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Scientia Pharmaceutica is published by MDPI from Volume 84 Issue 3 (2016). Articles in this Issue were published by another publisher in Open Access under a CC-BY (or CC-BY-NC-ND) licence. Articles are hosted by MDPI on mdpi.com as a courtesy and upon agreement with Austrian Pharmaceutical Society (Österreichische Pharmazeutische Gesellschaft, ÖPhG).

Table of Contents

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

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Open AccessArticle
Analysis of flavonoids in Achillea nobilis L. bv capillarv electrophoresis
Sci. Pharm. 2003, 71(2), 133-145; https://doi.org/10.3797/scipharm.aut-03-15
Received: 1 April 2003 / Revised: 15 May 2003 / Accepted: 15 May 2003 / Published: 15 June 2003
Cited by 1 | Viewed by 243 | PDF Full-text (3950 KB)
Abstract
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
Open AccessArticle
Pyrrolizidine Alkaloids from Ligularia sibirica Cass. and Tephroseris integrifolia L.
Sci. Pharm. 2003, 71(2), 129-132; https://doi.org/10.3797/scipharm.aut-03-14
Received: 12 November 2002 / Revised: 22 November 2002 / Accepted: 22 November 2002 / Published: 28 May 2003
Viewed by 291 | PDF Full-text (1059 KB)
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
Open AccessArticle
Quantitative determination of the faradiol esters in marigold flowers and extracts
Sci. Pharm. 2003, 71(2), 121-128; https://doi.org/10.3797/scipharm.aut-03-13
Received: 3 November 2002 / Revised: 28 April 2003 / Accepted: 28 April 2003 / Published: 23 May 2003
Cited by 1 | Viewed by 255 | PDF Full-text (2565 KB)
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
Open AccessArticle
Tropane alkaloids from a Brazilian bark traded as "Catuaba"
Sci. Pharm. 2003, 71(2), 113-119; https://doi.org/10.3797/scipharm.aut-03-12
Received: 2 November 2002 / Revised: 10 March 2003 / Accepted: 10 March 2003 / Published: 15 May 2003
Viewed by 249 | PDF Full-text (2168 KB)
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
Open AccessArticle
Formulation and Evaluation of Parenteral Sustained Release Microspheres of Diclofenac Sodium
Sci. Pharm. 2003, 71(2), 101-111; https://doi.org/10.3797/scipharm.aut-03-11
Received: 17 September 2002 / Revised: 14 January 2003 / Accepted: 14 January 2003 / Published: 10 May 2003
Viewed by 271 | PDF Full-text (3207 KB)
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 (Kr) 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
Open AccessArticle
Lacking of efflux mechanism in clinical isolate of Pseudomonas aerupinosa highly resistant to β-Lactams And imimnem
Sci. Pharm. 2003, 71(2), 89-100; https://doi.org/10.3797/scipharm.aut-03-10
Received: 11 October 2002 / Revised: 14 January 2003 / Accepted: 14 January 2003 / Published: 4 May 2003
Viewed by 242 | PDF Full-text (3547 KB)
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
Open AccessArticle
Composition and stability of complexes of Ephedrine hydrochloride with Ni2+, Zn2+, and Cd2+ as toxic ions
Sci. Pharm. 2003, 71(2), 75-88; https://doi.org/10.3797/scipharm.aut-03-09
Received: 5 November 2002 / Revised: 3 March 2003 / Accepted: 3 March 2003 / Published: 28 April 2003
Viewed by 249 | PDF Full-text (3758 KB)
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
Open AccessArticle
Synthesis and in vitro Anti-HIV Screening of Certain 2-(Benzoxazol-2-ylamino)-3H-4-oxopyrimidines
Sci. Pharm. 2003, 71(2), 57-74; https://doi.org/10.3797/scipharm.aut-03-08
Received: 8 January 2003 / Revised: 14 March 2003 / Accepted: 14 March 2003 / Published: 14 April 2003
Cited by 4 | Viewed by 357 | PDF Full-text (4599 KB)
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
Open AccessArticle
Atypisches Verhalten von Thiophenderivaten gegeniiber Reduktions- bzw. Thionierungs-Versuchen
Sci. Pharm. 2003, 71(2), 51-56; https://doi.org/10.3797/scipharm.aut-03-07
Received: 23 October 2002 / Revised: 29 November 2002 / Accepted: 29 November 2002 / Published: 10 April 2003
Viewed by 228 | PDF Full-text (1678 KB)
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
Open AccessArticle
Svnthesis of 3-(3.5-Dioxo-[1,2,4]-oxadiazolidin-2-vl)propylphosphonic Acids
Sci. Pharm. 2003, 71(2), 39-49; https://doi.org/10.3797/scipharm.aut-03-06
Received: 5 February 2003 / Revised: 4 April 2003 / Accepted: 4 April 2003 / Published: 5 April 2003
Viewed by 249 | PDF Full-text (3682 KB)
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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