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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 69, Issue 2 (June 2001) – 12 articles , Pages 109-234

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Open AccessArticle
STEROIDAL SAPONINS FROM SOLANUM UNGUICULATUM (A.) RICH
Sci. Pharm. 2001, 69(2), 219-234; https://doi.org/10.3797/scipharm.aut-01-23 - 30 Jun 2001
Cited by 4 | Viewed by 497
Abstract
Seven steroidal saponins were isolated for the first time from the green berries of Solanum unguiculatum. Their structures were determined by spectroscopic analysis as well as hydrolysis of the glycosides into the corresponding sapogenins, diosgenin, chlorogenin, diosgenin-3-O-β-D-galactopyranoside, diosgenin-3-O-β-D-glucopyranosyl-(1 → 4)-β-D-galactopyranoside, 3β-hydroxyl-(25R) 5 [...] Read more.
Seven steroidal saponins were isolated for the first time from the green berries of Solanum unguiculatum. Their structures were determined by spectroscopic analysis as well as hydrolysis of the glycosides into the corresponding sapogenins, diosgenin, chlorogenin, diosgenin-3-O-β-D-galactopyranoside, diosgenin-3-O-β-D-glucopyranosyl-(1 → 4)-β-D-galactopyranoside, 3β-hydroxyl-(25R) 5 α-spirostan-6-one (laxogenin) 3-O-α-L-rhamnopyranosyl-(1 → 2)-β-D-glucopyranoside, isonarthogenin-3-O-α-L-rhamnopyranosyl-(1 → 2)-O-[α-L-rhamnopyranosyl-(1 → 4)-β-D-glucopyranoside and 25(S) spirost-5-en-3 β, 17 α, 27 triol-3-O-[α-L-rhamnopyranosyl-(1 → 2)] [α-L-rhamnopyranosyl (1 → 4)]-β-D-glucopyranoside. Full article
Open AccessArticle
Flavonoid Glycosides from Achillea roseo-albax
Sci. Pharm. 2001, 69(2), 211-217; https://doi.org/10.3797/scipharm.aut-01-22 - 30 Jun 2001
Cited by 4 | Viewed by 440
Abstract
In the first detailed study of the flavonoid pattern of Achillea roseo-alba rutin, apigenin-7-O-ß-glucopyranoside, luteolin-7-O-ß-glucopyranoside, isorhamnetin-3-O-rutinoside, schaftoside, luteolin-4’-O-ß-glucopyranoside and 6-OH-luteolin-7-O-ß-glucopyranosid were proven in the methanolic extract of aerial parts of the plant. Additionally quercetin-3-O-[ß-apiofiranosyl-(1′′′→2′′)-ß-glucopyranoside] was identified for the first time in the genus [...] Read more.
In the first detailed study of the flavonoid pattern of Achillea roseo-alba rutin, apigenin-7-O-ß-glucopyranoside, luteolin-7-O-ß-glucopyranoside, isorhamnetin-3-O-rutinoside, schaftoside, luteolin-4’-O-ß-glucopyranoside and 6-OH-luteolin-7-O-ß-glucopyranosid were proven in the methanolic extract of aerial parts of the plant. Additionally quercetin-3-O-[ß-apiofiranosyl-(1′′′→2′′)-ß-glucopyranoside] was identified for the first time in the genus Achillea. Full article
Open AccessArticle
Antinociceptive Activity of Vigabatrin in Mice After Prolonged Treatment: Possible Development of Tolerance
Sci. Pharm. 2001, 69(2), 203-210; https://doi.org/10.3797/scipharm.aut-01-21 - 30 Jun 2001
Cited by 1 | Viewed by 398
Abstract
We have evaluated vigabatrin (γ-vinyi-γ-aminobutyric acid), an irreversible inhibitor of γ-aminobutyric acid (GABA)-transarninase responsible for GABA degradation, for its effects on nociceptive response, changes in spontaneous locomotor activity and body temperature in mice after a prolonged treatment regimen. The mice received [...] Read more.
We have evaluated vigabatrin (γ-vinyi-γ-aminobutyric acid), an irreversible inhibitor of γ-aminobutyric acid (GABA)-transarninase responsible for GABA degradation, for its effects on nociceptive response, changes in spontaneous locomotor activity and body temperature in mice after a prolonged treatment regimen. The mice received vigabatrin 0.26% w/v chronically in drinking water for 7, 14 and 21 days. Changes in locomotion, body temperature and nociception were recorded after 7, 14 and 21 days respectively in different groups. Also, possible withdrawal symptoms were determined up to three days after 7, 14 or 21 days of treatment. In another experiment the animals were given acutely, 250 mg/kg of vigabatrin by oral gavage and the changes in response to the said parameters were assessed 90 min after treatment. Acute treatment increased the latency in the hot-plate reaction time and a highly significant decline in locomotion and body temperature. In contrast to the acute treatment studies, there were essentially no effects of vigabatrin on nociception, locomotor activity or body temperature either on the last day of each treatment or upon withdrawal for the next consecutive three days. We conclude that the changes in nociception, locomotion and body temperature after acute treatment with vigabatrin are due to neuromediator interactions and a possible direct effect of GABA accumulation. After prolonged treatment tolerance to the pharmacological effects of vigabatrin develop that was evident by no change in nociception, locomotion and body temperature. This may be attributed to the possible failure in the maintenance of GABA pools resulting in a reduction in enhanced GABA release mediated by vigabatrin in acute treatment. Further studies of mechanisms by which vigabatrin tolerance develops to these pharmacological responses are warranted. Full article
Open AccessArticle
Utility of Nickel for Atomic Absorption Spectrophotometric Determination of Selected Acidic Drugs
Sci. Pharm. 2001, 69(2), 189-201; https://doi.org/10.3797/scipharm.aut-01-20 - 30 Jun 2001
Cited by 5 | Viewed by 388
Abstract
A simple and accurate method is described for the quantitative determination of flufenamic acid, mefenamic acid, tranexamic acid, furosemide, diclofenac sodium and thiaprofenic acid by precipitation reactions with nickel(II) followed by direct determination of the ions in the precipitate or indirect determination of [...] Read more.
A simple and accurate method is described for the quantitative determination of flufenamic acid, mefenamic acid, tranexamic acid, furosemide, diclofenac sodium and thiaprofenic acid by precipitation reactions with nickel(II) followed by direct determination of the ions in the precipitate or indirect determination of the ions in the filtrate by atomic absorption spectroscopy. Statistical analysis of the results compared to assays used in pharmacopeas and the Amax. methods revealed equal precision and accuracy. Furthermore the assays were also applied for the determination of these drugs in pharmaceutical preparations. Full article
Open AccessArticle
Pyrocatechol Violet in Pharmaceutical Analysis Part II. A Spectrophotometric Method for the Determination of Paracetamol in Pure and in Pharmaceutical Dosage Forms
Sci. Pharm. 2001, 69(2), 179-188; https://doi.org/10.3797/scipharm.aut-01-19 - 30 Jun 2001
Cited by 3 | Viewed by 465
Abstract
A spectrophotometric method for the selective determination of paracetamol based on its reaction with pyrochatechol violet under basic conditions to form an ion-pair complex is described. The absorption maximum of the coloured ion-pair formed is observed at 652 nm and the molar absorptivity [...] Read more.
A spectrophotometric method for the selective determination of paracetamol based on its reaction with pyrochatechol violet under basic conditions to form an ion-pair complex is described. The absorption maximum of the coloured ion-pair formed is observed at 652 nm and the molar absorptivity is 4.54 x10-3l mol-1 cm-1. Beer's law is obeyed over the concentration range 0.5-34.0 μg ml-1, while that obtained using Ringbom method is in the range 3.5 -32.0 μg ml-1. There is no interference from common additives, excipients and commercial drugs present in their formulations suggesting a highly selective procedure compared with others. Statistical analysis of the obtained results showed that there is, no significant difference and absence of any systematic error in the method compared with the official one. The method is simple, rapid and convenient and was applied successfully to the determination of paracetamol in pure and in its dosage forms compared with the official method. Full article
Open AccessArticle
METOPROLOL EFFECT ON FATTY ACIDS COMPOSITION OF CELL MEMBRANE PHOSPHOLIPIDS
Sci. Pharm. 2001, 69(2), 167-178; https://doi.org/10.3797/scipharm.aut-01-18 - 30 Jun 2001
Cited by 2 | Viewed by 401
Abstract
It is quite well known that β-blockers influence the stability of cell membranes, but the effect of metoprolol on the composition of cell membrane lipids is not established. On the other hand, synchronous culture of Chlorella vulgaris cells, which consists of cells brought [...] Read more.
It is quite well known that β-blockers influence the stability of cell membranes, but the effect of metoprolol on the composition of cell membrane lipids is not established. On the other hand, synchronous culture of Chlorella vulgaris cells, which consists of cells brought to the same developmental stage by cycling lighting, provides a convenient biological model in unidirectional analyses aimed at assessment of effects of xenobiotics on cells. Advantages of the model include short life cycle and possibility to control metabolic processes of the cells across the broad range. We assessed the effect of metoprolol on fatty acids composition of cell membrane phospholipids in consecutive life cycle stages of Chlorella vulgaris. Lipids were extracted using a chlorofonn/methanol method. Phospholipids were precipitated from the chloroform phase with cold acetone and following centrifugation the pellet of phospholipids was hydrolyzed in alkaline solution. Fatty acids were extracted with petroleum ether and then methylated with BF3-methanol. This protocol produced methyl esters of fatty acids which were subjected to GC-MS analysis. Metoprolol had no effect on the number of progeny cells of Chlorella vulgaris throughout their life cycle at the concentration range tested (5x10-5 M, 5x10-6 M, 5x10-7 M). However, we observed stimulation of biological activity of Chlorclla cells as measured by spectrophotomctry at λ=680 nm. Metoprolol, at the highest concentration, increased phospholipids content in mother cells. Simultaneously, relative amount and saturation level of thc fatty acids remained constant. Full article
Open AccessArticle
Reaction of Prop-2-ynylamine with Isochromadiones : Formation of Amides
Sci. Pharm. 2001, 69(2), 161-166; https://doi.org/10.3797/scipharm.aut-01-17 - 30 Jun 2001
Cited by 1 | Viewed by 392
Abstract
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 [...] Read more.
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. Full article
Open AccessArticle
Extractive Spectrophotometric Determination of Nortriptyline Hydrochloride Using Sudan II, IV and Black B
Sci. Pharm. 2001, 69(2), 151-160; https://doi.org/10.3797/scipharm.aut-01-16 - 30 Jun 2001
Viewed by 687
Abstract
A simple spectrophotometric methods has been developed for the determination of nortriptyline hydrochloride in pure and in pharmaceutical
formulations based on the formation of ion-pair complexes with sudun II (SII), sudan (IV) (SIV) and sudan black B (SBB
[...] Read more.
A simple spectrophotometric methods has been developed for the determination of nortriptyline hydrochloride in pure and in pharmaceutical
formulations based on the formation of ion-pair complexes with sudun II (SII), sudan (IV) (SIV) and sudan black B (SBB). The selectivity of the method was improved through extraction with chloroform. The optimum conditions for complete extracted colour development were assessed. The absorbance measurements were made at 534, 596 and 649 nm for SII, SIV and SBB complexes, respectively. The calibration graph was linear in the ranges 0.5- 280. 0.5- 37.5 and 0.5 – 31.0 μg ml−1 of the drug usiny the same reagents, respectively. The precision of the procedure was checked by calculating the relative standard deviation of ten replicate determinations on 15 μg ml−1 of nortriptyline HCI and was found to be 1.7, 1.3 and 1.55% using SII, SIV, and SBB complexes, respectively. The molar absorptivity and Sandell sensitivity for each ion-pair were calculated. The proposed methods were successfully applied to the deterniination of pure nortriptyline HCI and in pharmaceutical formulations, and the results demonstrated that the method is equally accurate, precise and reproducible as the official method.
Full article
Open AccessArticle
Spectrophotometric Estimation of Cefuroxime and Ceftazidime in Bulk and in Dosage Forms
Sci. Pharm. 2001, 69(2), 143-150; https://doi.org/10.3797/scipharm.aut-01-15 - 30 Jun 2001
Cited by 6 | Viewed by 422
Abstract
Three simple, accurate and sensitive spectrophotometric methods (A, B and C) for the determination of cefuroxime and ceftazidime in bulk samples and in dosage forms are described. They are based on the reaction with nitrous acid forming a nitroso derivatives which can be
[...] Read more.
Three simple, accurate and sensitive spectrophotometric methods (A, B and C) for the determination of cefuroxime and ceftazidime in bulk samples and in dosage forms are described. They are based on the reaction with nitrous acid forming a nitroso derivatives which can be measured at λmax 350 and 355 nm for cefuroxime (I) and ceftazidime (II), respectively (method A) or by oxidation of drug I or II with an excess of freshly prepared hypobromite and the residual hypobromite was treated with sodium fluorescein at the optimum experimental conditions and measured at λmax at 517 nm (method B). Method C is based on the formation of tris (0-phenanthroline) iron(II) complex (ferroin) upon the oxidation of the studied drug I or II with an iron (III)-o-phenanthroline mixture in acetate buffer solution of pH 3.6 and measuring at λmax 509 nm. Regression analysis of Beer-Lambert plots showed good correlation in the concentration ranges 0.2 – 6.0, 0.2 – 3.2 and 0.1 – 5.6 μg ml−1 for methods A, B and C, respectively. The apparent molar absorptivity, Sandell sensitivity, detection and quantitation limits were calculated. For more accurate results, Ringbom optimum concentration range was 0.2 – 5.6 μg ml−1. The validity of the proposed methods was tested by analysing dosage forms containing the studied drugs I and II. The relative standard deviations were ≤ 1.25% with recoveries 98.6 – 101.4% .
Full article
Open AccessArticle
A Study of Mucoadhesive Bond Strength of Buccoadhesive Compacts for Systemic Drug Delivery: In-vitro/ In-vivo correlation
Sci. Pharm. 2001, 69(2), 123-141; https://doi.org/10.3797/scipharm.aut-01-14 - 30 Jun 2001
Cited by 3 | Viewed by 375
Abstract
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
[...] Read more.
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.
Full article
Open AccessArticle
Nitraminanaloge Suosan-Derivate als potentielle Süßstoffe
Sci. Pharm. 2001, 69(2), 119-122; https://doi.org/10.3797/scipharm.aut-01-13 - 30 Jun 2001
Cited by 1 | Viewed by 434
Abstract
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.
Full article
Open AccessArticle
Synthesis and In Vitro Evaluation of Chitosan-Thioglycolic Acid Conjugates
Sci. Pharm. 2001, 69(2), 109-118; https://doi.org/10.3797/scipharm.aut-01-12 - 30 Jun 2001
Cited by 48 | Viewed by 778
Abstract
The cationic thiomer chitosan-thioglycolic acid (TGA) shows excellent mucoadhesive features. In order to deepen the knowledge concerning this new excipient the optimization of its synthesis and a detailed characterization of its properties was the objective of this study Mediated by increasing quantities of
[...] Read more.
The cationic thiomer chitosan-thioglycolic acid (TGA) shows excellent mucoadhesive features. In order to deepen the knowledge concerning this new excipient the optimization of its synthesis and a detailed characterization of its properties was the objective of this study Mediated by increasing quantities of a carbodiimide, thioglycolic acid was covalently attached to chitosan forming amide bonds with the primary amino groups of the polymer Determined with Ellman's reagent, 38 ± 3, 104 ± 2, 685 ± 43, and 885 ± 7 pmol thiol groups (n=3; ± SD) were bound per gram polymer at carbodiimide concentrations of 50, 75, 100, and 125 mM, respectively. The immobilized thiol groups displayed a comparatively higher reactivity to form disulfide bonds than the thiol groups in a corresponding mixture of chitosan and free unconjugated TGA. In an aqueous 0.5% (rnlv) chitosan-TGA gel 59 ± 5% of the thiol groups formed disulfide bonds within 6 hours at pH 6.0, whereas merely 5 ± 3% were oxidized in the corresponding physical mixture of chitosan and TGA. Diffusion studies showed that the modified polymer was capable of binding cysteine and cysteine methyl ester. The result supports the theory that the improved mucoadhesive properties of thiolated chitosan are based on the formation of disulfide bonds with cysteine moieties of mucus glycoproteins. Because of its availability via an efficient synthetic pathway and its mucoadhesive properties based on the capability to bind cysteine subunits, chitosan-TGA seems to be a promising new excipient for various drug delivery systems.
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