Next Issue
Volume 80, September
Previous Issue
Volume 80, March
Scientia Pharmaceutica is published by MDPI from Volume 84 Issue 3 (2016). Previous articles were published by another publisher in Open Access under a CC-BY (or CC-BY-NC-ND) licence, and they are hosted by MDPI on mdpi.com as a courtesy and upon agreement with Austrian Pharmaceutical Society (Österreichische Pharmazeutische Gesellschaft, ÖPhG).

Sci. Pharm., Volume 80, Issue 2 (June 2012) – 19 articles , Pages 265-496

  • Issues are regarded as officially published after their release is announced to the table of contents alert mailing list.
  • You may sign up for e-mail alerts to receive table of contents of newly released issues.
  • PDF is the official format for papers published in both, html and pdf forms. To view the papers in pdf format, click on the "PDF Full-text" link, and use the free Adobe Readerexternal link to open them.
Order results
Result details
Select all
Export citation of selected articles as:
Article
Equilibrium and Release Properties of Aqueous Dispersions of Non-Steroidal Anti-Inflammatory Drugs Complexed with Polyelectrolyte Eudragit E 100
Sci. Pharm. 2012, 80(2), 487-496; https://doi.org/10.3797/scipharm.1107-17 - 30 Apr 2012
Cited by 8 | Viewed by 743
Abstract
Equilibria and release properties of aqueous systems consisting of a set of five non-steroidal anti-inflammatory drugs (AH) complexed with the cationic polymethacrylate Eudragit E 100 (EU) are reported in this study. The composition (EU(AH)50 (HCl)50) having fifty mole percent of [...] Read more.
Equilibria and release properties of aqueous systems consisting of a set of five non-steroidal anti-inflammatory drugs (AH) complexed with the cationic polymethacrylate Eudragit E 100 (EU) are reported in this study. The composition (EU(AH)50 (HCl)50) having fifty mole percent of each counterion (A and Cl) produces clear, stable aqueous dispersions in which a remarkably high proportion of AH (higher than 98%) is condensed with the PE under the form of ion pairs. This property expands the interval of pH in which AH are aqueous soluble. The set of AH contains members with and without an alpha methyl group (-(CH3)CH-COOH: Flurbiprofen, Naproxen, Ketoprofen) and (-CH2-COOH: Diclofenac, Indomethacin). The proportion of ion pairs in the complexes was lower in the former group. Release of AH from the complexes toward a saline (NaCl 0.9%) solution was assayed in Franz cells. The five complexes behaved as drug carriers that exhibited a slow drug release with a remarkable zero order. In line with the percentages of counterionic condensation observed, release rates from -(CH3)CH-COOH complexes were clearly higher than those of -CH2-COOH ones. Full article
Article
In Vitro Drug Absorption Enhancement Effects of Aloe vera and Aloe ferox
Sci. Pharm. 2012, 80(2), 475-486; https://doi.org/10.3797/scipharm.1202-10 - 01 Apr 2012
Cited by 14 | Viewed by 819
Abstract
The effect of whole leaf and gel materials from two aloe species (Aloe vera and A. ferox) was compared with that of the precipitated polysaccharides from these aloe materials on the transepithelial electrical resistance (TEER) as well as transport of a [...] Read more.
The effect of whole leaf and gel materials from two aloe species (Aloe vera and A. ferox) was compared with that of the precipitated polysaccharides from these aloe materials on the transepithelial electrical resistance (TEER) as well as transport of a model compound (atenolol) in the apical-to-basolateral direction across rat intestinal tissue. All the aloe leaf materials and precipitated polysaccharides had a statistically significant effect of lowering the TEER (P < 0.05) compared to the control group, which indicates their ability to open tight junctions between adjacent epithelial cells. In contrast to the expectation from the TEER results, only the precipitated polysaccharides from dehydrated A. vera gel (Daltonmax 700®) had a statistically significant effect of enhancing the transport of atenolol (P < 0.05). These in vitro results therefore indicate that A. vera gel polysaccharides have potential as drug absorption enhancing agents in novel pharmaceutical drug delivery systems. Full article
Article
Stability-Indicating Liquid Chromatographic Method for the Quantification of the New Antipsychotic Agent Asenapine in Bulk and in Pharmaceutical Formulation
Sci. Pharm. 2012, 80(2), 407-418; https://doi.org/10.3797/scipharm.1112-07 - 01 Apr 2012
Cited by 17 | Viewed by 806
Abstract
A simple, specific and stability-indicating reversed phase high performance liquid chromatographic method was developed for the quantitative determination of asenapine in tablet dosage form. A SunFire C18, 5 μm column having 250×4.6 mm i.d. in isocratic mode, with mobile phase containing 0.02 M [...] Read more.
A simple, specific and stability-indicating reversed phase high performance liquid chromatographic method was developed for the quantitative determination of asenapine in tablet dosage form. A SunFire C18, 5 μm column having 250×4.6 mm i.d. in isocratic mode, with mobile phase containing 0.02 M potassium dihydrogen phosphate: acetonitrile (95:05, v/v, pH 3.5 adjusted with 1% o-phosphoric acid) was used. The flow rate was 1.0 mL min−1 and effluents were monitored at 232 nm. The retention time of asenapine was 5.51 min. The linearity for asenapine was in the range of 0.1–20 μg/ml. The recoveries obtained for asenapine were 98.31–101.51%. Asenapine stock solutions were subjected to acid and alkali hydrolysis, chemical oxidation, sunlight and dry heat degradation. The degraded product peaks were well resolved from the pure drug peak with significant difference in their retention time values. Stressed samples were assayed using developed LC method. The proposed method was validated with respect to linearity, accuracy, precision and robustness. The method was successfully applied to the estimation of asenapine in tablet dosage form. Full article
Article
Development and Validation of a Stability-Indicating RP-UPLC Method for Determination of Rosuvastatin and Related Substances in Pharmaceutical Dosage Form
Sci. Pharm. 2012, 80(2), 393-406; https://doi.org/10.3797/scipharm.1201-09 - 26 Mar 2012
Cited by 25 | Viewed by 1574
Abstract
A stability-indicating reversed phase ultra performance liquid chromatographic (RP-UPLC) method was developed for the determination of related substances in rosuvastatin calcium (ROSV) tablet dosage form. The chromatographic separation was achieved on an Acquity BEH C18 (100 mm × 2.1 mm, 1.7 μm) column [...] Read more.
A stability-indicating reversed phase ultra performance liquid chromatographic (RP-UPLC) method was developed for the determination of related substances in rosuvastatin calcium (ROSV) tablet dosage form. The chromatographic separation was achieved on an Acquity BEH C18 (100 mm × 2.1 mm, 1.7 μm) column with mobile phase containing a gradient mixture of solvent-A (0.1% trifluoroacetic acid) and solvent-B (methanol). The eluted compounds were monitored at 240 nm and the run time was 10.0 min. Degradation behavior of the ROSV was studied under various degradation stress conditions. Four major unknown degradation products (late eluting impurities) were found in acid stress condition and two unknown degradation products were found in oxidative stress condition. The developed method separates (six) unknown impurities, (three) known impurities and ROSV substance from each other, providing the stability-indicating power of the method. The developed RP-UPLC method was validated according to the International Conference on Harmonization (ICH) guidelines. The developed and validated RP-UPLC method is LC-MS compatible and can be applied for identification of eluted unknown impurities of ROSV. Full article
Article
Stability-Indicating LC Method for the Determination of Prasugrel Hydrochloride in Pharmaceutical Dosage Form
Sci. Pharm. 2012, 80(2), 379-392; https://doi.org/10.3797/scipharm.1201-05 - 20 Mar 2012
Cited by 11 | Viewed by 805
Abstract
A simple, rapid and precise method was developed for the quantitative estimation of prasugrel hydrochloride in pharmaceutical dosage form. A chromatographic separation of prasugrel and its degradants was achieved with Zorbax XDB C8, 150 x 4.6 mm, 3.5μm analytical column using aqueous solution [...] Read more.
A simple, rapid and precise method was developed for the quantitative estimation of prasugrel hydrochloride in pharmaceutical dosage form. A chromatographic separation of prasugrel and its degradants was achieved with Zorbax XDB C8, 150 x 4.6 mm, 3.5μm analytical column using aqueous solution of 0.05 M ammonium acetate pH 4.5 with acetic acid-acetonitrile (40:60 v/v). The instrumental settings include flow rate of 1.0 ml/min, column temperature at 30°C and detector wavelength of 254 nm using a photodiode array detector. Theoretical plates for prasugrel were 7023. Tailing factor for prasugrel was 1.11. Prasugrel was exposed to thermal, photolytic, hydrolytic and oxidative stress conditions, and the stressed samples were analyzed by the proposed method. Peak homogeneity data of prasugrel was obtained using photodiode array detector in the stressed sample chromatograms, which demonstrated the specificity of the method for the estimation in presence of degradants. The described method showed excellent linearity over a range of 10–300 μg/ml for prasugrel. The correlation coefficient is 0.999. The relative standard deviation of peak area for six measurements is always less than 2%. Overall, the proposed method was found to be suitable and accurate for quantitative determination and stability study of prasugrel in pharmaceutical dosage form. Full article
Article
Identification, Isolation and Characterization of an Unknown Impurity of Varenicline
Sci. Pharm. 2012, 80(2), 329-336; https://doi.org/10.3797/scipharm.1201-08 - 20 Mar 2012
Cited by 5 | Viewed by 1236
Abstract
An unknown impurity formed during stability sample analysis by a gradient reversed phase ultra-high pressure liquid chromatography (UHPLC) of varenicline tablets at 0.2% level. A simple isocratic preparative method was developed to isolate the unknown impurity with 20 min run time. This unknown [...] Read more.
An unknown impurity formed during stability sample analysis by a gradient reversed phase ultra-high pressure liquid chromatography (UHPLC) of varenicline tablets at 0.2% level. A simple isocratic preparative method was developed to isolate the unknown impurity with 20 min run time. This unknown impurity was identified and characterized by using spectroscopic techniques. Based on the spectral data, the unknown impurity has been characterized as 4,6,7,8,9,10-hexahydro-1H-6,10-methanopyrazino[2,3-h][3]benzazepine-2,3-dione. The structure of this impurity was also established unambiguously, prepared by isolation and co-injected into UHPLC to confirm the retention time. To the best of our knowledge, this impurity has not been reported elsewhere. Full article
Article
Stability-Indicating HPLC Method for Posaconazole Bulk Assay
Sci. Pharm. 2012, 80(2), 317-328; https://doi.org/10.3797/scipharm.1111-11 - 12 Mar 2012
Cited by 12 | Viewed by 1247
Abstract
A stability-indicating liquid chromatographic (LC) method was developed for the determination of posaconazole in bulk. Chromatographic separation was achieved using an isocratic elution in a reversed-phase system, with a mobile phase composed of methanol-water (75:25, v/v), at 1.0 mL min−1 flow. Samples [...] Read more.
A stability-indicating liquid chromatographic (LC) method was developed for the determination of posaconazole in bulk. Chromatographic separation was achieved using an isocratic elution in a reversed-phase system, with a mobile phase composed of methanol-water (75:25, v/v), at 1.0 mL min−1 flow. Samples were exposed to degradation under thermal, oxidative and acid/basic conditions, and no interference in the analysis was observed. System suitability was evaluated and results were satisfactory (N = 4,900.00 tailing factor 1.04; RSD between injections = 0.65). The retention time of posaconazole was about 8.5 min and the method was validated within the concentration range 5–60 μg mL−1 (r = 0.9996). Adequate results were obtained for repeatability (RSD % = 0.86–1.22), inter-day precision (RSD % = 1.21) and accuracy (98.13% mean recovery). Robustness was also determined to be satisfactory after evaluation. The proposed method was successfully applied to posaconazole bulk quantification, showing the method is useful for determination of the drug in routine analysis. Full article
Article
Characterization of Constituents and Anthelmintic Properties of Hagenia abyssinica
Sci. Pharm. 2012, 80(2), 433-446; https://doi.org/10.3797/scipharm.1109-04 - 02 Mar 2012
Cited by 21 | Viewed by 1115
Abstract
The dried female flowers of Hagenia abyssinica (Bruce) J. F. Gmel. (Rosaceae) are traditionally used as an anthelmintic remedy in Ethiopia and formerly were incorporated into the European Pharmacopoeia. One-, two- and tricyclic phloroglucinol derivatives (kosins) were suggested to be the active principles. [...] Read more.
The dried female flowers of Hagenia abyssinica (Bruce) J. F. Gmel. (Rosaceae) are traditionally used as an anthelmintic remedy in Ethiopia and formerly were incorporated into the European Pharmacopoeia. One-, two- and tricyclic phloroglucinol derivatives (kosins) were suggested to be the active principles. However, polar constituents may also contribute to the activity. Therefore, we investigated for the first time the polar constituents. We isolated typical Rosaceae constituents such as quercetin 3-O-β-glucuronide, quercetin 3-O-β-glucoside and rutin. Polar kosin glycosides or derivatives could not be detected.
The anthelmintic activity of fractions of different polarity were tested against the blood fluke Schistosoma mansoni, the liver flukes Clonorchis sinensis and Fasciola hepatica and the intestinal fluke Echinostoma caproni. The anthelmintic activity decreased with increasing polarity of the tested fractions. ESI-MS investigations indicated the predominant occurrence of kosins in the active fractions.
Using the anthelmintic active extracts of Hagenia abyssinica we developed a simple, inexpensive bioassay against the non-parasitic nematode Caenorhabditis elegans, which can be used as an initial screening procedure for anthelmintic properties of crude extracts of plants or fungi. The anthelmintic activity of test extracts against the model organism was determined in a microtiter plate assay by enumeration of living and dead nematodes under a microscope. Full article
Article
Randomized, Crossover and Single-Dose Bioquivalence Study of Two Oral Desogestrel Formulations (Film-Coated Tablets of 75 μg) in Healthy Female Volunteers
Sci. Pharm. 2012, 80(2), 419-432; https://doi.org/10.3797/scipharm.1111-18 - 01 Mar 2012
Cited by 5 | Viewed by 714
Abstract
Despite the increase in the substitution of branded medicinal product with generic drugs, this is a controversial issue for some pharmacological groups (such as contraceptives).
The aim of the present clinical trial was to assess the bioequivalence and tolerability of two oral formulations [...] Read more.
Despite the increase in the substitution of branded medicinal product with generic drugs, this is a controversial issue for some pharmacological groups (such as contraceptives).
The aim of the present clinical trial was to assess the bioequivalence and tolerability of two oral formulations of desogestrel.
Thirty-three healthy female volunteers participated in this randomized and two-way crossover study. During two separate experimental periods, with at least four weeks of washout period, women received a single oral dose of 75 μg of desogestrel from each of the formulations (test formulation and reference formulation). Desogestrel bioavailability was determined by the measurement of 3-ketodesogestrel plasma concentration.
Pharmacokinetic parameters were comparable and the 90% CI for the ratio of Cmax (96.14–114.53%) and AUC0–t (105.73–123.83%) values for the test and reference formulations fell within the established regulatory interval (80–125%). Both formulations were also comparable in terms of tolerability.
From the results of this study it can be concluded that test formulation (desogestrel 75 μg, Cyndea PHARMA S.L.) is bioequivalent to the reference formulation (Cerazet® 75 μg, Organon Española S.A.). Full article
Article
A New Isoflavone Glycoside from Dalbergia vacciniifolia (Fabaceae)
Sci. Pharm. 2012, 80(2), 469-474; https://doi.org/10.3797/scipharm.1112-23 - 27 Feb 2012
Cited by 1 | Viewed by 732
Abstract
5,5'-Dihydroxy-2',4'-dimethoxy-7-[(6-O-β-D-apiofuranosyl-β-D-glucopyranosyl)-oxy]isoflavone (1) was isolated as the major constituent of Dalbergia vacciniifolia root bark ethanol extract together with the four known compounds 5,7-dihydroxy-2',4',5'-trimethoxyisoflavone (3), 5,7-dihydroxy-2',4'-dimethoxy-isoflavone (4), 5-hydroxy-2',4',7-trimethoxyisoflavone (5) and 7-hydroxy-2',4',5'-trimethoxyisoflavone (6). Identification [...] Read more.
5,5'-Dihydroxy-2',4'-dimethoxy-7-[(6-O-β-D-apiofuranosyl-β-D-glucopyranosyl)-oxy]isoflavone (1) was isolated as the major constituent of Dalbergia vacciniifolia root bark ethanol extract together with the four known compounds 5,7-dihydroxy-2',4',5'-trimethoxyisoflavone (3), 5,7-dihydroxy-2',4'-dimethoxy-isoflavone (4), 5-hydroxy-2',4',7-trimethoxyisoflavone (5) and 7-hydroxy-2',4',5'-trimethoxyisoflavone (6). Identification of compounds was achieved through extensive analysis of 1D and 2D NMR and MS spectroscopy. Full article
Article
Method Development and Validation of Almotriptan in Human Plasma by HPLC Tandem Mass Spectrometry: Application to Pharmacokinetic Study
Sci. Pharm. 2012, 80(2), 367-378; https://doi.org/10.3797/scipharm.1112-01 - 27 Feb 2012
Cited by 8 | Viewed by 773
Abstract
A simple, sensitive and selective method has been developed for quantification of Almotriptan (AL) in human plasma using Almotriptan-d6 (ALD6) as an internal standard. Almotriptan and Almotriptan-d6 were detected with proton adducts at m/z 336.1→201.1 and 342.2→207.2 in multiple reaction monitoring (MRM) positive [...] Read more.
A simple, sensitive and selective method has been developed for quantification of Almotriptan (AL) in human plasma using Almotriptan-d6 (ALD6) as an internal standard. Almotriptan and Almotriptan-d6 were detected with proton adducts at m/z 336.1→201.1 and 342.2→207.2 in multiple reaction monitoring (MRM) positive mode, respectively. The method was linear over a concentration range of 0.5–150.0 ng/mL. The limit of detection (LOD) and limit of quantification (LOQ) for Almotriptan were 0.2 pg/mL and 0.5 ng/mL, respectively. Liquid-liquid extraction was used followed by MS/MS (ion spray). The method was shown to be precise with an average within-run and between-run variation of 0.68 to 2.78% and 0.57 to 0.86%, respectively. The average within-run and between-run accuracy of the method throughout its linear range was 98.94 to 102.64% and 99.43 to 101.44%, respectively. The mean recovery of drug and internal standard from human plasma was 92.12 ± 4.32% and 89.62 ± 6.32%. It can be applied for clinical and pharmacokinetic studies. Full article
Article
Pharmacophore Identification and QSAR Studies on Substituted Benzoxazinone as Antiplatelet Agents: kNN-MFA Approach
Sci. Pharm. 2012, 80(2), 283-294; https://doi.org/10.3797/scipharm.1112-09 - 26 Feb 2012
Cited by 3 | Viewed by 972
Abstract
The three-dimensional quantitative structure–activity relationship (3D-QSAR) and pharmacophore identification studies on 28 substituted benzoxazinone derivatives as antiplatelet agents have been carried out. Multiple linear regression (MLR) method was applied for QSAR model development considering training and test set approaches with various feature selection [...] Read more.
The three-dimensional quantitative structure–activity relationship (3D-QSAR) and pharmacophore identification studies on 28 substituted benzoxazinone derivatives as antiplatelet agents have been carried out. Multiple linear regression (MLR) method was applied for QSAR model development considering training and test set approaches with various feature selection methods. Stepwise (SW), simulated annealing (SA) and genetic algorithm (GA) were applied to derive QSAR models which were further validated for statistical significance and predictive ability by internal and external validation. The results of pharmacophore identification studies showed that hydrogen bond accepters, aromatic and hydrophobic, are the important features for antiplatelet activity. The selected best 3D kNN-MFA model A has a training set of 23 molecules and test set of 5 molecules with validation (q2) and cross validation (pred_r2) values 0.9739 and 0.8217, respectively. Additionally, the selected best 3D QSAR (MLR) model B has a training set of 23 molecules and test set of 5 molecules with validation (r2) and cross validation (pred_r2) values of 0.9435 and 0.7663, respectively, and four descriptors at the grid points S_123, E_407, E_311 and H_605. The information rendered by 3D-QSAR models may lead to a better understanding and designing of novel potent antiplatelet molecules. Full article
Article
Rapid Determination of Diclofenac in Pharmaceutical Formulations by Capillary Zone Electrophoresis
Sci. Pharm. 2012, 80(2), 311-316; https://doi.org/10.3797/scipharm.1201-02 - 23 Feb 2012
Cited by 5 | Viewed by 735
Abstract
Capillary electrophoresis is competitive to HPLC and other chromatographic methods, predominantly when charged analytes have to be separated. The time of analysis can be reduced by the use of very short capillaries applying a high voltage. In most instruments which are commercially available [...] Read more.
Capillary electrophoresis is competitive to HPLC and other chromatographic methods, predominantly when charged analytes have to be separated. The time of analysis can be reduced by the use of very short capillaries applying a high voltage. In most instruments which are commercially available the so-called ‘short end’ of the capillary can be used for separation, leading to very rapid separations. In this contribution we want to demonstrate this approach by using Diclofenac Sodium as an analyte. Full article
Article
Development of a Stability-Indicating RP-UPLC Method for Rapid Determination of Metaxalone and its Degradation Products in Solid Oral Dosage Form
Sci. Pharm. 2012, 80(2), 353-366; https://doi.org/10.3797/scipharm.1112-08 - 21 Feb 2012
Cited by 4 | Viewed by 734
Abstract
A simple, sensitive and reproducible reversed phase ultra performance liquid chromatography (RP-UPLC) coupled with a photodiode array detector method was developed for the quantitative determination of metaxalone (META) in pharmaceutical dosage forms. The method is applicable to the quantification of related substances and [...] Read more.
A simple, sensitive and reproducible reversed phase ultra performance liquid chromatography (RP-UPLC) coupled with a photodiode array detector method was developed for the quantitative determination of metaxalone (META) in pharmaceutical dosage forms. The method is applicable to the quantification of related substances and assay of drug product. Chromatographic separation was achieved on an Acquity® HSS-T3 (100 mm x 2.1 mm, 1.7 μm) column. The optimized isocratic mobile phase consists of a mixture of water, methanol, acetonitrile and triethylamine in the ratio of 50:25:25:0.1 % v/v (pH adjusted to 6.3 with orthophosphoric acid). The eluted compounds were monitored at 230 nm for META assay and 205 nm for related substances, the flow rate was 0.3 mL/min, and the column oven temperature was maintained at 45°C. The developed method separated META from its two known and two unknown impurities within 6.0 min. Metaxalone was subjected to the stress conditions of oxidative, acid, base, hydrolytic, thermal and photolytic degradation. Metaxalone was found to degrade significantly in base stress condition, degrade slightly in oxidative stress condition and remain stable in acid, hydrolytic, thermal and photolytic degradation conditions. All impurities were well resolved from each other and from the main peak, showing the stability-indicating power of the method. The developed method was validated as per International Conference on Harmonization (ICH) guidelines. Full article
Article
Protective Properties of Laggera alata Extract and its Principle Components Against D-Galactosamine-Injured Hepatocytes
Sci. Pharm. 2012, 80(2), 447-456; https://doi.org/10.3797/scipharm.1108-16 - 08 Feb 2012
Cited by 6 | Viewed by 716
Abstract
Laggera alata extract (LAE) was quantitatively analyzed, and its principle components isochlorogenic acids were isolated and authenticated. Protective properties of LAE were studied using a D-galactosamine (D-GalN)-induced injury model in neonatal rat hepatocytes and a D-GalN-induced acute liver damage model in mice. Meanwhile, [...] Read more.
Laggera alata extract (LAE) was quantitatively analyzed, and its principle components isochlorogenic acids were isolated and authenticated. Protective properties of LAE were studied using a D-galactosamine (D-GalN)-induced injury model in neonatal rat hepatocytes and a D-GalN-induced acute liver damage model in mice. Meanwhile, the effect of isochlorogenic acids derived from LAE on D-GalN-induced hepatocyte injury were also measured in vitro. LAE at concentrations of 10–100 μg/ml significantly reduced cellular leakage of aspartate aminotransferase (AST) and alanine aminotransferase (ALT) and improved cell viability. The isochlorogenic acids (4,5-O-dicaffeoylquinic acid, 3,5-O-dicaffeoylquinic acid and 3,4-O-dicaffeoylquinic acid) at concentrations of 1–100 μg/ml also remarkably improved viability of hepatocytes. The oral treatment of LAE at doses of 50, 100 and 200 mg/kg markedly reduced the serum AST and ALT activity of mice and resulted in significant recovery of hepatocytes in liver sections. Full article
Article
Application of HPLC for the Simultaneous Determination of Aceclofenac, Paracetamol and Tramadol Hydrochloride in Pharmaceutical Dosage Form
Sci. Pharm. 2012, 80(2), 337-352; https://doi.org/10.3797/scipharm.1108-04 - 31 Jan 2012
Cited by 20 | Viewed by 1423
Abstract
A simple, precise and accurate reversed-phase liquid chromatographic method has been developed for the simultaneous estimation of aceclofenac (ACF), paracetamol (PCM) and tramadol hydrochloride (TRM) in pharmaceutical dosage form. The chromatographic separation was achieved on a HiQ-Sil™ HS C18 column (250×4.6 mm i.d., [...] Read more.
A simple, precise and accurate reversed-phase liquid chromatographic method has been developed for the simultaneous estimation of aceclofenac (ACF), paracetamol (PCM) and tramadol hydrochloride (TRM) in pharmaceutical dosage form. The chromatographic separation was achieved on a HiQ-Sil™ HS C18 column (250×4.6 mm i.d., 5 μm particle size), kromatek analytical column at ambient temperature. The mobile phase consisted of 40: 60 (v/v); phosphate buffer (pH 6.0): methanol. The flow rate was set to 1.0 mL min−1 and UV detection was carried out at 270 nm. The retention time (tR) for ACF, PCM and TRM were found to be 14.567 ± 0.02, 3.133 ± 0.01 and 7.858 ± 0.02 min, respectively. The validation of the proposed method was carried out for linearity, precision, robustness, limit of detection, limit of quantitation, specificity, accuracy and system suitability. The linear dynamic ranges were from 40–160 μg mL−1 for ACF, 130–520 μg mL−1 for PCM and 15–60 μg mL−1 for TRM. The developed method can be used for routine quality control analysis of titled drugs in pharmaceutical dosage form. Full article
Article
A QSAR Study of Matrix Metalloproteinases Type 2 (MMP-2) Inhibitors with Cinnamoyl Pyrrolidine Derivatives
Sci. Pharm. 2012, 80(2), 265-282; https://doi.org/10.3797/scipharm.1112-21 - 31 Jan 2012
Cited by 6 | Viewed by 740
Abstract
A multivariate PLS-QSAR study with a data set of 31 cinnamoyl pyrrolidine derivatives described as type 2 matrix metalloproteinases (MMP-2) inhibitors is presented in this paper. The variable selection was performed with the Ordered Predictors Selection (OPS) algorithm. The PLS model presented six [...] Read more.
A multivariate PLS-QSAR study with a data set of 31 cinnamoyl pyrrolidine derivatives described as type 2 matrix metalloproteinases (MMP-2) inhibitors is presented in this paper. The variable selection was performed with the Ordered Predictors Selection (OPS) algorithm. The PLS model presented six descriptors and three Latent Variables (LV) that cumulated 71.845% of variance. Leave-N-out (LNO) cross validation and y-randomization tests showed that the model presented robustness and no chance correlation, respectively. The descriptors indicated that MMP-2 inhibition depends mainly on the electronic properties of the compounds. The model obtained can be useful as a support tool in the design of new MMP-2 inhibitors. Full article
Article
Identification and Characterization of an Oxidative Degradation Product of Fexofenadine, Development and Validation of a Stability-Indicating RP-UPLC Method for the Estimation of Process Related Impurities and Degradation Products of Fexofenadine in Pharmaceutical Formulations
Sci. Pharm. 2012, 80(2), 295-310; https://doi.org/10.3797/scipharm.1111-07 - 21 Jan 2012
Cited by 8 | Viewed by 1415
Abstract
A novel stability-indicating gradient RP-UPLC method was developed for the quantitative determination of process related impurities and forced degradation products of fexofenadine HCl in pharmaceutical formulations. The method was developed by using Waters Aquity BEH C18 (100 mm x 2.1 mm) 1.7 μm [...] Read more.
A novel stability-indicating gradient RP-UPLC method was developed for the quantitative determination of process related impurities and forced degradation products of fexofenadine HCl in pharmaceutical formulations. The method was developed by using Waters Aquity BEH C18 (100 mm x 2.1 mm) 1.7 μm column with mobile phase containing a gradient mixture of solvent A (0.05% triethyl amine, pH adjusted to 7.0 with ortho-phosphoric acid) and B (10:90 v/v mixture of water and acetonitrile). The flow rate of mobile phase was 0.4 mL/min with column temperature of 30°C and detection wavelength at 220nm. Fexofenadine HCl was subjected to the stress conditions including oxidative, acid, base, hydrolytic, thermal and photolytic degradation. Fexofenadine HCl was found to degrade significantly in oxidative stress conditions, and degradation product was identified and characterized by ESI-MS/MS, 1H and 13C NMR spectroscopic method as the N-oxide 2-[4-(1-hydroxy-4-{4-[hydroxy(diphenyl)methyl]-1-oxido-piperidin-1-yl}butyl)phenyl]-2-methylpropanoic acid. The degradation products were well resolved from fexofenadine and its impurities. The mass balance was found to be satisfactory in all the stress conditions, thus proving the stability-indicating capability of the method. The developed method was validated as per ICH guidelines with respect to specificity, linearity, limit of detection and quantification, accuracy, precision and robustness. Full article
Article
Relaxant Effect of Essential Oil of Artemisia herba-alba Asso. on Rodent Jejunum Contractions
Sci. Pharm. 2012, 80(2), 457-468; https://doi.org/10.3797/scipharm.1106-13 - 12 Jan 2012
Cited by 17 | Viewed by 927
Abstract
Artemisia herba-alba Asso. is a shrub commonly encountered in Morocco. It is used in traditional medicine for treating intestinal disorders. The essential oil extracted from the plant’s aerial parts reversibly relaxed the spontaneous tonus of the rabbit jejunum in a reversible concentration dependent [...] Read more.
Artemisia herba-alba Asso. is a shrub commonly encountered in Morocco. It is used in traditional medicine for treating intestinal disorders. The essential oil extracted from the plant’s aerial parts reversibly relaxed the spontaneous tonus of the rabbit jejunum in a reversible concentration dependent manner with an IC50 value of 97.33 ± 2.59 ng/ml and reversed the tonic contraction of rat jejunum induced by 75 mM KCl and 10−6 M carbachol with IC50 values of 115.5 ± 3.05 and 119.4 ± 20.86 ng/ml, respectively. The pre-treatment of the latter isolated intestine with this essential oil produced a dose-dependent shift of the Ca++ and CCh dose-response curve to the right, with suppression of the maximal effect, similar to the non-competitive antagonist effect on muscarinic receptors and calcium channel, respectively. Full article
Previous Issue
Back to TopTop