http://sedici.unlp.edu.ar:80/handle/10915/237 2013-05-23T05:31:21Z 2013-05-23T05:31:21Z Casal, Francieli Mallmann, Michele Pedroni, Helen C. Grazziotin, Manoela M. Tasso, Leandro http://sedici.unlp.edu.ar:80/handle/10915/8224 2012-12-22T02:01:47Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 4 A simple and specific method was validated for quantification of boldine in fluid extract of boldo (Peumus boldus Mol.) using high-performance liquid chromatography. A reversed-phase C₁₈ , Phenomenex® (150 x 4.6 mm, 4 µm) column was employed. The mobile phase consisted of 0.1 % trifluoroacetic acid and acetonitrile (78:22, v/v) at a flow rate of 0.8 mL/min. The column was maintained at 30 °C and the boldine peak detection was performed at a wavelength of 281 nm. The parameters used in the validation process were: linearity, specificity, precision, accuracy, limit of detection, limit of quantification and robustness. The validated method was selective and linear (r≥0.9991) for boldine concentration considering 5.0, 10.0, 15.0, 20.0 and 25.0 micro;g/mL. The recovery ranged from 90.93 % to 96.24 % and the limit of quantification was 2.41 micro;g/mL. The precision determined was reported as RSD (1.73 %). The method can be successfully applied to measure boldine concentrations in Boldo extract and be included in routine analysis of quality control.

2011-01-01T00:00:00Z A simple and specific method was validated for quantification of boldine in fluid extract of boldo (Peumus boldus Mol.) using high-performance liquid chromatography. A reversed-phase C₁₈ , Phenomenex® (150 x 4.6 mm, 4 µm) column was employed. The mobile phase consisted of 0.1 % trifluoroacetic acid and acetonitrile (78:22, v/v) at a flow rate of 0.8 mL/min. The column was maintained at 30 °C and the boldine peak detection was performed at a wavelength of 281 nm. The parameters used in the validation process were: linearity, specificity, precision, accuracy, limit of detection, limit of quantification and robustness. The validated method was selective and linear (r≥0.9991) for boldine concentration considering 5.0, 10.0, 15.0, 20.0 and 25.0 micro;g/mL. The recovery ranged from 90.93 % to 96.24 % and the limit of quantification was 2.41 micro;g/mL. The precision determined was reported as RSD (1.73 %). The method can be successfully applied to measure boldine concentrations in Boldo extract and be included in routine analysis of quality control. Ló, Stella M. S. Duarte, Márcia do Rocio http://sedici.unlp.edu.ar:80/handle/10915/8223 2012-12-22T02:01:47Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 4 Cordia americana (L.) Gottschling & J.S. Mill. is a tree which belongs to the Boraginaceae family and is native to the South of Brazil, Paraguay and Argentine, where it is commonly known as guajuvira and guayaibí. In folk medicine, the leaves are used as emollient, antimicrobial and anti-inflammatory, as well as the stem has antidiarrheal and hepatoprotective effects. Preliminary phytochemical studies have shown the presence of tannins, coumarins, quinones and cinnamaldehyde derivatives. This work has investigated the leaf and stem morpho-anatomy of C. americana, in order to contribute to the pharmacognostic quality control. Samples of adult leaves and young stems were fixed, either sectioned by freehand or embedded in glycol methacrylate and sectioned by microtome, and then the sections were stained. In parallel, microchemical tests and scanning electron microscopy were also performed. The leaves are alternate, simple, elliptic-obovate and slightly serrate. Anomocytic stomata occur on the abaxial surface. The mesophyll is dorsiventral and the midrib has a plano-convex cross-section and various collateral vascular bundles in closed arc. In the stem, it is encountered phellogen installed superficially and a discontinuous sclerenchymatic sheath encircling the vascular system. The phloem is stratified and cuneiform. Phenolic compounds and calcium oxalate crystals are present in the leaf and stem.

2011-01-01T00:00:00Z Cordia americana (L.) Gottschling & J.S. Mill. is a tree which belongs to the Boraginaceae family and is native to the South of Brazil, Paraguay and Argentine, where it is commonly known as guajuvira and guayaibí. In folk medicine, the leaves are used as emollient, antimicrobial and anti-inflammatory, as well as the stem has antidiarrheal and hepatoprotective effects. Preliminary phytochemical studies have shown the presence of tannins, coumarins, quinones and cinnamaldehyde derivatives. This work has investigated the leaf and stem morpho-anatomy of C. americana, in order to contribute to the pharmacognostic quality control. Samples of adult leaves and young stems were fixed, either sectioned by freehand or embedded in glycol methacrylate and sectioned by microtome, and then the sections were stained. In parallel, microchemical tests and scanning electron microscopy were also performed. The leaves are alternate, simple, elliptic-obovate and slightly serrate. Anomocytic stomata occur on the abaxial surface. The mesophyll is dorsiventral and the midrib has a plano-convex cross-section and various collateral vascular bundles in closed arc. In the stem, it is encountered phellogen installed superficially and a discontinuous sclerenchymatic sheath encircling the vascular system. The phloem is stratified and cuneiform. Phenolic compounds and calcium oxalate crystals are present in the leaf and stem. Gupta, Sumeet Mehla, Kritika Chauhan, Devesh Nair, Anroop http://sedici.unlp.edu.ar:80/handle/10915/8222 2012-12-22T02:01:47Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 4 Natural products play a significant role in human health in relation to the prevention and treatment of inflammation conditions. Although not fully understood, several action mechanisms are proposed to explain in vivo inflammatory action. The aim of this study was to assay different extracts from leaves of Michelia champaca (Magnoliaceae) on carrageenan induced inflammation rat model. The results were analyzed by One Way Analysis of Variance (ANOVA). The ethanolic extract (200 mg/kg) was found to be highly significant (p < 0.0001) with maximum inhibition (60.99 %) at 3 h against to positive control group. The findings conclude that M. champaca leaves extract exhibits an anti-inflammatory activity in pro-inflammatory conditions.

2011-01-01T00:00:00Z Natural products play a significant role in human health in relation to the prevention and treatment of inflammation conditions. Although not fully understood, several action mechanisms are proposed to explain in vivo inflammatory action. The aim of this study was to assay different extracts from leaves of Michelia champaca (Magnoliaceae) on carrageenan induced inflammation rat model. The results were analyzed by One Way Analysis of Variance (ANOVA). The ethanolic extract (200 mg/kg) was found to be highly significant (p < 0.0001) with maximum inhibition (60.99 %) at 3 h against to positive control group. The findings conclude that M. champaca leaves extract exhibits an anti-inflammatory activity in pro-inflammatory conditions. Royer, Lauri A.J. Necchi, Raquel M.M. Marín, Aline Zanetti, Gilberto Dolejal Manfron, Melânia Palermo http://sedici.unlp.edu.ar:80/handle/10915/8221 2012-12-22T02:01:47Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 4 Poiretia tetraphylla is an erect herb to subshrub, perennial, native to Brazil, Argentina, Paraguay and Uruguay. It is popularly known as erva-de-touro-miúda and used in traditional medicine as tonic, in stomach disorders and verminosis. The stem is angular, striate, glabrous with copious amounts of oblong and translucent glands. The epidermis is uniestratified and persistent, stomata well pronounced, thick, smooth and plain cuticle and oval mucilaginous glandular formations. The cortex has parenchyma cells, and the innermost layer is distinguished from others by having large cells with little cytoplasmic content. In this region, protecting the phloem, has a group up to six layers of sclerenchyma fibers. The central cylinder presents vascular system of sifonestelic continuous ectofolic type. The pith is composed of parenchyma cells with intercellular space of meatus type. The whole of these diagnostic traits are useful on the botanical quality control of this species.

2011-01-01T00:00:00Z Poiretia tetraphylla is an erect herb to subshrub, perennial, native to Brazil, Argentina, Paraguay and Uruguay. It is popularly known as erva-de-touro-miúda and used in traditional medicine as tonic, in stomach disorders and verminosis. The stem is angular, striate, glabrous with copious amounts of oblong and translucent glands. The epidermis is uniestratified and persistent, stomata well pronounced, thick, smooth and plain cuticle and oval mucilaginous glandular formations. The cortex has parenchyma cells, and the innermost layer is distinguished from others by having large cells with little cytoplasmic content. In this region, protecting the phloem, has a group up to six layers of sclerenchyma fibers. The central cylinder presents vascular system of sifonestelic continuous ectofolic type. The pith is composed of parenchyma cells with intercellular space of meatus type. The whole of these diagnostic traits are useful on the botanical quality control of this species. Colla, Guilherme Brighente, Inês Maria Costa Queiroz, Gustavo S. Silva, Mariana A. da Pizzolatti, Moacir Geraldo http://sedici.unlp.edu.ar:80/handle/10915/8220 2012-12-22T02:01:47Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 4 Ochna serrulata (Ochnaceae) is an ornamental plant introduced into Brazil from Asia and Africa. Species of the Ochna genus are rich in phenolic compounds, mainly flavonoids. The biological screening of extracts and fractions showed that this plant exhibited a significant antioxidant activity, when evaluated by the DPPH and reducing potential assays. Ochna serrulata also demonstrated slight toxic activity against Artemia salina and a potential inhibitory allelopathic activity, when evaluated using the Lactuca sativa seed germination test. The ethyl acetate fraction, the most active one, was partitioned on a silica gel column to obtain epicatechin, which showed potential antioxidant activity.

2011-01-01T00:00:00Z Ochna serrulata (Ochnaceae) is an ornamental plant introduced into Brazil from Asia and Africa. Species of the Ochna genus are rich in phenolic compounds, mainly flavonoids. The biological screening of extracts and fractions showed that this plant exhibited a significant antioxidant activity, when evaluated by the DPPH and reducing potential assays. Ochna serrulata also demonstrated slight toxic activity against Artemia salina and a potential inhibitory allelopathic activity, when evaluated using the Lactuca sativa seed germination test. The ethyl acetate fraction, the most active one, was partitioned on a silica gel column to obtain epicatechin, which showed potential antioxidant activity. Alves, Mauro M. S. Mendes, Patrizia C. Vieira, Janaína G. P. Jardim, Mário A. G. Ozela, Eliana F. Costa, Roseane M.R. Barbosa, Wagner L.R. Silva Júnior, José O. C. http://sedici.unlp.edu.ar:80/handle/10915/8219 2012-12-22T02:01:47Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 4 The quality control of herbal drugs and their intermediates is essential, especially when they are used as feedstock for medicine development. This study aimed at applying the methodologies established by Brazilian legislation for the development of parameters concerning the characterization and quality control of leaf powder and tincture of Arrabidaea chica (H & B) Verlot. Known as cipó-pau (vinestick), carajeru, pariri, among others, it presents antifungal activity and is used in several diseases such as mycosis and ringworm. The physico-chemical characteristics of the plant drug. The phytochemical screening of the t inc tur e indi cat ed the pr e s enc e of r educ ing sugar s , anthocyanidins , anthocyanins , anthraquinones, steroids, triterpenoids, phenols, flavanonols, flavanols, flavanones, saponins and tannins catechists. HPLC chromatograms showed peaks at 275 nm and 290 nm, with Rt of 8.91 and 13.57 min, whose corresponding spectra showed absorption maxima which is characteristic of flavones and biflavonols -283 nm and 334 nm. Some metabolites found in the phytochemical screening and detected by HPLC may justify the popular use of A. chica as antimicrobial and antifungal medicine.

2011-01-01T00:00:00Z The quality control of herbal drugs and their intermediates is essential, especially when they are used as feedstock for medicine development. This study aimed at applying the methodologies established by Brazilian legislation for the development of parameters concerning the characterization and quality control of leaf powder and tincture of Arrabidaea chica (H & B) Verlot. Known as cipó-pau (vinestick), carajeru, pariri, among others, it presents antifungal activity and is used in several diseases such as mycosis and ringworm. The physico-chemical characteristics of the plant drug. The phytochemical screening of the t inc tur e indi cat ed the pr e s enc e of r educ ing sugar s , anthocyanidins , anthocyanins , anthraquinones, steroids, triterpenoids, phenols, flavanonols, flavanols, flavanones, saponins and tannins catechists. HPLC chromatograms showed peaks at 275 nm and 290 nm, with Rt of 8.91 and 13.57 min, whose corresponding spectra showed absorption maxima which is characteristic of flavones and biflavonols -283 nm and 334 nm. Some metabolites found in the phytochemical screening and detected by HPLC may justify the popular use of A. chica as antimicrobial and antifungal medicine. Kshirsagar, Sanjay J. Patel, Smit J. Madgulkar, Ashwini R. Bhalekar, Mangesh R. http://sedici.unlp.edu.ar:80/handle/10915/8218 2012-12-22T02:01:47Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 4 Repaglinide is a potent second generation oral hypoglycaemic agent widely used in treatment of non insulin dependent diabetic mellitus. The objective of the present study was to develop sustained release microspheres of repaglinide using ethyl cellulose and PEG 6000 as a matrix forming polymer. Microspheres were prepared by taking various concentrations of ethyl cellulose and PEG 6000 by spray drying technique. Prepared microspheres were evaluated for process yield, drug entrapment, particle size, SEM, FTIR, DSC and in vitro drug release. Process yield and drug entrapment was 40-45 % and 90-95 %, respectively. Particle size ranged in 5-22 µm and SEM study showed spherical shape and rough surface of microspheres. FTIR study and DSC analysis revealed the stable nature and amorphous dispersion of drug in the polymer matrix. In vitro release studies indicate retardation of release upto 12 h which can control both fasting blood glucose level and postprandial blood glucose.

2011-01-01T00:00:00Z Repaglinide is a potent second generation oral hypoglycaemic agent widely used in treatment of non insulin dependent diabetic mellitus. The objective of the present study was to develop sustained release microspheres of repaglinide using ethyl cellulose and PEG 6000 as a matrix forming polymer. Microspheres were prepared by taking various concentrations of ethyl cellulose and PEG 6000 by spray drying technique. Prepared microspheres were evaluated for process yield, drug entrapment, particle size, SEM, FTIR, DSC and in vitro drug release. Process yield and drug entrapment was 40-45 % and 90-95 %, respectively. Particle size ranged in 5-22 µm and SEM study showed spherical shape and rough surface of microspheres. FTIR study and DSC analysis revealed the stable nature and amorphous dispersion of drug in the polymer matrix. In vitro release studies indicate retardation of release upto 12 h which can control both fasting blood glucose level and postprandial blood glucose. Bindaiya, Shailendra K. Sahu, Kapendra Bhaisare, Mukesh Karthikeyan, Chandrabose Moorthy, N.S.H.N. Mehta, Farhad F. Trivedi, Piyush http://sedici.unlp.edu.ar:80/handle/10915/8217 2012-12-22T02:01:47Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 4 A sensitive and specific high performance reversed phase liquid chromatographic method was developed for quantification of citicoline monosodium (CTM) in human plasma. The active drug was isocratically eluted at a flow rate of 1 ml/min at ambient temperature in a nucleosil C18 analytical column with a mobile phase composed of tetrabutyl ammonium hydro gen sulfate buffer (0.005 M, pH5.0): methanol (95:05, v/v). Photodiode array (PDA) was performed at 270 nm and the retention time of the drug was found to be 6.64 min. The lowest limit of quantification (LLOQ) and of detection (LOD) were found to be 30 and 10 ng/ml, respectively. The method was validated and the response was found to be linear in the drug (CTM in spiked plasma) concentration range 150-900 ng/ml. The method was found to be accurate, with ranging from 96.38 to 98.65 % and precise, with intra-day, inter-day as well as analyst-toanalyst precision. The total recoveries of the method ranged between 95.69 and 97.89 %. Stability data revealed that the drug is stable in human plasma under various test conditions and the method can be successfully used for analysis of CTM in human plasma and in pharmacokinetic studies.

2011-01-01T00:00:00Z A sensitive and specific high performance reversed phase liquid chromatographic method was developed for quantification of citicoline monosodium (CTM) in human plasma. The active drug was isocratically eluted at a flow rate of 1 ml/min at ambient temperature in a nucleosil C18 analytical column with a mobile phase composed of tetrabutyl ammonium hydro gen sulfate buffer (0.005 M, pH5.0): methanol (95:05, v/v). Photodiode array (PDA) was performed at 270 nm and the retention time of the drug was found to be 6.64 min. The lowest limit of quantification (LLOQ) and of detection (LOD) were found to be 30 and 10 ng/ml, respectively. The method was validated and the response was found to be linear in the drug (CTM in spiked plasma) concentration range 150-900 ng/ml. The method was found to be accurate, with ranging from 96.38 to 98.65 % and precise, with intra-day, inter-day as well as analyst-toanalyst precision. The total recoveries of the method ranged between 95.69 and 97.89 %. Stability data revealed that the drug is stable in human plasma under various test conditions and the method can be successfully used for analysis of CTM in human plasma and in pharmacokinetic studies. Datir, Sandip B. Nirmal, Sunil A. Ganjare, Anjali B. Patil, Manohar J. Dighe, Nachiket S. Mandal, Subhash C. http://sedici.unlp.edu.ar:80/handle/10915/8216 2012-12-22T02:01:48Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 4 Achyranthes aspera is traditionally used in the treatment of cough and bronchitis and therefore it was our objective to study the effect various extracts of the plant on clonidine and haloperidol induced catalepsy to study its antihistaminic effect. Petroleum ether extract (200 mg/kg, i.p.) of the plant significantly inhibited clonidine-induced catalepsy but not inhibited haloperidol-induced catalepsy. This proves the antihistaminic activity of the plant. The extract was standardized by HPTLC in presence of standard β-sitosterol, which proves that the antihistaminic activity may be due to β-sitosterol.

2011-01-01T00:00:00Z Achyranthes aspera is traditionally used in the treatment of cough and bronchitis and therefore it was our objective to study the effect various extracts of the plant on clonidine and haloperidol induced catalepsy to study its antihistaminic effect. Petroleum ether extract (200 mg/kg, i.p.) of the plant significantly inhibited clonidine-induced catalepsy but not inhibited haloperidol-induced catalepsy. This proves the antihistaminic activity of the plant. The extract was standardized by HPTLC in presence of standard β-sitosterol, which proves that the antihistaminic activity may be due to β-sitosterol. Necchi, Raquel M.M. Maki, Tiago D.T. Canto, Gizele S. do Moresco, Rafael N. Dalmora, Sérgio Luiz Manfron, Melânia Palermo http://sedici.unlp.edu.ar:80/handle/10915/8215 2012-12-22T02:01:48Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 4 We evaluated the antiinflammatory activity of ethanol 70 % extract of Nopalea cochenillifera in a model of induction of granulomatous tissue and the kidney and liver toxicity through serum dosage in rats. During 7 days were administered orally 1.5 ml, 3 times a day, of the ethanol extract of cladodes of N. cochenillifera. We used nimesulide 5 mg/kg/day as positive control and 20 % propylene glycol as a negative control. After the treatment period, we assessed the formation of granulomas and the serum levels of AST, ALT, albumin, creatinine and urea in all groups, noting that the animals treated with the extract showed 53.5 % inhibition formation of granulomatous tissue while the positive control group showed 58.5 %, confirming a significant antiinflammatory activity. There was not a significant elevation of biochemical markers in relation to negative control.

2011-01-01T00:00:00Z We evaluated the antiinflammatory activity of ethanol 70 % extract of Nopalea cochenillifera in a model of induction of granulomatous tissue and the kidney and liver toxicity through serum dosage in rats. During 7 days were administered orally 1.5 ml, 3 times a day, of the ethanol extract of cladodes of N. cochenillifera. We used nimesulide 5 mg/kg/day as positive control and 20 % propylene glycol as a negative control. After the treatment period, we assessed the formation of granulomas and the serum levels of AST, ALT, albumin, creatinine and urea in all groups, noting that the animals treated with the extract showed 53.5 % inhibition formation of granulomatous tissue while the positive control group showed 58.5 %, confirming a significant antiinflammatory activity. There was not a significant elevation of biochemical markers in relation to negative control. Rahman, Mohammad S. Rashid, Mohammad A. Sikder, Al Amin Rahman, Arifur Kaisar, Mohammad A. Hasan, Choudhury M. http://sedici.unlp.edu.ar:80/handle/10915/8214 2012-12-22T02:01:48Z 2011-01-01T00:00:00Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 4 Different extractives of Syzygium cumini seeds were evaluated by free radical (DPPH) scavenging assay, phosphomolybdenum total antioxidant assay and reducing power determination in order to identify promising sources of antioxidants along with its membrane stabilizing activity. The total phenolic content was also determined and expressed in gallic acid equivalent. Here, butylated hydroxytoluene (BHT) and ascorbic acid (ASA) were used as standard antioxidants. The membrane stabilizing activity was assessed by using erythrocytes in hypotonic solution and was compared with acetyl salicylic acid. A positive correlation was observed between total phenolic content and total antioxidant activity as well as reducing power of S. cumini having correlation coefficient (R² ) values of 0.8177 and 0.9818, respectively. In the present studies, the methanol extract and its aqueous and petroleum ether soluble partitionates demonstrated significant antioxidant potentials.

2011-01-01T00:00:00Z Different extractives of Syzygium cumini seeds were evaluated by free radical (DPPH) scavenging assay, phosphomolybdenum total antioxidant assay and reducing power determination in order to identify promising sources of antioxidants along with its membrane stabilizing activity. The total phenolic content was also determined and expressed in gallic acid equivalent. Here, butylated hydroxytoluene (BHT) and ascorbic acid (ASA) were used as standard antioxidants. The membrane stabilizing activity was assessed by using erythrocytes in hypotonic solution and was compared with acetyl salicylic acid. A positive correlation was observed between total phenolic content and total antioxidant activity as well as reducing power of S. cumini having correlation coefficient (R² ) values of 0.8177 and 0.9818, respectively. In the present studies, the methanol extract and its aqueous and petroleum ether soluble partitionates demonstrated significant antioxidant potentials. Sawant, Ramesh L. Wadekar, Jyoti B. Lanke, Prashant D. http://sedici.unlp.edu.ar:80/handle/10915/8213 2012-12-22T02:01:48Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 4 A series of structurally similar isatin analogues with antitubercular activity have been subjected for 2D and 3D QSAR analysis using V life MDS 3.5 software. The compounds were divided into training and test set of 44 and 11 each. Best QSAR models were selected on the basis of various statistical parameters like square correlation coefficient (<sup>2<sup> ), cross validated square correlation coefficient (q<sup>2<sup> ), standard error of estimation (SE) and sequential Fischer test (F). QSAR studies reveals that new isatin analogues with less bulky substitution on nitrogen of first position and at third position electropositive side chain of optimum four atoms length whose terminal atom is substituted with aromatic system bearing polar group may be better antitubercular agents.

2011-01-01T00:00:00Z A series of structurally similar isatin analogues with antitubercular activity have been subjected for 2D and 3D QSAR analysis using V life MDS 3.5 software. The compounds were divided into training and test set of 44 and 11 each. Best QSAR models were selected on the basis of various statistical parameters like square correlation coefficient (<sup>2<sup> ), cross validated square correlation coefficient (q<sup>2<sup> ), standard error of estimation (SE) and sequential Fischer test (F). QSAR studies reveals that new isatin analogues with less bulky substitution on nitrogen of first position and at third position electropositive side chain of optimum four atoms length whose terminal atom is substituted with aromatic system bearing polar group may be better antitubercular agents. Falcão, Deborah Q. Santos, Arith R. Ortiz Silva, Bianca Louro, Ricardo P. Seiceira, Rafael Finotelli, Priscilla V. Ferreira, José Luis P. De Simone, Salvatore G. Amaral, Ana C. F. http://sedici.unlp.edu.ar:80/handle/10915/8212 2012-12-22T02:01:48Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 4 Cymbopogon citratus essential oil (CCEO) is widely used in food, cosmetics and pharmaceutical fields. The aim of this study was to compare two different methods of encapsulating CCEO. The o/w emulsion method was employed here for the first time for producing CCEO nanoparticles with polycaprolactone (PCL) and a molecular inclusion in &beta;-cyclodextrin (CyD) using the precipitation method. The nanoparticles were spherical in shape, with 240.0 nm mean diameter and demonstrated a higher encapsulation efficiency (36.51 %) as the citral content. The efficiency of CCEO/CyD complex was lower (9.46 %) and it showed some specificity for the smallest molecules present in the original oil. It was irregular in shape and had a larger mean diameter (441.2 nm). It was concluded that the o/w emulsion method was the most effective for CCEO encapsulation. The positive findings in this study encourage further research and provide perspectives for the development of phytotherapeutic products from CCEO.

2011-01-01T00:00:00Z Cymbopogon citratus essential oil (CCEO) is widely used in food, cosmetics and pharmaceutical fields. The aim of this study was to compare two different methods of encapsulating CCEO. The o/w emulsion method was employed here for the first time for producing CCEO nanoparticles with polycaprolactone (PCL) and a molecular inclusion in &beta;-cyclodextrin (CyD) using the precipitation method. The nanoparticles were spherical in shape, with 240.0 nm mean diameter and demonstrated a higher encapsulation efficiency (36.51 %) as the citral content. The efficiency of CCEO/CyD complex was lower (9.46 %) and it showed some specificity for the smallest molecules present in the original oil. It was irregular in shape and had a larger mean diameter (441.2 nm). It was concluded that the o/w emulsion method was the most effective for CCEO encapsulation. The positive findings in this study encourage further research and provide perspectives for the development of phytotherapeutic products from CCEO. Figueroa, Lauro Díaz, Francisco López, María Camacho, Abelardo García, Elodia Ozaeta, Rolando http://sedici.unlp.edu.ar:80/handle/10915/8211 2012-12-22T02:01:48Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 4 In this work the antibacterial activity of two pregnenolone-derivatives was evaluated on V. cholerae and E. coli, using a NCCLS broth dilution modified method. Additionally, to delineate the structural chemical requirements of the steroid derivatives as antibacterial agents on E. coli and V. cholerae, other parameters such as the physicochemical descriptors LogP and &pi; were calculated. The results obtained indicate that bacterial growth of E. coli and V. cholerae was inhibited with pregnenolone-vitamin B1 (MIC = 6.64. x 10^-4 mmol/mL) and pregnenolone-carbamazepine (MIC = 3.18 x 10^-4 mmol/mL). Other results showed an increase in LogP and &pi; values in the carbamazepine-pregnenolone conjugate with respect to pregnenolone-vitamin B1. These results suggest that antibacterial activity of two pregnenoloneconjugates can depend of the nature of functional groups involved in their chemical structure that seems to be the key required for their antibacterial activity.

2011-01-01T00:00:00Z In this work the antibacterial activity of two pregnenolone-derivatives was evaluated on V. cholerae and E. coli, using a NCCLS broth dilution modified method. Additionally, to delineate the structural chemical requirements of the steroid derivatives as antibacterial agents on E. coli and V. cholerae, other parameters such as the physicochemical descriptors LogP and &pi; were calculated. The results obtained indicate that bacterial growth of E. coli and V. cholerae was inhibited with pregnenolone-vitamin B1 (MIC = 6.64. x 10^-4 mmol/mL) and pregnenolone-carbamazepine (MIC = 3.18 x 10^-4 mmol/mL). Other results showed an increase in LogP and &pi; values in the carbamazepine-pregnenolone conjugate with respect to pregnenolone-vitamin B1. These results suggest that antibacterial activity of two pregnenoloneconjugates can depend of the nature of functional groups involved in their chemical structure that seems to be the key required for their antibacterial activity. Çelebier, Mustafa Süslü, Incilay Altinöz, Sacide http://sedici.unlp.edu.ar:80/handle/10915/8210 2012-12-22T02:01:48Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 4 A simple, efficient and reliable capillary zone electrophoresis method with diode array detection was developed and validated for the simultaneous determination of olmesartan medoxomil and amlodipine besylate in their binary mixtures. The optimum separation for these compounds was achieved with a fused - silica capillary column (i.d. 75.0 &micro;m, total length 48.5 cm and effective length 40.0 cm) and 40.0 mM citrate buffer at pH 6.0 as the running buffer. The samples were injected hydrodynamically for 3 s at 50 mbar and applied voltage was + 15 kV at 30 °C capillary temperature. Detection wavelength was set at 235 nm. Valsartan was used as internal standard. The method was validated with respect to stability, linearity, sensitivity, precision, accuracy, recovery and selectivity. The linear calibration range was found to be 2.00 - 30.00 &micro;g/mL for olmesartan medoxomil and amlodipine besylate. The limits of detection (LOD) were 0.05 &micro;g/mL for both compounds. The relative standard deviations (RSD) of the proposed method ranged between 1.51 and 2.49 % for intra-day precision and 1.51 and 3.73 % for inter-day precision. The developed and validated method successfully applied for the simultaneous determination of olmesartan medoxomil and amlodipine besylate in their pharmaceutical formulations.

2011-01-01T00:00:00Z A simple, efficient and reliable capillary zone electrophoresis method with diode array detection was developed and validated for the simultaneous determination of olmesartan medoxomil and amlodipine besylate in their binary mixtures. The optimum separation for these compounds was achieved with a fused - silica capillary column (i.d. 75.0 &micro;m, total length 48.5 cm and effective length 40.0 cm) and 40.0 mM citrate buffer at pH 6.0 as the running buffer. The samples were injected hydrodynamically for 3 s at 50 mbar and applied voltage was + 15 kV at 30 °C capillary temperature. Detection wavelength was set at 235 nm. Valsartan was used as internal standard. The method was validated with respect to stability, linearity, sensitivity, precision, accuracy, recovery and selectivity. The linear calibration range was found to be 2.00 - 30.00 &micro;g/mL for olmesartan medoxomil and amlodipine besylate. The limits of detection (LOD) were 0.05 &micro;g/mL for both compounds. The relative standard deviations (RSD) of the proposed method ranged between 1.51 and 2.49 % for intra-day precision and 1.51 and 3.73 % for inter-day precision. The developed and validated method successfully applied for the simultaneous determination of olmesartan medoxomil and amlodipine besylate in their pharmaceutical formulations. Tavares, Vanessa F. Patto, Daniela C.S. Singh, Anil K. Prado, Maria S. A. Kedor-Hackmann, Erika R.M. Santoro, Maria Ines Rocha Miritello http://sedici.unlp.edu.ar:80/handle/10915/8209 2012-12-22T02:01:48Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 4 The aim of this study was to develop and validate selective and sensitive methods for quantitative determination of an antibacterial agent, gemifloxacin, in tablets by high performance liquid chromatography (HPLC) and capillary zone electrophoresis (CZE). The HPLC method was carried out on a LiChrospher® 100 RP-8e, 5 &#956;m (125 x 4 mm) column with a mobile phase composed of tetrahydrofuranwater (25:75, v/v) with 0.5 % of triethylamine and pH adjusted to 3.0 with orthophosphoric acid. The CZE method was performed using 50 mM sodium tetraborate buffer (pH 8.6). Samples were injected hydrodynamicaly (0.5 psi, 5 s) and the electrophoretic system was operated under normal polarity, at +20 kV and capillary temperature of 18 ºC. A fused-silica capillary 40.2 cm (30 cm effective length) x 75 &#956;m i.d. was used. Both, HPLC and CZE could be interesting and efficient techniques to be applied for quality control in pharmaceutical industries.

2011-01-01T00:00:00Z The aim of this study was to develop and validate selective and sensitive methods for quantitative determination of an antibacterial agent, gemifloxacin, in tablets by high performance liquid chromatography (HPLC) and capillary zone electrophoresis (CZE). The HPLC method was carried out on a LiChrospher® 100 RP-8e, 5 &#956;m (125 x 4 mm) column with a mobile phase composed of tetrahydrofuranwater (25:75, v/v) with 0.5 % of triethylamine and pH adjusted to 3.0 with orthophosphoric acid. The CZE method was performed using 50 mM sodium tetraborate buffer (pH 8.6). Samples were injected hydrodynamicaly (0.5 psi, 5 s) and the electrophoretic system was operated under normal polarity, at +20 kV and capillary temperature of 18 ºC. A fused-silica capillary 40.2 cm (30 cm effective length) x 75 &#956;m i.d. was used. Both, HPLC and CZE could be interesting and efficient techniques to be applied for quality control in pharmaceutical industries. Resende, Renata C. Tahan, Gabriella P. Oliveira, Antônio F.F. Maia, Patrícia P. Martins, Isarita http://sedici.unlp.edu.ar:80/handle/10915/8208 2012-12-22T02:01:49Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 4 A simple and rapid SPE-HPLC-DAD method was developed for the determination of 5-fluorouracil (5-FU) in surface samples. A C18 column (250 x 4.6 mm i.d., 5 &micro;m) and a similar pre-column were used for the separation at 25 ºC, using 20 mM ammonium acetate buffer solution pH 4.7: methanol (95:5, v/v) as mobile phase at a flow rate of 1.2 mL/min. Under optimal conditions, the linearity was 0.9993, in a range of 25-100 &micro;g/mL. The limits of detection and quantification were 5 and 25 &micro;g/mL, respectively. The relative standard deviation (%) was below 15 % for the evaluation of precision and the mean recovery was 77 %. The extracting procedure followed HPLC analysis showed their applicability in order to examine 5- FU in surfaces samples. Moreover, it could be suggested that the developed method is an alternative in the monitoring of the occupational exposure to antineoplastic agents, once the analyte in question is considered an indicator for this purpose.

2011-01-01T00:00:00Z A simple and rapid SPE-HPLC-DAD method was developed for the determination of 5-fluorouracil (5-FU) in surface samples. A C18 column (250 x 4.6 mm i.d., 5 &micro;m) and a similar pre-column were used for the separation at 25 ºC, using 20 mM ammonium acetate buffer solution pH 4.7: methanol (95:5, v/v) as mobile phase at a flow rate of 1.2 mL/min. Under optimal conditions, the linearity was 0.9993, in a range of 25-100 &micro;g/mL. The limits of detection and quantification were 5 and 25 &micro;g/mL, respectively. The relative standard deviation (%) was below 15 % for the evaluation of precision and the mean recovery was 77 %. The extracting procedure followed HPLC analysis showed their applicability in order to examine 5- FU in surfaces samples. Moreover, it could be suggested that the developed method is an alternative in the monitoring of the occupational exposure to antineoplastic agents, once the analyte in question is considered an indicator for this purpose. Villanova, Janaina C.O. Consiglieri, Vladi http://sedici.unlp.edu.ar:80/handle/10915/8207 2012-12-22T02:01:49Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 4 The purpose of this paper was to produce controlled-release matrices with 120 mg of propranolol hydrochloride (PHCl) employing hydroxypropyl methylcellulose (HPMC, Methocel® K100) as the gel forming barrier. Although this class of polymers has been commonly used for direct compression, with the intent of use reduced polymer concentrations to achieve controlled drug release, in this study tablets were produced by the wet granulation process. HPMC percentages ranged from 15-34 % and both soluble and non soluble diluents were tested in the 10 proposed tablet compositions. Dissolution testing of matrices was performed over a 12 h period in 1.2 pH medium (the first 2 h) and in pH 6.8 (10 h). Dissolution kinetic analysis was performed by applying Zero-order, First-order and Higuchi models with the aim of elucidating the drug release mechanism. All physical-chemical characteristics such as average weight, friability, hardness, diameter, height, and drug content were in accordance to the pharmacopeial specifications. Taking into account that PHCl is a very soluble drug, low concentrations (15 %) of HPMC were sufficient to reduce the drug release and to promote controlled release of PHCl, presenting good dissolution efficiencies, between 50 % and 63 %. The Higuchi model has presented the best fit to the 15 % HPMC formulations, indicating that the main release mechanism was diffusion. It could be concluded that the application of the wet granulation method reduced matrices erosion and promoted controlled release of the drug at low HPMC percentages.

2011-01-01T00:00:00Z The purpose of this paper was to produce controlled-release matrices with 120 mg of propranolol hydrochloride (PHCl) employing hydroxypropyl methylcellulose (HPMC, Methocel® K100) as the gel forming barrier. Although this class of polymers has been commonly used for direct compression, with the intent of use reduced polymer concentrations to achieve controlled drug release, in this study tablets were produced by the wet granulation process. HPMC percentages ranged from 15-34 % and both soluble and non soluble diluents were tested in the 10 proposed tablet compositions. Dissolution testing of matrices was performed over a 12 h period in 1.2 pH medium (the first 2 h) and in pH 6.8 (10 h). Dissolution kinetic analysis was performed by applying Zero-order, First-order and Higuchi models with the aim of elucidating the drug release mechanism. All physical-chemical characteristics such as average weight, friability, hardness, diameter, height, and drug content were in accordance to the pharmacopeial specifications. Taking into account that PHCl is a very soluble drug, low concentrations (15 %) of HPMC were sufficient to reduce the drug release and to promote controlled release of PHCl, presenting good dissolution efficiencies, between 50 % and 63 %. The Higuchi model has presented the best fit to the 15 % HPMC formulations, indicating that the main release mechanism was diffusion. It could be concluded that the application of the wet granulation method reduced matrices erosion and promoted controlled release of the drug at low HPMC percentages. Mangamoori, Lakshmi N. Yamsani, Madhusudan R. http://sedici.unlp.edu.ar:80/handle/10915/8206 2012-12-22T02:01:49Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 4 In the present study matrix and multilayered matrix tablets of diltiazem HCl were formulated by using guar gum as matrix core component and cellulose derivative, Sodium Carboxy Methyl Cellulose (SCMC) as barrier layers. Marked difference in dissolution characteristics of D3 and D3L3 was observed and showed a statistically significant difference. The study revealed that the matrix tablets prolonged the release, but predominantly in a first order fashion. Layering with SCMC granules on the matrix core, provided linear drug release with zero order kinetics. Mean dissolution time for D3 and D3L3 were found to be 4.17 h and 16.45 h, while dissolution efficiency decreased, indicating slower drug release. In vivo transit time of the formulation D3L3 shows that it crossed the small intestine at 6 h and retained for longer time in colon at 12 h. FT-IR and DSC studies show there is no drug-excipeints interaction. Stability studies portray that no change either in physical manifestation or in dissolution profile after storage at 40 ± 2 °C/RH 75 ± 5 % for 3 and 6 months.

2011-01-01T00:00:00Z In the present study matrix and multilayered matrix tablets of diltiazem HCl were formulated by using guar gum as matrix core component and cellulose derivative, Sodium Carboxy Methyl Cellulose (SCMC) as barrier layers. Marked difference in dissolution characteristics of D3 and D3L3 was observed and showed a statistically significant difference. The study revealed that the matrix tablets prolonged the release, but predominantly in a first order fashion. Layering with SCMC granules on the matrix core, provided linear drug release with zero order kinetics. Mean dissolution time for D3 and D3L3 were found to be 4.17 h and 16.45 h, while dissolution efficiency decreased, indicating slower drug release. In vivo transit time of the formulation D3L3 shows that it crossed the small intestine at 6 h and retained for longer time in colon at 12 h. FT-IR and DSC studies show there is no drug-excipeints interaction. Stability studies portray that no change either in physical manifestation or in dissolution profile after storage at 40 ± 2 °C/RH 75 ± 5 % for 3 and 6 months. Alexandre, Grazielle P. Prado, Maria S. A. Kedor-Hackmann, Erika R.M. Singh, Anil K. Santoro, Maria Ines Rocha Miritello http://sedici.unlp.edu.ar:80/handle/10915/8205 2012-12-22T02:01:49Z 2011-01-01T00:00:00Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 4 Choline citrate (CC) and acetylmethionine (AM) are lipotropic drugs used in several pharmaceutical formulations. The objective of this research was to develop and validate a high performance liquid chromatographic (HPLC) method for simultaneous determination of CC and AM in injectable solutions, aiming its application in routine analysis for quality control of these pharmaceutical formulations. The method was validated using a Shim-Pack® C18 (250 x 4.6 mm, 5 &micro;m) column. The mobile phase was constituted of 25 mM potassium phosphate buffer solution, pH 5.7, adjusted with 10 % orthophosphoric acid, acetonitrile and methanol (88:10:2, v/v/v). The flow rate was 1.1 mL.min^-1 and the UV detection was made at 210 nm. The analyses were made at room temperature (25 ± 1 ºC). The method is precise, selective, accurate and robust, and was successfully applied for simultaneous quantitative determination of CC and AM in injectables.

2011-01-01T00:00:00Z Choline citrate (CC) and acetylmethionine (AM) are lipotropic drugs used in several pharmaceutical formulations. The objective of this research was to develop and validate a high performance liquid chromatographic (HPLC) method for simultaneous determination of CC and AM in injectable solutions, aiming its application in routine analysis for quality control of these pharmaceutical formulations. The method was validated using a Shim-Pack® C18 (250 x 4.6 mm, 5 &micro;m) column. The mobile phase was constituted of 25 mM potassium phosphate buffer solution, pH 5.7, adjusted with 10 % orthophosphoric acid, acetonitrile and methanol (88:10:2, v/v/v). The flow rate was 1.1 mL.min^-1 and the UV detection was made at 210 nm. The analyses were made at room temperature (25 ± 1 ºC). The method is precise, selective, accurate and robust, and was successfully applied for simultaneous quantitative determination of CC and AM in injectables.