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Détails du magazine
Format
Magazine
eISSN
1846-9558
Première publication
28 Feb 2007
Période de publication
4 fois par an
Langues
Anglais

Chercher

Volume 65 (2015): Edition 1 (March 2015)

Détails du magazine
Format
Magazine
eISSN
1846-9558
Première publication
28 Feb 2007
Période de publication
4 fois par an
Langues
Anglais

Chercher

10 Articles
Accès libre

Formulation and characterization of solid lipid nanoparticles, nanostructured lipid carriers and nanoemulsion of lornoxicam for transdermal delivery

Publié en ligne: 11 Mar 2015
Pages: 1 - 13

Résumé

Abstract

Solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC) and nanoemulsion (NE) of lornoxicam (LRX) were prepared for the treatment of painful and inflammatory conditions of the skin. Compritol® 888 ATO, Lanette® O and oleic acid were used as solid and liquid lipids. SLN, NLC and NE were found physically stable at various temperatures for 6 months. Case I diffusional drug release was detected as the dominant mechanism indicating Fickian drug diffusion from nanoparticles and nanoemulsion. The highest rate of drug penetration through rat skin was obtained with NE followed by NLC, SLN and a gel formulation. Nanoformulations significantly increased drug penetration through rat skin compared to the gel (p < 0.05). Thus, SLN, NLC and NE of LRX can be suggested for relieving painful and inflammatory conditions of the skin

Mots clés

  • lornoxicam
  • solid lipid nanoparticles
  • nanostructured lipid carriers
  • nanoemulsion
  • transdermal delivery
  • inflammation
Accès libre

Alginate microspheres obtained by the spray drying technique as mucoadhesive carriers of ranitidine

Publié en ligne: 11 Mar 2015
Pages: 15 - 27

Résumé

Abstract

The present study is aimed at formulation of alginate (ALG) microspheres with ranitidine (RNT) by the spray drying method. Obtained microspheres were characterized for particle size, surface morphology, entrapment efficiency, drug loading, in vitro drug release and zeta potential. Mucoadhesive properties were examined by a texture analyser and three types of adhesive layers - gelatine discs, mucin gel and porcine stomach mucosa. Microspheres showed a smooth surface with narrow particle size distribution and RNT loading of up to 70.9 %. All formulations possessed mucoadhesive properties and exhibited prolonged drug release according to the first-order kinetics. DSC reports showed that there was no interaction between RNT and ALG. Designed microspheres can be considered potential carriers of ranitidine with prolonged residence time in the stomach

Mots clés

  • ranitidine
  • sodium alginate
  • microspheres
  • spray drying technique
  • mucoadhesiveness
Accès libre

Dissolution improvement of solid self-emulsifying drug delivery systems of fenofi brate using an inorganic high surface adsorption material

Publié en ligne: 11 Mar 2015
Pages: 29 - 42

Résumé

Abstract

Solidification of lipid formulations using adsorbents is a recent technique attracting great interest due to its favourable properties including flexibility in dose division, reduction of intra-subject and inter-subject variability, improvement in efficacy/safety profile and enhancement of physical/ chemical stability. The current study aims to convert liquid self-emulsifying/nanoemulsifying drug delivery systems (SEDDS/SNEDDS) into solid SEDDS/SNEDDS and to assess how adsorption of the drug onto an inorganic high surface area material, NeusilinR grade US2 (NUS2), affects its in vitro dissolution performance. Lipid formulation classification systems (LFCS) Type III formulations were designed for the model anti-cholesterol drug fenofibrate. NUS2 was used to solidify the SEDDS/SNEDDS. Particle size and SEM analyses of solid SEDDS/SNEDDS powder were carried out to investigate the adsorption efficiency. In vitro dissolution studies were conducted to compare the developed formulations with the marketed product. The results of characterization studies showed that the use of 50 % (m/m) adsorbent resulted in superior flowability and kept the drug stable is amorphous state. Dissolution studies allow the conclusion that the formulation containing a surfactant of higher water solubility (particularly, Type IIIB SNEDDS) has comparably faster and higher release profiles than Type IIIA (SEDDS) and marketed product

Mots clés

  • self-emulsifying/nanoemulsifying drug delivery systems
  • fenofibrate
  • in vitro dissolution test
  • solidification technique
  • adsorption
Accès libre

Development and validation of a simple and sensitive size-exclusion chromatography method for quantitative determination of heparin in pharmaceuticals

Publié en ligne: 11 Mar 2015
Pages: 43 - 52

Résumé

Abstract

Heparin is widely used as an anticoagulant for the treatment and prevention of various thrombotic diseases. However, due to its high anionic charge, heterogeneity in size distribution and high polarity, its analysis is very challenging. In this paper, a novel method based on size-exclusion chromatography (SEC) for quantitative determination of intact heparin in pharmaceuticals is presented. Analyses were performed on a BioSep-SEC-S 2000 column with Larginine solution at pH 6.5 as mobile phase and UV detection at 210 nm. The proposed method was found to be selective, linear (R2 > 0.997) over the concentration range of 3.1 to 1222 μg mL-1, with a limit of detection of 1.0 μg mL-1. Intraday and inter-day precision were below 5.1 % and inaccuracy expressed as bias did not exceed 6.5 %. The reported method is simple, selective, sensitive, and requires no laborious sample preparation, which makes it appropriate for routine quantitative analysis of heparin in pharmaceuticals

Mots clés

  • heparin
  • quantitative analysis
  • size-exclusion chromatography
  • L-arginine
Accès libre

Potential antiproliferative effect of isoxazolo- and thiazolo coumarin derivatives on breast cancer mediated bone and lung metastases

Publié en ligne: 11 Mar 2015
Pages: 53 - 63

Résumé

Abstract

The study highlights the current progress in the development of coumarin scaffolds for drug discovery as novel anticancer agents in metastatic breast cancer. Eight compounds, combining the coumarin core and five membered heterocycles (isoxazoles and thiazoles) in hydrazinyldiene- -chroman-2,4-diones, were characterized in terms of a potential antiproliferative effect on bone (SCP1833) and lung (SCP4175) metastatic breast cancer cell lines using the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide assay. Cell viability was evaluated after 48 and 72 h of treatment and the 50 % inhibitory concentrations were determined. The results demonstrated dose- and time-dependent activity, with the most potent molecules having a thiazole moiety, without or with additional methyl group(s) attached to the carbon(s) at position(s) 5 and/or 4 in the thiazole ring. These molecules possessed significantly higher potency against both test cell lines compared to 4-hydroxycoumarin

Mots clés

  • chromandiones
  • breast cancer
  • metastatic cells
  • antiproliferative effect
Accès libre

Effect of oral administration of green tea extract in various dosage schemes on oxidative stress status of mice in vivo

Publié en ligne: 11 Mar 2015
Pages: 65 - 73

Résumé

Abstract

Green tea is a favorite beverage and its extracts are popular components of dietary supplements. The aim of the present in vivo study was to obtain detailed information about the effect of a standard green tea extract (Polyphenon, P), at different doses, on antioxidant enzymes and oxidative stress markers in murine blood, liver, small and large intestine. In all doses, P improved the oxidative stress status via an increased content of plasmatic SH-groups (by 21-67 %). Regarding antioxidant enzymes in tissues, the low dose of P had the best positive effect as it elevated the activity of NADPH quinone reductase in liver and small intestine, thioredoxin reductase in small intestine and hepatic superoxide dismutase. Based on these facts, consumption of green tea seems to be safe and beneficial, while consumption of dietary supplements containing high doses of catechins may disturb oxidative balance by lowering the activity of thioredoxin reductase, glutathione S-transferase, glutathione reductase and superoxide dismutase

Mots clés

  • green tea extract
  • dietary supplement
  • flavonoids
  • green tea catechins
  • antioxidant enzymes
Accès libre

Effect of 1-(phenyl)-N’-(4-methoxybenzylidene)-9H-pyrido[3,4-b] indole-3-carbohydrazide on in vitro poliovirus replication

Publié en ligne: 11 Mar 2015
Pages: 75 - 81

Résumé

Abstract

The effect of the alkaloid 1-(phenyl)-N’-(4-methoxybenzylidene)- 9H-pyrido[3,4-b]indole-3-carbohydrazide (PMC) on the poliovirus (PV) replication cycle in Vero cells was assayed by inhibition of the cytopathic effect (CPE) and inhibition of plaque forming units (PFU). Both methodologies suggested that the mode of action was avoidance of infection progression in the host cell. The compound was able to prevent CPE and PFU formation when the cells were pretreated with PMC for 24 h prior to PV infection. In addition, when the alkaloid was continuously maintained in the infected cultures, the spread of PV to adjacent cells was impaired. The pre-exposure and post-exposure prophylactic applications are possible situations in which an anti-PV drug might be used. Future studies are needed to elucidate the PMC mode of action and verify the feasibility of PMC use in vivo. No antipicornavirus agent is currently approved for clinical use

Mots clés

  • 1-(phenyl)-N’-(4-methoxybenzylidene)-9H-pyrido[ 3,4-b]indole-3-carbohydrazide
  • b-carboline
  • poliovirus
  • antiviral activity
Accès libre

Development and optimization of the activated charcoal suspension composition based on a mixture design approach

Publié en ligne: 11 Mar 2015
Pages: 83 - 90

Résumé

Abstract

In this study, a new drug product containing activated charcoal was designed and developed. The excipient levels in the pharmaceutical formulation were optimized using a mixture design approach. The adsorption power of the activated charcoal suspension was selected as the critical quality attribute influencing the efficacy of medical treatment. Significant prognostic models (p < 0.05) were obtained to describe in detail the interrelations between excipient levels and the adsorption power of the formulation. Liquid flavour had a critical impact on the adsorption power of the suspension. Formulations containing the largest amount of liquid flavour showed the lowest adsorption power. Sorbitol was not adsorbed onto activated charcoal so strongly as liquid flavour. A slight increase in the content of carboxymethylcellulose sodium led to a marked decrease in adsorption power. The obtained mathematical models and response surface allowed selection of the optimal composition of excipients in a final drug product

Mots clés

  • activated charcoal
  • adsorption power
  • phenazone
  • experimental design
  • Quality by Design concept
Accès libre

Compressibility of tableting materials and properties of tablets with glyceryl behenate

Publié en ligne: 11 Mar 2015
Pages: 91 - 98

Résumé

Abstract

The paper studies the compressibility of directly compressible tableting materials with dry binders, spray-dried lactose and microcrystalline cellulose, and glyceryl dibehenate at various concentrations. Compressibility was evaluated by means of the energy profile of compression and tensile strength of tablets. Release rate of the active ingredient, salicylic acid, from the tablets was also examined. In the case of microcrystalline cellulose, a higher concentration of glyceryl dibehenate increased the strength of tablets, while this did not occur in the case of spray-dried lactose. Increasing concentration of glyceryl dibehenate prolonged the release of salicylic acid; however, no statistically significant difference was found compared to the type of the dry binder used

Mots clés

  • lipophilic matrix tablet
  • glyceryl dibehenate
  • salicylic acid
  • energy profile of compression
  • tensile strength of tablets
  • dissolution profile
Accès libre

Differences in antioxidant properties of ginkgo leaves collected from male and female trees

Publié en ligne: 11 Mar 2015
Pages: 99 - 104

Résumé

Abstract

Total phenolic content and antioxidant capacity (FRAP method) of Ginkgo biloba L. leaves collected from male and female trees were determined and compared. Different water and aqueous ethanolic (water/ethanol 80/20, V/V) extracts were prepared by varying the time of infusing, boiling and steeping in order to determine the effect of the extraction method on the above parameters. Antioxidant activity and phenolic content of ginkgo leaf extracts correlated well with significant correlation coefficients. Slopes of linear regression lines were not statistically different for either sex

Mots clés

  • Ginkgo biloba L.
  • male ginkgo
  • female ginkgo
  • ginkgo extracts phenolics
  • FRAP
10 Articles
Accès libre

Formulation and characterization of solid lipid nanoparticles, nanostructured lipid carriers and nanoemulsion of lornoxicam for transdermal delivery

Publié en ligne: 11 Mar 2015
Pages: 1 - 13

Résumé

Abstract

Solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC) and nanoemulsion (NE) of lornoxicam (LRX) were prepared for the treatment of painful and inflammatory conditions of the skin. Compritol® 888 ATO, Lanette® O and oleic acid were used as solid and liquid lipids. SLN, NLC and NE were found physically stable at various temperatures for 6 months. Case I diffusional drug release was detected as the dominant mechanism indicating Fickian drug diffusion from nanoparticles and nanoemulsion. The highest rate of drug penetration through rat skin was obtained with NE followed by NLC, SLN and a gel formulation. Nanoformulations significantly increased drug penetration through rat skin compared to the gel (p < 0.05). Thus, SLN, NLC and NE of LRX can be suggested for relieving painful and inflammatory conditions of the skin

Mots clés

  • lornoxicam
  • solid lipid nanoparticles
  • nanostructured lipid carriers
  • nanoemulsion
  • transdermal delivery
  • inflammation
Accès libre

Alginate microspheres obtained by the spray drying technique as mucoadhesive carriers of ranitidine

Publié en ligne: 11 Mar 2015
Pages: 15 - 27

Résumé

Abstract

The present study is aimed at formulation of alginate (ALG) microspheres with ranitidine (RNT) by the spray drying method. Obtained microspheres were characterized for particle size, surface morphology, entrapment efficiency, drug loading, in vitro drug release and zeta potential. Mucoadhesive properties were examined by a texture analyser and three types of adhesive layers - gelatine discs, mucin gel and porcine stomach mucosa. Microspheres showed a smooth surface with narrow particle size distribution and RNT loading of up to 70.9 %. All formulations possessed mucoadhesive properties and exhibited prolonged drug release according to the first-order kinetics. DSC reports showed that there was no interaction between RNT and ALG. Designed microspheres can be considered potential carriers of ranitidine with prolonged residence time in the stomach

Mots clés

  • ranitidine
  • sodium alginate
  • microspheres
  • spray drying technique
  • mucoadhesiveness
Accès libre

Dissolution improvement of solid self-emulsifying drug delivery systems of fenofi brate using an inorganic high surface adsorption material

Publié en ligne: 11 Mar 2015
Pages: 29 - 42

Résumé

Abstract

Solidification of lipid formulations using adsorbents is a recent technique attracting great interest due to its favourable properties including flexibility in dose division, reduction of intra-subject and inter-subject variability, improvement in efficacy/safety profile and enhancement of physical/ chemical stability. The current study aims to convert liquid self-emulsifying/nanoemulsifying drug delivery systems (SEDDS/SNEDDS) into solid SEDDS/SNEDDS and to assess how adsorption of the drug onto an inorganic high surface area material, NeusilinR grade US2 (NUS2), affects its in vitro dissolution performance. Lipid formulation classification systems (LFCS) Type III formulations were designed for the model anti-cholesterol drug fenofibrate. NUS2 was used to solidify the SEDDS/SNEDDS. Particle size and SEM analyses of solid SEDDS/SNEDDS powder were carried out to investigate the adsorption efficiency. In vitro dissolution studies were conducted to compare the developed formulations with the marketed product. The results of characterization studies showed that the use of 50 % (m/m) adsorbent resulted in superior flowability and kept the drug stable is amorphous state. Dissolution studies allow the conclusion that the formulation containing a surfactant of higher water solubility (particularly, Type IIIB SNEDDS) has comparably faster and higher release profiles than Type IIIA (SEDDS) and marketed product

Mots clés

  • self-emulsifying/nanoemulsifying drug delivery systems
  • fenofibrate
  • in vitro dissolution test
  • solidification technique
  • adsorption
Accès libre

Development and validation of a simple and sensitive size-exclusion chromatography method for quantitative determination of heparin in pharmaceuticals

Publié en ligne: 11 Mar 2015
Pages: 43 - 52

Résumé

Abstract

Heparin is widely used as an anticoagulant for the treatment and prevention of various thrombotic diseases. However, due to its high anionic charge, heterogeneity in size distribution and high polarity, its analysis is very challenging. In this paper, a novel method based on size-exclusion chromatography (SEC) for quantitative determination of intact heparin in pharmaceuticals is presented. Analyses were performed on a BioSep-SEC-S 2000 column with Larginine solution at pH 6.5 as mobile phase and UV detection at 210 nm. The proposed method was found to be selective, linear (R2 > 0.997) over the concentration range of 3.1 to 1222 μg mL-1, with a limit of detection of 1.0 μg mL-1. Intraday and inter-day precision were below 5.1 % and inaccuracy expressed as bias did not exceed 6.5 %. The reported method is simple, selective, sensitive, and requires no laborious sample preparation, which makes it appropriate for routine quantitative analysis of heparin in pharmaceuticals

Mots clés

  • heparin
  • quantitative analysis
  • size-exclusion chromatography
  • L-arginine
Accès libre

Potential antiproliferative effect of isoxazolo- and thiazolo coumarin derivatives on breast cancer mediated bone and lung metastases

Publié en ligne: 11 Mar 2015
Pages: 53 - 63

Résumé

Abstract

The study highlights the current progress in the development of coumarin scaffolds for drug discovery as novel anticancer agents in metastatic breast cancer. Eight compounds, combining the coumarin core and five membered heterocycles (isoxazoles and thiazoles) in hydrazinyldiene- -chroman-2,4-diones, were characterized in terms of a potential antiproliferative effect on bone (SCP1833) and lung (SCP4175) metastatic breast cancer cell lines using the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide assay. Cell viability was evaluated after 48 and 72 h of treatment and the 50 % inhibitory concentrations were determined. The results demonstrated dose- and time-dependent activity, with the most potent molecules having a thiazole moiety, without or with additional methyl group(s) attached to the carbon(s) at position(s) 5 and/or 4 in the thiazole ring. These molecules possessed significantly higher potency against both test cell lines compared to 4-hydroxycoumarin

Mots clés

  • chromandiones
  • breast cancer
  • metastatic cells
  • antiproliferative effect
Accès libre

Effect of oral administration of green tea extract in various dosage schemes on oxidative stress status of mice in vivo

Publié en ligne: 11 Mar 2015
Pages: 65 - 73

Résumé

Abstract

Green tea is a favorite beverage and its extracts are popular components of dietary supplements. The aim of the present in vivo study was to obtain detailed information about the effect of a standard green tea extract (Polyphenon, P), at different doses, on antioxidant enzymes and oxidative stress markers in murine blood, liver, small and large intestine. In all doses, P improved the oxidative stress status via an increased content of plasmatic SH-groups (by 21-67 %). Regarding antioxidant enzymes in tissues, the low dose of P had the best positive effect as it elevated the activity of NADPH quinone reductase in liver and small intestine, thioredoxin reductase in small intestine and hepatic superoxide dismutase. Based on these facts, consumption of green tea seems to be safe and beneficial, while consumption of dietary supplements containing high doses of catechins may disturb oxidative balance by lowering the activity of thioredoxin reductase, glutathione S-transferase, glutathione reductase and superoxide dismutase

Mots clés

  • green tea extract
  • dietary supplement
  • flavonoids
  • green tea catechins
  • antioxidant enzymes
Accès libre

Effect of 1-(phenyl)-N’-(4-methoxybenzylidene)-9H-pyrido[3,4-b] indole-3-carbohydrazide on in vitro poliovirus replication

Publié en ligne: 11 Mar 2015
Pages: 75 - 81

Résumé

Abstract

The effect of the alkaloid 1-(phenyl)-N’-(4-methoxybenzylidene)- 9H-pyrido[3,4-b]indole-3-carbohydrazide (PMC) on the poliovirus (PV) replication cycle in Vero cells was assayed by inhibition of the cytopathic effect (CPE) and inhibition of plaque forming units (PFU). Both methodologies suggested that the mode of action was avoidance of infection progression in the host cell. The compound was able to prevent CPE and PFU formation when the cells were pretreated with PMC for 24 h prior to PV infection. In addition, when the alkaloid was continuously maintained in the infected cultures, the spread of PV to adjacent cells was impaired. The pre-exposure and post-exposure prophylactic applications are possible situations in which an anti-PV drug might be used. Future studies are needed to elucidate the PMC mode of action and verify the feasibility of PMC use in vivo. No antipicornavirus agent is currently approved for clinical use

Mots clés

  • 1-(phenyl)-N’-(4-methoxybenzylidene)-9H-pyrido[ 3,4-b]indole-3-carbohydrazide
  • b-carboline
  • poliovirus
  • antiviral activity
Accès libre

Development and optimization of the activated charcoal suspension composition based on a mixture design approach

Publié en ligne: 11 Mar 2015
Pages: 83 - 90

Résumé

Abstract

In this study, a new drug product containing activated charcoal was designed and developed. The excipient levels in the pharmaceutical formulation were optimized using a mixture design approach. The adsorption power of the activated charcoal suspension was selected as the critical quality attribute influencing the efficacy of medical treatment. Significant prognostic models (p < 0.05) were obtained to describe in detail the interrelations between excipient levels and the adsorption power of the formulation. Liquid flavour had a critical impact on the adsorption power of the suspension. Formulations containing the largest amount of liquid flavour showed the lowest adsorption power. Sorbitol was not adsorbed onto activated charcoal so strongly as liquid flavour. A slight increase in the content of carboxymethylcellulose sodium led to a marked decrease in adsorption power. The obtained mathematical models and response surface allowed selection of the optimal composition of excipients in a final drug product

Mots clés

  • activated charcoal
  • adsorption power
  • phenazone
  • experimental design
  • Quality by Design concept
Accès libre

Compressibility of tableting materials and properties of tablets with glyceryl behenate

Publié en ligne: 11 Mar 2015
Pages: 91 - 98

Résumé

Abstract

The paper studies the compressibility of directly compressible tableting materials with dry binders, spray-dried lactose and microcrystalline cellulose, and glyceryl dibehenate at various concentrations. Compressibility was evaluated by means of the energy profile of compression and tensile strength of tablets. Release rate of the active ingredient, salicylic acid, from the tablets was also examined. In the case of microcrystalline cellulose, a higher concentration of glyceryl dibehenate increased the strength of tablets, while this did not occur in the case of spray-dried lactose. Increasing concentration of glyceryl dibehenate prolonged the release of salicylic acid; however, no statistically significant difference was found compared to the type of the dry binder used

Mots clés

  • lipophilic matrix tablet
  • glyceryl dibehenate
  • salicylic acid
  • energy profile of compression
  • tensile strength of tablets
  • dissolution profile
Accès libre

Differences in antioxidant properties of ginkgo leaves collected from male and female trees

Publié en ligne: 11 Mar 2015
Pages: 99 - 104

Résumé

Abstract

Total phenolic content and antioxidant capacity (FRAP method) of Ginkgo biloba L. leaves collected from male and female trees were determined and compared. Different water and aqueous ethanolic (water/ethanol 80/20, V/V) extracts were prepared by varying the time of infusing, boiling and steeping in order to determine the effect of the extraction method on the above parameters. Antioxidant activity and phenolic content of ginkgo leaf extracts correlated well with significant correlation coefficients. Slopes of linear regression lines were not statistically different for either sex

Mots clés

  • Ginkgo biloba L.
  • male ginkgo
  • female ginkgo
  • ginkgo extracts phenolics
  • FRAP

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