coleus forskohlii can alleviate imiquimod-induced psoriasis,which may be used as a therapeutic candidate for the treatment of psoriasis.

关键词： Psoriasis Coleus forskohlii Emulgel Ex vivo Imiquimod Carbopol

Preparation and characterization of spray-dried valsartan-loaded Eudragit~? EPO solid dispersion microparticles

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Asian Journal of Pharmaceutical sciences 2016年第6期11卷 744-750页

作者： Roshan Pradhan sung Yub Kim Chul soon Yong Jong Oh Kim college of pharmacy Yeungnam University

The purpose of this study was to develop the immediate release stomach-specific spraydried formulation of valsartan(VAL) using Eudragit?E PO(EPO) as the carrier for enhancing dissolution rate in a gastric environment. Enhanced solubility and dissolution in gastric pH was achieved by formulating the solid dispersion using a spray drying technique. Different combinations of drug–polymer–surfactant were dissolved in 10% ethanol solution and spraydried in order to obtain solid dispersion microparticles. Use of the VAL–EPO solid dispersion microparticles resulted in significant improvement of the dissolution rate of the drug at pH 1.2 and pH 4.0, compared to the free drug powder and the commercial product. A hard gelatin capsule was filled with the VAL–EPO solid dispersion powder prior to the dissolution *** increased dissolution of VAL from solid dispersion microparticles in gastric pH was attributed to the effect of EPO and most importantly the transformation of crystalline drugs to amorphous solid dispersion powder, which was clearly shown by scanning electron microscopy(sEM), differential scanning calorimetry(DsC), and powder X-ray diffraction(PXRD) studies. Thus, VAL, a potential antihypertensive drug in the form of a solid dispersion microparticulate powder, can be effectively delivered in the immediate release dosage form for stomach-specific drug delivery.

关键词： Valsartan Eudragit E PO solubility solid dispersion spray-drying

Three Co(Ⅱ) Coordination Polymers Incorporated with a bent Connector: Crystal structures and Magnetic Properties

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Chinese Journal of structural Chemistry 2019年第4期38卷 587-596页

作者： LIU Han-Fu LI Hai-Ye YAO Peng-Fei sHU Chun-Yue HUANG Fu-Ping school of Chemistry and pharmacy Guangxi Normal University college of pharmacy Guilin Medical University

based on the bent ligand 1 H-3-(3-pyridyl)-5-(4-pyridyl)-1,2,4-triazole(3,4?-Hbpt) with Co(Ⅱ) ions as well as a series of polycarboxylate co-ligands, three new coordination polymers were yielded, namely, {[Co(op)(3,4?-Hbpt)(H_2O)_3]?2 H_2O}n(1), [Co(cyc)(3,4′-Hbpt)(H_2O)]n(2) and [Co(pro)(3,4′-Hbpt)(H_2O)]n(3)(here, op = o-phthalic anion, cyc = 1,1-cyclobutanedicarboxylic anion, pro = propanedioic anion). In cooperation with the auxiliary polycarboxylate co-ligands, a variety of Co(Ⅱ) coordination networks, such as 1-D chain 1 and 2-D layer 2 and 3 have been assembled. The magnetic behaviors of compounds 1～3 were studied. All of them indicated the existence of interesting spin-canting behavior.

关键词： Co(Ⅱ) complexes bent connector spin canting behavior

Pharmacological effects of aqueous-ethanolic extract of Hibiscus rosasinensis on volume and acidity of stimulated gastric secretion

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Asian Pacific Journal of Tropical Medicine 2011年第11期4卷 883-888页

作者： Rajesh J Mandade sA sreenivas DM sakarkar Avijit Choudhury Pharmacology Department S.N.Institute of PharmacyPusadIndia Guru Nanak Institute of pharmacy IbrahimpattnamHyderabad.(A.P.) India s.N.Institute of pharmacy PusadIndia Pharmacology Department Shree Dhanvantary college pharmacyKimIndia

Objective:To explore the effects of extract of Hibiscus rosasinensis(***) on the volume,free and total acidity of gastric secretion induced by ***:Animals were kept on fasting for 48 *** the pylorus of each animal was *** were randomly divided into 5 groups and treated by carbachol at 600μg/*** animals in groupⅡ-Ⅴwere treated by *** extract at 250 and 500 mg/kg body weight,cimetidine at 2.5 mg/ kg and verapamil at 10 mg/kg body weight intraperitoneally,*** volume,free and total acidity of gastric secretion were observed and ***:It was found that the extract significantly reduced the volume,free and total acidity of gastric secretion(Pse reductions were comparable to cimetidine and *** the reduction in the volume and free acidity were more significant in cimetidine and verapamil treated group indicating that cimetidine and verapamil were more ***:The extract of *** can reduced the volume,free and total acidity of gastric secretion,and can be used effectively in the treatment of peptic ulcer.

关键词： Verapamil Cimetidine Carbachol Hibiscus rosasinensis Rats

Antinociceptive activity of Ricinus communis ***

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Asian Pacific Journal of Tropical biomedicine 2011年第2期1卷 139-141页

作者： Dnyaneshwar J Taur Maruti G Waghmare Rajendra s bandal Ravindra Y Patil Department of Pharmacognosy SVPM's College of Pharmacy Department of Pharmaceutical Chemistry SVPM's College of Pharmacy Department of Pharmacognosy PDEA's Shankarrao Ursal College of Pharmaceutical Sciences and Research Center

Objective:To evaluate the antinociceptive activity of the methanol extract of Ricinus communis leaves(MRCL).Methods:Antinociceptive activity was evaluated using acetic acid induced writhing test,formalin induced paw licking and tail immersion method in mice at doses of 100,125 and 130 mg/kg ***:The results indicated that MRCL exhibited considerable antinociceptive activity against three classical models of pain in *** phytochemical analysis suggested the presence of saponin,steroids and ***:It can be concluded that MRCL possesses antinociceptive potential that may be due to saponin,steroids and alkaloids in it.

关键词： Ricinus communis Analgesic Antinociceptive Writhing Formalin

β-Cyclodextrin as a supramolecular catalyst for the synthesis of 2Hindazolo[2,1-b]phthalazine-trione derivatives in water and their antimicrobial activities

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Chinese Chemical Letters 2017年第7期28卷 1577-1582页

作者： Asha V.Chate Priyanka K.bhadke Manisha A.Khande Jaiprakash N.sangshetti Charansingh H.Gill Department of Chemistry Dr.Babasaheb Ambedkar Marathwada UniversityAurangabad 431004M.S.India Y.b.Chavan college of pharmacy Rafiq Zakaria CampusAurangabad 431001India

An efficient and green method has been developed for the synthesis of 2H-indazolo[2,1-b]phthalazinetriones derivatives by employing 15 mol%β-cyclodextrinvia a one-pot multicomponent reaction of aldehyde,dimedone,hydrazine hydrate with succinic anhydride/phthalic anhydride in water at 80 ℃ for first *** catalyst could be recovered and reused for four consecutive cycles without appreciable loss in catalytic activity and evaluated for in vitro antimicrobial activity against different Gram-positive and Gram-negative bacterial *** outcome of the screening study showed that compound 6d,6f and7 n exhibited excellent activity against ***,compound 6f and 6h exhibited excellent activity against ***,and compound 6c,and 6e displayed again excellent activity against staphylococcus aureus whereas compound 7o shows excellent activity against *** and *** when compared with Ampicillin（standard control）.The results indicated that maximum compounds are moderately effective against bacterial growth and their effectiveness is highest against standard drugs.

关键词： Multicomponent reactions(MCRs) Pyridazino[1 2-a]indazole-triones 2H-Indazolo[2 1-b]phthalazine-trione β-Cyclodextrin Aqueous medium Green method Antimicrobial activity