bluuebunny/crossref_metadata_2025 huggingface dataset:
Zur Synthese von ionenkanalblockierenden Substanzen mit Thieno[2,3-b][1,4]thiazin-, 1,4-Benzoxazin und 1,4-Benzothiazin-Grundgerüst
Authors: Schreder M. E. , Erker T.
Published: May 2019

The syntheses of the thieno[2,3-b)[1,4]thiazine derivatives 8 and 9 are described. Reaction of compound 4 with different acyl halides followed by substitution with various ethanamines gave the products 8 and 9. The new 3,4-dihydro-2H-1,4-benzoxazine derivatives 14, 16, 18 and 3,4-dihydro-2H-1,4-benzothiazine derivatives 15 and 17 with an urea moiety have been synthesized. Substitution of 10 respectively 11 with 4-nitrophenyl chloroformate gave the required reactivity for substitution with diamines. Structural modifications of the amino side chain were carried out.
Monomethylierte 3-Thiacyclopentylsulfaminsäuren und ihre Süßstoffeigenschaften
Authors: Unterhalt B. , Kerckhoff L. , Möllers M.
Published: May 2019

Methyl-3-thiacyclopentanarnines 4a-c were reacted to their sulfamic acid sodiurn salts 5a-c, and their structures determined.Only sodium 4-methyl-3-thiacyclopentylsulfamate (5b) is sweet. The oxa analogues 8a-b however are tasteless.
Betrachtungen zur Herstellung von Methadon-nitril und Isomethadon-nitril sowie verwandten Verbindungen
Authors: Unterhalt B. , Coesfeld B.
Published: May 2019

The 2-chloro-1-dialkylamino-propanes 4a-d are reacted with diphenylacetonitrile under phase transfer conditions to give a mixture of the nitriles 1a-d and 2a-d. Both chloro-dialkylamino-1-phenyl-ethanes 7a-d and 8a-d lead to 4-dialkylamino-2,2,3-triphenyl-butyronitriles 6a-d.
Construction and Evaluation of Scopolamine Ion- Selective Electrode
Authors: Shalaby A. , El-Maamly M. , Abdellatef H.
Published: May 2019

The construction of plasticised PVC matrix-type scopolamine ion- selective membrane electrode and its use in the potentiometric determination of scopolamine in pharmaceutical preparations are described. It is based on the use of tlie ion-associate species, fonned by scopolainine cation and 5-nitrobarbitoric counter ion. The basic electrode peifonnance characteristics are evaluated according to IUPAC I-ecoininendatioiis. It exhibited a linear response for 1x10-2–1x10-5 M of scopolamine solutions with a cationic Nernstian slope over the pH range of 4-7. Common organic and inorganic cations showed negligible interference. Direct potentiometric determination of 1x10-2–1x10-5 M aqueous tubocurarine chloride using this membrane electrode system showed an average recovery of 99.05 with a mean standard deviation of 0.12. This electrode system was successfully applied to the potentiometric determination of scopolamine in some pharmaceutical preparations.
Kinetic Method for the Determination of Cisapride in Pharmaceutical Preparations
Authors: Hassan Ekram M. , Hagga Mohammed E.M. , Al Johar Haya I.
Published: May 2019

An accurate kinetic method for the determination of cisapride is described. The method is based on the reaction of cisapride with potassium dichromate in 2.5 M sulphuric acid at room temperature for a fixed-time of 10 min, afterwards the absorbance of the reaction product is measured at 527 nm. The concentration of cisapride is computed using the corresponding calibration equation for the fixed-time method. The method is applied successfully to commercial tablets and oral suspension dosage forms. The results obtained are compared statistically with the British Pharmacopoeia method. The determination of cisapride by other kinetic methods is feasible with calibration equation obtained but the fixed-time method proves to be more applicable.
Spectrophotometric and Conductometric Study of the Complexation of Ranitidine to Fez+, Fe3+, Al*, Mg*+, Cu", Ni2+ and PtP+ Metal Ions: Pharmaceutical Implications
Authors: Hamdan lmad I. , Taha Motasem
Published: May 2019

Complexation properties of ranitidine (Ran) with Fe2+, Fe3+, A13+, Mg2+, Cu2+, Ni2+ and Pb2+ were studied using UV/V|S spectroscopy and conductometric titrations respectively. Ranitidine was found to form 1:1 complexes in methanol or aqueous buffer (pH 6.5) with all cations except magnesium. In case of Fe3+ complexes of the formula [(Fe3+)2Ran] were evident.
SPECTROPHOTOMETRIC DETERMINATION OF SOME PHARMACEUTICAL COMPOUNDS USING 2,2-DIPHENYL-1-PICRYLHYDRAZYL
Authors: Salem Hesham
Published: May 2019

A simple, rapid and sensitive spectrophotometric procedure for the assay of some drugs has been developed. The method is based on the reaction of the studied drugs with 2,2-diphenyl-1-picrylhydrazyl (DPPH). The latter is employed to abstract a hydrogen atom from the drugs thereby promoting a process of radical coupling. This results in a reduction of the violet color of DPPH with the formation of the yellow colored 2,2-diphenyl-1-picrylhydrazine (DPPH2). The decrease in the intensity of the violet color is used to measure the concentration of the drugs. All measurements are made at λ= 520 nm on methanolic solutions of the reagent and drugs. Beer's law is obeyed in the ranges of 5-30 µg/ml (for aceclofenac, diclofenac sodium and thiaprofenic acid), 2-15 µg/ml (for tenoxicam, furosemide and lansoprazole) and 2-12 µg/ml (for benoxinate hydrochloride and ritodrine). The validity of the method was tested by carrying out standard addition procedure analyzing the studied drugs in pure form as well as in their pharmaceutical preparations without interference from common additives. Results of the proposed methods are in good agreement with those of the official or reported methods.
Darstellung und Atropisomerie von 1-[2-(2,2-Dimethylpiperidino)phenyl]ethanol
Authors: Möhrle H. , Jeandrée M.
Published: May 2019

The title compound was prepared by Hg(II)-edta dehydrogenation of the aminoalkohol 2 via the benzoxazine 4, which reacted with methylmagnesiumiodide to 6. This compound shows in the NMR spectrum atropisomerism for the restricted rotation of the piperidine moiety about the aryl-C-N bond. The dehydrogenation of 6 stopped after a two electron withdrawal generating the benzoxazine 7, because the angular hydrogen atom occupies an equatorial position, which prevents stereoelectronic conditions for a further oxidation.
Antiplatelet-Eigenschaften von 4-Oxo-4H-pyrazol-1,2-dioxiden
Authors: Unterhalt B. , Bensliman C. Bensliman
Published: May 2019

New 4-oxo-4H-pyrazol-1,2-dioxides were tested for their antiplatelet effects. Compound 2i has the highest activity in the Born test with 200 nMol/L.
ANALGESIC AND ANTI-INFLAMMATORY ACTIVITIES OF 2-PHENYL (6, 8-DISUBSTITUTED 3,4-DIHYDRO-4-OXOQUINAZLIN-3-YCL) ACETO ACETAMIDES AND THEIR ß (4-SUBSTITUTED PHENYL) AZO ANALOGS
Authors: Gopa N. , Porchezhian E. , Sarma G.V.S. Rama
Published: May 2019

2-phenyl-(3,4-dihydro-4-oxoquinazolin-3-yalc)e to acetamides (1&2) and their B-(4-substituted phenyl) azo derivatives (3-10) were evaluated for their analgesic and antiinflammatory activities. The bromophenyl azo derivative (4) showed significant activity as comparable to standard drugs viz pentazocine, aspirin and other compounds exhibited moderate activities. All the synthesized compounds were tested for their toxicity have not shown any abnormality up to 1500 mg/kg Body weight in experimental animals.
Diterpenoid Alkaloids from Consolida regalis S. F.Gray subsp.paniculata (Host) Soo var. paniculata
Authors: MERICL Filiz , MERICLI Ali , DESAI Haridutt , ULUBELEN Ayhan , PELLETIER S.
Published: May 2019

Seven diterpenoid alkaloids : delcosine(1), delsoline(2), gigactonine(3), lycoctonine(4), takaosamine(5), atisine(6) and hetisinone(7) have been isolated from the aerial parts of Consolida regalis subsp. paniculata var. paniculata. The presence of compounds 1,2,5,6 and 7 in this plant has not been previously reported.
Nitraminanaloge Suosan-Derivate als potentielle Süßstoffe
Authors: Unterhalt B. , Adam T. , Bagherzadeh H.
Published: May 2019

Substituted phenylaminocarbonylaziridines are reacted with N-nitro-ethylcarbamate and then with ammonia to give N-aryl-N′-nitroaminoethyl-ureas 5-11 after acidification. 5 and 6 have a sweet taste, 7 is bitter.
A Study of Mucoadhesive Bond Strength of Buccoadhesive Compacts for Systemic Drug Delivery: In-vitro/ In-vivo correlation
Authors: Kumar D. , Balasubramaniam J. , Pandit J.
Published: May 2019

Compacts prepared from binary combinations of Carbopol® 934 P (CP), Polycarbophil (Noveon® AA1, PC) and Hydroxy propyl cellulose (Klucel®, HPC) and coated on all but one flat surface with Poly Methyl Methacrylate - PMMA (chloroformic solution) were evaluated for mucoadhesive bond strength on a modified mucoadhesive bond strength apparatus using rabbit stomach mucosa (SM) and small intestine mucosa (SIM). In -vitro mucoadhesion tests indicated that the detachment force increased linearly with concentration of CP/PC in the compacts. Mucoadhesion of the compacts with SIM were higher when compared to SM. The compacts with higher proportions of CPIPC showed longer buccoadhesion time (time the compact remained in contact with the buccal mucosa) than HPC alone in humans. In-vivo buccoadhesevity of the coated compacts was studied in healthy human volunteers. An index was used to study the redness and ulceration of the contact buccal mucosa.

Compacts with higher proportions of CP/PC showed longer buccoadhesion time than HPC alone. Significant correlation coefficient (r) values (P<0.01) were obtained between in-vitro fracture strength of the compacts and in-vivo buccoadhesion time. Hence, the in-vitro mucoadhesive model developed by us provides useful information on the residence time of the compact for systemic drug delivery in the oral cavity, and compacts containing less than 50% of CP/PC were safer to use in humans.
Reaction of Prop-2-ynylamine with Isochromadiones : Formation of Amides
Authors: Usifoh C. , Okunrobo L. , Ukoh G.
Published: May 2019

The ring opening of isochromadiones by prop-2-ynylamine was accomplished in non-polar solvents to form N-prop-2-ynylbenzamide-2-acetic acid 3 N-prop-2-ynylhomophthalimide 4. Compound 3 was found out to be an intermediate product in the formation of 4. These compounds were screened for anticonvulsant and antibacterial properties and were found to have no activity.
Plenary lectures
Authors:   Osterreichische Pharmazeutische Gesellschaft
Published: May 2019

Recombinant proteins can be very potent, but their therapeutic application can be strongly hampered by inappropriate distribution. [...]
16th Scientific Congress of the Austrian Pharmaceutical Society/Poster presentations
Authors:   Osterreichische Pharmazeutische Gesellschaft
Published: May 2019

Nichtsteroidale Antirheumatika und Antiphlogistika vom Typ der Arylessig- und Arylpropionsäuren. [...]
Haltbarkeit von Arzneimitteln nach Anbruch: Von der Marktüberwachungsstudie zur EU-Guideline
Authors: I. Edlinger , I. Liebenberger , R. Macas , A. Mayrhofer , S. Stouer , C. Wirthumer-Hoche
Published: May 2019

The in-use stability of 25 drug products (oralliquids) with sensitive active ingredients was tested with a new test design simulating the stress of practical use. The results showed in so me cases a dramatic degradation of the active ingredient and the need of a reduced shelf life after first opening. Therefore the topic "in-use stability testing of human medicinal products" was brought forward to the QWP of the CPMPc by a member of the BlfA. Austria was appointed as rapporteur for the elaboration of the corresponding guideline.
Preparation and evaluation of tolmetin sodium conventional and sustained-release suppositories
Authors: B. Baloǧlu , O. Kirkaǧaçhoǧlu
Published: May 2019

Conventional suppositories of tolmetin sodium were prepared by using two different types of Witepsol as an oily base and two different ratios of polyethylene glycol 400: polyethylene glycol 4000 as an water-soluble base. In addition, sustained- release suppositories were prepared by adding Eudragit L-100 ta the suppositories. The effects of the suppository base and the ratios of the polyethylene glycol 400: polyethylene glycols 4000 on the in vitro release characteristics were investigated. The release rate of tolmetin sodium from the conventional suppositories prepared with polyethylene glycol was slower than the other suppositories prepared with Witepsol. All of the suppositories with Eudragit L-100 showed slow-release profiles and the drug release rates clearly depended on the Eudragit L-100 content. When dissolution results were evaluated kinetically, zero order kinetic was observed with the sustained- release suppositories of tolmetin sodium prepared with polyethyleneglycol 400: polyethyleneglycol 4000 by adding Eudragit L-100.
Determination of taxa of the Achillea millefolium qroup and Achillea crithmifolia bv morpholoqical and ~hvtochemicaml ethods I. Characterisation of Central European taxa1
Authors: Florian Rauchensteiner , Shahbaz Nejati , Ingrid Werner , Sabine Glasl , Johannes Saukel , Johann Jurenitsch , Wolfgang Kubelka
Published: May 2019

A survey of morphological and phytochemical data characteristic for several taxa of the Achillea millefoliurn group (A. aspleniifolia VENT., A. roseoalba EHREND., A. collina J. BECKER ex REICHENB., A. ceretanica SENNEN, A. setacea W. ET K., A. pratensis SAUKEL & LANGER, A. styriaca SAUKEL ined., A. pannonica SC H E ELE, A. distans W. ET K., A. millefolium s. I., A. millefolium ssp. sudetica OPIZ) and A. crithmifolia W. ET K. is presented. For each taxon a short morphological description and a guide for microscopic analysis is given as well as its sesquiterpene composition including the TLC characteristics. Based on GLC analyses of 1523 single plants collected in Central Europe the sums of sabinene + β-pinene + β-caryophyllene (SUM I), a-pinene + 1,8-cineole (SUM 2), camphene + camphor + borneol (SUM 3), camphene + camphor (SUM 4) and 1,8-cineole + borneol (SUM 5) were found to be highly significant for distinct taxa or groups of taxa.
Formation of Leukotrienes From Calcium Ionophore-A23187 Stimulated Rabbit, Rat and Mice White Blood Cells
Authors: Mahrnoud A. Mansour , Fahad I. AI-Jenoobi , Saleh A. Al-Suwayeh , Abdulhakeem A. Al-Majed , Othman Al-Shabanah
Published: May 2019

Leukotrienes (LTs) producing capacity was investigated in calcium ionophore A23 187- stimulated rabbit. rat and mice peripheral white blood cells suspension. A reverse phase high performance liquid chromatography technique and computerized UV spectroscopy were employed to isolate and quantitate the released LTs namely. LTC4 and LTB4. Preincubation of rabbit white blood cells at 37°C for 5 min followed by calcium ionophore-A23 187 (1 pM) stimulation for another 5 min produced an equal amounts of LTC4 as compared to LTC4 produced by human white blood cells (105±11 versus 95±9.5 pmol/107 cells respectively; mean ±SEM). In contrast rabbit white blood cells synthesized significantly lower LTB4 in comparison with LTB4 produced by peripheral white blood cells from healthy control (168±18 versus 228±19 pmol/107 cells respectively: mean ±SEM). When rat and mice white blood cells suspension were stimulated with calcium ionophore A23187 (1 µM) after preincubation at 37°C for 5 min, equivalent amounts of LTC4 and LTB4 were observed. However, LTB4 and LTC4 produced by rat and mice white blood cells were significantly lower in comparison with LTB4 and LTCj produced by human white blood cells stimulated with calcium ionophore-A23 187. These results demonstrate that rabbit. rat and mice white blood cells suspension possess the capacity to produce LTC4 and LTB4 from endogenous substrate after calcium ionophore-A23 187 stimulation.
SYNTHESIS AND ANTIBACTERIAL EVALUATION OF NEW FLAVONOID DERIVATIVES FROM 4,6-DIACETYL RESORCINOL
Authors: M.S.Y. Khan , S. Sharma , A. Husain
Published: May 2019

In order to check the antibacterial potential of bischalcones derived from 4,6-diacetyl resorcinol, a number of chalcone derivatives were synthesized by condensation with appropriate aromatic aldehydes. Out of these compounds 3b-i, 4a and 4b showed a good antibacterial activity. Methylation of the two chelated hydroxyls reduced the activity. However, oxidative cyclization of 3a and 3b resulted in compounds 4a and 4b which were found to be considerably active. The alternative method of synthesis of 4a and 4b via Baker-Venkatararnan rearrangement did not succeed.
EFFECT OF CARRIER TYPES ON THE PHYSICOCHEMICAL AND DISSOLUTION CHARACTERISTICS OF OFLOXACIN SOLID DISPERSION
Authors: S Okonogi , J Sirithunyalung , B Sirithunyalig , P Wolschann , H Viernstein
Published: May 2019

Solid dispersions of ofloxacin (OFX) and of a number of carriers including chitosan and the water soluble polymers polyethylene glycol (PEG) 4000, PEG 20000, and polyvinylpyrrolidone K- 90 were prepared by solvent evaporation method in order to increase the dissolution of the drug. The solid dispersions were subjected to X-ray diffraction, DSC, and dissolution to characterize their physicochemical and dissolution properties. The results demonstrated a decrease in drug crystallinity at higher amounts of carrier. Dissolution studies indicated that the dissolution rate of OFX was markedly increased in these solid dispersion systems compared with the pure drug. The results also showed that the increase in dissolution rate was higher when the weight fraction of carriers increased. An influence of molecular weight of PEG on OFX dissolution could also be observed. In solid dispersion with 1:9 ratio drug to carrier, PEG 4000 gave highest drug dissolution rate, whereas in 1:1 ratio, chitosan seems to be the best carrier for drug release. It was concluded that chitosan might be the carrier of choice for dissolution enhancement in solid dispersions with high content of drug.
Thiolated polymers: Stability of thiol moieties under different storage conditions
Authors: A. Bernkop-Schnürch , M.D. Hornof , C.E. Kast , N. Langoth
Published: May 2019

The purpose of this study was to evaluate the stability of thiolated polymers - so-called thiomers. A polycarbophil-cysteine conjugate and a chitosan-thioglycolic acid conjugate were chosen as representative anionic and cationic thiomer. The thiol group bearing compounds L-cysteine and thioglycolic acid were introduced to polycarbophil and chitosan, respectively with a coupling reaction mediated by a carbodiimide. The resulting thiolated polymers were freeze-dried and the amount of thiol groups on the thiomer was determined spectrophotometrically. Each kind of polymer was directly used or compressed into 1 mg matrix-tablets. Polymers were stored for a period of six months at four different storage conditions, namely at -20°C (56% relative humidity; RH), 4°C (53% RH), at 20°C (70% RH), and at 22°C (25% RH). Samples were taken after 6 months to determine the formation of disulfide bonds and the remaining thiol groups on the polymer. When the polycarbophil-cysteine and chitosan-thioglycolic acid conjugate were stored as powder a decrease of free thiol groups was observed only after storage at 20°C and 70% RH. Both polymers were found to be stable under all storage conditions when compressed into matrix tablets. The results provide the base for the use of thiomers as auxiliary agents in commercial products.
EFFECT OF DIFFERENT VEHICLES ON HEPATO- PROTECTIVE EFFICIENCY OF DESFERRIOXAMNE IN RADIATED CARBON TETRACHLORIDE TREATED MICE
Authors: El-Bagory lbrahim , Mansour Mahmoud
Published: May 2019

The effect of desferrioxamine (DFO) in different vehicle ( Aqueous and oily) against hepatotoxicity induced by carbon tetrachloride (CC14) in irradiated mice and irradiated carbon tetrachloride (IR-CCI4) in normal mice was investigated. A single dose of CC14 and IR-CCI4 (20 @/kg, i.p.) in irradiated mice (IR-mice) and normal mice induced hepatotoxicrty, manifested biochemically by significant elevation of serum enzyme activities, such as alanine trarsaminase (ALT, EC:2.6.1.2 ) and aspartate transaminase (AST, EC:2.6.1.1). Hepatotoxiaty was further evidenced by significant decrease of total sulfttydryl (-SH) content, and catalase (EC: 1.1 1.1.6) activrty in hepatic tissues and significant increase in hepatic lipid peroxidation measured as malondialdhyde (MDA). Pretreatment of normal mice and IR-mice with DFO (200 mg/kg i.p dissolved either in water or arachis oil vehicle) 1 h before CC14 or IR-CC14 injection ameliorated the hepatotoxicrty as evidenced by a significant reduction in the elevated levels of serum enzymes as well as a significant decrease in the hepatic MDA content and a significant increase in the total sulfhydryl content 24 h after CC14 or IR-CCI4 administration.. These results indicated that both of oily and watery DFO can effectively ameliorated the hepatotoxicity induced by CC14 in IR-mice or IR-CC14 in normal mice. Although, the efficiency of the hepatoprotective effect of DFO in oily vehicle was higher than that DFO in aqueous vehicle. The hepatoprotective effect of DFO possibly through inhibition of the production of oxygen free radicals that cause lipid peroxidation.
Synthesis and in vitro Anti-HIV Screening of Certain 2-(Benzoxazol-2-ylamino)-3H-4-oxopyrimidines
Authors: Rostom Sherif , Fahmy Hesharn , Ssaudi Manal
Published: May 2019

Intensive efforts are underway worldwide to develop chemotherapeutic agents effective against HIV, the etiological agent of AIDS. In this view, it was designed to synthesize and investigate the anti-HIV activity of some new 2-(benzoxazol-2-ylamino)-3H-4-oxopyrimidines following the lead benzoxazole (L 697, 661), which was reported to inhibit the spread of the HIV infection by 95 % in MT4 cell culture. Only the 2-(benzoxazol-2-ylarnino)-6-hydroxy-3H-4-oxopyrdine 8 (NSC 722448) was confirmed to exhibit moderate in vitro anti-HIV activity (percentage of protection 76.83 %).
Mass uniformity of nasal sprays
Authors: Grobuschek Nina , Lecnik Oliver , Schmid Martin , Gubitz Gerald
Published: May 2019

The uniformity of nasal spray dose delivery was investigated. Four selected nasal sprays commercially available on the European market were checked for their mass uniformity according to the guidelines of the European Pharmacopoeia and recent draft guidelines of the Food and Drug Administration (FDA). Mass uniformity was also determined with simulation of a patient's use daily, and at 3- and 7- day intervals. The influence of the degree of filling and different storage positions on mass uniformity were also investigated. At first usage, all preparations fulfilled the specifications of the Ph.Eur. and the FDA draft guidelines. When patient application was simulated, however, the dose accuracy decreased significantly with some of the preparations with increasing time of non-usage, presumably due to evaporation of liquid in the application system. This is indicated by a loss of weight of the nasal spray flasks observed during simulated weekly usage. Under these conditions (6 days' storage without use, same demands for uniformity of mass of the delivered dose), one of the preparations even failed to meet the Ph.Eur. and FDA limits.
Development of Buccoadhesive Systems of Pentarocine for Systemic Drug Delivery
Authors: Sampathkumar D. , Thilek Kumar M. , Balasubrarnaniam J. , Pandit J.
Published: May 2019

Bucoadhesive patches of Pentazocine (PZ) for unidirectional drug delivery were prepared by casting carboxy methyl cellulose (CMC) with glycerol or propylene glycol and CMC-hydroxy ethyl cellulose (HEC) with glycerol. In vitro mucoadhesivity of the prepared patches were determined using a modified mucoadhesive bond strength apparatus using rabbit small intestine mucosa (SIM). Drug release kinetics was evaluated from composite patches, prepared by covering all but one side of the PZ patches with 3M backing material. Biocompatability / buccoadhesion time and in vivo permeation of placebo and PZ loaded patches were determined using a double blind cross over study in healthy human volunteers. Drug release from CMC-glycerol patches and pure HEC patches showed zero order kinetics with diffusional exponent (n) ranging between 0.79 to 1.046, while that from CMC-HEC and CMC-propylene glycol patches showed an apparent zero order release kinetics. The prepared patches were well tolerated by the human volunteers as they did not produce any side effects at the contact surface. The in vitro mucoadhesivity of CMC-propylene glycol patches were significantly lower than CMC- glycerol based patches. The in vivo permeation of selected PZ patches delivered the drug well above the minimum buccal permeation rate, so as to attain effective blood concentration
Ratio Derivative S~ectrophotometricM ethod for the Determination of Some Oxicams in Presence of their Alkaline Dearadation Products
Authors: Taha Elham , El- Zanfally Eman , Salama Nahla
Published: May 2019

A new spectrophotometric method has been developed for the determination of some oxicams namely, lornoxicam (LX) , tenoxicam (TX) and meloxicam (MX), in the presence of their main alkaline degradation products, 2-aminopyridine ( I ) and 2-amino-5-methylthiazole (II) for (TX&MX), 2-aminopyridine and TX for lornoxicam. The method is based on the use of the first derivative of the ratio spectra (1DD) of the mentioned compounds and their corresponding degradates. The procedure does not require any separation steps. Linear calibration graphs of 1DD were obtained by measurement of the amplitudes at 316, 249 and 260nm for LX, 248.8 , 258.8 nm for TX and 287.2nm for MX. On carrying out measurements at the above mentioned wavelengths, the linearity range is found to be 2.5 - 35 μg ml-1 for LX and TX, 1.25 - 30 μg ml-1 for MX. The validity of the method was assessed by applying the standard addition technique. Statistical analysis of the results has been carried out revealing high accuracy and good precision. The suggested procedure could be used for the determination of the above mentioned drugs in pure and dosage forms as well as in presence of their degradation products.
Die Emerson-Reaktion des Salbutamols
Authors: Kallmayer H.-J. , Engels H.-J.
Published: May 2019

Kaliumhexacyanoferrat(lll) kuppelt 4-Aminoantipyrin (1) mit Salbutamol (2) oxidativ nach Emerson zu den roten E-/Z-isomeren 1,4-Benzochinon-4-iminen 7a und b. Die Desalkylierung des Salbutamols wird als Grob'sche Fragmentierung interpretiert.
Alpha amylase inhibitory activitv of some plant extracts with hyporrlycemic activity
Authors: Abu Soud Rawand S. , Hamdan lmad I. , Afifi Fatma U.
Published: May 2019

Thirteen plant species which are claimed to have anti-diabetic activity (based on folk medicine and/or scientific reports) were tested for alpha amylase inhibitory activity. Two of the screened plants exhibited significant (more than 80%) alpha amylase inhibitory activity. lC50 of these plants was estimated based on the dried crude extract and found to be 0.08, and 0.2 mg/ml for Aloe vera and Paronychia argentea respectively. In A. vera the activity was most likely due to cinnamic acid derivatives. In P. argentea the activity was attributed to flavonoid components. These findings support the hypoglycemic activity of these species and give insight about the potential mechanism of their hypoglycemic activity.
Synthesis of Tetrahydro-2H-[1,3,5]thiadiazine-5-(4-pyridylcarboxamido)-2-thione with antitubercular activity
Authors: Sriram D. , Jyothi Mallika K. , Yogeeswari P.
Published: May 2019

3-Substituted-5-(4-pyridylcarboxamide)tetrahydro-2H-[1,3,5]thiadizine-2-thione derivatives (1-9) were synthesized as derivatives of isoniazid (INH) to overcome the resistance developed with its therapeutic use. The structures were confirmed by their spectral and elemental analyses data. These derivatives revealed higher lipophilicity compared with INH. The antimycobacterial activity of the synthesized compounds and INH was evaluated in vitro against Mycobacterium tuberculosis H37Rv at 6.25 µg/ml in BACTEC 12B medium using the BACTEC 460 radiometric system. The derivatives exhibited antitubercular activity.
Medicinal used plants from lndia: analysis of the essential oil of air-dried Biophvtum sensitivum (L.) DC.
Authors: Jirovetz Leopold , Buchbauer Gerhard , Wobus Andrea , Shafi Mohamed P. , Jose Beena
Published: May 2019

The essential oil of the air-dried plant Biophytum sensitivum (L.) DC. (Oxalidaceae) from Southern lndia was investigated by gas chromatographic-spectroscopic (GC-FID and GC-MS) and olfactoric methods to identify compounds responsible for the characteristic odor as well as partly for the folk medicinal use of this plant. Especially benzene derivatives, such as 1,4-dimethoxy benzene (24.9%), 1,2-dimethoxy benzene (10.6%) and 2-methoxy-4-methyl phenol (3.5%), the monoterpenes (Z)-linalool oxide (8.1%), (E)-linalool oxide (5.2%) and linalyl acetate (3.4%) as well as l-octen-3-ol (9.5%) and isophorone (3.1%) were found to be main constituents (concentrations higher than 3%, calculated as relative %-peak area of GC-FID analysis using an apolar column) of this essential oil, with totally 69 compounds identified. In addition, the odor impression of the sample is described and the possible biological activity of single volatiles discussed.
Synthesis, physico-chemical properties and bioloclical activitv of 1-(4-fluorophenvl)-4-[3-(2-,3- and 4-alkyloxyphenylcarbamoyloxy)-2-hydroxypropyl] piperaziniumchlorides
Authors: Malík Ivan , Sedlárová Eva , Csöllel Jozef , Račanská Eva , Čižmárik Jozef , Kurfürst Pavel
Published: May 2019

1-(4-fluoropheny1)-4-[3-(2-,3- and 4-alkyloxyphenylcarbamoyloxy)-2-hydroxypropyl]piperaziniumchlorides, with one to four carbon atoms in the alkoxy group on aromatic ring have been synthesized as the derivatives of substituted phenylcarbamic acid. The structures were confirmed by their spectral data. Potential antiarrhythmic activity was evaluated in guinea-pigs model. Preliminary studies demonstrated that the evaluated compounds, using ouabain arrhythmia model, appear to possess only moderate antiarrhythmic activity. Only compound marked as 4f appears to be more potent and lead us to focus our attention on structures with more bulky substituent in the m-position at aromatic ring in the hydrophilic part of molecule.
Abstracts of the Constributions of the Joint Meeting on Medicinal Chemistrv June 20th to June 23rd 2005, Vienna, Austria
Authors:   Österreichische Pharmazeutische Gesellschaft
Published: May 2019

n/a
Thermodynamic Investigations on the Inclusion Complexation of Piroxicam with Cyclodextrin Derivatives
Authors: S. Charumanee , P. Weiss-Greiler , P. Wolschann , H. Viernstein , A. Titwan , J. Sirithunyalug , S. Okonogi
Published: May 2019

Thermodynamic studies of piroxicam in aqueous solution complexed with β-cyclodextrin (β-CD), γ-cyclodextrin (γ-CD) and two β-cyclodextrin derivatives, hydroxypropyl-β-cyclodextrin (HP-P-CD) and methyl-β-cyclodextrin (Me-β-CD) were performed at different temperatures and pH values using the phase solubility method. The phase solubility diagrams of β-CD, γ-CD and HP-β-CD is of AL-type behavior, indicating the formation of 1:l complexes. The related stability constants range from β-CD > γ-CD > Me-β-CD > HP-β-CD, respectively. An Ap-type solubility diagram is observed for Me-β-CD, indicating the formation of 1:2 complexes at higher CD concentrations. From the temperature dependence of the equilibrium constants the reaction enthalpies and entropies have been determined. The contributions of the reaction entropies are small and no enthalpy-entropy-compensation is observed, except for γ-CD, where a very small negative reaction entropy could be estimated. Moreover, the influence of the pH value is rather high because the differently charged forms of piroxicam show different solubility behavior in water.
Flow Injection Analysis With Trimetazidine Dihydrochloride Ion-Selective Electrode
Authors: Issa Yousry , Abdel-Ghani Nour , Ahmed Howayda
Published: May 2019

New Plastic membrane ion-selective electrode for trimetazidine dihydrochloride based on trimetazidinium-tetraphenylborate was prepared. The electrode exhibited mean calibration graph slope of 29.5 mV per decade of (TrimCl2) concentration at 25°C. The electrode can be used within the concentration range 3.2×10-5-10-2 M (TrimCl2) at pH ranges of 1.5-3.8 and 4.5-7.5. The standard electrode potentials were determined at different temperatures and used to calculate the isothermal coefficient of the electrode, which was (0.00088 V°C-1). The electrode showed a very good selectivity for (TrimCl2) with respect to a number of inorganic cations, sugars and amino acids. The electrode was applied to the potentiometric determination of the trimetazidine ion and its pharmaceutical preparation under batch and flow injection conditions. Graphite coated wire was prepared and characterized as sensor for the drug under investigation. Also, trimetazidine was determined by conductimetric titrations.
Line Ratios Reveal N2H+ Emission Originates above the Midplane in TW Hydrae
Authors: Schwarz Kamber R. , Teague Richard , Bergin Edwin A.
Published: May 2019

Line ratios for different transitions of the same molecule have long been used as a probe of gas temperature. Here we use ALMA observations of the N2H+
J = 1–0 and J = 4–3 lines in the protoplanetary disk around TW Hya to derive the temperature at which these lines emit. We find an averaged temperature of 39 K with a 1σ uncertainty of 2 K for the radial range 0.″8–2″, which is significantly warmer than the expected midplane temperature beyond 0.″5 in this disk. We conclude that the N2H+ emission in TW Hya is not emitting from near the midplane, but rather from higher in the disk, in a region likely bounded by processes such as photodissociation or chemical reprocessing of CO and N2 rather than freeze-out.
Long-term changes of the trophic status in transitional ecosystems of the northern Adriatic Sea, key parameters and future expectations: The lagoon of Venice as a study case
Authors: Sfriso Adriano , Buosi Alessandro , Mistri Michele , Munari Cristina , Franzoi Piero , Sfriso Andrea Augusto
Published: May 2019

The determination of the trophic status of transitional ecosystems from the physico-chemical and biological point of view is one of the requirements of the European Water Framework Directive (WFD 2000/60/EC). In Italy, its determination is implemented by the Regional Agencies for Environmental Protection (ARPAs) that have activated multi-annual monitoring programs. However, as the availability of funds is increasingly scarce, the number of environmental parameters to detect environmental changes should be conveniently managed.

The high number of environmental parameters, nutrient and macrophyte datasets available for the LTER-Italia site “Venice lagoon” can be an useful tool to analyze the trophic changes over recent years and to foresee environmental evolutions. Nutrient data on a spatial basis have been available since 1948, whereas macroalgal maps date back to 1980. The aim of this paper is to highlight the changes of the trophic status of the lagoon since the middle of the 20th century by considering the concentrations of nutrients in the surface sediments and in the water column, the variation of some physico-chemical parameters and the biomass of macroalgae and also to foresee the way it will possibly evolve. In fact, after many anthropogenic impacts that in the second half of the 20th century affected the lagoon, starting from the year 2010, the ecological status is progressively improving. Nutrients show a significant reduction both in the water column and in surface sediments, and the macrophytes are represented by species of higher ecological value while the opportunistic species such as the Ulvaceae are in strong regression.
Phytoplankton temporal dynamics in the coastal waters of the north-eastern Adriatic Sea (Mediterranean Sea) from 2010 to 2017
Authors: Cerino Federica , Fornasaro Daniela , Kralj Martina , Giani Michele , Cabrini Marina
Published: May 2019

Phytoplankton community structure was analysed from 2010 to 2017 at C1-LTER, the coastal Long-Term Ecological Research station located in the Gulf of Trieste, which is the northernmost part of the Mediterranean Sea. Phytoplankton abundance and relevant oceanographic parameters were measured monthly in order to describe the seasonal cycle and interannual variability of the main phytoplankton taxa (diatoms, dinoflagellates, coccolithophores and flagellates) and to analyse their relationship with environmental conditions. Overall, phytoplankton abundances showed a marked seasonal cycle characterised by a bloom in spring, with the peak in May. During the summer, phytoplankton abundances gradually decreased until September, then slightly increased again in October and reached their minima in winter. In general, the phytoplankton community was dominated by flagellates (generally <10 µm) and diatoms co-occurring in the spring bloom. In this period, diatoms were also represented by nano-sized species, gradually replaced by larger species in summer and autumn. Phytoplankton assemblages differed significantly between seasons (Pseudo-F= 9.59;p< 0.01) and temperature and salinity were the best predictor variables explaining the distribution of the multivariate data cloud. At the interannual scale, a strong decrease of the late-winter bloom was observed in recent years with the spring bloom being the main phytoplankton increase of the year.
Butterfly distribution along altitudinal gradients: temporal changes over a short time period
Authors: Cerrato Cristiana , Rocchia Emanuel , Brunetti Massimo , Bionda Radames , Bassano Bruno , Provenzale Antonello , Bonelli Simona , Viterbi Ramona
Published: May 2019

Mountain ecosystems are particularly sensitive to changes in climate and land cover, but at the same time, they can offer important refuges for species on the opposite of the more altered lowlands. To explore the potential role of mountain ecosystems in butterfly conservation and to assess the vulnerability of the alpine species, we analyzed the short-term changes (2006–2008 vs. 2012–2013) of butterflies’ distribution along altitudinal gradients in the NW Italian Alps. We sampled butterfly communities once a month (62 sampling stations, 3 seasonal replicates per year, from June to August) by semi-quantitative sampling techniques. The monitored gradient ranges from the montane to the alpine belt (600–2700 m a.s.l.) within three protected areas: Gran Paradiso National Park (LTER, Sitecode: LTER_EU_IT_109), Orsiera Rocciavrè Natural Park and Veglia Devero Natural Park. We investigated butterflies’ temporal changes in accordance with a hierarchical approach to assess potential relationships between species and community level. As a first step, we characterized each species in terms of habitat requirements, elevational range and temperature preferences and we compared plot occupancy and altitudinal range changes between time periods (2006–2008 vs. 2012–2013). Secondly, we focused on community level, analyzing species richness and community composition temporal changes. The species level analysis highlighted a general increase in mean occupancy level and significant changes at both altitudinal boundaries. Looking at the ecological groups, we observed an increase of generalist and highly mobile species at the expense of the specialist and less mobile ones. For the community level, we noticed a significant increase in species richness, in the community temperature index and a tendency towards homogenization within communities. Besides the short time period considered, butterflies species distribution and communities changed considerably. In light of these results, it is fundamental to continue monitoring activities to understand if we are facing transient changes or first signals of an imminent trend.
Climatic and pedoclimatic factors driving C and N dynamics in soil and surface water in the alpine tundra (NW-Italian Alps)
Authors: Freppaz Michele , Viglietti Davide , Balestrini Raffaella , Lonati Michele , Colombo Nicola
Published: May 2019

In alpine tundra the interannual and seasonal variability of C and N forms in soil and lake water during the short snow-free season could be significant and related to climatic and pedoclimatic variables. The hypothesis that not only the climatic and pedoclimatic parameters recorded during the summer season but also the ones measured during the previous snow-covered season could contribute to explaining the C and N dynamics in soil and surface water was tested along 10 snow-free seasons in 3 sites in the alpine tundra in the north-western Italian Alps (LTER site Istituto Mosso). Among the considered parameters, the snow cover duration (SCD) exerted a primary control on soil N-NH4+, DOC, Cmicr, Nmicr and DOC:DON ratio, with an inverse relationship. A long SCD might cause the consumption of all the subnival substrata by the soil microorganisms, determining a C starvation during the subsequent snow-free season. An opposite trend was observed for the lake water, where a longer SCD corresponded to a higher content of inorganic N forms. Among the pedoclimatic indices, the number of soil freeze/thaw cycles (FTC) recorded during the snow-covered season had a positive relation with most of soil C and N forms and N-NO3− in lake water. Only the soil DON showed an inverse pattern, and this result is consistent with the hypothesis that FTC released soil DON, subsequently decomposed and mineralized. Only N-NO3− had a significant intraseasonal variability, reaching the highest values in September both in soil and water, revealing a significant slowdown of the contribution of soil N immobilization processes.
Dynamic of nitrogen and dissolved organic carbon in an alpine forested catchment: atmospheric deposition and soil solution trends
Authors: Balestrini Raffaella , Delconte Carlo Andrea , Buffagni Andrea , Fumagalli Alessio , Freppaz Michele , Buzzetti Italo , Calvo Enrico
Published: May 2019

A number of studies have reported decreasing trends of acidifying and N deposition inputs to forest areas throughout Europe and the USA in recent decades. There is a need to assess the responses of the ecosystem to declining atmospheric pollution by monitoring the variations of chemical species in the various compartments of the forest ecosystem on a long temporal scale. In this study, we report on patterns and trends in throughfall deposition concentrations of inorganic N, dissolved organic N (DON) and C (DOC) over a 20-year (1995–2015) period in the LTER site -Val Masino (1190 m a.s.l.), a spruce forest, in the Central Italian Alps. The same chemical species were studied in the litter floor leachates and mineral soil solution, at three different depths (15, 40 and 70 cm), over a 10-year period (2005–2015). Inorganic N concentration was drastically reduced as throughfall and litter floor leachates percolated through the topsoil, where the measured mean values (2 µeq L-1) were much lower than the critical limits established for coniferous stands (14 µeq L-1). The seasonal temperature dependence of throughfall DOC and DON concentration suggests that the microbial community living on the needles was the main source of dissolved organic matter. Most of DOC and DON infiltrating from the litter floor were retained in the mineral soil. The rainfall amount was the only climatic factor exerting a control on DOC and N compounds in throughfall and forest floor leachates over a decadal period. Concentration of SO4 and NO3 declined by 50% and 26% respectively in throughfall deposition. Trends of NO3 and SO4 in forest floor leachates and mineral soil solution mirrored declining depositions. No trends in both DON and DOC concentration and in DOC/DON ratio in soil solutions were observed. These outcomes suggest that the declining NO3 and SO4 atmospheric inputs did not influence the dynamic of DON and DOC in the Val Masino forest. The results of this study are particularly relevant, as they are based on a comprehensive survey of all the main compartments of the forest ecosystem. Moreover, this kind of long-term research has rarely been carried out in the Alpine region.
Similarities, differences and mechanisms of climate impact on terrestrial vs. marine ecosystems
Authors: Ribera d’Alcalà Maurizio
Published: May 2019

Comparisons between terrestrial and marine ecosystems are generally not in the main stream of scientific literature even though Webb (2012) listed several points for which the transfer of knowledge and concepts related to one or to the other system would benefit our understanding of both. Even sharing this view, the leading hypothesis behind this contribution is that the pelagic system, where the dominant biotic component by number and biomass is microscopic, has specific features which strongly differentiate it from the above-the-surface terrestrial systems. Due to this, climate change, i.e. changes in temperature, precipitation and most importantly in the dynamics of the two fluid media, atmosphere and ocean, act with different mechanisms which prevents proceeding with analogies in many cases. In addition, the non-linearity of most of the processes and responses to perturbations requires, in order to obtain reliable forecasts or hindcasts, a detailed analysis of the path followed by the system which is normally overlooked in the step-change simulations or projections.
Myrmarachnine jumping spiders of the new subtribe Levieina from Papua New Guinea (Araneae, Salticidae, Myrmarachnini)
Authors: Maddison Wayne P. , Szűts Tamás
Published: May 2019

A previously unreported radiation of myrmarachnine jumping spiders from New Guinea is described, which, although having few known species, is remarkably diverse in body forms. This clade is the new subtribe Levieina, represented by seven new species in three new genera. WithinLevieagen. n.are three new species,L.herbertisp. n.,L.lornaesp. n., andL.francesaesp. n., all of which are unusual among the myrmarachnines in appearing as typical salticids, not antlike.Papuamyrgen. n.superficially resemblesLigonipesKarsch, 1878 orRhombonotusL. Koch, 1879 as a compact antlike spider, but lacks their laterally-compressed palp and bears an ectal spur on the paturon of the chelicera. Two species ofPapuamyrgen. n.are described,Papuamyromhifosgasp. n.andP.pandorasp. n.Agorioidesgen. n., containingA.cherubinosp. n.andA.papagenasp. n., is antlike, with the carapace sunken inwards (concave) between the posterior lateral and posterior median eyes. Phylogenetic analysis of data from the 28S, 16SND1, and COI gene regions of 29 species of myrmarachnines shows that the three new genera form a clade that is sister to the subtribe Myrmarachnina (Myrmarachnesensu lato), with the subtribe Ligonipedina less closely related.
Functional Electrical Exercise: A Comprehensive Approach for Physical Conditioning of the Spinal Cord Injured Patient
Authors: Phillips Chandler A , Petrofsky Jerrold S , Hendershot Debra M , Stafford Donald
Published: May 2019

ABSTRACT: The purpose of the present study was to define a comprehensive approach to the rehabilitation of the paralyzed individual. Consequently, we have examined the cardiopulmonary effects of active physical therapy (APT) (as measured by blood pressure [BP], heart rate [HR], equivalent ventilatory rate [ VE], oxygen consumption rate [VO
2
], blood lactate [LA], and selected blood gases [pO
2
, pCO
2
and pH]), and the skeletal effects of APT (bone density changes). The equipment utilized in this study were an isokinetic leg trainer, an exercise bicycle ergometer, and a single axis vibration platform. The procedures involved standard exercise protocols followed by the eight SCI subjects (four paraplegics and four quadriplegics) utilizing the above equipment, an evaluation of the cardiopulmonary response to the leg trainer and bicycle ergometer, and a computed tomography study of bone density changes in response to lower leg vibration. The following conclusions were reached: 1) APT results in an increase in cardiovascular stability; over a four-week period mean resting BP increased by an average 29 mmHg in four quadriplegic subjects, while mean exercising BP was reduced by an average 10 mmHg. 2) BP and HR responses to exercise are variable as a function of the level of the injury and type of location of exercise. 3) VO
2
correctly showed level of the exercise and LA showed the stress; however, ventilation was variable with hyperventilation in some subjects. 4) Arterial pO
2
, pCO
2
, pH are variable during exercise; with complete quadriplegics typical pO
2
at rest was 82 mmHg, showing venous admixture as with Pickwickian syndrome with CO2 retention and low arterial pO
2
during exercise. 5) APT results in an increase in bone mineral density through impact loading of the paralyzed extremity.