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Dettagli della rivista
Formato
Rivista
eISSN
1846-9558
Pubblicato per la prima volta
28 Feb 2007
Periodo di pubblicazione
4 volte all'anno
Lingue
Inglese

Cerca

Volume 67 (2017): Edizione 1 (March 2017)

Dettagli della rivista
Formato
Rivista
eISSN
1846-9558
Pubblicato per la prima volta
28 Feb 2007
Periodo di pubblicazione
4 volte all'anno
Lingue
Inglese

Cerca

10 Articoli

Original research paper

Accesso libero

Switching antipsychotics: Results of 16-month non-interventional, prospective, observational clinical research of inpatients with schizophrenia spectrum disorders

Pubblicato online: 21 Feb 2017
Pagine: 99 - 112

Astratto

Abstract

The study aims to identify prescribing and switching patterns of antipsychotics in clinical practice. A 16-month, prospective study was conducted at the Psychiatric Hospital Idrija, Slovenia. Inpatients (N = 311) with schizophrenia spectrum disorders were observed. The causes for switching antipsychotics and switching strategies were analyzed. Analyzing a total of 3954 prescriptions, the collected data confirmed that treatment strategies in this psychiatric hospital are very complex. It was found that 37 percent of inpatients had at least one switch. Moreover, switches that included three or more antipsychotics were detected. The most common causes for switching antipsychotics were adverse reactions and inefficacy or lack of efficacy. Among switching options, abrupt switch was recorded several times. As some patients are receiving several antipsychotics at the same time, it is possible that unusual switching occurs in clinical practice. It seems that the choice of switching strategy is also affected by the cause and urgency for switching an antipsychotic.

Parole chiave

  • schizophrenia
  • switching antipsychotics
  • causes
  • strategies
Accesso libero

Characterization and taste masking evaluation of microparticles with cetirizine dihydrochloride and methacrylate-based copolymer obtained by spray drying

Pubblicato online: 21 Feb 2017
Pagine: 113 - 124

Astratto

Abstract

Taste of a pharmaceutical formulation is an important parameter for the effectiveness of pharmacotherapy. Cetirizine dihydrochloride (CET) is a second-generation antihistamine that is commonly administered in allergy treatment. CET is characterized by extremely bitter taste and it is a great challenge to successfully mask its taste; therefore the goal of this work was to formulate and characterize the microparticles obtained by the spray drying method with CET and poly(butyl methacrylate-co-(2-dimethylaminoethyl) methacrylate-co-methyl methacrylate 1:2:1 copolymer (Eudragit E PO) as a barrier coating. Assessment of taste masking by the electronic tongue has revealed that designed formulations created an effective taste masking barrier. Taste masking effect was also confirmed by the in vivo model and the in vitro release profile of CET. Obtained data have shown that microparticles with a drug/polymer ratio (0.5:1) are promising CET carriers with efficient taste masking potential and might be further used in designing orodispersible dosage forms with CET.

Parole chiave

  • taste masking
  • electronic tongue
  • cetirizine dihydrochloride
  • microparticles
  • methacrylate copolymer
  • spray drying
Accesso libero

Synthesis and antitumor activity of some novel thiophene, pyrimidine, coumarin, pyrazole and pyridine derivatives

Pubblicato online: 21 Feb 2017
Pagine: 15 - 33

Astratto

Abstract

2-Cyano-N-(thiazol-2-yl) acetamide (2a) and 2-cyano-N-(oxazol- 2-yl) acetamide (2b) were obtained via the reaction of ethyl cyanoacetate with either 2-aminothiazole (1a) or 2-aminooxazole (1b). The formed products were directed toward the reaction with cyclopentanone and elemental sulfur in the presence of triethylamine to give cyclopenta[b]thiophene derivatives (3a,b). The latter products were reacted with either ethyl cyanoacetate or malononitrile to form compounds 4a,b and 5a,b, respectively. Compounds 4a,b were aimed at synthesizing some heterocyclic compounds; thus internal cyclization reactions were introduced to form compounds 6a,b. Also, compounds 4a,b reacted with salicylaldehyde, hydrazine derivatives and either urea or thiourea to produce coumarin derivatives (7a,b), pyrazole derivatives (8a-d) and pyrimidine derivatives (9a-d), respectively. Reaction of either benzaldehyde or benzene diazonium chloride (11) with compounds 4a,b afforded compounds 10a,b and 12a,b, respectively. On the other hand, compounds 5a,b underwent internal cyclization to form pyrimidine derivatives 13a,b. Also, when compounds 5a,b reacted with either ethyl cyanoacetate or malononitrile, they gave pyridine derivatives (15a-d) through the formation of intermediates (14a-d). Finally, formation of fused pyrimidine derivatives (17a,b) was achieved through the reaction of compounds 5a,b and salicylaldehyde applying two different pathways. The first pathway used a catalytic amount of piperidine to form compounds 16a,b; the latter products underwent cyclization to give compounds 17a,b. The second pathway, using a catalytic amount of sodium ethoxide solution directly in one step, afforded compounds 17a,b. Structures of the newly synthesized compounds were established using IR, 1H NMR, 13C NMR and mass spectrometry and their antitumor activity was investigated. Some of these compounds showed promising inhibitory effects on three different cell lines. However, fused pyrimidine acetonitrile derivatives 6a and 6b exerted the highest inhibitory effect, comparable to that of doxorubicin.

Parole chiave

  • thiophene
  • pyrimidine
  • coumarin
  • pyrazole
  • pyridine
  • antitumor activity
Accesso libero

Hydrazinyldiene-chroman-2,4-diones in inducing growth arrest and apoptosis in breast cancer cells: Synergism with doxorubicin and correlation with physicochemical properties

Pubblicato online: 21 Feb 2017
Pagine: 35 - 52

Astratto

Abstract

This study evaluates the effects of previously synthesized hydrazinyldiene-chroman-2,4-diones on cell proliferation and apoptosis, cell cycle distribution and migration capacity of MCF-7 breast cancer cells in synergy with doxorubicin. Physicochemical properties of the synthesized compounds were correlated with their structure and activity. Significant cell viability decrease in comparison with the effect of doxorubicin alone and the reference 4-hydroxycoumarin was observed when combination treatment comprising doxorubicin and the title compounds was applied. Synergistic effect with doxorubicin was also observed in down-regulation of phospho-Thr308Akt levels, confirming reduced proliferation and increased apoptosis. Combined treatment increased the percentage of cells arrested at the G2/M stage. Additive inhibition of cell migration was also observed, pointing to the possibility of reducing the risk of metastases. With their solubility profile and log D7.4, all the synthesized compounds follow Lipinski’s rule of five for good permeability (absorption) potential.

Parole chiave

  • hydrazinyldiene chroman 2,4 diones
  • physicochemical properties
  • doxorubicin
  • cytotoxicity
  • breast cancer cells
Accesso libero

A superior preparation method for daidzein-hydroxypropyl-β-cyclodextrin complexes with improved solubility and dissolution: Supercritical fluid process

Pubblicato online: 21 Feb 2017
Pagine: 85 - 97

Astratto

Abstract

Advantages of the supercritical fluid (SCF) process compared to the conventional solution stirring method (CSSM) in the preparation of daidzein-hydroxypropyl-β-cyclodextrin (HPβCD) complexes were investigated. Formation of daidzein/ HPβCD inclusion complexes was confirmed by Fourier transformed-infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), X-ray diffraction (XRD) and scanning electron microscopy (SEM). Particle size, inclusion yield, drug solubility and dissolution of daidzein/HPβCD complexes were evaluated. Compared to CSSM, the SCF process resulted in higher inclusion yield and higher solubility. Also, extended dissolution of daidzein from the SCF processed HPβCD inclusion complexes was observed, with only 22.94 % released in 45 min, compared to its rapid release from those prepared by CSSM, with 98.25 % drug release in 15 min. This extended release of daidzein from SCF prepared inclusion complexes was necessary to avoid drug precipitation and improve drug solubilisation in the gastrointestinal tract. The results showed that the SCF process is a superior preparation method for daidzein-hydroxypropyl-β-cyclodextrin complexes.

Parole chiave

  • daidzein
  • hydroxypropyl β cyclodextrin
  • supercritical fluid
  • inclusion complex
Accesso libero

Formulation and pharmaceutical development of quetiapine fumarate sustained release matrix tablets using a QbD approach

Pubblicato online: 21 Feb 2017
Pagine: 53 - 70

Astratto

Abstract

The main objective of the present study was to apply QbD methodology in the development of once-a-day sustained release quetiapine tablets. The quality target product profile (QTPP) was defined after the pharmaceutical properties and kinetic release of the innovator product, Seroquel XR 200 mg. For the D-optimal experimental design, the level and ratio of matrix forming agents and the type of extragranular diluent were chosen as independent inputs, which represented critical formulation factors. The critical quality attributes (CQAs) studied were the cumulative percentages of quetiapine released after certain time intervals. After the analysis of the experimental design, optimal formulas and the design space were defined. Optimal formulas demonstrated zero-order release kinetics and a dissolution profile similar to the innovator product, with f2 values of 74.53 and 83.74. It was concluded that the QbD approach allowed fast development of sustained release tablets with similar dissolution behavior as the innovator product.

Parole chiave

  • quality by design
  • design of experiments
  • sustained release
  • hydrophilic matrix
  • quetiapine
Accesso libero

Public health care system, a quasi-experimental study: Acceptance and attitude to implicate clinical services

Pubblicato online: 21 Feb 2017
Pagine: 71 - 83

Astratto

Abstract

A six-month longitudinal intervention arm study with a pre-post cross-sectional questionnaire-based survey was performed. A 3-phase objective structured clinical examination (OSCE) design was utilized for evaluation of acceptance and attitude of pharmacy students towards clinical pharmacy services. The pre-OSCE survey showed increased disagreement with the role of clinical pharmacists, compared to a significant positive shift in attitude towards their services in the healthcare team after 6 months of the trial. Responses improved for awareness (the current healthcare system could be improved by involving pharmacists, p < 0.02) and positive attitude categories (doctors and nurses would be happy to welcome the services of competent clinical pharmacists as part of their team, p < 0.01) in addition to competency (pharmacists have sufficient clinical training to advise doctors and nurses, p < 0.01). The predictive model suggested a strong positive effect on patient interaction, medical information tasks, clinical decisions on drug-related problems (DRPs), and communication with healthcare professionals (R2 = 0.41, F = 1.51, p < 0.001).

Parole chiave

  • clinical pharmacy
  • pharmacy education
  • clinical training
  • objectively structured clinical examination
Accesso libero

Pulmonary prophylactic impact of melatonin and/or quercetin: A novel therapy for inflammatory hypoxic stress in rats

Pubblicato online: 21 Feb 2017
Pagine: 125 - 135

Astratto

Abstract

The study aims to compare, through histological and biochemical studies, the effects of quercetin, melatonin and their combination in regulation of immuno-inflammatory mediators and heat shock protein expressions in sodium nitrite induced hypoxia in rat lungs. The results revealed that NaNO2 injection caused a significant decrease in Hb in rats, while serum levels of TNF-α, IL-6 and CRP, VEGF and HSP70 were elevated compared to the control group. Administration of melatonin, quercetin or their combination before NaNO2 injection markedly reduced these parameters. Histopathological examination of the lung tissue supported these biochemical findings. The study suggests that melatonin and/or quercetin are responsible for lung tissue protection in hypoxia by downregulation of immuno-inflammatory mediators and heat shock protein expressions. Pre-treatment of hypoxic animals with a combination of melatonin and quercetin was effective in modulating most of the studied parameters to near-normal levels.

Parole chiave

  • hypoxia
  • melatonin
  • quercetin
  • inflammatory mediators
  • heat shock protein

Review

Accesso libero

The role of peroxisome proliferator-activated receptor in the treatment of non-alcoholic fatty liver disease

Pubblicato online: 21 Feb 2017
Pagine: 1 - 13

Astratto

Abstract

Non-alcoholic fatty liver disease (NAFLD) has been defined as a spectrum of histological abnormalities and is characterized by significant and excessive accumulation of triglycerides in the hepatocytes in patients without alcohol consumption or other diseases. Current studies are targeting new molecular mechanisms that underlie NAFLD and associated metabolic disorders. Many therapeutic targets have been found and used in clinical studies. Peroxisome proliferator-activated receptors (PPARs) are among the potential targets and have been demonstrated to exert a pivotal role in modulation of NAFLD. Many drugs developed so far are targeted at PPARs. Thus, the aim of this paper is to summarize the roles of PPARs in the treatment of NAFLD.

Parole chiave

  • non alcoholic fatty liver disease
  • peroxisome proliferator activated receptors
  • agonists
  • insulin resistance
  • inflammation

Short communication

Accesso libero

Challenges relating to comparison of flavonoid glycosides dissolution profiles from Sutherlandia frutescens products

Pubblicato online: 21 Feb 2017
Pagine: 137 - 146

Astratto

Abstract

Unlike the case of conventional drug formulations, dissolution tests have hitherto not been required for herbal medicinal products commercially available in South Africa. This study investigated dissolution of the South African Sutherlandia frutescens using selected flavonoid glycosides as marker compounds. Dissolution of markers was assessed in three dissolution media at pH 1.2, 4.5 and 6.8, and samples were analysed using a validated HPLC method. The dissolution profile of each marker varied for the different materials investigated. All three media utilised showed differences in flavonoid glycoside dissolution between the S. frutescens products evaluated, with f2 values < 50 for comparison of flavonoid dissolution from any two of the materials. Dissolution of S. frutescens materials could thus be characterised using the markers in all the media tested. This tool may be employed in the future for comparison of orally administered S. frutescens products, provided between- batch variability is evaluated and found less than between-sample variability.

Parole chiave

  • Sutherlandia frutescens
  • herbal products
  • dissolution testing
  • flavonoid
  • discriminatory medium
  • similarity factor
10 Articoli

Original research paper

Accesso libero

Switching antipsychotics: Results of 16-month non-interventional, prospective, observational clinical research of inpatients with schizophrenia spectrum disorders

Pubblicato online: 21 Feb 2017
Pagine: 99 - 112

Astratto

Abstract

The study aims to identify prescribing and switching patterns of antipsychotics in clinical practice. A 16-month, prospective study was conducted at the Psychiatric Hospital Idrija, Slovenia. Inpatients (N = 311) with schizophrenia spectrum disorders were observed. The causes for switching antipsychotics and switching strategies were analyzed. Analyzing a total of 3954 prescriptions, the collected data confirmed that treatment strategies in this psychiatric hospital are very complex. It was found that 37 percent of inpatients had at least one switch. Moreover, switches that included three or more antipsychotics were detected. The most common causes for switching antipsychotics were adverse reactions and inefficacy or lack of efficacy. Among switching options, abrupt switch was recorded several times. As some patients are receiving several antipsychotics at the same time, it is possible that unusual switching occurs in clinical practice. It seems that the choice of switching strategy is also affected by the cause and urgency for switching an antipsychotic.

Parole chiave

  • schizophrenia
  • switching antipsychotics
  • causes
  • strategies
Accesso libero

Characterization and taste masking evaluation of microparticles with cetirizine dihydrochloride and methacrylate-based copolymer obtained by spray drying

Pubblicato online: 21 Feb 2017
Pagine: 113 - 124

Astratto

Abstract

Taste of a pharmaceutical formulation is an important parameter for the effectiveness of pharmacotherapy. Cetirizine dihydrochloride (CET) is a second-generation antihistamine that is commonly administered in allergy treatment. CET is characterized by extremely bitter taste and it is a great challenge to successfully mask its taste; therefore the goal of this work was to formulate and characterize the microparticles obtained by the spray drying method with CET and poly(butyl methacrylate-co-(2-dimethylaminoethyl) methacrylate-co-methyl methacrylate 1:2:1 copolymer (Eudragit E PO) as a barrier coating. Assessment of taste masking by the electronic tongue has revealed that designed formulations created an effective taste masking barrier. Taste masking effect was also confirmed by the in vivo model and the in vitro release profile of CET. Obtained data have shown that microparticles with a drug/polymer ratio (0.5:1) are promising CET carriers with efficient taste masking potential and might be further used in designing orodispersible dosage forms with CET.

Parole chiave

  • taste masking
  • electronic tongue
  • cetirizine dihydrochloride
  • microparticles
  • methacrylate copolymer
  • spray drying
Accesso libero

Synthesis and antitumor activity of some novel thiophene, pyrimidine, coumarin, pyrazole and pyridine derivatives

Pubblicato online: 21 Feb 2017
Pagine: 15 - 33

Astratto

Abstract

2-Cyano-N-(thiazol-2-yl) acetamide (2a) and 2-cyano-N-(oxazol- 2-yl) acetamide (2b) were obtained via the reaction of ethyl cyanoacetate with either 2-aminothiazole (1a) or 2-aminooxazole (1b). The formed products were directed toward the reaction with cyclopentanone and elemental sulfur in the presence of triethylamine to give cyclopenta[b]thiophene derivatives (3a,b). The latter products were reacted with either ethyl cyanoacetate or malononitrile to form compounds 4a,b and 5a,b, respectively. Compounds 4a,b were aimed at synthesizing some heterocyclic compounds; thus internal cyclization reactions were introduced to form compounds 6a,b. Also, compounds 4a,b reacted with salicylaldehyde, hydrazine derivatives and either urea or thiourea to produce coumarin derivatives (7a,b), pyrazole derivatives (8a-d) and pyrimidine derivatives (9a-d), respectively. Reaction of either benzaldehyde or benzene diazonium chloride (11) with compounds 4a,b afforded compounds 10a,b and 12a,b, respectively. On the other hand, compounds 5a,b underwent internal cyclization to form pyrimidine derivatives 13a,b. Also, when compounds 5a,b reacted with either ethyl cyanoacetate or malononitrile, they gave pyridine derivatives (15a-d) through the formation of intermediates (14a-d). Finally, formation of fused pyrimidine derivatives (17a,b) was achieved through the reaction of compounds 5a,b and salicylaldehyde applying two different pathways. The first pathway used a catalytic amount of piperidine to form compounds 16a,b; the latter products underwent cyclization to give compounds 17a,b. The second pathway, using a catalytic amount of sodium ethoxide solution directly in one step, afforded compounds 17a,b. Structures of the newly synthesized compounds were established using IR, 1H NMR, 13C NMR and mass spectrometry and their antitumor activity was investigated. Some of these compounds showed promising inhibitory effects on three different cell lines. However, fused pyrimidine acetonitrile derivatives 6a and 6b exerted the highest inhibitory effect, comparable to that of doxorubicin.

Parole chiave

  • thiophene
  • pyrimidine
  • coumarin
  • pyrazole
  • pyridine
  • antitumor activity
Accesso libero

Hydrazinyldiene-chroman-2,4-diones in inducing growth arrest and apoptosis in breast cancer cells: Synergism with doxorubicin and correlation with physicochemical properties

Pubblicato online: 21 Feb 2017
Pagine: 35 - 52

Astratto

Abstract

This study evaluates the effects of previously synthesized hydrazinyldiene-chroman-2,4-diones on cell proliferation and apoptosis, cell cycle distribution and migration capacity of MCF-7 breast cancer cells in synergy with doxorubicin. Physicochemical properties of the synthesized compounds were correlated with their structure and activity. Significant cell viability decrease in comparison with the effect of doxorubicin alone and the reference 4-hydroxycoumarin was observed when combination treatment comprising doxorubicin and the title compounds was applied. Synergistic effect with doxorubicin was also observed in down-regulation of phospho-Thr308Akt levels, confirming reduced proliferation and increased apoptosis. Combined treatment increased the percentage of cells arrested at the G2/M stage. Additive inhibition of cell migration was also observed, pointing to the possibility of reducing the risk of metastases. With their solubility profile and log D7.4, all the synthesized compounds follow Lipinski’s rule of five for good permeability (absorption) potential.

Parole chiave

  • hydrazinyldiene chroman 2,4 diones
  • physicochemical properties
  • doxorubicin
  • cytotoxicity
  • breast cancer cells
Accesso libero

A superior preparation method for daidzein-hydroxypropyl-β-cyclodextrin complexes with improved solubility and dissolution: Supercritical fluid process

Pubblicato online: 21 Feb 2017
Pagine: 85 - 97

Astratto

Abstract

Advantages of the supercritical fluid (SCF) process compared to the conventional solution stirring method (CSSM) in the preparation of daidzein-hydroxypropyl-β-cyclodextrin (HPβCD) complexes were investigated. Formation of daidzein/ HPβCD inclusion complexes was confirmed by Fourier transformed-infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), X-ray diffraction (XRD) and scanning electron microscopy (SEM). Particle size, inclusion yield, drug solubility and dissolution of daidzein/HPβCD complexes were evaluated. Compared to CSSM, the SCF process resulted in higher inclusion yield and higher solubility. Also, extended dissolution of daidzein from the SCF processed HPβCD inclusion complexes was observed, with only 22.94 % released in 45 min, compared to its rapid release from those prepared by CSSM, with 98.25 % drug release in 15 min. This extended release of daidzein from SCF prepared inclusion complexes was necessary to avoid drug precipitation and improve drug solubilisation in the gastrointestinal tract. The results showed that the SCF process is a superior preparation method for daidzein-hydroxypropyl-β-cyclodextrin complexes.

Parole chiave

  • daidzein
  • hydroxypropyl β cyclodextrin
  • supercritical fluid
  • inclusion complex
Accesso libero

Formulation and pharmaceutical development of quetiapine fumarate sustained release matrix tablets using a QbD approach

Pubblicato online: 21 Feb 2017
Pagine: 53 - 70

Astratto

Abstract

The main objective of the present study was to apply QbD methodology in the development of once-a-day sustained release quetiapine tablets. The quality target product profile (QTPP) was defined after the pharmaceutical properties and kinetic release of the innovator product, Seroquel XR 200 mg. For the D-optimal experimental design, the level and ratio of matrix forming agents and the type of extragranular diluent were chosen as independent inputs, which represented critical formulation factors. The critical quality attributes (CQAs) studied were the cumulative percentages of quetiapine released after certain time intervals. After the analysis of the experimental design, optimal formulas and the design space were defined. Optimal formulas demonstrated zero-order release kinetics and a dissolution profile similar to the innovator product, with f2 values of 74.53 and 83.74. It was concluded that the QbD approach allowed fast development of sustained release tablets with similar dissolution behavior as the innovator product.

Parole chiave

  • quality by design
  • design of experiments
  • sustained release
  • hydrophilic matrix
  • quetiapine
Accesso libero

Public health care system, a quasi-experimental study: Acceptance and attitude to implicate clinical services

Pubblicato online: 21 Feb 2017
Pagine: 71 - 83

Astratto

Abstract

A six-month longitudinal intervention arm study with a pre-post cross-sectional questionnaire-based survey was performed. A 3-phase objective structured clinical examination (OSCE) design was utilized for evaluation of acceptance and attitude of pharmacy students towards clinical pharmacy services. The pre-OSCE survey showed increased disagreement with the role of clinical pharmacists, compared to a significant positive shift in attitude towards their services in the healthcare team after 6 months of the trial. Responses improved for awareness (the current healthcare system could be improved by involving pharmacists, p < 0.02) and positive attitude categories (doctors and nurses would be happy to welcome the services of competent clinical pharmacists as part of their team, p < 0.01) in addition to competency (pharmacists have sufficient clinical training to advise doctors and nurses, p < 0.01). The predictive model suggested a strong positive effect on patient interaction, medical information tasks, clinical decisions on drug-related problems (DRPs), and communication with healthcare professionals (R2 = 0.41, F = 1.51, p < 0.001).

Parole chiave

  • clinical pharmacy
  • pharmacy education
  • clinical training
  • objectively structured clinical examination
Accesso libero

Pulmonary prophylactic impact of melatonin and/or quercetin: A novel therapy for inflammatory hypoxic stress in rats

Pubblicato online: 21 Feb 2017
Pagine: 125 - 135

Astratto

Abstract

The study aims to compare, through histological and biochemical studies, the effects of quercetin, melatonin and their combination in regulation of immuno-inflammatory mediators and heat shock protein expressions in sodium nitrite induced hypoxia in rat lungs. The results revealed that NaNO2 injection caused a significant decrease in Hb in rats, while serum levels of TNF-α, IL-6 and CRP, VEGF and HSP70 were elevated compared to the control group. Administration of melatonin, quercetin or their combination before NaNO2 injection markedly reduced these parameters. Histopathological examination of the lung tissue supported these biochemical findings. The study suggests that melatonin and/or quercetin are responsible for lung tissue protection in hypoxia by downregulation of immuno-inflammatory mediators and heat shock protein expressions. Pre-treatment of hypoxic animals with a combination of melatonin and quercetin was effective in modulating most of the studied parameters to near-normal levels.

Parole chiave

  • hypoxia
  • melatonin
  • quercetin
  • inflammatory mediators
  • heat shock protein

Review

Accesso libero

The role of peroxisome proliferator-activated receptor in the treatment of non-alcoholic fatty liver disease

Pubblicato online: 21 Feb 2017
Pagine: 1 - 13

Astratto

Abstract

Non-alcoholic fatty liver disease (NAFLD) has been defined as a spectrum of histological abnormalities and is characterized by significant and excessive accumulation of triglycerides in the hepatocytes in patients without alcohol consumption or other diseases. Current studies are targeting new molecular mechanisms that underlie NAFLD and associated metabolic disorders. Many therapeutic targets have been found and used in clinical studies. Peroxisome proliferator-activated receptors (PPARs) are among the potential targets and have been demonstrated to exert a pivotal role in modulation of NAFLD. Many drugs developed so far are targeted at PPARs. Thus, the aim of this paper is to summarize the roles of PPARs in the treatment of NAFLD.

Parole chiave

  • non alcoholic fatty liver disease
  • peroxisome proliferator activated receptors
  • agonists
  • insulin resistance
  • inflammation

Short communication

Accesso libero

Challenges relating to comparison of flavonoid glycosides dissolution profiles from Sutherlandia frutescens products

Pubblicato online: 21 Feb 2017
Pagine: 137 - 146

Astratto

Abstract

Unlike the case of conventional drug formulations, dissolution tests have hitherto not been required for herbal medicinal products commercially available in South Africa. This study investigated dissolution of the South African Sutherlandia frutescens using selected flavonoid glycosides as marker compounds. Dissolution of markers was assessed in three dissolution media at pH 1.2, 4.5 and 6.8, and samples were analysed using a validated HPLC method. The dissolution profile of each marker varied for the different materials investigated. All three media utilised showed differences in flavonoid glycoside dissolution between the S. frutescens products evaluated, with f2 values < 50 for comparison of flavonoid dissolution from any two of the materials. Dissolution of S. frutescens materials could thus be characterised using the markers in all the media tested. This tool may be employed in the future for comparison of orally administered S. frutescens products, provided between- batch variability is evaluated and found less than between-sample variability.

Parole chiave

  • Sutherlandia frutescens
  • herbal products
  • dissolution testing
  • flavonoid
  • discriminatory medium
  • similarity factor

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