Scientia Pharmaceutica

3950 KiB

Open AccessArticle

Analysis of flavonoids in Achillea nobilis L. bv capillarv electrophoresis

by Elke Marchart, Almut Hattenberger, Liselotte Krenn and Brigitte Kopp

Sci. Pharm. 2003, 71(2), 133-145; https://doi.org/10.3797/scipharm.aut-03-15 - 15 Jun 2003

Cited by 5 | Viewed by 924

The separation and quantification of the flavonoids occurring in Achillea nobilis L. by a CE-method is described. Using 20 mM sodium borate at pH 9.5 with 20 % of methanol as buffer, the flavonoids were sufficiently separated within 11 minutes. Kaempferol-7-O-neohesperidoside was used [...] Read more.

The separation and quantification of the flavonoids occurring in Achillea nobilis L. by a CE-method is described. Using 20 mM sodium borate at pH 9.5 with 20 % of methanol as buffer, the flavonoids were sufficiently separated within 11 minutes. Kaempferol-7-O-neohesperidoside was used as internal standard for the quantification. Analysis of six different samples showed the flavon-C-glycosides isoorientin, orientin and vitexin as the characteristic main compounds. The contents of flavon-C-glycosides determined by this CE-method correlated with the results achieved by a spectrophotometric determination. Full article

1059 KiB

Open AccessArticle

Pyrrolizidine Alkaloids from Ligularia sibirica Cass. and Tephroseris integrifolia L.

by Helmut Wiedenfeld, S. Narantuya, M. Dumaa and A. Monhbaatar

Sci. Pharm. 2003, 71(2), 129-132; https://doi.org/10.3797/scipharm.aut-03-14 - 28 May 2003

Cited by 5 | Viewed by 1122

Abstract

Tussilagine, isotussilagine, neo-tussilagine and neo-isotussilagine were isolated from Ligularia sibirica whereas Tephroseris integrifolia was found to contain senkirkine, otosenine, hydroxysenkirkine and 07-angeloylheliotridine. The structures were determined using spectroscopical methods (GC-MS; NMR). Full article

2565 KiB

Open AccessArticle

Quantitative determination of the faradiol esters in marigold flowers and extracts

by Gottfried Reznicek and Karin Zitterl-Eglseer

Sci. Pharm. 2003, 71(2), 121-128; https://doi.org/10.3797/scipharm.aut-03-13 - 23 May 2003

Cited by 7 | Viewed by 1402

Abstract

An HPLC method is introduced for the precise quantitative determination of the anti-inflammatory active faradiol esters from marigold flowers and extracts. After a prepurification the HPLC analysis allows the proof of the quality of marigold flowers or C0₂-extracts used for pharmaceutical preparations. Full article

2168 KiB

Open AccessArticle

Tropane alkaloids from a Brazilian bark traded as "Catuaba"

by Sabine Glasl, Armin Presser, Ingrid Werner, Ernst Haslinger and Johann Jurenitsch

Sci. Pharm. 2003, 71(2), 113-119; https://doi.org/10.3797/scipharm.aut-03-12 - 15 May 2003

Cited by 1 | Viewed by 1166

Abstract

Dichloromethane extracts of a Brazilian bark assigned as Anemopaegma mirandum contained four tropane alkaloids. MS-, UV-, IR-, ¹H NMR-data and specific optical rotation allowed the identification of catuabin C and its 7-exo-hydroxy-20-methyl-derivative. As no alkaloids are described for Anemopaegma these [...] Read more.

Dichloromethane extracts of a Brazilian bark assigned as Anemopaegma mirandum contained four tropane alkaloids. MS-, UV-, IR-, ¹H NMR-data and specific optical rotation allowed the identification of catuabin C and its 7-exo-hydroxy-20-methyl-derivative. As no alkaloids are described for Anemopaegma these results indicate heterogeneity for the investigated drug and require a further review. Full article

3207 KiB

Open AccessArticle

Formulation and Evaluation of Parenteral Sustained Release Microspheres of Diclofenac Sodium

by C. Sajeev, R. Archna, V. Gupta, A. Sobti and R. N. Saha

Sci. Pharm. 2003, 71(2), 101-111; https://doi.org/10.3797/scipharm.aut-03-11 - 10 May 2003

Cited by 1 | Viewed by 1162

Abstract

The aim of this study was to formulate and evaluate microsphere based depot type parenteral sustained release formulation of diclofenac sodium (DFS). Drug was formulated in the form of microspheres, using varying proportion of ethylcellulose (EC) as the retardant material to extend the [...] Read more.

The aim of this study was to formulate and evaluate microsphere based depot type parenteral sustained release formulation of diclofenac sodium (DFS). Drug was formulated in the form of microspheres, using varying proportion of ethylcellulose (EC) as the retardant material to extend the release, by phase separation-coacervation technique. The in vitro release pattern of the designed formulations was studied using modified Franz diffusion cell. In vivo pharmacodynamic study was carried out by determining the index of analgesia (increase in response time to thermal stress as percentage of basal response time). Tail flick method was employed to measure both the degree of analgesia and its duration of action. The prepared microspheres were white, free flowing, and spherical in shape with a mean particle size of 50 μm. In vitro release study of the micro-spheres in aqueous media was found to extend the release of DFS beyond 24 hours with DFS and EC ratio 1:3. The plot of log percentage remaining to be released vs. time gave a linear relationship indicating first-order release kinetics. The in vitro release rate constant (K_r) for different microspheres varied between 0.1448 hr^-1 and 0.0256 hr^-1. A good correlation was obtained between K, and proportion of EC in the microspheres. In vivo pharmacodynamic studies indicated that the duration of analgesic action is prolonged beyond 24 hrs in case of microsphere products of 1:3 ratio of DFS to EC, whereas administration of marketed parenteral preparation showed activity only up to 11hrs. Also, a good correlation was obtained between analgesic activity in vivo and cumulative percentage of drug release from the formulations. Full article

3547 KiB

Open AccessArticle

Lacking of efflux mechanism in clinical isolate of Pseudomonas aerupinosa highly resistant to β-Lactams And imimnem

by Ashraf. A. Kadry

Sci. Pharm. 2003, 71(2), 89-100; https://doi.org/10.3797/scipharm.aut-03-10 - 4 May 2003

Viewed by 874

Abstract

In this investigation, the isolate of Pseudomonas aeruginosa from cystic fibrosis was highly resistant to β-lactarns and β-lactamase inhibitors. The resistant determinants of clinical isolate to imipenem, ceftazidime, ceftriaxone and cefepime were conjugally non-transfer. The slow or non-enzymatically mediated breakdown of imipenem and [...] Read more.

In this investigation, the isolate of Pseudomonas aeruginosa from cystic fibrosis was highly resistant to β-lactarns and β-lactamase inhibitors. The resistant determinants of clinical isolate to imipenem, ceftazidime, ceftriaxone and cefepime were conjugally non-transfer. The slow or non-enzymatically mediated breakdown of imipenem and other broad spectrum p-lactams suggest the resistance of P.aeruginosa isolate to these drugs might be attributed to either permeability or efflux. Impaired penetration of imipenem and other p-lactams through the membrane was detected by a diminished expression of outer membrane (OM) proteins of approximate weight of 46 and 39 Kdal, matched to Opr D and OprF, respectively. Efflux resistance mechanism for meropenem and p-lactams has been ruled out since the isolate failed to express outer membrane protein of about 50 Kdal, which is matched to Opr M protein channel. Thus, reduced permeability in the clinical isolate may be the main mechanism conferring resistance against p-lactarns including imipenem. Full article

3758 KiB

Open AccessArticle

Composition and stability of complexes of Ephedrine hydrochloride with Nⁱ²⁺, Zn²⁺, and Cd²⁺ as toxic ions

by Nabawia M. EL Guindi

Sci. Pharm. 2003, 71(2), 75-88; https://doi.org/10.3797/scipharm.aut-03-09 - 28 Apr 2003

Viewed by 855

Abstract

The complexes of Ephedrine with Nickel, Zinc and Cadmium ions have been investigated spectrophotometricalfy using the method of corresponding solutions [I-3] and pH-metrically using Irving and Rossoti technique [4] Two compositions were observed spectrophotometrically 1 : 1 and 2: 1 (L: M) for [...] Read more.

The complexes of Ephedrine with Nickel, Zinc and Cadmium ions have been investigated spectrophotometricalfy using the method of corresponding solutions [I-3] and pH-metrically using Irving and Rossoti technique [4] Two compositions were observed spectrophotometrically 1 : 1 and 2: 1 (L: M) for concentration of metal ions (0.5 x 10^-3 M and 1 x 10^-3 M) hile the first composition only predominate at concentration of metal ions (1.5 x 10^-3 M and 2 x 10^-3 M ). The stability of complexes show that complexes of Ni²⁺ are more stable than that of Zn²⁺ an Cd²⁺, Moreover, the composition and stabilities of complexes were studied pHmetrically in aqueous medium at 0.1 M NaCl and two different temperatures 30°C and 40°C; hence the value of the free energy change (ΔG°), the enthalpy (ΔH°) and the entropy (ΔS°) were calculated at 30°C. Beside the role of Ephedrine as chelating agent to toxic elements, the complexometric method was used for the determination of Ephedrine in its pure form and in tablets. Full article

4599 KiB

Open AccessArticle

Synthesis and in vitro Anti-HIV Screening of Certain 2-(Benzoxazol-2-ylamino)-3H-4-oxopyrimidines

by Sherif A. F. Rostom, Hesharn T. Y. Fahmy and Manal N. Ssaudi

Sci. Pharm. 2003, 71(2), 57-74; https://doi.org/10.3797/scipharm.aut-03-08 - 14 Apr 2003

Cited by 17 | Viewed by 1043

Abstract

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), [...] Read more.

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 %).
Full article

1678 KiB

Open AccessArticle

Atypisches Verhalten von Thiophenderivaten gegeniiber Reduktions- bzw. Thionierungs-Versuchen

by T. Erker and K. Trinkl

Sci. Pharm. 2003, 71(2), 51-56; https://doi.org/10.3797/scipharm.aut-03-07 - 10 Apr 2003

Cited by 2 | Viewed by 854

Abstract

To prepare required thiolactarns. initial experiments were done with the lactarns 1 - 3 and Lawessol reagent. However in preliminary trials. treatment of the compounds failed to give the desired molecules. Modification of the reaction conditions. paticularly with regard to the solvent and [...] Read more.

To prepare required thiolactarns. initial experiments were done with the lactarns 1 - 3 and Lawessol reagent. However in preliminary trials. treatment of the compounds failed to give the desired molecules. Modification of the reaction conditions. paticularly with regard to the solvent and the reaction temperature. did not permit the preparation of the corresponding thiolactams. The keto function in position 6 was thought to be responsible for this atypical behaviour. Therefore. as the following step. the acetyl group in compounds 1 - 3 should be reduced to the corresponding ethyl derivatives. This reaction did not give the needed bicycles. Reduction of compounds 4 - 6 with triethylsilanel trifluoroacetic acid brought up compounds 7 - 9. Full article

3682 KiB

Open AccessArticle

Svnthesis of 3-(3.5-Dioxo-[1,2,4]-oxadiazolidin-2-vl)propylphosphonic Acids

by Thomas Kurz, Detlef Geffken and Claudia Wackendorff

Sci. Pharm. 2003, 71(2), 39-49; https://doi.org/10.3797/scipharm.aut-03-06 - 5 Apr 2003

Cited by 2 | Viewed by 1027

Abstract

Cyclic carbonylation of hydroxyureas 3 with 1,1'-carbonyldiimidazole gave 3-(3,5-dioxo-[1,2,4]oxadiazolidin-2yl)propylphosphonic acid diethyl esters 4 which were converted into the corresponding phosphonic acids 5 with bromotrimethylsilane. Full article

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Sci. Pharm., Volume 71, Issue 2 (June 2003) – 10 articles , Pages 39-145

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