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Journal Details
Format
Journal
eISSN
1846-9558
ISSN
1330-0075
First Published
28 Feb 2007
Publication timeframe
4 times per year
Languages
English

Search

Volume 58 (2008): Issue 2 (June 2008)

Journal Details
Format
Journal
eISSN
1846-9558
ISSN
1330-0075
First Published
28 Feb 2007
Publication timeframe
4 times per year
Languages
English

Search

10 Articles
Open Access

In vitro antitumor and antiviral activities of new benzothiazole and 1,3,4-oxadiazole-2-thione derivatives

Published Online: 30 May 2008
Page range: 135 - 149

Abstract

<italic>In vitro</italic> antitumor and antiviral activities of new benzothiazole and 1,3,4-oxadiazole-2-thione derivatives

A series of new benzothiazole derivatives 6a-h have been synthesized, in five steps, from substituted phenols via the 1,3,4-oxadiazole-2-thiones 5a-h. The in vitro antitumor activity of the compounds obtained was investigated and the benzothiazol derivatives 6d and 6e showed strong effects on leukaemia cell lines CCRF-CEM (CC50 = 12 ± 2 μmol L-1, 8 ± 1 μmol L-1, respectively). These compounds are leading candidates for further development. The title compounds were tested against representatives of several virus families containing single stranded RNA genomes, either positive-sense (ssRNA+), or negativesense (RNA-), and against double-stranded RNA genomes (dsRNA), as well as some Flaviviridae viruses.

Keywords

  • 1,3,4-oxathiazoles
  • substituted benzothiazoles
  • antitumor activity
  • antiviral activity
Open Access

Effect of various surfactants and their concentration on controlled release of captopril from polymeric matrices

Published Online: 30 May 2008
Page range: 151 - 162

Abstract

Effect of various surfactants and their concentration on controlled release of captopril from polymeric matrices

Various methods are available to formulate water soluble drugs into sustained release dosage forms by retarding the dissolution rate. One of the methods used to control drug release and thereby prolong therapeutic activity is to use hydrophilic and lipophilic polymers. In this study, the effects of various polymers such as hydroxypropyl methylcellulose (HPMC), ethylcellulose (EC) and sodium carboxymethylcellulose (CMC) and surfactants (sodium lauryl sulphate, cetyltrimethylammonium bromide and Arlacel 60) on the release rate of captopril were investigated. The results showed that an increase in the amount of HPMC K15M resulted in reduction of the release rate of captopril from these matrices. When HPMC was partly replaced by NaCMC (the ratio of HPMC/NaCMC was 5:1), the release rate of the drug significantly decreased. However, there was no significant difference in release rate of captopril from matrices produced with ratios of 5:1 and 2:1 of HPMC/NaCMC. The presence of lactose in matrices containing HPMC and NaCMC increased the release rate of captopril. It was interesting to note that although partial replacement of HPMC by EC reduced the release rate of the drug (ratio of HPMC/EC 2:1), the release rate was increased when the ratio of HPMC/EC was reduced to 1:1. The effects of various surfactants on the release rate of captopril from HPMC/EC (1:1) matrices were also investigated. The results showed that the surfactants did not significantly change the release rate of the drug. Release data were examined kinetically and the ideal kinetic models were estimated for the drug release. The kinetic analysis of drug release data from various formulations showed that incorporation of surfactants in HPMC/EC matrices did not produce a zero-order release pattern.

Keywords

  • captopril
  • polymers
  • controlled release
  • surfactant
  • release kinetic
Open Access

Comparison between two cyclooxygenase inhibitors in an experimental dry eye model in albino rabbits

Published Online: 30 May 2008
Page range: 163 - 173

Abstract

Comparison between two cyclooxygenase inhibitors in an experimental dry eye model in albino rabbits

The purpose of this study was to compare the topical anti-inflammatory effects of the nonselective cyclooxygenase (COX) inhibitor, ketorolac, with the selective COX-2 inhibitor, nimesulide, in an animal model of dry eye in albino rabbits. All animals were examined by the Schirmer test, tear break-up time (TBUT) and fluorescein corneal staining test. Dry eye model showed significant reduction in tear volume, TBUT, corneal staining and histopathological signs of dryness and inflammation. On treating dry eye model with nimesulide 0.1% eye drops and ketorolac 0.5% eye drops, there were improvements in Schirmer test values, TBUT and fluorescein corneal staining and histopathologically reduced inflammatory reaction, with signs of healing and regeneration. Both nimesulide and ketorolac ameliorate atropine sulphate induced dry eye in albino rabbits. The use of selective COX-2 inhibitor, nimesulide, is preferred to avoid local and systemic side effects which may occur with the use of the nonselective COX inhibitor, ketorolac.

Keywords

  • dry eye model
  • rabbit
  • atropine sulphate
  • Schirmer test I
  • nimesulide
  • ketorolac
Open Access

Anti-inflammatory and analgesic activities of some newly synthesized pyridinedicarbonitrile and benzopyranopyridine derivatives

Published Online: 30 May 2008
Page range: 175 - 186

Abstract

Anti-inflammatory and analgesic activities of some newly synthesized pyridinedicarbonitrile and benzopyranopyridine derivatives

In continuation of our search for new substituted pyridine based anti-inflammatories, reaction of 1-(2-thienyl or furanyl)-3-(2-hydroxyphenyl)-2-propen-1-ones (1) with malononitrile in alcoholic KOH solution afforded a mixture of 4-alkoxy-2-(2-thienyl or furanyl)-5H-[1]benzopyrano[3,4-c]pyridine-5-ones (2) and 2-alkoxy-4-amino-6- (2-thienyl or furanyl)-3,5-pyridinedicarbonitriles (3). Some of the synthesized compounds were evaluated for their anti-inflammatory and analgesic activities compared to diclofenac potassium as positive control. Detailed synthesis, spectroscopic and toxicity data are reported.

Keywords

  • pyridinedicarbonitrile
  • benzopyranopyridine
  • anti-inflammatory
  • analgesic agents
Open Access

Formulation and evaluation of oil entrapped gastroretentive floating gel beads of loratadine

Published Online: 30 May 2008
Page range: 187 - 197

Abstract

Formulation and evaluation of oil entrapped gastroretentive floating gel beads of loratadine

A gastro retentive controlled release system of loratadine was formulated to increase the residence time in stomach and to modulate the release behaviour of the drug. Oil entrapped floating microbeads prepared by the emulsion gelation method were optimized by 23 factorial design and a polymer ratio of 2.5:1.5 (pectin/sodium alginate) by mass, 15% (m/V) of oil (mineral oil or castor oil) and 0.45 mol L-1 calcium chloride solution as the optimized processing conditions for the desired buoyancy and physical stability. In vitro drug release in the fed state conditions demonstrated sustained release of loratadine for 8 h, which best fitted the Peppas model with n < 0.45. The ethyl cellulose coating on microbeads optimized by 22 factorial design resulted in a controlled release formulation of loratadine that provided zero-order release for 8 h.

Keywords

  • loratadine
  • gastroretentive
  • factorial design
  • ethyl cellulose coating
  • zero-order release
Open Access

Studying the formation of aggregates in recombinant human granulocyte-colony stimulating factor (rHuG-CSF), lenograstim, using size-exclusion chromatography and SDS-PAGE

Published Online: 30 May 2008
Page range: 199 - 206

Abstract

Studying the formation of aggregates in recombinant human granulocyte-colony stimulating factor (rHuG-CSF), lenograstim, using size-exclusion chromatography and SDS-PAGE

The stability of proteins is a subject of intense current interest. Aggregation, as a dominant degradation pathway for therapeutic proteins, may cause multiple adverse effects, including loss of efficacy and immunogenicity. In the present study, the formation of aggregates in lenograstim under physiological conditions was monitored. For this purpose, a simple and selective size-exclusion high-performance liquid chromatography method for detection and separation of aggregates from intact protein was developed. Sodium dodecyl sulphate-polyacrylamide gel electrophoresis was performed under reducing and non-reducing conditions to determine the nature of aggregate bond formation. Using both techniques, the presence of a low aggregate content attached via disulfide bonds was detected.

Keywords

  • lenograstim
  • aggregate formation
  • size-exclusion high-performance liquid chromatography
  • sodium dodecyl sulphate-polyacrylamide gel electrophoresis
Open Access

Identification of chemical compounds from the leaves of Leea indica

Published Online: 30 May 2008
Page range: 207 - 214

Abstract

Identification of chemical compounds from the leaves of <italic>Leea indica</italic>

Twenty-three known chemical compounds were identified in the leaves of Leea indica (Burm. f.) Merr. (Leeaceae) by GC-MS analysis, spectroscopic techniques and co-TLC with authentic samples. The identified compounds include eleven hydrocarbons, phthalic acid, palmitic acid, 1-eicosanol, solanesol, farnesol, three phthalic acid esters, gallic acid, lupeol, β-sitosterol and ursolic acid. Gallic acid was isolated as n-butyl gallate and identified by co-TLC. This seems to be the first report of the presence of gallic acid in the leaves of L. indica.

Keywords

  • Leea indica (Leeaceae)
  • GC-MS
  • gallic acid
  • -butyl gallate
  • antioxidant activity
Open Access

Antioxidant and free radical scavenging potential of Citrullus colocynthis (L.) Schrad. methanolic fruit extract

Published Online: 30 May 2008
Page range: 215 - 220

Abstract

Antioxidant and free radical scavenging potential of <italic>Citrullus colocynthis</italic> (L.) Schrad. methanolic fruit extract

Citrullus colocynthis (L.) Schrad. (Cucurbitaceae) is a medicinal plant traditionally used as an abortifacient and to treat constipation, oedema, bacterial infections, cancer and diabetes. Preliminary phytochemical screening of the plant showed the presence of large amounts of phenolics and flavonoids. Subsequent quantification showed the presence of 0.74% (m/m) phenolics (calculated as gallic acid) and 0.13% (m/m) flavonoids calculated as catechin equivalents per 100 g of fresh mass. The presence of phenolic compounds prompted us to evaluate its antioxidant activity. In the present study, methanolic fruit extract of C. colocynthis was screened to evaluate its freeradical scavenging effect. The highest antioxidant and free radical scavenging ability of the fruit extract was observed at a concentration of 2500 μg mL-1.

Keywords

  • Citrullus colocynthis fruit
  • Cucurbitaceae
  • methanolic extract
  • antioxidants
  • free radical scavenging
Open Access

Gastric floating matrix tablets: Design and optimization using combination of polymers

Published Online: 30 May 2008
Page range: 221 - 229

Abstract

Gastric floating matrix tablets: Design and optimization using combination of polymers

The purpose of the present study was to develop an optimized gastric floating drug delivery system (GFDDS) containing domperidone as a model drug. Box-Behnken design was employed in formulating the GFDDS with three polymers: hydroxypropyl methylcellulose K4M (HPMC K4M) (X1), Carbopol 934P (X2) and sodium alginate (X3), as independent variables. Floating lag time (FLT), total floating time (TFT), time required to release 50% of the drug (t50) and diffusion exponent (n) were selected as dependent variables. Seventeen formulations were prepared, dissolution data obtained was fitted to the power law and floating profiles were analyzed. HPMC loading was found to be significant for floating properties. Carbopol loading had a negative effect on floating properties but was found helpful in controlling the release rate of the drug. No significant effect of sodium alginate on floating properties was observed but it was important for gel formation. The quadratic mathematical model developed could be used to predict formulations with desired release and floating properties.

Keywords

  • domperidone
  • floating matrix tablet
  • Box-Behnken design
  • GFDDS
  • release kinetics
Open Access

N-Phthaloyl-glycine-hydroxamic acid as serum iron chelator in rats

Published Online: 30 May 2008
Page range: 231 - 236

Abstract

<italic>N</italic>-Phthaloyl-glycine-hydroxamic acid as serum iron chelator in rats

The aim of this study was to investigate the activity of N-phthaloyl-glycine-hydroxamic acid (Phth-Gly-HA) as a new iron chelator in vivo to be used in iron overload diseases. After intraperitoneal application of Phth-Gly-HA to male rats (1 mg kg-1 body mass) once a day for seven days, iron serum level decreased by 21%, whereas the iron value dropped by 32% in female rats (1.5 mg kg-1 body mass). The results indicate that the tested substance has the ability to bind serum iron by complexation. Besides transferrin iron release, mobilization of ferritin iron is also possible.

Keywords

  • -phthaloyl-glycine-hydroxamic acid
  • iron chelators
  • iron overload
10 Articles
Open Access

In vitro antitumor and antiviral activities of new benzothiazole and 1,3,4-oxadiazole-2-thione derivatives

Published Online: 30 May 2008
Page range: 135 - 149

Abstract

<italic>In vitro</italic> antitumor and antiviral activities of new benzothiazole and 1,3,4-oxadiazole-2-thione derivatives

A series of new benzothiazole derivatives 6a-h have been synthesized, in five steps, from substituted phenols via the 1,3,4-oxadiazole-2-thiones 5a-h. The in vitro antitumor activity of the compounds obtained was investigated and the benzothiazol derivatives 6d and 6e showed strong effects on leukaemia cell lines CCRF-CEM (CC50 = 12 ± 2 μmol L-1, 8 ± 1 μmol L-1, respectively). These compounds are leading candidates for further development. The title compounds were tested against representatives of several virus families containing single stranded RNA genomes, either positive-sense (ssRNA+), or negativesense (RNA-), and against double-stranded RNA genomes (dsRNA), as well as some Flaviviridae viruses.

Keywords

  • 1,3,4-oxathiazoles
  • substituted benzothiazoles
  • antitumor activity
  • antiviral activity
Open Access

Effect of various surfactants and their concentration on controlled release of captopril from polymeric matrices

Published Online: 30 May 2008
Page range: 151 - 162

Abstract

Effect of various surfactants and their concentration on controlled release of captopril from polymeric matrices

Various methods are available to formulate water soluble drugs into sustained release dosage forms by retarding the dissolution rate. One of the methods used to control drug release and thereby prolong therapeutic activity is to use hydrophilic and lipophilic polymers. In this study, the effects of various polymers such as hydroxypropyl methylcellulose (HPMC), ethylcellulose (EC) and sodium carboxymethylcellulose (CMC) and surfactants (sodium lauryl sulphate, cetyltrimethylammonium bromide and Arlacel 60) on the release rate of captopril were investigated. The results showed that an increase in the amount of HPMC K15M resulted in reduction of the release rate of captopril from these matrices. When HPMC was partly replaced by NaCMC (the ratio of HPMC/NaCMC was 5:1), the release rate of the drug significantly decreased. However, there was no significant difference in release rate of captopril from matrices produced with ratios of 5:1 and 2:1 of HPMC/NaCMC. The presence of lactose in matrices containing HPMC and NaCMC increased the release rate of captopril. It was interesting to note that although partial replacement of HPMC by EC reduced the release rate of the drug (ratio of HPMC/EC 2:1), the release rate was increased when the ratio of HPMC/EC was reduced to 1:1. The effects of various surfactants on the release rate of captopril from HPMC/EC (1:1) matrices were also investigated. The results showed that the surfactants did not significantly change the release rate of the drug. Release data were examined kinetically and the ideal kinetic models were estimated for the drug release. The kinetic analysis of drug release data from various formulations showed that incorporation of surfactants in HPMC/EC matrices did not produce a zero-order release pattern.

Keywords

  • captopril
  • polymers
  • controlled release
  • surfactant
  • release kinetic
Open Access

Comparison between two cyclooxygenase inhibitors in an experimental dry eye model in albino rabbits

Published Online: 30 May 2008
Page range: 163 - 173

Abstract

Comparison between two cyclooxygenase inhibitors in an experimental dry eye model in albino rabbits

The purpose of this study was to compare the topical anti-inflammatory effects of the nonselective cyclooxygenase (COX) inhibitor, ketorolac, with the selective COX-2 inhibitor, nimesulide, in an animal model of dry eye in albino rabbits. All animals were examined by the Schirmer test, tear break-up time (TBUT) and fluorescein corneal staining test. Dry eye model showed significant reduction in tear volume, TBUT, corneal staining and histopathological signs of dryness and inflammation. On treating dry eye model with nimesulide 0.1% eye drops and ketorolac 0.5% eye drops, there were improvements in Schirmer test values, TBUT and fluorescein corneal staining and histopathologically reduced inflammatory reaction, with signs of healing and regeneration. Both nimesulide and ketorolac ameliorate atropine sulphate induced dry eye in albino rabbits. The use of selective COX-2 inhibitor, nimesulide, is preferred to avoid local and systemic side effects which may occur with the use of the nonselective COX inhibitor, ketorolac.

Keywords

  • dry eye model
  • rabbit
  • atropine sulphate
  • Schirmer test I
  • nimesulide
  • ketorolac
Open Access

Anti-inflammatory and analgesic activities of some newly synthesized pyridinedicarbonitrile and benzopyranopyridine derivatives

Published Online: 30 May 2008
Page range: 175 - 186

Abstract

Anti-inflammatory and analgesic activities of some newly synthesized pyridinedicarbonitrile and benzopyranopyridine derivatives

In continuation of our search for new substituted pyridine based anti-inflammatories, reaction of 1-(2-thienyl or furanyl)-3-(2-hydroxyphenyl)-2-propen-1-ones (1) with malononitrile in alcoholic KOH solution afforded a mixture of 4-alkoxy-2-(2-thienyl or furanyl)-5H-[1]benzopyrano[3,4-c]pyridine-5-ones (2) and 2-alkoxy-4-amino-6- (2-thienyl or furanyl)-3,5-pyridinedicarbonitriles (3). Some of the synthesized compounds were evaluated for their anti-inflammatory and analgesic activities compared to diclofenac potassium as positive control. Detailed synthesis, spectroscopic and toxicity data are reported.

Keywords

  • pyridinedicarbonitrile
  • benzopyranopyridine
  • anti-inflammatory
  • analgesic agents
Open Access

Formulation and evaluation of oil entrapped gastroretentive floating gel beads of loratadine

Published Online: 30 May 2008
Page range: 187 - 197

Abstract

Formulation and evaluation of oil entrapped gastroretentive floating gel beads of loratadine

A gastro retentive controlled release system of loratadine was formulated to increase the residence time in stomach and to modulate the release behaviour of the drug. Oil entrapped floating microbeads prepared by the emulsion gelation method were optimized by 23 factorial design and a polymer ratio of 2.5:1.5 (pectin/sodium alginate) by mass, 15% (m/V) of oil (mineral oil or castor oil) and 0.45 mol L-1 calcium chloride solution as the optimized processing conditions for the desired buoyancy and physical stability. In vitro drug release in the fed state conditions demonstrated sustained release of loratadine for 8 h, which best fitted the Peppas model with n < 0.45. The ethyl cellulose coating on microbeads optimized by 22 factorial design resulted in a controlled release formulation of loratadine that provided zero-order release for 8 h.

Keywords

  • loratadine
  • gastroretentive
  • factorial design
  • ethyl cellulose coating
  • zero-order release
Open Access

Studying the formation of aggregates in recombinant human granulocyte-colony stimulating factor (rHuG-CSF), lenograstim, using size-exclusion chromatography and SDS-PAGE

Published Online: 30 May 2008
Page range: 199 - 206

Abstract

Studying the formation of aggregates in recombinant human granulocyte-colony stimulating factor (rHuG-CSF), lenograstim, using size-exclusion chromatography and SDS-PAGE

The stability of proteins is a subject of intense current interest. Aggregation, as a dominant degradation pathway for therapeutic proteins, may cause multiple adverse effects, including loss of efficacy and immunogenicity. In the present study, the formation of aggregates in lenograstim under physiological conditions was monitored. For this purpose, a simple and selective size-exclusion high-performance liquid chromatography method for detection and separation of aggregates from intact protein was developed. Sodium dodecyl sulphate-polyacrylamide gel electrophoresis was performed under reducing and non-reducing conditions to determine the nature of aggregate bond formation. Using both techniques, the presence of a low aggregate content attached via disulfide bonds was detected.

Keywords

  • lenograstim
  • aggregate formation
  • size-exclusion high-performance liquid chromatography
  • sodium dodecyl sulphate-polyacrylamide gel electrophoresis
Open Access

Identification of chemical compounds from the leaves of Leea indica

Published Online: 30 May 2008
Page range: 207 - 214

Abstract

Identification of chemical compounds from the leaves of <italic>Leea indica</italic>

Twenty-three known chemical compounds were identified in the leaves of Leea indica (Burm. f.) Merr. (Leeaceae) by GC-MS analysis, spectroscopic techniques and co-TLC with authentic samples. The identified compounds include eleven hydrocarbons, phthalic acid, palmitic acid, 1-eicosanol, solanesol, farnesol, three phthalic acid esters, gallic acid, lupeol, β-sitosterol and ursolic acid. Gallic acid was isolated as n-butyl gallate and identified by co-TLC. This seems to be the first report of the presence of gallic acid in the leaves of L. indica.

Keywords

  • Leea indica (Leeaceae)
  • GC-MS
  • gallic acid
  • -butyl gallate
  • antioxidant activity
Open Access

Antioxidant and free radical scavenging potential of Citrullus colocynthis (L.) Schrad. methanolic fruit extract

Published Online: 30 May 2008
Page range: 215 - 220

Abstract

Antioxidant and free radical scavenging potential of <italic>Citrullus colocynthis</italic> (L.) Schrad. methanolic fruit extract

Citrullus colocynthis (L.) Schrad. (Cucurbitaceae) is a medicinal plant traditionally used as an abortifacient and to treat constipation, oedema, bacterial infections, cancer and diabetes. Preliminary phytochemical screening of the plant showed the presence of large amounts of phenolics and flavonoids. Subsequent quantification showed the presence of 0.74% (m/m) phenolics (calculated as gallic acid) and 0.13% (m/m) flavonoids calculated as catechin equivalents per 100 g of fresh mass. The presence of phenolic compounds prompted us to evaluate its antioxidant activity. In the present study, methanolic fruit extract of C. colocynthis was screened to evaluate its freeradical scavenging effect. The highest antioxidant and free radical scavenging ability of the fruit extract was observed at a concentration of 2500 μg mL-1.

Keywords

  • Citrullus colocynthis fruit
  • Cucurbitaceae
  • methanolic extract
  • antioxidants
  • free radical scavenging
Open Access

Gastric floating matrix tablets: Design and optimization using combination of polymers

Published Online: 30 May 2008
Page range: 221 - 229

Abstract

Gastric floating matrix tablets: Design and optimization using combination of polymers

The purpose of the present study was to develop an optimized gastric floating drug delivery system (GFDDS) containing domperidone as a model drug. Box-Behnken design was employed in formulating the GFDDS with three polymers: hydroxypropyl methylcellulose K4M (HPMC K4M) (X1), Carbopol 934P (X2) and sodium alginate (X3), as independent variables. Floating lag time (FLT), total floating time (TFT), time required to release 50% of the drug (t50) and diffusion exponent (n) were selected as dependent variables. Seventeen formulations were prepared, dissolution data obtained was fitted to the power law and floating profiles were analyzed. HPMC loading was found to be significant for floating properties. Carbopol loading had a negative effect on floating properties but was found helpful in controlling the release rate of the drug. No significant effect of sodium alginate on floating properties was observed but it was important for gel formation. The quadratic mathematical model developed could be used to predict formulations with desired release and floating properties.

Keywords

  • domperidone
  • floating matrix tablet
  • Box-Behnken design
  • GFDDS
  • release kinetics
Open Access

N-Phthaloyl-glycine-hydroxamic acid as serum iron chelator in rats

Published Online: 30 May 2008
Page range: 231 - 236

Abstract

<italic>N</italic>-Phthaloyl-glycine-hydroxamic acid as serum iron chelator in rats

The aim of this study was to investigate the activity of N-phthaloyl-glycine-hydroxamic acid (Phth-Gly-HA) as a new iron chelator in vivo to be used in iron overload diseases. After intraperitoneal application of Phth-Gly-HA to male rats (1 mg kg-1 body mass) once a day for seven days, iron serum level decreased by 21%, whereas the iron value dropped by 32% in female rats (1.5 mg kg-1 body mass). The results indicate that the tested substance has the ability to bind serum iron by complexation. Besides transferrin iron release, mobilization of ferritin iron is also possible.

Keywords

  • -phthaloyl-glycine-hydroxamic acid
  • iron chelators
  • iron overload

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