http://sedici.unlp.edu.ar:80/handle/10915/242 Sun, 08 Nov 2026 22:06:07 GMT 2026-11-08T22:06:07Z http://sedici.unlp.edu.ar:80/handle/10915/8388 Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 9 To select the suitable concentration level of controlled release polymer for the formulation of predefined extended release formulation based on the solubility behaviour of active substance, we have formulated and evaluated the extended release matrix tablets of two different antihypertensive drugs having different solubility profile by direct compression process. The selected antihypertensive drugs are metoprolol succinate of freely soluble category and propranolol hydrochloride of soluble category (solubility in terms of water). The selected drugs were formulated with various concentrations of selected highest viscosity grades of controlled release polymers viz. HPMC K200M & Polyox WSR 303 and evaluated for drug release profile. Dissolution methods were conducted using USP official methods. From the studies conducted it was found that drug solubility behavior also plays an important role in selection of controlled release polymer concentration for formulation of extended release formulation and observed that a higher concentration level of controlled release polymer is required for the formulation of freely soluble drug than soluble drug. Sat, 01 Jan 2011 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8388 2011-01-01T00:00:00Z To select the suitable concentration level of controlled release polymer for the formulation of predefined extended release formulation based on the solubility behaviour of active substance, we have formulated and evaluated the extended release matrix tablets of two different antihypertensive drugs having different solubility profile by direct compression process. The selected antihypertensive drugs are metoprolol succinate of freely soluble category and propranolol hydrochloride of soluble category (solubility in terms of water). The selected drugs were formulated with various concentrations of selected highest viscosity grades of controlled release polymers viz. HPMC K200M & Polyox WSR 303 and evaluated for drug release profile. Dissolution methods were conducted using USP official methods. From the studies conducted it was found that drug solubility behavior also plays an important role in selection of controlled release polymer concentration for formulation of extended release formulation and observed that a higher concentration level of controlled release polymer is required for the formulation of freely soluble drug than soluble drug. http://sedici.unlp.edu.ar:80/handle/10915/8387 Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 9 Copper compounds and, in particular, Cu(II) complexes show relevant pharmacological interest. Copper complexes of most of the simplest amino acids showed a particular relevance, appearing even useful for copper supplementation in human and veterinary medicine. In this contribution, the infrared and Raman spectra of the Cu(II) complex of L-lysine of composition [Cu(L-Lysinato)₂Cl₂]·2H₂O were recorded and analyzed in relation to its structural peculiarities and by comparison with the spectra of L-lysine hydrochloride. The electronic spectrum of the complex is also briefly discussed. Sat, 01 Jan 2011 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8387 2011-01-01T00:00:00Z Copper compounds and, in particular, Cu(II) complexes show relevant pharmacological interest. Copper complexes of most of the simplest amino acids showed a particular relevance, appearing even useful for copper supplementation in human and veterinary medicine. In this contribution, the infrared and Raman spectra of the Cu(II) complex of L-lysine of composition [Cu(L-Lysinato)₂Cl₂]·2H₂O were recorded and analyzed in relation to its structural peculiarities and by comparison with the spectra of L-lysine hydrochloride. The electronic spectrum of the complex is also briefly discussed. http://sedici.unlp.edu.ar:80/handle/10915/8386 Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 9 Alpinia zerumbet (Zingiberaceae) presents a high medicinal value, in part by its production of volatile compounds. Organogenic in vitro cultures of A. zerumbet were treated with the elicitor methyl jasmonate (MeJA), a natural volatile signaling molecule in biotic and abiotic stress, and the effect was evaluated on the in vitro production of volatiles. Leaves of plantlets were subjected to simultaneous distillation-extraction (SDE), and sabinene, β-pinene, 1,8 cineole and terpinen-4-ol were the main volatiles detected. However, after exposure to a solution of of MeJA for 3 and 10 days, terpinen-4-ol showed a remarkable increase, corresponding to 18.01 and 14.75 %, respectively, when compared to control with ethanol. In contrast, exposure of plantlets to the addition of ethanol induced levels of sabinene and 1,8 cineole higher than those produced by MeJA. Sat, 01 Jan 2011 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8386 2011-01-01T00:00:00Z Alpinia zerumbet (Zingiberaceae) presents a high medicinal value, in part by its production of volatile compounds. Organogenic in vitro cultures of A. zerumbet were treated with the elicitor methyl jasmonate (MeJA), a natural volatile signaling molecule in biotic and abiotic stress, and the effect was evaluated on the in vitro production of volatiles. Leaves of plantlets were subjected to simultaneous distillation-extraction (SDE), and sabinene, β-pinene, 1,8 cineole and terpinen-4-ol were the main volatiles detected. However, after exposure to a solution of of MeJA for 3 and 10 days, terpinen-4-ol showed a remarkable increase, corresponding to 18.01 and 14.75 %, respectively, when compared to control with ethanol. In contrast, exposure of plantlets to the addition of ethanol induced levels of sabinene and 1,8 cineole higher than those produced by MeJA. http://sedici.unlp.edu.ar:80/handle/10915/8385 Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 9 Substrate-dependent inhibition of CYP3A4 might influence the extrapolation of drug interactions from the in vitro to in vivo situation. The aim of the present study is to investigate reversible and time-dependent inhibition of CYP3A4-mediated nifedipine oxidation by noscapine. Furthermore, in vitroin vivo extrapolation (IVIVE) was performed using in vitro parameters. The results showed that CYP3A4- mediated nifedipine oxidation activity was strongly inhibited with an IC₅₀ of 25.7 ± 5.4 μM. Kinetic analysis showed that inhibition of CYP3A4-mediated nifedipine oxidation by noscapine was best fit to a noncompetitive manner with Ki value of 10.9 μM. IC50 shift experiment showed that IC50 was significantly decreased from 25.7 ± 5.4 μM to 0.34 ± 0.07 μM after pre-incubation with noscapine for 30 min, which indicated that time-dependent inhibition existed for inhibition of CYP3A4 by noscapine. The AUC of (R)- warfarin was predicted to increase by 0.5 % using C_max or 0.2 % using unbound C_max with reversible inhibition prediction equation, while the AUC of (R)-warfarin was estimated to increase by 23.1 % using C_max or 10.4 % using unbound C_max with TDI prediction equation. Inhibition of CYP3A4 by noscapine showed substrate-dependent inhibition behaviour. However, the results obtained from IVIVE are very similar using testosterone or nifedipine as probe substrates. Sat, 01 Jan 2011 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8385 2011-01-01T00:00:00Z Substrate-dependent inhibition of CYP3A4 might influence the extrapolation of drug interactions from the in vitro to in vivo situation. The aim of the present study is to investigate reversible and time-dependent inhibition of CYP3A4-mediated nifedipine oxidation by noscapine. Furthermore, in vitroin vivo extrapolation (IVIVE) was performed using in vitro parameters. The results showed that CYP3A4- mediated nifedipine oxidation activity was strongly inhibited with an IC₅₀ of 25.7 ± 5.4 μM. Kinetic analysis showed that inhibition of CYP3A4-mediated nifedipine oxidation by noscapine was best fit to a noncompetitive manner with Ki value of 10.9 μM. IC50 shift experiment showed that IC50 was significantly decreased from 25.7 ± 5.4 μM to 0.34 ± 0.07 μM after pre-incubation with noscapine for 30 min, which indicated that time-dependent inhibition existed for inhibition of CYP3A4 by noscapine. The AUC of (R)- warfarin was predicted to increase by 0.5 % using C_max or 0.2 % using unbound C_max with reversible inhibition prediction equation, while the AUC of (R)-warfarin was estimated to increase by 23.1 % using C_max or 10.4 % using unbound C_max with TDI prediction equation. Inhibition of CYP3A4 by noscapine showed substrate-dependent inhibition behaviour. However, the results obtained from IVIVE are very similar using testosterone or nifedipine as probe substrates. http://sedici.unlp.edu.ar:80/handle/10915/8384 Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 9 A sensitive and simple liquid chromatography/electrospray mass spectrometry (LC-ESI-MS) method for determination of ketamine in rabbit plasma using one-step protein precipitation was developed and validated. After addition of methadone as internal standard (IS), protein precipitation by acetonitrile was used as sample preparation. Chromatographically separation was achieved on an SB-C18 (2.1 mm × 50 mm, 3.5 μm) column with methanol-0.1 % formic acid as the 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 237.7 → 219.7 for ketamine and m/z 309.9 → 264.8 for the IS. Calibration plots were linear over the range of 5-1000 ng/mL for ketamine in rabbit plasma. Lower limit of quantification (LLOQ) for ketamine was 5 ng/mL. Mean recovery of ketamine from plasma was in the range of 97.5-100.1 %. RSD of intra-day and inter-day precision were both less than 11 %. This method is simple and sensitive enough to be used in pharmacokinetic research for determination of ketamine in rabbit plasma. Sat, 01 Jan 2011 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8384 2011-01-01T00:00:00Z A sensitive and simple liquid chromatography/electrospray mass spectrometry (LC-ESI-MS) method for determination of ketamine in rabbit plasma using one-step protein precipitation was developed and validated. After addition of methadone as internal standard (IS), protein precipitation by acetonitrile was used as sample preparation. Chromatographically separation was achieved on an SB-C18 (2.1 mm × 50 mm, 3.5 μm) column with methanol-0.1 % formic acid as the 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 237.7 → 219.7 for ketamine and m/z 309.9 → 264.8 for the IS. Calibration plots were linear over the range of 5-1000 ng/mL for ketamine in rabbit plasma. Lower limit of quantification (LLOQ) for ketamine was 5 ng/mL. Mean recovery of ketamine from plasma was in the range of 97.5-100.1 %. RSD of intra-day and inter-day precision were both less than 11 %. This method is simple and sensitive enough to be used in pharmacokinetic research for determination of ketamine in rabbit plasma. http://sedici.unlp.edu.ar:80/handle/10915/8383 Articulo Latin American Journal of Pharmacy; vol. 30, no. 9 In this study, the essential oil composition, total contents of phenolics and proanthocyanidins, antioxidant and antimicrobial activities from different plant parts (root, stem, leaf and fruit) of Campomanesia pubescens (DC) O. Berg from Brazilian Cerrado are reported. The root essential oil is distinguished from others by having only one representative of monoterpenes (alpha-terpenylacetate). The aerial parts of C. pubescens are rich in volatile terpenes, as expected, especially in fruits whose essential oil contained approximately 80 % of monoterpenes. The essential oils showed antimicrobial activity against oral pathogens. The root essential oil showed the strongest inhibition against Fusobacterium nucleatum (ATCC 25586). The leaf extract presented the highest concentration of phenolic and proanthocyanidins compounds. The lowest concentration necessary for inhibition of DPPH to 50 % ranged between 6.6 ± 1.6 and 56.6 ± 2.3 μg/mL. The leaf extract exhibited the highest inhibition, close to BHT. Sat, 01 Jan 2011 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8383 2011-01-01T00:00:00Z In this study, the essential oil composition, total contents of phenolics and proanthocyanidins, antioxidant and antimicrobial activities from different plant parts (root, stem, leaf and fruit) of Campomanesia pubescens (DC) O. Berg from Brazilian Cerrado are reported. The root essential oil is distinguished from others by having only one representative of monoterpenes (alpha-terpenylacetate). The aerial parts of C. pubescens are rich in volatile terpenes, as expected, especially in fruits whose essential oil contained approximately 80 % of monoterpenes. The essential oils showed antimicrobial activity against oral pathogens. The root essential oil showed the strongest inhibition against Fusobacterium nucleatum (ATCC 25586). The leaf extract presented the highest concentration of phenolic and proanthocyanidins compounds. The lowest concentration necessary for inhibition of DPPH to 50 % ranged between 6.6 ± 1.6 and 56.6 ± 2.3 μg/mL. The leaf extract exhibited the highest inhibition, close to BHT. http://sedici.unlp.edu.ar:80/handle/10915/8382 Articulo Latin American Journal of Pharmacy; vol. 30, no. 9 Hydroquinone (HQ) is a drug reported to possess manifold biological activities. HQ is highly unstable into various topical vehicles, presenting low topical bioavailability and a relevant level of toxicity. The Pluronic® Lecithin Organogel (PLOme) is a phospholipidic microemulsion designed for transdermal purposes. The aim of this work was therefore to incorporate HQ into PLOme. We evaluated the stability, the kinetic profile and the antimicrobial activity of HQ- incorporated PLOme. No relevant pH variation was observed. Long-term stability test showed an HQ degradation which led to a short shelf life. HQ permeation rate obtained was lower from PLOme than from a gel matrix. Free and PLOme-encapsulated hydroquinone showed to have a great in vitro inhibitory potential against of S. aureus strains. The encapsulation of HQ due its unstable characteristics could be an alternative to optimize its therapeutic usage, and so further investigation is required on this pharmaceutical form before commercialization. Sat, 01 Jan 2011 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8382 2011-01-01T00:00:00Z Hydroquinone (HQ) is a drug reported to possess manifold biological activities. HQ is highly unstable into various topical vehicles, presenting low topical bioavailability and a relevant level of toxicity. The Pluronic® Lecithin Organogel (PLOme) is a phospholipidic microemulsion designed for transdermal purposes. The aim of this work was therefore to incorporate HQ into PLOme. We evaluated the stability, the kinetic profile and the antimicrobial activity of HQ- incorporated PLOme. No relevant pH variation was observed. Long-term stability test showed an HQ degradation which led to a short shelf life. HQ permeation rate obtained was lower from PLOme than from a gel matrix. Free and PLOme-encapsulated hydroquinone showed to have a great in vitro inhibitory potential against of S. aureus strains. The encapsulation of HQ due its unstable characteristics could be an alternative to optimize its therapeutic usage, and so further investigation is required on this pharmaceutical form before commercialization. http://sedici.unlp.edu.ar:80/handle/10915/8381 Articulo Latin American Journal of Pharmacy; vol. 30, no. 9 Oral route of drug administration is the most preferred route of drug administration but this route has its own limitations like pH of gastric media and controlling release rate of water soluble drug. To overcome these limitations, formulations containing controlled release matrix need to be developed. Controlled release of drug can be achieved by incorporating the drug into a release rate controlling carriers. Chitosan (CH)/Chondroitin Sulphate (CS) complex microcapsules were prepared to encapsulate the cardio vascular drug Propranolol hydrochloride (PHCl) by emulsion-chemical crosslinking method using sodium tripolyphosphate (STPP) as cross-linking agent. The FT-IR and DSC spectra’s revealed that there is no chemical interaction between drug and polymers used. Encapsulation efficiency and in-vitro drug release was found to be 64-84 % and 55-85 % respectively. Among all the formulations the F4.1 showed controlled drug release. This study revealed that the cross linked microcapsules of chitosan and chondroitin sulphate can be used to control drug release rate of water soluble drug. Sat, 01 Jan 2011 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8381 2011-01-01T00:00:00Z Oral route of drug administration is the most preferred route of drug administration but this route has its own limitations like pH of gastric media and controlling release rate of water soluble drug. To overcome these limitations, formulations containing controlled release matrix need to be developed. Controlled release of drug can be achieved by incorporating the drug into a release rate controlling carriers. Chitosan (CH)/Chondroitin Sulphate (CS) complex microcapsules were prepared to encapsulate the cardio vascular drug Propranolol hydrochloride (PHCl) by emulsion-chemical crosslinking method using sodium tripolyphosphate (STPP) as cross-linking agent. The FT-IR and DSC spectra’s revealed that there is no chemical interaction between drug and polymers used. Encapsulation efficiency and in-vitro drug release was found to be 64-84 % and 55-85 % respectively. Among all the formulations the F4.1 showed controlled drug release. This study revealed that the cross linked microcapsules of chitosan and chondroitin sulphate can be used to control drug release rate of water soluble drug. http://sedici.unlp.edu.ar:80/handle/10915/8380 Articulo Latin American Journal of Pharmacy; vol. 30, no. 9 The objective of the present work was to formulate chitosan nanoparticles as carriers for the lovastatin, since this drug undergoes extensive first pass extraction in the liver, and bioavailibity is low (< 5 %). Nanoparticles were prepared by modified ionotropic gelation method using 32 full factorial design. From the preliminary trials, the constraints for independent variables X1 (concentration of chitosan) and X2 (concentration of sodium tripolyphosphate) have been fixed and examined to investigate effect on particle size, encapsulation efficiency, zeta potential, % release, SEM, FTIR, XRD and DSC analysis of lovastatin. The diameter of prepared nanoparticles was controlled in the range of 100-800 nm, spherical shape and narrow diameter distribution. The release profiles of all batches were very well fitted by both the zero order model and the anomalous transport. These results indicate that lovastatin nanoparticles could be effective in sustaining drug release for a prolonged period. Sat, 01 Jan 2011 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8380 2011-01-01T00:00:00Z The objective of the present work was to formulate chitosan nanoparticles as carriers for the lovastatin, since this drug undergoes extensive first pass extraction in the liver, and bioavailibity is low (< 5 %). Nanoparticles were prepared by modified ionotropic gelation method using 32 full factorial design. From the preliminary trials, the constraints for independent variables X1 (concentration of chitosan) and X2 (concentration of sodium tripolyphosphate) have been fixed and examined to investigate effect on particle size, encapsulation efficiency, zeta potential, % release, SEM, FTIR, XRD and DSC analysis of lovastatin. The diameter of prepared nanoparticles was controlled in the range of 100-800 nm, spherical shape and narrow diameter distribution. The release profiles of all batches were very well fitted by both the zero order model and the anomalous transport. These results indicate that lovastatin nanoparticles could be effective in sustaining drug release for a prolonged period. http://sedici.unlp.edu.ar:80/handle/10915/8379 Articulo Latin American Journal of Pharmacy; vol. 30, no. 9 The aim of the study was to formulate and evaluate controlled release microspheres. Ciprofloxacin HCl, belonging to the class of fluroquinolones, was chosen as the model drug. The drugloaded microspheres were prepared with different ratios of polymers like sodium alginate and sodium carboxy methyl cellulose (CMC) by w/o emulsification solvent evaporation method. The prepared microspheres were characterized by FT-IR spectroscopy, differential scanning colorimetry for drug polymer compatibility studies and scanning electron microscopy for surface morphology. The resulting microspheres were found to be small, discrete, spherical and free flowing. They were further evaluated for their micromeritic properties, particle size analysis, drug loading and entrapment efficiency. The mean particle size was 201.21 μm. In vitro drug release studies revealed that formulation Fm6 containing sodium CMC as the polymer showed greater sustained effect for 10 hours. Stability studies showed no significant changes in the drug content and physical appearance. Sat, 01 Jan 2011 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8379 2011-01-01T00:00:00Z The aim of the study was to formulate and evaluate controlled release microspheres. Ciprofloxacin HCl, belonging to the class of fluroquinolones, was chosen as the model drug. The drugloaded microspheres were prepared with different ratios of polymers like sodium alginate and sodium carboxy methyl cellulose (CMC) by w/o emulsification solvent evaporation method. The prepared microspheres were characterized by FT-IR spectroscopy, differential scanning colorimetry for drug polymer compatibility studies and scanning electron microscopy for surface morphology. The resulting microspheres were found to be small, discrete, spherical and free flowing. They were further evaluated for their micromeritic properties, particle size analysis, drug loading and entrapment efficiency. The mean particle size was 201.21 μm. In vitro drug release studies revealed that formulation Fm6 containing sodium CMC as the polymer showed greater sustained effect for 10 hours. Stability studies showed no significant changes in the drug content and physical appearance. http://sedici.unlp.edu.ar:80/handle/10915/8378 Articulo Latin American Journal of Pharmacy; vol. 30, no. 9 Simultaneous multiple prescription drugs increases the possibility of drug interactions, situation particularly critical in a hospital. The objective of the present work was to identify interactions by evaluating the originals of prescriptions archived from ward clinical of a hospital specializing in cardiology in the city of Campina Grande/PB, Brazil. The study had transversal, retrospective, and observational character with quantitative approach, and was held in the period from June to July 2010. A total of 196 prescriptions were analyzed and of these, 89.6 % had some type of interaction, and 28.0 % of prescriptions had at least one interaction. The most frequent involved were deslanosideo and furosemide (15.1 %), being classified as moderate. This study showed the importance of the pharmacist in the analysis of requirements, who may exercise the clinical pharmacy and contribute to the continuos education on medicines. Sat, 01 Jan 2011 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8378 2011-01-01T00:00:00Z Simultaneous multiple prescription drugs increases the possibility of drug interactions, situation particularly critical in a hospital. The objective of the present work was to identify interactions by evaluating the originals of prescriptions archived from ward clinical of a hospital specializing in cardiology in the city of Campina Grande/PB, Brazil. The study had transversal, retrospective, and observational character with quantitative approach, and was held in the period from June to July 2010. A total of 196 prescriptions were analyzed and of these, 89.6 % had some type of interaction, and 28.0 % of prescriptions had at least one interaction. The most frequent involved were deslanosideo and furosemide (15.1 %), being classified as moderate. This study showed the importance of the pharmacist in the analysis of requirements, who may exercise the clinical pharmacy and contribute to the continuos education on medicines. http://sedici.unlp.edu.ar:80/handle/10915/8377 Articulo Latin American Journal of Pharmacy; vol. 30, no. 9 A simple isocratic method for quantification of hydroxyzine dihydrochloride by HPLC with UV detection at 232 nm in syrup has been developed and validated. Separation was achieved on a C18 column (250 x 4.6 mm, 5 μm) maintained at 90 ºC with 0.5 mol/L potassium dihydrogen phosphate buffer : acetonitrile (1:1, v/v) as mobile phase at a flow rate of 2.0 mL/min. The method was proven to be linear over the range of 80–120 μg/mL, accurate (recovery = 97.8 %), precise (coefficient of variation = 1.52 % for sample) and robust. Sat, 01 Jan 2011 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8377 2011-01-01T00:00:00Z A simple isocratic method for quantification of hydroxyzine dihydrochloride by HPLC with UV detection at 232 nm in syrup has been developed and validated. Separation was achieved on a C18 column (250 x 4.6 mm, 5 μm) maintained at 90 ºC with 0.5 mol/L potassium dihydrogen phosphate buffer : acetonitrile (1:1, v/v) as mobile phase at a flow rate of 2.0 mL/min. The method was proven to be linear over the range of 80–120 μg/mL, accurate (recovery = 97.8 %), precise (coefficient of variation = 1.52 % for sample) and robust. http://sedici.unlp.edu.ar:80/handle/10915/8376 Articulo Latin American Journal of Pharmacy; vol. 30, no. 9 Microspheres were prepared using the emulsion/solvent evaporation method with the aim of obtaining diclofenac sodium (DFS) prolonged release dosage forms. The effects of the drug:polymer ratio and addition of Pluronic F68® to the formulations on drug content, particle size and DFS release rate were evaluated using a 22 factorial design. The DFS encapsulation efficiency (%) and the drug content varied from 40 to 70 % and from 4.5 to 13 mg/100 mg, respectively. The mean particle diameter varied from 720 to 850 μm. The addition of Pluronic F68® to the formulations led to an increase in the roughness of the surface. The differential scanning calorimetry (DSC) and infrared spectroscopy (FTIR) studies indicated the presence of Pluronic F68® in the particles. The statistical analysis revealed that the drug content and the release rate of DFS were significantly increased when 1:4 drug:polymer ratio and Pluronic F68® was used to prepare the microspheres. Sat, 01 Jan 2011 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8376 2011-01-01T00:00:00Z Microspheres were prepared using the emulsion/solvent evaporation method with the aim of obtaining diclofenac sodium (DFS) prolonged release dosage forms. The effects of the drug:polymer ratio and addition of Pluronic F68® to the formulations on drug content, particle size and DFS release rate were evaluated using a 22 factorial design. The DFS encapsulation efficiency (%) and the drug content varied from 40 to 70 % and from 4.5 to 13 mg/100 mg, respectively. The mean particle diameter varied from 720 to 850 μm. The addition of Pluronic F68® to the formulations led to an increase in the roughness of the surface. The differential scanning calorimetry (DSC) and infrared spectroscopy (FTIR) studies indicated the presence of Pluronic F68® in the particles. The statistical analysis revealed that the drug content and the release rate of DFS were significantly increased when 1:4 drug:polymer ratio and Pluronic F68® was used to prepare the microspheres. http://sedici.unlp.edu.ar:80/handle/10915/8375 Articulo Latin American Journal of Pharmacy; vol. 30, no. 9 In the present work, orodispersible tablets of atomoxetine HCl were designed by preparing tasteless complexes of atomoxetine HCl with weak cation ion exchange resins (Kyron T 134). The ion exchange complex were prepared by the batch process using activated Kyron T 134 with a drug: resin ratios 1:1, 1:2, 1:3 and 1:4 (% w/w). IR analysis, assay content and decomplexation studies confirmed complex formation. It was found that maximum complexation of drug with resin was noted between pH range 5-7, while activation of ion exchange resin affects the percent drug loading. Drug release from drug: resin complex in salivary pH was insufficient to impart bitter taste. A study on super-disintegrants along with directly compressible diluents is studied and its effect on disintegration time and enhance mouth feel. The prepared batches of tablets were evaluated for hardness, friability, drug content uniformity and in vitro dispersion time. Based on in vitro disintegration time (approximately 30 s), formulations were tested for in vitro drug release pattern in 0.1N HCl. Sat, 01 Jan 2011 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8375 2011-01-01T00:00:00Z In the present work, orodispersible tablets of atomoxetine HCl were designed by preparing tasteless complexes of atomoxetine HCl with weak cation ion exchange resins (Kyron T 134). The ion exchange complex were prepared by the batch process using activated Kyron T 134 with a drug: resin ratios 1:1, 1:2, 1:3 and 1:4 (% w/w). IR analysis, assay content and decomplexation studies confirmed complex formation. It was found that maximum complexation of drug with resin was noted between pH range 5-7, while activation of ion exchange resin affects the percent drug loading. Drug release from drug: resin complex in salivary pH was insufficient to impart bitter taste. A study on super-disintegrants along with directly compressible diluents is studied and its effect on disintegration time and enhance mouth feel. The prepared batches of tablets were evaluated for hardness, friability, drug content uniformity and in vitro dispersion time. Based on in vitro disintegration time (approximately 30 s), formulations were tested for in vitro drug release pattern in 0.1N HCl. http://sedici.unlp.edu.ar:80/handle/10915/8374 Articulo Latin American Journal of Pharmacy; vol. 30, no. 9 The hepato- and nephro-protective effects of sea buckthorn berries (Hippophae rhamnoides L) were investigated in paracetamol-induced toxicity in animals and hypoglycemic effects in type II diabetic patients. Crude drug preparation and its methanol extract have shown a profound decrease in paracetamol-induced elevated serum levels of liver and kidney functions under investigation, which suggests a possible therapeutic role of its constituents in hepatic injury and altered kidney functions. Similarly, in human patients with raised glucose levels, sea buckthorn shows hypoglycemic effect which could likely make it a potential therapeutic agent to mange type II diabetes mellitus. However, further investigations are required to unveil the mechanism of action of sea buckthorn preparations in these ailments. Sat, 01 Jan 2011 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8374 2011-01-01T00:00:00Z The hepato- and nephro-protective effects of sea buckthorn berries (Hippophae rhamnoides L) were investigated in paracetamol-induced toxicity in animals and hypoglycemic effects in type II diabetic patients. Crude drug preparation and its methanol extract have shown a profound decrease in paracetamol-induced elevated serum levels of liver and kidney functions under investigation, which suggests a possible therapeutic role of its constituents in hepatic injury and altered kidney functions. Similarly, in human patients with raised glucose levels, sea buckthorn shows hypoglycemic effect which could likely make it a potential therapeutic agent to mange type II diabetes mellitus. However, further investigations are required to unveil the mechanism of action of sea buckthorn preparations in these ailments. http://sedici.unlp.edu.ar:80/handle/10915/8373 Articulo Latin American Journal of Pharmacy; vol. 30, no. 9 A sensitive and selective liquid chromatography-mass spectrometry (LC-MS) method for determination of sulpiride in rabbit plasma was developed and validated. The analyte and internal standard (IS) were extracted from plasma by liquid-liquid extraction using ethyl acetate, and chromatography involved Agilent Extend-C18 column (2.1 mm x 50 mm, 3.5 μm) using 0.2 % formic acid in water and acetonitrile (60: 40, v/v) as a mobile phase. Detection involved positive ion mode electrospray ionization (ESI), and selective ion monitoring (SIM) mode was used for quantification of target fragmentions m/z 342.0 for sulpiride and m/z 294.8 for estazolam (internal standard, IS). The assay was linear over the range of 10-2000 ng/mL for sulpiride, with a lower limit of quantitation (LLOQ) of 10 ng/mL for sulpiride. Intraand inter-day precisions were less than 12 % and the accuracies were in the range of 94.1-108.7 % for sulpiride. This developed method was successfully applied for the determination of sulpiride in rabbit plasma for pharmacokinetic study. Sat, 01 Jan 2011 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8373 2011-01-01T00:00:00Z A sensitive and selective liquid chromatography-mass spectrometry (LC-MS) method for determination of sulpiride in rabbit plasma was developed and validated. The analyte and internal standard (IS) were extracted from plasma by liquid-liquid extraction using ethyl acetate, and chromatography involved Agilent Extend-C18 column (2.1 mm x 50 mm, 3.5 μm) using 0.2 % formic acid in water and acetonitrile (60: 40, v/v) as a mobile phase. Detection involved positive ion mode electrospray ionization (ESI), and selective ion monitoring (SIM) mode was used for quantification of target fragmentions m/z 342.0 for sulpiride and m/z 294.8 for estazolam (internal standard, IS). The assay was linear over the range of 10-2000 ng/mL for sulpiride, with a lower limit of quantitation (LLOQ) of 10 ng/mL for sulpiride. Intraand inter-day precisions were less than 12 % and the accuracies were in the range of 94.1-108.7 % for sulpiride. This developed method was successfully applied for the determination of sulpiride in rabbit plasma for pharmacokinetic study. http://sedici.unlp.edu.ar:80/handle/10915/8372 Articulo Latin American Journal of Pharmacy; vol. 30, no. 9 This study is the first attempt in UAE to prove the trustworthiness of the in vitro evaluation to assess the reliability of the generic medications comparing to the brand name. Five generic medicines, two Local (codes: L1, L2), three Arabic (codes: A1, A2 and A3) and the International brand (code: I1) of diclofenac sodium (DS) sustained release tablets, as a model product, was collected randomly from the UAE pharma market. The products were characterized by physical parameters including weight variation, thickness, friability, hardness and moisture content. The in vitro release study was conducted in simulated gastric medium (0.1 N HCl, pH 1.2) for 2 h and simulated intestinal medium (phosphate buffer pH 6.8) for 9 h using type II (paddle type) USP reference dissolution apparatus. The drug was assayed by using UV spectrophotometry at 277 nm. Different kinetics models were applied to drug release data in order to evaluate mechanism of drug release. Physical properties of all products compiled with the acceptable limits. However moisture content was higher than the standard value in the generic products except the brand. All the products succeed to fulfill their official requirement of 80 % drug release within 8 h, in simulated intestinal medium except A3. Zero order release kinetics was predominant for al L2 and the International brand while more data fitting to Hixson- Crowell kinetics was obtained with the L1 and A1, A2 and A3. The results of our study question the suitability of the generic products as a replacement for the branded product. Therefore, we strongly suggest that evaluation on the marketed samples has to be made in order to establish bioequivalency between the branded and the generic products. Sat, 01 Jan 2011 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8372 2011-01-01T00:00:00Z This study is the first attempt in UAE to prove the trustworthiness of the in vitro evaluation to assess the reliability of the generic medications comparing to the brand name. Five generic medicines, two Local (codes: L1, L2), three Arabic (codes: A1, A2 and A3) and the International brand (code: I1) of diclofenac sodium (DS) sustained release tablets, as a model product, was collected randomly from the UAE pharma market. The products were characterized by physical parameters including weight variation, thickness, friability, hardness and moisture content. The in vitro release study was conducted in simulated gastric medium (0.1 N HCl, pH 1.2) for 2 h and simulated intestinal medium (phosphate buffer pH 6.8) for 9 h using type II (paddle type) USP reference dissolution apparatus. The drug was assayed by using UV spectrophotometry at 277 nm. Different kinetics models were applied to drug release data in order to evaluate mechanism of drug release. Physical properties of all products compiled with the acceptable limits. However moisture content was higher than the standard value in the generic products except the brand. All the products succeed to fulfill their official requirement of 80 % drug release within 8 h, in simulated intestinal medium except A3. Zero order release kinetics was predominant for al L2 and the International brand while more data fitting to Hixson- Crowell kinetics was obtained with the L1 and A1, A2 and A3. The results of our study question the suitability of the generic products as a replacement for the branded product. Therefore, we strongly suggest that evaluation on the marketed samples has to be made in order to establish bioequivalency between the branded and the generic products. http://sedici.unlp.edu.ar:80/handle/10915/8371 Articulo Latin American Journal of Pharmacy; vol. 30, no. 9 The aim of this study was to formulate gliclazide loaded controlled release microspheres. Microspheres were prepared by quasi emulsion solvent diffusion technique using eudragit RLPO, eudragit RSPO and with their various combinations. The effect of different formulation variables (drug-polymer ratio and polymer-polymer ratio) on percent yield, mean particle size, encapsulation efficiency and in vitro release of drug were evaluated. In vivo test of the optimized formulation was performed on streptozotocin induced type-2 diabetic rat model. The formulated microspheres showed higher encapsulation efficiencies within the range of 72-84 %. Mean particle size, encapsulation efficiency and in vitro release were found to be affected by changing in formulation variables. In vitro release study revealed the gliclazide release from the microspheres was extended for more than 12 h. In vivo hypoglycemic effect of microspheres was more than 25 h suggesting microspheres are a valuable system for sustained delivery of gliclazide. Sat, 01 Jan 2011 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8371 2011-01-01T00:00:00Z The aim of this study was to formulate gliclazide loaded controlled release microspheres. Microspheres were prepared by quasi emulsion solvent diffusion technique using eudragit RLPO, eudragit RSPO and with their various combinations. The effect of different formulation variables (drug-polymer ratio and polymer-polymer ratio) on percent yield, mean particle size, encapsulation efficiency and in vitro release of drug were evaluated. In vivo test of the optimized formulation was performed on streptozotocin induced type-2 diabetic rat model. The formulated microspheres showed higher encapsulation efficiencies within the range of 72-84 %. Mean particle size, encapsulation efficiency and in vitro release were found to be affected by changing in formulation variables. In vitro release study revealed the gliclazide release from the microspheres was extended for more than 12 h. In vivo hypoglycemic effect of microspheres was more than 25 h suggesting microspheres are a valuable system for sustained delivery of gliclazide. http://sedici.unlp.edu.ar:80/handle/10915/8370 Articulo Latin American Journal of Pharmacy; vol. 30, no. 9 The aim of this study was: a) the determination of the relation between composition of mixture for microencapsulation (gelatin concentration 5, 10, and 15 %; sodium alginate 2, 4, and 6 %; acetic acid 15, 20, and 30 %) and the efficiency of the obtained microcapsules, b) the degree of human serum albumin (HSA) incorporation, and c) the release time of HSA from microcapsules. Existing relations was described by multiple regression equations on the basis of which it can be obtained HSA gelatin-alginate micocapsules with specified release time and with specified efficiency and degree of protein incorporation. The aim was realized by modeling the composition of mixture for microencapsulation. HSA microcapsules were prepared using complex coacervation method. Based on presented multiple regression equations it was possible to obtain HSA microcapsules with specified efficiency, degree of incorporation and release time. Sat, 01 Jan 2011 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8370 2011-01-01T00:00:00Z The aim of this study was: a) the determination of the relation between composition of mixture for microencapsulation (gelatin concentration 5, 10, and 15 %; sodium alginate 2, 4, and 6 %; acetic acid 15, 20, and 30 %) and the efficiency of the obtained microcapsules, b) the degree of human serum albumin (HSA) incorporation, and c) the release time of HSA from microcapsules. Existing relations was described by multiple regression equations on the basis of which it can be obtained HSA gelatin-alginate micocapsules with specified release time and with specified efficiency and degree of protein incorporation. The aim was realized by modeling the composition of mixture for microencapsulation. HSA microcapsules were prepared using complex coacervation method. Based on presented multiple regression equations it was possible to obtain HSA microcapsules with specified efficiency, degree of incorporation and release time. http://sedici.unlp.edu.ar:80/handle/10915/8369 Articulo Latin American Journal of Pharmacy; vol. 30, no. 9 In this work was evaluated the pharmacotherapeutic profile of HIV/AIDS bearers registered in the Service of Specialized Attendance located in Campina Grande–PB, Brazil. The research was of the type traverse, documental, descriptive and analytical and was realized in the period of August to October 2010. Were appraised the patient records of 188 people being 66 % males and 34% females. The most part (36 %) just studied the education fundamental level and presented age group between 40-49 years old. Antiretrovirals more prescribed were nucleoside reverse transcriptase inhibitors (NRTIs) and non-nucleoside reverse-transcriptase inhibitors (NNRTIs). Schemes no recommended by the Ministry of Health also were evidenced. The Negative Results associated to the use of medicine was registered in the three supra-categories. It is necessary a larger integration of the multidisciplinary team of prescribers (physicians and dentists) and pharmacists in the evaluation of the pharmacotherapy to guarantee the reduction of the morbidity and the presence of opportunists infections, guaranteeing so a better surviving for the seropositive patients. Sat, 01 Jan 2011 00:00:00 GMT http://sedici.unlp.edu.ar:80/handle/10915/8369 2011-01-01T00:00:00Z In this work was evaluated the pharmacotherapeutic profile of HIV/AIDS bearers registered in the Service of Specialized Attendance located in Campina Grande–PB, Brazil. The research was of the type traverse, documental, descriptive and analytical and was realized in the period of August to October 2010. Were appraised the patient records of 188 people being 66 % males and 34% females. The most part (36 %) just studied the education fundamental level and presented age group between 40-49 years old. Antiretrovirals more prescribed were nucleoside reverse transcriptase inhibitors (NRTIs) and non-nucleoside reverse-transcriptase inhibitors (NNRTIs). Schemes no recommended by the Ministry of Health also were evidenced. The Negative Results associated to the use of medicine was registered in the three supra-categories. It is necessary a larger integration of the multidisciplinary team of prescribers (physicians and dentists) and pharmacists in the evaluation of the pharmacotherapy to guarantee the reduction of the morbidity and the presence of opportunists infections, guaranteeing so a better surviving for the seropositive patients.