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Detalles de la revista
Formato
Revista
eISSN
1846-9558
Publicado por primera vez
28 Feb 2007
Periodo de publicación
4 veces al año
Idiomas
Inglés

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Volumen 66 (2016): Edición 4 (December 2016)

Detalles de la revista
Formato
Revista
eISSN
1846-9558
Publicado por primera vez
28 Feb 2007
Periodo de publicación
4 veces al año
Idiomas
Inglés

Buscar

10 Artículos
Acceso abierto

Pleiotropic effects of niacin: Current possibilities for its clinical use

Publicado en línea: 15 Oct 2016
Páginas: 449 - 469

Resumen

Abstract

Niacin was the first hypolipidemic drug to significantly reduce both major cardiovascular events and mortality in patients with cardiovascular disease. Niacin favorably influences all lipoprotein classes, including lipoprotein[a],and belongs to the most potent hypolipidemic drugs for increasing HDL-C. Moreover, niacin causes favorable changes to the qualitative composition of lipoprotein HDL. In addition to its pronounced hypolipidemic action, niacin exerts many other, non-hypolipidemic effects (e.g., antioxidative, anti-inflammatory, antithrombotic), which favorably influence the development and progression of atherosclerosis. These effects are dependent on activation of the specific receptor HCA2. Recent results published by the two large clinical studies, AIM-HIGH and HPS2-THRIVE, have led to the impugnation of niacin’s role in future clinical practice. However, due to several methodological flaws in the AIM-HIGH and HPS2-THRIVE studies, the pleiotropic effects of niacin now deserve thorough evaluation. This review summarizes the present and possible future use of niacin in clinical practice in light of its newly recognized pleiotropic effects.

Palabras clave

  • niacin
  • pleiotropic effects
  • HCA2 receptor
  • dyslipidemia
  • cardiovascular mortality/morbidity
Acceso abierto

Side effects of retinoid therapy on the quality of vision

Publicado en línea: 15 Oct 2016
Páginas: 471 - 478

Resumen

Abstract

Retinoids are compounds chemically related to vitamin A, which are frequently used in dermatological practice (1). They are characterized by numerous mechanisms of action leading to normalization of keratinocyte proliferation and maturation. They have anti-seborrhoeic, immunomodulatory and anti-inflammatory effects (1, 2). A number of side effects to retinoid treatment have been recorded; one group of such side effects relates to eyes and vision. Dry eye syndrome and blepharoconjunctivitis are the most common side effects, appearing in 20-50 % of patients treated with retinoids. They often contribute to the occurrence of other side-effects such as eye discomfort and contact lens intolerance. Due to the widespread use in clinical practice, the adverse effects, including ocular side effects, should be studied. To confirm the variety of adverse effects of retinoids, several case reports of rare side-effects are presented.

Palabras clave

  • retinoids
  • isotretinoin
  • adverse effects
  • eyes
  • acne
Acceso abierto

Development and validation of HPLC and CE methods for simultaneous determination of amlodipine and atorvastatin in the presence of their acidic degradation products in tablets

Publicado en línea: 15 Oct 2016
Páginas: 479 - 490

Resumen

Abstract

Two methods were developed for separation and quantitation of amlodipine (AML) and atorvastatin (ATV) in the presence of their acidic degradation products. The first method was a simple isocratic RP-HPLC method while the second was capillary electrophoresis (CE). Degradation products were obtained by acidic hydrolysis of the two drugs and their structures were elucidated for the first time by IR and MS spectra. Degradation products did not interfere with the determination of either drug and the assays were therefore stability-indicating. The linearity of the proposed methods was established over the ranges 1-50 μg mL-1 for AML and ATV in the HPLC method and in the range of 3-50 and 4-50 μg mL-1 for AML and ATV, respectively, in the CE method. The proposed methods were validated according to ICH guidelines. The methods were successfully applied to estimation of AML and ATV in combined tablets.

Palabras clave

  • atorvastatin
  • amlodipine
  • capillary zone electrophoresis
  • HPLC
  • stability
  • acidic degradation
Acceso abierto

Modulatory effects of rutin on the expression of cytochrome P450s and antioxidant enzymes in human hepatoma cells

Publicado en línea: 15 Oct 2016
Páginas: 491 - 502

Resumen

Abstract

Expression of a drug and xenobiotic metabolizing enzymes, cytochrome P450s (CYPs), and antioxidant enzymes can be modulated by various factors. The flavonoid rutin was investigated for its anti-carcinogen and protective effects as well as modulatory action on CYPs and phase II enzymes in human hepatocellular carcinoma cells. Rutin inhibited proliferation of HEPG2 cells in a dose-dependent manner with the IC50 value of 52.7 μmol L-1 and invasion of HEPG2 cells (21.6 %, p = 0.0018) and colony formation of those invaded cells (57.4 %, p < 0.0001). Rutin treatment also significantly increased early/late-stage apoptosis in HEPG2 cells (28.9 %, p < 0.001). Treatment by rutin significantly inhibited protein expressions of cytochrome P450-dependent CYP3A4 (75.3 %, p < 0.0001), elevated CYP1A1 enzymes (1.7-fold, p = 0.0084) and increased protein expressions of antioxidant and phase II reaction catalyzing enzymes, NQO1 (2.42-fold, p < 0.0001) and GSTP1 (2.03-fold, p < 0.0001). Besides, rutin treatment significantly inhibited mRNA expression of CYP3A4 (73.2 %, p=0.0014). Also, CYP1A1, NQO1 and GSTP1 mRNA expressions were significantly increased 2.77-fold (p = 0.029), 4.85- fold (p = 0.0051) and 9.84-fold (p < 0.0001), respectively.

Palabras clave

  • rutin
  • cytochrome P450s
  • phase II enzymes
  • cell proliferation
  • HEPG2
Acceso abierto

Ionophore-based potentiometric PVC membrane sensors for determination of phenobarbitone in pharmaceutical formulations

Publicado en línea: 15 Oct 2016
Páginas: 503 - 514

Resumen

Abstract

The fabrication and development of two polyvinyl chloride (PVC) membrane sensors for assaying phenobarbitone sodium are described. Sensors 1 and 2 were fabricated utilizing β- or γ-cyclodextrin as ionophore in the presence of tridodecylmethylammonium chloride as a membrane additive, and PVC and dioctyl phthalate as plasticizer. The analytical parameters of both sensors were evaluated according to the IUPAC guidelines. The proposed sensors showed rapid, stable anionic response (-59.1 and -62.0 mV per decade) over a relatively wide phenobarbitone concentration range (5.0 × 10-6-1 × 10-2 and 8 × 10-6-1 × 10-2 mol L-1) in the pH range of 9-11. The limit of detection was 3.5 × 10-6 and 7.0 × 10-6 mol L-1 for sensors 1 and 2, respectively. The fabricated sensors showed high selectivity for phenobarbitone over the investigated foreign species. An average recovery of 2.54 μg mL-1 phenobarbitone sodium was 97.4 and 101.1 %, while the mean relative standard deviation was 3.0 and 2.1 %, for sensors 1 and 2, respectively. The results acquired for determination of phenobarbitone in its dosage forms utilizing the proposed sensors are in good agreement with those obtained by the British Pharmacopoeial method.

Palabras clave

  • phenobarbitone sodium
  • membrane selective electrode
  • β-cyclodextrin
  • γ-cyclodextrin
  • PVC
  • potentiometry
Acceso abierto

A dual strategy to improve psychotic patients’ compliance using sustained release quetiapine oral disintegrating tablets

Publicado en línea: 15 Oct 2016
Páginas: 515 - 532

Resumen

Abstract

Quetiapine (QT) is a short acting atypical antipsychotic drug effective in schizophrenia and bipolar disorder. This study aims at designing a novel dosage form of sustained release taste-masked QT orally disintegrating tablets (ODTs) based on solid lipid micro-pellets (SLMPs). QT SLMPs were prepared using the hot melt extrusion technique and utilizing three lipid carriers: Compritol, Precirol and white beeswax either alone or in mixtures. They showed sustained QT release and a taste masking effect. The selected QT SLMP was further blended with an aqueous solution containing polyvinylpyrollidone (2.5 %), croscarmellose sodium (2 %) and mannitol (50 %); it was then lyophilized into ODT in a mass ratio of 1:2, respectively. ODTs containing QT SLMPs showed: average wetting time (40.92 s), average oral disintegration time (21.49 s), average hardness (16.85 N) and also imparted suitable viscosity to suspend pellets during the lyophilization process. In conclusion, lyophilization is a promising technique for the formulation of multiparticulate systems into ODTs.

Palabras clave

  • solid lipid micro pellets
  • multiparticulate
  • quetiapine
  • orally disintegrating tablets
Acceso abierto

Charge transfer interaction of organic p-acceptors with the anti-hyperuricemic drug allopurinol: Insights from IR, Raman, 1H NMR and 13C NMR spectroscopies

Publicado en línea: 15 Oct 2016
Páginas: 533 - 542

Resumen

Abstract

The topic of charge-transfer (CT) complexation of vital drugs has attracted considerable attention in recent years owing to their significant physical and chemical properties. In this study, CT complexes derived from the reaction of the anti-hyperuricemic drug allopurinol (Allop) with organic p-acceptors [(picric acid (PA), dichlorodicyanobenzoquinone (DDQ) and chloranil (CHL)] were prepared, isolated and characterized by a range of physicochemical methods, such as IR, Raman, 1H NMR and 13C NMR spectroscopy. The stoichiometry of the complexes was verified by elemental analysis. The results show that all complexes that were formed were based on a 1:1 stoichiometric ratio. This study suggests that the complexation of Allop with either the DDQ or CHL acceptor leads to a direct p®p* transition, whereas the molecules of Allop and PA are linked by intermolecular hydrogen- bonding interactions.

Palabras clave

  • allopurinol
  • p-acceptor
  • charge-transfer
  • proton- transfer
Acceso abierto

TLC determination of flavonoids from different cultivars of Allium cepa and Allium ascalonicum

Publicado en línea: 15 Oct 2016
Páginas: 543 - 554

Resumen

Abstract

This study comprises the optimization and validation of a new TLC method for determination of flavonols in the bulbs of seven cultivars of onions and shallots. Separation was performed on RP-18 plates with the solvent mixture tetrahydrofuran/water/formic acid (40+60+6, V/V/V) as a mobile phase. The method was evaluated for precision, linearity, LOD, LOQ, accuracy and robustness. Chromatographic analysis of the extracts revealed the presence of three main flavonols, quercetin, quercetin-4′-O-glucoside and quercetin-3,4′-O-diglucoside in the majority of analyzed cultivars. The content of flavonols in the analyzed extracts of onion bulbs varied from 123 (‘Exihibition’) to 1079 mg kg-1 fresh mass (fm) (‘Hybing’) in edible parts, and from 1727 (‘Hyline’) to 28949 mg kg-1 fm (‘Red Baron’) in outer scales. The bulbs of two shallot cultivars contained 209 (‘Ambition’) and 523 mg kg-1 fm (‘Matador’) of flavonols in edible parts and 5426 and 8916 mg kg-1 fm in outer scales, respectively.

Palabras clave

  • Allium cepa
  • Allium ascalonicum
  • cultivar varieties
  • flavonols
  • TLC
  • quantitative analysis
Acceso abierto

Preparation and in vivo evaluation of a gel-based nasal delivery system for risperidone

Publicado en línea: 15 Oct 2016
Páginas: 555 - 562

Resumen

Abstract

The aim of this study was to prepare a nasal gel of risperidone and to investigate the pharmacokinetics and relative bioavailability of the drug in rats. Compared with oral dosing, the risperidone nasal gel exhibited very fast absorption and high bioavailability. Maximal plasma concentration (cmax) and the time to reach cmax (tmax) were 15.2 μg mL-1 and 5 min for the nasal gel, 3.6 μg mL-1 and 30 min for the oral drug suspension, respectively. Pharmacokinetic parameters such as tmax′, cmax and AUC of oral and nasal routes were significantly different (p < 0.01). Relative bioavailability of the drug nasal preparation to the oral suspension was up to 1600.0 %. Further, the in vitro effect of the risperidone nasal gel on nasal mucociliary movement was also investigated using a toad palate model. The risperidone nasal formulation showed mild ciliotoxicity, but the adverse effect was temporary and reversible.

Palabras clave

  • risperidone
  • nasal gel
  • formulation
  • pharmacokinetics
  • bioavailability
  • ciliotoxicity
Acceso abierto

Pharmacokinetic evaluation of the interaction between oral kaempferol and ethanol in rats

Publicado en línea: 15 Oct 2016
Páginas: 563 - 568

Resumen

Abstract

This study was aimed at investigating the effect of ethanol on oral bioavailability of kaempferol in rats, namely, at disclosing their possible interaction. Kaempferol (100 or 250 mg kg-1 bm) was administered to the rats by oral gavage with or without ethanol (600 mg kg-1 bm) co-administration. Intravenous administration (10 and 25 mg kg-1 bm) of kaempferol was used to determine the bioavailability. The concentration of kaempferol in plasma was estimated by ultra high performance liquid chromatography. During coadministration, a significant increase of the area under the plasma concentration-time curve as well as the peak concentration were observed, along with a dramatic decrease in total body clearance. Consequently, the bioavailability of kaempferol in oral control groups was 3.1 % (100 mg kg-1 bm) and 2.1 % (250 mg kg-1 bm). The first was increased by 4.3 % and the other by 2.8 % during ethanol co-administration. Increased permeability of cell membrane and ethanolkaempferol interactions on CYP450 enzymes may enhance the oral bioavailability of kaempferol in rats.

Palabras clave

  • kaempferol
  • bioavailability
  • pharmacokinetics
  • ethanol
  • cytochrome P450s
10 Artículos
Acceso abierto

Pleiotropic effects of niacin: Current possibilities for its clinical use

Publicado en línea: 15 Oct 2016
Páginas: 449 - 469

Resumen

Abstract

Niacin was the first hypolipidemic drug to significantly reduce both major cardiovascular events and mortality in patients with cardiovascular disease. Niacin favorably influences all lipoprotein classes, including lipoprotein[a],and belongs to the most potent hypolipidemic drugs for increasing HDL-C. Moreover, niacin causes favorable changes to the qualitative composition of lipoprotein HDL. In addition to its pronounced hypolipidemic action, niacin exerts many other, non-hypolipidemic effects (e.g., antioxidative, anti-inflammatory, antithrombotic), which favorably influence the development and progression of atherosclerosis. These effects are dependent on activation of the specific receptor HCA2. Recent results published by the two large clinical studies, AIM-HIGH and HPS2-THRIVE, have led to the impugnation of niacin’s role in future clinical practice. However, due to several methodological flaws in the AIM-HIGH and HPS2-THRIVE studies, the pleiotropic effects of niacin now deserve thorough evaluation. This review summarizes the present and possible future use of niacin in clinical practice in light of its newly recognized pleiotropic effects.

Palabras clave

  • niacin
  • pleiotropic effects
  • HCA2 receptor
  • dyslipidemia
  • cardiovascular mortality/morbidity
Acceso abierto

Side effects of retinoid therapy on the quality of vision

Publicado en línea: 15 Oct 2016
Páginas: 471 - 478

Resumen

Abstract

Retinoids are compounds chemically related to vitamin A, which are frequently used in dermatological practice (1). They are characterized by numerous mechanisms of action leading to normalization of keratinocyte proliferation and maturation. They have anti-seborrhoeic, immunomodulatory and anti-inflammatory effects (1, 2). A number of side effects to retinoid treatment have been recorded; one group of such side effects relates to eyes and vision. Dry eye syndrome and blepharoconjunctivitis are the most common side effects, appearing in 20-50 % of patients treated with retinoids. They often contribute to the occurrence of other side-effects such as eye discomfort and contact lens intolerance. Due to the widespread use in clinical practice, the adverse effects, including ocular side effects, should be studied. To confirm the variety of adverse effects of retinoids, several case reports of rare side-effects are presented.

Palabras clave

  • retinoids
  • isotretinoin
  • adverse effects
  • eyes
  • acne
Acceso abierto

Development and validation of HPLC and CE methods for simultaneous determination of amlodipine and atorvastatin in the presence of their acidic degradation products in tablets

Publicado en línea: 15 Oct 2016
Páginas: 479 - 490

Resumen

Abstract

Two methods were developed for separation and quantitation of amlodipine (AML) and atorvastatin (ATV) in the presence of their acidic degradation products. The first method was a simple isocratic RP-HPLC method while the second was capillary electrophoresis (CE). Degradation products were obtained by acidic hydrolysis of the two drugs and their structures were elucidated for the first time by IR and MS spectra. Degradation products did not interfere with the determination of either drug and the assays were therefore stability-indicating. The linearity of the proposed methods was established over the ranges 1-50 μg mL-1 for AML and ATV in the HPLC method and in the range of 3-50 and 4-50 μg mL-1 for AML and ATV, respectively, in the CE method. The proposed methods were validated according to ICH guidelines. The methods were successfully applied to estimation of AML and ATV in combined tablets.

Palabras clave

  • atorvastatin
  • amlodipine
  • capillary zone electrophoresis
  • HPLC
  • stability
  • acidic degradation
Acceso abierto

Modulatory effects of rutin on the expression of cytochrome P450s and antioxidant enzymes in human hepatoma cells

Publicado en línea: 15 Oct 2016
Páginas: 491 - 502

Resumen

Abstract

Expression of a drug and xenobiotic metabolizing enzymes, cytochrome P450s (CYPs), and antioxidant enzymes can be modulated by various factors. The flavonoid rutin was investigated for its anti-carcinogen and protective effects as well as modulatory action on CYPs and phase II enzymes in human hepatocellular carcinoma cells. Rutin inhibited proliferation of HEPG2 cells in a dose-dependent manner with the IC50 value of 52.7 μmol L-1 and invasion of HEPG2 cells (21.6 %, p = 0.0018) and colony formation of those invaded cells (57.4 %, p < 0.0001). Rutin treatment also significantly increased early/late-stage apoptosis in HEPG2 cells (28.9 %, p < 0.001). Treatment by rutin significantly inhibited protein expressions of cytochrome P450-dependent CYP3A4 (75.3 %, p < 0.0001), elevated CYP1A1 enzymes (1.7-fold, p = 0.0084) and increased protein expressions of antioxidant and phase II reaction catalyzing enzymes, NQO1 (2.42-fold, p < 0.0001) and GSTP1 (2.03-fold, p < 0.0001). Besides, rutin treatment significantly inhibited mRNA expression of CYP3A4 (73.2 %, p=0.0014). Also, CYP1A1, NQO1 and GSTP1 mRNA expressions were significantly increased 2.77-fold (p = 0.029), 4.85- fold (p = 0.0051) and 9.84-fold (p < 0.0001), respectively.

Palabras clave

  • rutin
  • cytochrome P450s
  • phase II enzymes
  • cell proliferation
  • HEPG2
Acceso abierto

Ionophore-based potentiometric PVC membrane sensors for determination of phenobarbitone in pharmaceutical formulations

Publicado en línea: 15 Oct 2016
Páginas: 503 - 514

Resumen

Abstract

The fabrication and development of two polyvinyl chloride (PVC) membrane sensors for assaying phenobarbitone sodium are described. Sensors 1 and 2 were fabricated utilizing β- or γ-cyclodextrin as ionophore in the presence of tridodecylmethylammonium chloride as a membrane additive, and PVC and dioctyl phthalate as plasticizer. The analytical parameters of both sensors were evaluated according to the IUPAC guidelines. The proposed sensors showed rapid, stable anionic response (-59.1 and -62.0 mV per decade) over a relatively wide phenobarbitone concentration range (5.0 × 10-6-1 × 10-2 and 8 × 10-6-1 × 10-2 mol L-1) in the pH range of 9-11. The limit of detection was 3.5 × 10-6 and 7.0 × 10-6 mol L-1 for sensors 1 and 2, respectively. The fabricated sensors showed high selectivity for phenobarbitone over the investigated foreign species. An average recovery of 2.54 μg mL-1 phenobarbitone sodium was 97.4 and 101.1 %, while the mean relative standard deviation was 3.0 and 2.1 %, for sensors 1 and 2, respectively. The results acquired for determination of phenobarbitone in its dosage forms utilizing the proposed sensors are in good agreement with those obtained by the British Pharmacopoeial method.

Palabras clave

  • phenobarbitone sodium
  • membrane selective electrode
  • β-cyclodextrin
  • γ-cyclodextrin
  • PVC
  • potentiometry
Acceso abierto

A dual strategy to improve psychotic patients’ compliance using sustained release quetiapine oral disintegrating tablets

Publicado en línea: 15 Oct 2016
Páginas: 515 - 532

Resumen

Abstract

Quetiapine (QT) is a short acting atypical antipsychotic drug effective in schizophrenia and bipolar disorder. This study aims at designing a novel dosage form of sustained release taste-masked QT orally disintegrating tablets (ODTs) based on solid lipid micro-pellets (SLMPs). QT SLMPs were prepared using the hot melt extrusion technique and utilizing three lipid carriers: Compritol, Precirol and white beeswax either alone or in mixtures. They showed sustained QT release and a taste masking effect. The selected QT SLMP was further blended with an aqueous solution containing polyvinylpyrollidone (2.5 %), croscarmellose sodium (2 %) and mannitol (50 %); it was then lyophilized into ODT in a mass ratio of 1:2, respectively. ODTs containing QT SLMPs showed: average wetting time (40.92 s), average oral disintegration time (21.49 s), average hardness (16.85 N) and also imparted suitable viscosity to suspend pellets during the lyophilization process. In conclusion, lyophilization is a promising technique for the formulation of multiparticulate systems into ODTs.

Palabras clave

  • solid lipid micro pellets
  • multiparticulate
  • quetiapine
  • orally disintegrating tablets
Acceso abierto

Charge transfer interaction of organic p-acceptors with the anti-hyperuricemic drug allopurinol: Insights from IR, Raman, 1H NMR and 13C NMR spectroscopies

Publicado en línea: 15 Oct 2016
Páginas: 533 - 542

Resumen

Abstract

The topic of charge-transfer (CT) complexation of vital drugs has attracted considerable attention in recent years owing to their significant physical and chemical properties. In this study, CT complexes derived from the reaction of the anti-hyperuricemic drug allopurinol (Allop) with organic p-acceptors [(picric acid (PA), dichlorodicyanobenzoquinone (DDQ) and chloranil (CHL)] were prepared, isolated and characterized by a range of physicochemical methods, such as IR, Raman, 1H NMR and 13C NMR spectroscopy. The stoichiometry of the complexes was verified by elemental analysis. The results show that all complexes that were formed were based on a 1:1 stoichiometric ratio. This study suggests that the complexation of Allop with either the DDQ or CHL acceptor leads to a direct p®p* transition, whereas the molecules of Allop and PA are linked by intermolecular hydrogen- bonding interactions.

Palabras clave

  • allopurinol
  • p-acceptor
  • charge-transfer
  • proton- transfer
Acceso abierto

TLC determination of flavonoids from different cultivars of Allium cepa and Allium ascalonicum

Publicado en línea: 15 Oct 2016
Páginas: 543 - 554

Resumen

Abstract

This study comprises the optimization and validation of a new TLC method for determination of flavonols in the bulbs of seven cultivars of onions and shallots. Separation was performed on RP-18 plates with the solvent mixture tetrahydrofuran/water/formic acid (40+60+6, V/V/V) as a mobile phase. The method was evaluated for precision, linearity, LOD, LOQ, accuracy and robustness. Chromatographic analysis of the extracts revealed the presence of three main flavonols, quercetin, quercetin-4′-O-glucoside and quercetin-3,4′-O-diglucoside in the majority of analyzed cultivars. The content of flavonols in the analyzed extracts of onion bulbs varied from 123 (‘Exihibition’) to 1079 mg kg-1 fresh mass (fm) (‘Hybing’) in edible parts, and from 1727 (‘Hyline’) to 28949 mg kg-1 fm (‘Red Baron’) in outer scales. The bulbs of two shallot cultivars contained 209 (‘Ambition’) and 523 mg kg-1 fm (‘Matador’) of flavonols in edible parts and 5426 and 8916 mg kg-1 fm in outer scales, respectively.

Palabras clave

  • Allium cepa
  • Allium ascalonicum
  • cultivar varieties
  • flavonols
  • TLC
  • quantitative analysis
Acceso abierto

Preparation and in vivo evaluation of a gel-based nasal delivery system for risperidone

Publicado en línea: 15 Oct 2016
Páginas: 555 - 562

Resumen

Abstract

The aim of this study was to prepare a nasal gel of risperidone and to investigate the pharmacokinetics and relative bioavailability of the drug in rats. Compared with oral dosing, the risperidone nasal gel exhibited very fast absorption and high bioavailability. Maximal plasma concentration (cmax) and the time to reach cmax (tmax) were 15.2 μg mL-1 and 5 min for the nasal gel, 3.6 μg mL-1 and 30 min for the oral drug suspension, respectively. Pharmacokinetic parameters such as tmax′, cmax and AUC of oral and nasal routes were significantly different (p < 0.01). Relative bioavailability of the drug nasal preparation to the oral suspension was up to 1600.0 %. Further, the in vitro effect of the risperidone nasal gel on nasal mucociliary movement was also investigated using a toad palate model. The risperidone nasal formulation showed mild ciliotoxicity, but the adverse effect was temporary and reversible.

Palabras clave

  • risperidone
  • nasal gel
  • formulation
  • pharmacokinetics
  • bioavailability
  • ciliotoxicity
Acceso abierto

Pharmacokinetic evaluation of the interaction between oral kaempferol and ethanol in rats

Publicado en línea: 15 Oct 2016
Páginas: 563 - 568

Resumen

Abstract

This study was aimed at investigating the effect of ethanol on oral bioavailability of kaempferol in rats, namely, at disclosing their possible interaction. Kaempferol (100 or 250 mg kg-1 bm) was administered to the rats by oral gavage with or without ethanol (600 mg kg-1 bm) co-administration. Intravenous administration (10 and 25 mg kg-1 bm) of kaempferol was used to determine the bioavailability. The concentration of kaempferol in plasma was estimated by ultra high performance liquid chromatography. During coadministration, a significant increase of the area under the plasma concentration-time curve as well as the peak concentration were observed, along with a dramatic decrease in total body clearance. Consequently, the bioavailability of kaempferol in oral control groups was 3.1 % (100 mg kg-1 bm) and 2.1 % (250 mg kg-1 bm). The first was increased by 4.3 % and the other by 2.8 % during ethanol co-administration. Increased permeability of cell membrane and ethanolkaempferol interactions on CYP450 enzymes may enhance the oral bioavailability of kaempferol in rats.

Palabras clave

  • kaempferol
  • bioavailability
  • pharmacokinetics
  • ethanol
  • cytochrome P450s

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