vol. 30, no. 07http://sedici.unlp.edu.ar:80/handle/10915/2402024-03-29T14:46:36Z2024-03-29T14:46:36ZVibrational spectra of tris(maltolato)gallium(III): a new interesting antitumoral agentWagner, Claudia C.Parajón Costa, Beatriz S.Barán, Enrique Joséhttp://sedici.unlp.edu.ar:80/handle/10915/83232019-07-04T04:02:45Z2011-01-01T00:00:00ZComunicacion
Latin American Journal of Pharmacy; vol. 30, no. 7
The FTIR and FT-Raman spectra of the gallium(III) complex of 3-hydroxy-2-methyl-4-pyrone (maltol), tris(maltolato)gallium(III), a new very promising antitumoral drug, were recorded and briefly discussed by comparison with the spectra of uncoordinated maltol and with some related species.
2011-01-01T00:00:00ZThe FTIR and FT-Raman spectra of the gallium(III) complex of 3-hydroxy-2-methyl-4-pyrone (maltol), tris(maltolato)gallium(III), a new very promising antitumoral drug, were recorded and briefly discussed by comparison with the spectra of uncoordinated maltol and with some related species.Preparation, crystal structure and prodrug studies of genistein benzensulfonatePeng, YouGan, Li- JunDeng, Ze-yuanhttp://sedici.unlp.edu.ar:80/handle/10915/83222019-07-04T04:02:43Z2011-01-01T00:00:00ZComunicacion
Latin American Journal of Pharmacy; vol. 30, no. 7
4'-ethyl-7-phenylsulfonylgenistein (EPG, 3), a potential prodrug for genistein (1), was synthesized in high yield and its crystal structure was reported firstly. It possesses better physical and chemical properties such as solubility, lipid/water partition coefficient, LogP, and hydrolysis kinetics than its original form. The LogP value (2.07) and the half-life of the hydrolysis value (13.4 h) show that its oral bioavailability is possibly improved evidently compared with that of genistein. These results indicate that EPG can be considered a potential prodrug for genistein.
2011-01-01T00:00:00Z4'-ethyl-7-phenylsulfonylgenistein (EPG, 3), a potential prodrug for genistein (1), was synthesized in high yield and its crystal structure was reported firstly. It possesses better physical and chemical properties such as solubility, lipid/water partition coefficient, LogP, and hydrolysis kinetics than its original form. The LogP value (2.07) and the half-life of the hydrolysis value (13.4 h) show that its oral bioavailability is possibly improved evidently compared with that of genistein. These results indicate that EPG can be considered a potential prodrug for genistein.Enantiomeric separation and determination of stereospecific drug release from marketed racemic omeprazole products by chiral HPLCSomagoni, Jagan M.Katakam, Vinay K.Reddy, SunilGande, SureshManda, SarangapaniYamsani, Madhusudan R.http://sedici.unlp.edu.ar:80/handle/10915/83212019-07-04T04:02:41Z2011-01-01T00:00:00ZComunicacion
Latin American Journal of Pharmacy; vol. 30, no. 7
The objective of carrying out this research work was to investigate the effect of chirality on stereospecific dissolution of omeprazole enantiomers from various marketed racemic omeprazole products. Omeprazole is used for the treatment of gastro-duodenal ulcers and symptomatic gastro-oesophageal reflux. Dissolution of various marketed products was performed using USP type I apparatus in 0.1 N HCl for 2 h and in pH 6.8 phosphate buffer for 1 h at 100 rpm. The separation of enantiomers was done using a chiral HPLC method on CHIRAL AGP column (100 x 4.6 mm i.d.). The wavelength for UV detection was set at 210 nm. The mobile phase was 10 mM phosphate buffer with 5 % acetonitrile adjusted to pH 6.5 at a flow rate of 0.9 ml min-1 with an injector valve fitted to a 50 μL volume sample loop. The retention times for R and S enantiomers of omeprazole were 5 and 7.5 min, respectively. The dissolution of S enantiomer of Ocid-20 and Omee was found to be significantly more compared to their R enantiomer at 5 and 10 min dissolution time points after which there was no stereospecific discrimination in the dissolution. From the S/R ratios of different racemic omeprazole marketed products it was concluded that at 5 and 10 min dissolution time points there was a stereospecific drug release between the S and R enantiomers with the brands Ocid-20 and Omee (p < 0.05) but no stereospecificity was observed with Omez-20 (p > 0.05).
2011-01-01T00:00:00ZThe objective of carrying out this research work was to investigate the effect of chirality on stereospecific dissolution of omeprazole enantiomers from various marketed racemic omeprazole products. Omeprazole is used for the treatment of gastro-duodenal ulcers and symptomatic gastro-oesophageal reflux. Dissolution of various marketed products was performed using USP type I apparatus in 0.1 N HCl for 2 h and in pH 6.8 phosphate buffer for 1 h at 100 rpm. The separation of enantiomers was done using a chiral HPLC method on CHIRAL AGP column (100 x 4.6 mm i.d.). The wavelength for UV detection was set at 210 nm. The mobile phase was 10 mM phosphate buffer with 5 % acetonitrile adjusted to pH 6.5 at a flow rate of 0.9 ml min-1 with an injector valve fitted to a 50 μL volume sample loop. The retention times for R and S enantiomers of omeprazole were 5 and 7.5 min, respectively. The dissolution of S enantiomer of Ocid-20 and Omee was found to be significantly more compared to their R enantiomer at 5 and 10 min dissolution time points after which there was no stereospecific discrimination in the dissolution. From the S/R ratios of different racemic omeprazole marketed products it was concluded that at 5 and 10 min dissolution time points there was a stereospecific drug release between the S and R enantiomers with the brands Ocid-20 and Omee (p < 0.05) but no stereospecificity was observed with Omez-20 (p > 0.05).Electroanalytical characterization of 4-nerolidylcatechol and its derivativesLeal, Ana Flávia V. B.Rezende, Kênnia R.Gil, Éric S.http://sedici.unlp.edu.ar:80/handle/10915/83202019-07-04T04:02:39Z2011-01-01T00:00:00ZComunicacion
Latin American Journal of Pharmacy; vol. 30, no. 7
4-Nerolidylcatechol (4-NRC) is the most abundant antioxidant product isolated from the roots of Pothomorphe umbellata (L) Miq. It displays important sunscreen protection and other pharmacological properties comprising analgesic, anti-inflammatory and antimicrobial activity. However, low water solubility and chemical instability has limited its use and analysis. Therefore, chemical modifications such as silylated derivatives and inclusion complexes have been proposed. Regarding antioxidants, electrochemical investigation techniques are important tools in comprehensive characterization of phenol molecules, showing higher selectivity than spectroscopic methods. In the present study, the 4-NRC and its derivatives are characterizated by voltammetric analysis in order to support physicochemical properties of 4-NRC inclusion-complex and catechol silylation products. It is observed that in both liquid- or solid-state the redox process of the 4-NRC is non-reversible and occurs in two stages, seen as two anodic peaks, respectively, at 0.75 and 1.12 V. The electrochemical techniques showed to be also a powerful tool to evaluate the efficiency of chemical modification on electroactive groups.
2011-01-01T00:00:00Z4-Nerolidylcatechol (4-NRC) is the most abundant antioxidant product isolated from the roots of Pothomorphe umbellata (L) Miq. It displays important sunscreen protection and other pharmacological properties comprising analgesic, anti-inflammatory and antimicrobial activity. However, low water solubility and chemical instability has limited its use and analysis. Therefore, chemical modifications such as silylated derivatives and inclusion complexes have been proposed. Regarding antioxidants, electrochemical investigation techniques are important tools in comprehensive characterization of phenol molecules, showing higher selectivity than spectroscopic methods. In the present study, the 4-NRC and its derivatives are characterizated by voltammetric analysis in order to support physicochemical properties of 4-NRC inclusion-complex and catechol silylation products. It is observed that in both liquid- or solid-state the redox process of the 4-NRC is non-reversible and occurs in two stages, seen as two anodic peaks, respectively, at 0.75 and 1.12 V. The electrochemical techniques showed to be also a powerful tool to evaluate the efficiency of chemical modification on electroactive groups.Quality control of radiopharmaceutical 99mTc-MAG3Guimarães, Tiago TeixeiraBordim, AugustoSouza Albernaz, Marta deSantos Oliveira, Ralphhttp://sedici.unlp.edu.ar:80/handle/10915/83192019-07-04T04:02:37Z2011-01-01T00:00:00ZComunicacion
Latin American Journal of Pharmacy; vol. 30, no. 7
The use of mercaptoacetyltriglycine (MAG3) as a radiopharmaceutical is well known. The MAG3 is formerly called Technetium-99m (99mTc) mercaptoacetyltriglycine and it is the standard radiopharmaceuticals for renal scintilography . In this study we propose three methodologies based on the use of a new stationary phase (paper Hahnemuhle) and a mobile phase. The results showed that all the three conditions were very close, and for this reason can be interchangeable.
2011-01-01T00:00:00ZThe use of mercaptoacetyltriglycine (MAG3) as a radiopharmaceutical is well known. The MAG3 is formerly called Technetium-99m (99mTc) mercaptoacetyltriglycine and it is the standard radiopharmaceuticals for renal scintilography . In this study we propose three methodologies based on the use of a new stationary phase (paper Hahnemuhle) and a mobile phase. The results showed that all the three conditions were very close, and for this reason can be interchangeable.High-performance liquid chromatographic determination of fluconazole in plasma and its application to a bioequivalence studySousa, Carlos E.M.Bedor, Danilo C. G.Sampaio Fhilo, L. C. A.Silva, T. M.Bonifácio, F. N.Albuquerque, Miracy M.Santana, Davi P.http://sedici.unlp.edu.ar:80/handle/10915/83182019-07-04T04:02:34Z2011-01-01T00:00:00ZComunicacion
Latin American Journal of Pharmacy; vol. 30, no. 7
A sensitive and accurate HPLC-UV method for the quantification of fluconazole (FNZ) in human plasma has been developed. The sample was prepared by liquid–liquid extraction (LLE) of FNZ from plasma using ethyl acetate. Nevirapine (NVP) was used as internal standard. The chromatographic retention times of FNZ and NVP were 3.4 and 5.7 min, respectively. The lower limit of quantitation (LLOQ) was 0.5 μg/mL, and no interferences were detected in the chromatograms. The HPLC-UV method was validated by evaluating its intra-day and inter-day precisions and accuracies in a linear concentration range between 0.5 and 8.0 μg/mL. The method was developed, validated and successfully applied to bioequivalence studies involving the oral administration of a single 150 mg FNZ capsules in healthy Brazilian male volunteers.
2011-01-01T00:00:00ZA sensitive and accurate HPLC-UV method for the quantification of fluconazole (FNZ) in human plasma has been developed. The sample was prepared by liquid–liquid extraction (LLE) of FNZ from plasma using ethyl acetate. Nevirapine (NVP) was used as internal standard. The chromatographic retention times of FNZ and NVP were 3.4 and 5.7 min, respectively. The lower limit of quantitation (LLOQ) was 0.5 μg/mL, and no interferences were detected in the chromatograms. The HPLC-UV method was validated by evaluating its intra-day and inter-day precisions and accuracies in a linear concentration range between 0.5 and 8.0 μg/mL. The method was developed, validated and successfully applied to bioequivalence studies involving the oral administration of a single 150 mg FNZ capsules in healthy Brazilian male volunteers.Synthesis and in vitro antimicrobial activity of novel hydrazide-hydrazone derivatives of dodecanoic acidKumar, MaheshJain, SandeepDeep, AakashPhogat, Priyankahttp://sedici.unlp.edu.ar:80/handle/10915/83172019-07-04T04:02:33Z2011-01-01T00:00:00ZComunicacion
Latin American Journal of Pharmacy; vol. 30, no. 7
Six new dodecanoic acid hydrazide-hydrazones (compounds 4a–f), unsubstituted or carrying hydroxy, methoxy, nitro and chloro groups on the benzene ring, were synthesized and tested, in vitro, for their antimicrobial activity against two Gram negative bacteria strains (Escherichia coli and Pseudomonas aeruginosa) and two Gram positive bacteria strains (Bacillus subtilis and Staphylococcus aureus) and two fungal strains (Candida albicans and Aspergillus niger). The microbial screening results indicated that compounds having chloro and nitro substituents were the most active ones. These hydrazone derivatives were characterized by CHN analysis, IR, and 1H NMR spectral data. All newly synthesized compounds exhibited promising results.
2011-01-01T00:00:00ZSix new dodecanoic acid hydrazide-hydrazones (compounds 4a–f), unsubstituted or carrying hydroxy, methoxy, nitro and chloro groups on the benzene ring, were synthesized and tested, in vitro, for their antimicrobial activity against two Gram negative bacteria strains (Escherichia coli and Pseudomonas aeruginosa) and two Gram positive bacteria strains (Bacillus subtilis and Staphylococcus aureus) and two fungal strains (Candida albicans and Aspergillus niger). The microbial screening results indicated that compounds having chloro and nitro substituents were the most active ones. These hydrazone derivatives were characterized by CHN analysis, IR, and 1H NMR spectral data. All newly synthesized compounds exhibited promising results.Administration of oral solid pharmaceutical forms through enteral feeding tubes at a university hospital in southern BrazilSantos, Luciana dosJacoby, ThalitaMartinbiancho, Jacqueline K.Almeida, Silvia H. deAyres, Márcio V.Santos, María Elisahttp://sedici.unlp.edu.ar:80/handle/10915/83162019-07-04T04:02:31Z2011-01-01T00:00:00ZComunicacion
Latin American Journal of Pharmacy; vol. 30, no. 7
Besides enteral tubes are used for administration of enteral feeding, they are also alternative ways to manage drugs in patients with impaired swallowing. When the drug is not available in the oral liquid form, the extemporaneous preparations from solid oral dosage forms (SODF) function as alternative means. This study aimed to analyze the standardized solid oral dosage forms at Hospital de Clínicas de Porto Alegre (HCPA) that are at risk of obstruction and pharmacokinetics alterations when administered via probe, and the feasibility of carrying out extemporaneous preparations. The SODF in the Selection of Medications were included. 222 medications - from which, 20.3 % were at risk of obstructing the probe, and 16.7 % could present pharmacokinetic changes – were assessed. It has been noted that it is possible to perform the oral extemporaneous preparation at 46 %, concerning the SODF surveyed. In order to avoid problems in the administration of medications through feeding tubes, this study promoted the development of an administration guide.
2011-01-01T00:00:00ZBesides enteral tubes are used for administration of enteral feeding, they are also alternative ways to manage drugs in patients with impaired swallowing. When the drug is not available in the oral liquid form, the extemporaneous preparations from solid oral dosage forms (SODF) function as alternative means. This study aimed to analyze the standardized solid oral dosage forms at Hospital de Clínicas de Porto Alegre (HCPA) that are at risk of obstruction and pharmacokinetics alterations when administered via probe, and the feasibility of carrying out extemporaneous preparations. The SODF in the Selection of Medications were included. 222 medications - from which, 20.3 % were at risk of obstructing the probe, and 16.7 % could present pharmacokinetic changes – were assessed. It has been noted that it is possible to perform the oral extemporaneous preparation at 46 %, concerning the SODF surveyed. In order to avoid problems in the administration of medications through feeding tubes, this study promoted the development of an administration guide.Preparation, characterization and in vitro evaluation of stable mucoadhesive intranasal microsphere of L-DopaGhodke, Dhananjay S.Naikwade, Nilofar S.http://sedici.unlp.edu.ar:80/handle/10915/83152019-07-04T04:02:29Z2011-01-01T00:00:00ZArticulo
Latin American Journal of Pharmacy; vol. 30, no. 7
Novel stable mucoadhesive chitosan microspheres were developed to explore the possibility of nasal delivery of L-dopa to avoid first pass metabolism and to improve therapeutic efficiency in treating the symptoms of parkinsonism. The mucoadhesive microspheres were prepared by spray drying using 23 full factorial design with inlet temperature (A), liquid feed flow rate (B), and drug to polymer concentration (C) as independent variable. Then microspheres were characterized in terms of morphology (Scanning Electron Microscopy, SEM), drug content, production yield, particle size and thermal behavior (Differential Scanning Calorimetry (DSC) and mucoadhesion test. In vitro drug release studies were performed in simulated nasal electrolyte fluid. Factorial design results indicated that main effect of factor A alone has significant effect on moisture content whereas AC had effect on moisture content. Microspheres containing moisture below 11 % were found to be stable. Treatment of in vitro data to mathematical model of different kinetic equations indicated that drug release from the microspheres was best characterized by the Korsmeyer-Peppas model. The results of DSC studies revealed molecular amorphous dispersion of Ldopa into the chitosan microspheres. Stability studies showed that microspheres were stable over a period of three months.
2011-01-01T00:00:00ZNovel stable mucoadhesive chitosan microspheres were developed to explore the possibility of nasal delivery of L-dopa to avoid first pass metabolism and to improve therapeutic efficiency in treating the symptoms of parkinsonism. The mucoadhesive microspheres were prepared by spray drying using 23 full factorial design with inlet temperature (A), liquid feed flow rate (B), and drug to polymer concentration (C) as independent variable. Then microspheres were characterized in terms of morphology (Scanning Electron Microscopy, SEM), drug content, production yield, particle size and thermal behavior (Differential Scanning Calorimetry (DSC) and mucoadhesion test. In vitro drug release studies were performed in simulated nasal electrolyte fluid. Factorial design results indicated that main effect of factor A alone has significant effect on moisture content whereas AC had effect on moisture content. Microspheres containing moisture below 11 % were found to be stable. Treatment of in vitro data to mathematical model of different kinetic equations indicated that drug release from the microspheres was best characterized by the Korsmeyer-Peppas model. The results of DSC studies revealed molecular amorphous dispersion of Ldopa into the chitosan microspheres. Stability studies showed that microspheres were stable over a period of three months.Inhibition of fluconazole in vitro antifungal activity in formulations containing propylene glycolSalerno, ClaudiaCarlucci, Adriana M.Chiappetta, Diego A.Bregni, Carloshttp://sedici.unlp.edu.ar:80/handle/10915/83142019-07-04T04:02:25Z2011-01-01T00:00:00ZArticulo
Latin American Journal of Pharmacy; vol. 30, no. 7
Inhibition action of propylene glycol (PG) on the antifungal activity of fluconazole has been investigated. PG was used as cosolvent and penetration enhancer in different solutions and topical dosage forms. The interaction was analyzed by comparing with Transcutol P® (TCL), another cosolvent and penetration enhancer. Solubility of the drug was evaluated in aqueous solutions containing PG or TCL and the crystallized drug was studied by both DSC and FTIR. Solutions of the drug in the solvents were studied by FTIR and UV spectroscopy. Antifungal activity was determined for solutions with several concentrations of PG/TCL and in dosage forms with PG 10 %. Candida albicans was used as a model fungus and a procedure with standardized inoculum concentration was used. Results showed lower antifungal activity of fluconazole solutions and topical dosage forms when propylene glycol is included. Although crystallization is faster in PG solutions, solubility proved not to be the cause, but changes in FTIR spectra suggested that different hydrogen bond formation could explain the decrease in activity.
2011-01-01T00:00:00ZInhibition action of propylene glycol (PG) on the antifungal activity of fluconazole has been investigated. PG was used as cosolvent and penetration enhancer in different solutions and topical dosage forms. The interaction was analyzed by comparing with Transcutol P® (TCL), another cosolvent and penetration enhancer. Solubility of the drug was evaluated in aqueous solutions containing PG or TCL and the crystallized drug was studied by both DSC and FTIR. Solutions of the drug in the solvents were studied by FTIR and UV spectroscopy. Antifungal activity was determined for solutions with several concentrations of PG/TCL and in dosage forms with PG 10 %. Candida albicans was used as a model fungus and a procedure with standardized inoculum concentration was used. Results showed lower antifungal activity of fluconazole solutions and topical dosage forms when propylene glycol is included. Although crystallization is faster in PG solutions, solubility proved not to be the cause, but changes in FTIR spectra suggested that different hydrogen bond formation could explain the decrease in activity.Factors associated with pharmaceutical expenditures by elderly people in Belo Horizonte, BrazilLima, Marina G.Ribeiro, AndréiaRozenfeld, SuelyKlein, Carlos H.Acurcio, Francisco de A.http://sedici.unlp.edu.ar:80/handle/10915/83132019-07-03T20:03:48Z2011-01-01T00:00:00ZArticulo
Latin American Journal of Pharmacy; vol. 30, no. 7
A study was carried out to analyze the factors associated with drug spending by the elderly population in Belo Horizonte, Brazil. Data were obtained using a household survey of 667 communitydwelling persons aged 60 years or older conducted in 2003. A Tobit multivariate model was used to analyze factors associated with pharmaceutical expenditures. Data from 590 respondents were used for the analysis. The mean out-of-pocket pharmaceutical expenditure was US$ 38.91. Better sociodemographic conditions, worse health conditions and greater use of health services were associated with out-of-pocket pharmaceutical expenditures by elderly people in Belo Horizonte. The out-of-pocket pharmaceutical expenditures by elderly people were high considering their income level. The factors that influence spending should be considered in the formulation of pharmaceutical policies that improve the health conditions of elderly people.
2011-01-01T00:00:00ZA study was carried out to analyze the factors associated with drug spending by the elderly population in Belo Horizonte, Brazil. Data were obtained using a household survey of 667 communitydwelling persons aged 60 years or older conducted in 2003. A Tobit multivariate model was used to analyze factors associated with pharmaceutical expenditures. Data from 590 respondents were used for the analysis. The mean out-of-pocket pharmaceutical expenditure was US$ 38.91. Better sociodemographic conditions, worse health conditions and greater use of health services were associated with out-of-pocket pharmaceutical expenditures by elderly people in Belo Horizonte. The out-of-pocket pharmaceutical expenditures by elderly people were high considering their income level. The factors that influence spending should be considered in the formulation of pharmaceutical policies that improve the health conditions of elderly people.Effects of nonionic surfactant lauryl alcohol ethoxylated on stratum corneum alternative model biomembranes evaluated by biophysical techniquesBaby, André R.Lacerda, Áurea C. L.Prestes, Paula S.Velasco, María Valéria R.Kawano, YoshioKaneko, Telma Maryhttp://sedici.unlp.edu.ar:80/handle/10915/83122019-07-03T20:03:46Z2011-01-01T00:00:00ZArticulo
Latin American Journal of Pharmacy; vol. 30, no. 7
The influence of the nonionic surfactant lauryl alcohol ethoxylate with 12 moles ethylene oxide (LAE-12OE) was evaluated on the Stratum corneum model biomembrane (SCMM) of shed snake skin (Bothrops jararaca and Spilotes pullatus) through the biophysical techniques Fourier transform Raman spectroscopy (FT-Raman) and Fourier transform infrared photoacoustic spectroscopy (PAS-FTIR). The surfactant was used in aqueous solutions above and below the critical micelle concentration (cmc), 50.0 and 0.21 g/L, respectively. The SCMM samples were pre-treated for periods of 8 h (whole SCMM) and for 12 h (SCMM after tape stripping procedure). The LAE-12OE did not promote increase in the hydration of the B. jararaca and S. pullatus SCMM but exhibited some action as far as lipid extraction.
2011-01-01T00:00:00ZThe influence of the nonionic surfactant lauryl alcohol ethoxylate with 12 moles ethylene oxide (LAE-12OE) was evaluated on the Stratum corneum model biomembrane (SCMM) of shed snake skin (Bothrops jararaca and Spilotes pullatus) through the biophysical techniques Fourier transform Raman spectroscopy (FT-Raman) and Fourier transform infrared photoacoustic spectroscopy (PAS-FTIR). The surfactant was used in aqueous solutions above and below the critical micelle concentration (cmc), 50.0 and 0.21 g/L, respectively. The SCMM samples were pre-treated for periods of 8 h (whole SCMM) and for 12 h (SCMM after tape stripping procedure). The LAE-12OE did not promote increase in the hydration of the B. jararaca and S. pullatus SCMM but exhibited some action as far as lipid extraction.Development of glutaraldehyde cross-linked metronidazole loaded chitosan microcapsules: analysis of dissolution data using DD-SolverMurtaza, Ghulamhttp://sedici.unlp.edu.ar:80/handle/10915/83112019-07-03T20:03:44Z2011-01-01T00:00:00ZArticulo
Latin American Journal of Pharmacy; vol. 30, no. 7
The aim of this study was to develop sustained release formulation for improving bioavailability of metronidazole designing metronidazole loaded chitosan microcapsules (MLCM) using coacervation technique. Two solutions with different pH nature i.e. chitosan solution in 5 % glacial acetic acid containing metronidazole and 2 M NaOH solution were employed for the induction of coacervation. Glutaraldehyde was used as cross-linking agent. Different MLCM formulations were fabricated by varying chitosan and glutaraldehyde concentrations. Dissolution data was evaluated using new software, DDSolver. Microcapsules were discrete, brown, spherical and porous. Microcapsule size range was 343.6 ± 8.9 μm – 401.9 ± 9.6 μm and the entrapment efficiency ranged from 45.2 ± 6.4 – 64.3 ± 5.7 for all formulations. The F6 formulation with drug/polymer ratio 1:2 (w/w) was optimum regarding entrapment efficiency (64.3 ± 5.7 %), flow characteristics (Hausner’s ratio = 1.3-1.5) and drug release properties, in all cases. The kinetic analysis of dissolution data confirmed diffusion controlled release of metronidazole from its microcapsules. From the results, it can be concluded that metronidazole can be successfully microencapsulated into the chitosan shells by coacervation and is influenced significantly by the quantity of chitosan and glutaraldehyde employed.
2011-01-01T00:00:00ZThe aim of this study was to develop sustained release formulation for improving bioavailability of metronidazole designing metronidazole loaded chitosan microcapsules (MLCM) using coacervation technique. Two solutions with different pH nature i.e. chitosan solution in 5 % glacial acetic acid containing metronidazole and 2 M NaOH solution were employed for the induction of coacervation. Glutaraldehyde was used as cross-linking agent. Different MLCM formulations were fabricated by varying chitosan and glutaraldehyde concentrations. Dissolution data was evaluated using new software, DDSolver. Microcapsules were discrete, brown, spherical and porous. Microcapsule size range was 343.6 ± 8.9 μm – 401.9 ± 9.6 μm and the entrapment efficiency ranged from 45.2 ± 6.4 – 64.3 ± 5.7 for all formulations. The F6 formulation with drug/polymer ratio 1:2 (w/w) was optimum regarding entrapment efficiency (64.3 ± 5.7 %), flow characteristics (Hausner’s ratio = 1.3-1.5) and drug release properties, in all cases. The kinetic analysis of dissolution data confirmed diffusion controlled release of metronidazole from its microcapsules. From the results, it can be concluded that metronidazole can be successfully microencapsulated into the chitosan shells by coacervation and is influenced significantly by the quantity of chitosan and glutaraldehyde employed.Preparation and characterization of spherical agglomerates of piroxicamDixit, MuditKulkarni, Parthasarathi K.http://sedici.unlp.edu.ar:80/handle/10915/83102019-07-03T20:03:44Z2011-01-01T00:00:00ZArticulo
Latin American Journal of Pharmacy; vol. 30, no. 7
The purpose of the present study was to prepare spherical agglomerates (SA) of piroxicam by solvent change method. Crystallization medium used for spherical agglomerates of piroxicam consisted of DMF:water and chloroform. The presence of solvents residual in SA was determined by gas chromatography and were particles were characterized by DSC, FT-IR, XRD and SEM. The respective solubility study and dissolution behavior studies were carried out. The samples were stored in stability chamber to investigate their physical stabilities. Solvents residuals in SA were found to be within the limits and exhibited decreased crystallinity of piroxicam in SA than pure piroxicam. The solubility and dissolution of the spherical agglomerates was improved compared with pure piroxicam and recrystallized sample. In stability test, the release profile of the spherical agglomeration was almost unchanged as compared with the freshly prepared spherical agglomeration stored at 20 °C and 45 % relative humidity for 90 days. Hence this technique can be used to obtain modified drug raw material for formulation of tablets of piroxicam by direct compression with directly compressible tablet excipients.
2011-01-01T00:00:00ZThe purpose of the present study was to prepare spherical agglomerates (SA) of piroxicam by solvent change method. Crystallization medium used for spherical agglomerates of piroxicam consisted of DMF:water and chloroform. The presence of solvents residual in SA was determined by gas chromatography and were particles were characterized by DSC, FT-IR, XRD and SEM. The respective solubility study and dissolution behavior studies were carried out. The samples were stored in stability chamber to investigate their physical stabilities. Solvents residuals in SA were found to be within the limits and exhibited decreased crystallinity of piroxicam in SA than pure piroxicam. The solubility and dissolution of the spherical agglomerates was improved compared with pure piroxicam and recrystallized sample. In stability test, the release profile of the spherical agglomeration was almost unchanged as compared with the freshly prepared spherical agglomeration stored at 20 °C and 45 % relative humidity for 90 days. Hence this technique can be used to obtain modified drug raw material for formulation of tablets of piroxicam by direct compression with directly compressible tablet excipients.Effect of total flavones of buckwheat flowers and leaves on protein tyrosine phosphatase 1B expression in type 2 diabetic ratsGou, Xiang- BoHan, Shu-YingXu, Jing-ManYu, HongChu, Jin-XiuWang, Zhi- LuBai, JingCao, Fu-YuanHan, Tinghttp://sedici.unlp.edu.ar:80/handle/10915/83092019-07-03T20:03:43Z2011-01-01T00:00:00ZArticulo
Latin American Journal of Pharmacy; vol. 30, no. 7
The total flavone content was obtained from flowers and leaf of buckwheat (Fagopyrum esculentum Moench) by heating reflux method. The effects of the total flavone extract on the protein tyrosine phosphatase 1B (PTP1B) expression in type 2 diabetic rats were evaluated by immunofluorescence, western blotting and real-time quantitative PCR. The results suggested that the total flavone fraction from buckwheat flowers and leaves can significantly decrease the PTP1B expression in liver.
2011-01-01T00:00:00ZThe total flavone content was obtained from flowers and leaf of buckwheat (Fagopyrum esculentum Moench) by heating reflux method. The effects of the total flavone extract on the protein tyrosine phosphatase 1B (PTP1B) expression in type 2 diabetic rats were evaluated by immunofluorescence, western blotting and real-time quantitative PCR. The results suggested that the total flavone fraction from buckwheat flowers and leaves can significantly decrease the PTP1B expression in liver.Determination of diphenhydramine hydrochloride in rabbit plasma by LC-MS/MS and its application to a pharmacokinetic studyMa JiansheZhang, MeilingShentu, YangpingZhang, YuqingFan, XiaofangGong, Yongshenghttp://sedici.unlp.edu.ar:80/handle/10915/83082019-07-03T20:03:40Z2011-01-01T00:00:00ZArticulo
Latin American Journal of Pharmacy; vol. 30, no. 7
A sensitive and selective liquid chromatography tandem mass spectrometry (LC-MS/MS) method for determination of diphenhydramine hydrochloride in rabbit plasma was developed and validated. After addition of triazolam as internal standard (IS), protein precipitation by acetonitrile was used as sample preparation. Chromatographic separation was achieved on a Zorbax SB-C18 (2.1 mm × 50 mm, 3.5 μm) column with acetonitrile-0.1 % formic acid as mobile phase with gradient elution. Electrospray ionization (ESI) source was applied and operated in positive ion mode; multiple reaction monitoring (MRM) mode was used to quantification using target fragment ions m/z 255.8 → 166.6 for diphenhydramine hydrochloride and m/z 342.9 → 308.0 for the IS. Calibration plots were linear over the range of 5- 200 ng/mL for diphenhydramine hydrochloride in rabbit plasma. Lower limit of quantitation (LLOQ) for diphenhydramine hydrochloride was 5 ng/mL. RSD of intra-day and inter-day precisions were both less than 10 %. This developed method is successfully used in pharmacokinetic study of diphenhydramine hydrochloride in rabbit.
2011-01-01T00:00:00ZA sensitive and selective liquid chromatography tandem mass spectrometry (LC-MS/MS) method for determination of diphenhydramine hydrochloride in rabbit plasma was developed and validated. After addition of triazolam as internal standard (IS), protein precipitation by acetonitrile was used as sample preparation. Chromatographic separation was achieved on a Zorbax SB-C18 (2.1 mm × 50 mm, 3.5 μm) column with acetonitrile-0.1 % formic acid as mobile phase with gradient elution. Electrospray ionization (ESI) source was applied and operated in positive ion mode; multiple reaction monitoring (MRM) mode was used to quantification using target fragment ions m/z 255.8 → 166.6 for diphenhydramine hydrochloride and m/z 342.9 → 308.0 for the IS. Calibration plots were linear over the range of 5- 200 ng/mL for diphenhydramine hydrochloride in rabbit plasma. Lower limit of quantitation (LLOQ) for diphenhydramine hydrochloride was 5 ng/mL. RSD of intra-day and inter-day precisions were both less than 10 %. This developed method is successfully used in pharmacokinetic study of diphenhydramine hydrochloride in rabbit.Accumulation and distribution of diterpenic acids in leaves of Montanoa tomentosaRobles Zepeda, Ramón E.Lozoya Gloria, EdmundoLópez, Mercedes G.Molina Torres, Jorgehttp://sedici.unlp.edu.ar:80/handle/10915/83072019-07-03T20:03:37Z2011-01-01T00:00:00ZArticulo
Latin American Journal of Pharmacy; vol. 30, no. 7
Montanoa tomentosa has been used for at least last five centuries in traditional medicine in Mexico as a remedy for reproductive impairments. The accumulation of diterpenic acids in M. tomentosa leaves was determined. Using Scanning Electron Microscopy, the type and distribution of glandular trichomes (GTs) was observed on the abaxial and adaxial sides of leaves. GTs and non-glandular trichomes (NGTs) were observed on leaf surface, but the latter are confined to the leaves abaxial side. On the adaxial surface, only non-glandular trichomes were observed. Accumulation in GTs and leaf lamina of kaurenoic (KA) and grandiflorenic (GFA) acids was determined by Gas Chromatography coupled to an Electron Impact Mass Spectrometric Detector (GC/EI-MSD). GC-MSD analysis indicated that GTs accumulated KA and GFA, with KA accumulation being at a higher level than GFA in these structures. Attention on GFA and KA is due to their importance as plant growth regulator precursors with potential pharmacological applications.
2011-01-01T00:00:00ZMontanoa tomentosa has been used for at least last five centuries in traditional medicine in Mexico as a remedy for reproductive impairments. The accumulation of diterpenic acids in M. tomentosa leaves was determined. Using Scanning Electron Microscopy, the type and distribution of glandular trichomes (GTs) was observed on the abaxial and adaxial sides of leaves. GTs and non-glandular trichomes (NGTs) were observed on leaf surface, but the latter are confined to the leaves abaxial side. On the adaxial surface, only non-glandular trichomes were observed. Accumulation in GTs and leaf lamina of kaurenoic (KA) and grandiflorenic (GFA) acids was determined by Gas Chromatography coupled to an Electron Impact Mass Spectrometric Detector (GC/EI-MSD). GC-MSD analysis indicated that GTs accumulated KA and GFA, with KA accumulation being at a higher level than GFA in these structures. Attention on GFA and KA is due to their importance as plant growth regulator precursors with potential pharmacological applications.Optimization and validation of the quantitative assay of flavonoids in Achyrocline satureioides and A. flaccidaRetta, DaianaLópez, Paula G.Gattuso, MarthaGattuso, SusanaFilip, RosanaFerraro, Graciela EsterBandoni, Arnaldo L.http://sedici.unlp.edu.ar:80/handle/10915/83062019-07-03T20:03:31Z2011-01-01T00:00:00ZArticulo
Latin American Journal of Pharmacy; vol. 30, no. 7
Several populations of Achyrocline satureioides and Achyrocline flaccida from Argentina, two aromatic herbal species widely used in traditional medicine in South America and both known as marcela, were analyzed. The aims of this work were to evaluate the amounts of flavonoids that characterize these species in this country and provide a quantitative assay to be included in the monograph of marcela for future Argentine Pharmacopoeia editions. The extraction method and analysis by HPLC of the main flavonoids, quercetin and 3-O-methylquercetin, were optimized. The validation parameters of the method were determined. The analysis of the different parts of these plants was carried out thereafter. Inflorescences were the parts displaying the highest content of such flavonoids. It was found that A. flaccida had a slightly higher content of flavonoids than A. satureioides (1.2 ± 0.4 % of quercetin, 0.8 ± 0.3 % of 3-Omethylquercetin; 0.8 ± 0.2 % of quercetin and 0.7 ± 0.5 % of 3-O-methylquercetin, respectively).
2011-01-01T00:00:00ZSeveral populations of Achyrocline satureioides and Achyrocline flaccida from Argentina, two aromatic herbal species widely used in traditional medicine in South America and both known as marcela, were analyzed. The aims of this work were to evaluate the amounts of flavonoids that characterize these species in this country and provide a quantitative assay to be included in the monograph of marcela for future Argentine Pharmacopoeia editions. The extraction method and analysis by HPLC of the main flavonoids, quercetin and 3-O-methylquercetin, were optimized. The validation parameters of the method were determined. The analysis of the different parts of these plants was carried out thereafter. Inflorescences were the parts displaying the highest content of such flavonoids. It was found that A. flaccida had a slightly higher content of flavonoids than A. satureioides (1.2 ± 0.4 % of quercetin, 0.8 ± 0.3 % of 3-Omethylquercetin; 0.8 ± 0.2 % of quercetin and 0.7 ± 0.5 % of 3-O-methylquercetin, respectively).Synthesis and biological activities of novel danshensu amide derivatives as anti-myocardial ischemia agentsWang, TingfangShu, JingjingZheng, LipingXiong, LiyanWang, JingJin, LeiWu, QiuyeZou, HaoZhang, Chuanhttp://sedici.unlp.edu.ar:80/handle/10915/83052019-07-03T20:03:31Z2011-01-01T00:00:00ZArticulo
Latin American Journal of Pharmacy; vol. 30, no. 7
A series of novel danshensu amide derivatives were synthesized, and the protective effects of all the compounds on rat myocardial cell lines H9C2 by hypoxia were investigated. The results showed that all the seven compounds could significantly increased cell viability compared with hypoxia group. Among these compounds, 3-(3,4-dimethoxyphenyl)-2-hydroxy-N-propylpropanamide (6) exhibited good activities, with cell viability reached 94.2 % compared to the normal. The novel danshensu amide derivatives, possessing an additional lipophilic alkyl chain showed a good lipophilicity.
2011-01-01T00:00:00ZA series of novel danshensu amide derivatives were synthesized, and the protective effects of all the compounds on rat myocardial cell lines H9C2 by hypoxia were investigated. The results showed that all the seven compounds could significantly increased cell viability compared with hypoxia group. Among these compounds, 3-(3,4-dimethoxyphenyl)-2-hydroxy-N-propylpropanamide (6) exhibited good activities, with cell viability reached 94.2 % compared to the normal. The novel danshensu amide derivatives, possessing an additional lipophilic alkyl chain showed a good lipophilicity.Association between the morisky medication adherence scale and medication complexity and patient prescription knowledge in primary health careFröhlich, Samanta E.Vigo, AlvaroMengue, Sotero Serratehttp://sedici.unlp.edu.ar:80/handle/10915/83042019-07-03T20:03:30Z2011-01-01T00:00:00ZArticulo
Latin American Journal of Pharmacy; vol. 30, no. 7
The aim of the study was to check the association of the Morisky Medication Adherence Scale with the prescription complexity and with the patient’s level of knowledge about the prescription. A cross-sectional study was conducted by means of an interview and analysis of the prescription received by patients selected at Family Health Strategy Units. A Poisson regression model with robust variance was used to describe the association between the variables. Low adherence was significantly associated with highly complex prescriptions: Prevalence Ratio (PR) = 1.53; 95 % Confidence Interval (CI) = 1.28-1.82, in comparison with low and moderate complexity. Low adherence was also significantly associated with very low levels of knowledge: regarding the highest level (third tertile), the first and second tertiles had PR = 4.44; 95 % CI = 3.26-6.06 and PR = 3.22; 95 % CI = 2.33-4.47, respectively. The Morisky scale is useful to measure low adherence, with the advantage of being an easily understood instrument, which can be quickly administered, presenting simple interpretation and application
2011-01-01T00:00:00ZThe aim of the study was to check the association of the Morisky Medication Adherence Scale with the prescription complexity and with the patient’s level of knowledge about the prescription. A cross-sectional study was conducted by means of an interview and analysis of the prescription received by patients selected at Family Health Strategy Units. A Poisson regression model with robust variance was used to describe the association between the variables. Low adherence was significantly associated with highly complex prescriptions: Prevalence Ratio (PR) = 1.53; 95 % Confidence Interval (CI) = 1.28-1.82, in comparison with low and moderate complexity. Low adherence was also significantly associated with very low levels of knowledge: regarding the highest level (third tertile), the first and second tertiles had PR = 4.44; 95 % CI = 3.26-6.06 and PR = 3.22; 95 % CI = 2.33-4.47, respectively. The Morisky scale is useful to measure low adherence, with the advantage of being an easily understood instrument, which can be quickly administered, presenting simple interpretation and application