vol. 30, no. 08

Short and stereoselective synthesis of α-methylene-β-hydroxy-γ-butyrolactone diastereomers: Structures revised by theoretical investigations

Sat, 01 Jan 2011 00:00:00 GMT

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 8 A short synthetic approach allowed the preparation, in two steps, of (3S,4R)- and (3R,4R)-2- methylene-3-hydroxy-4-(hydroxymethyl)-γ-butyrolactones from 2,3-O-(3-pentylidene)-D-glyceraldehyde, with overall yields of 32 % and 9 %, respectively. The structure of these γ-butyrolactones was revised by experimental and theoretical investigations.

Antidiabetic principle from Eclipta prostrata

Sat, 01 Jan 2011 00:00:00 GMT

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 8 The methanol extract of the whole plant of Eclipta prostrata and one of its isolated compounds, eclalbasaponin II were administered to alloxan-induced diabetic rats for 28 and 7 consecutive days, respectively. During the study, a potent antidiabetic activity was observed. Blood sugar was significantly (p < 0.001) reduced by E. prostrata extract (300 mg/kg) and eclalbasaponin II (10 mg/kg), as compared to untreated diabetic rats. Analyses of alanine aminotransferase (ALT), aspartate aminotransferase (AST) and alkaline phosphatase (ALP) showed no significant (p < 0.001) hepatotoxicity by E. prostrata extractive in alloxan-induced diabetic rats when compared to the diabetic control rats.

Simultaneous determination of caffeic acid and rosmarinic acid in Ziziphora clinopodioides Lam. from different sources in Xinjiang by a novel rapid resolution liquid chromatography method

Sat, 01 Jan 2011 00:00:00 GMT

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 8 A simple and sensitive rapid resolution liquid chromatography method with a short run time was developed for the simultaneous determination of caffeic acid and rosmarinic acid in Ziziphora clinopodioides Lam. A good chromatographic separation was obtained on an XDB-C18 reversed-phase analytical column (50 mm × 4.6 mm, 1.8 μm) by gradient elution with methanol and water containing 1 % acetic acid (v/v) at 0.9 mL/min flow rate. The detection wavelength was set at 330 nm. The mean recoveries of the two compounds were 101.6 % for caffeic acid and 104.2 % for rosmarinic acid. The method was successfully applied to determine the two compounds in 10 Z. clinopodioides Lam. samples of different origins. A significant variation in the contents of the two compounds among the 10 samples was observed. Therefore, this method provides a new basis for the overall routine quality control assessment of Z. clinopodioides Lam.

Improvement of anti inflammatory activity of quercetin with cyclodextrin complexes

Sat, 01 Jan 2011 00:00:00 GMT

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 8 The objective of this study was to enhance the anti-inflammatory activity of quercetin through complexation, by kneading method, with β cyclodextrin (βCD), hydroxy propyl β cyclodextrin (HP-βCD), and sulpha butyl ether β cyclodextrin (SBE-βCD). The anti inflammatory activity was determined by rat paw edema method. The anti-inflammatory activity of the kneaded complexes of quercetin- βCD/ HP-βCD/ SBE-βCD inclusion complexes demonstrated enhanced of anti-inflammatory activity in the order SBE-βCD> HP-βCD> βCD > pure quercetin.

New vaccine for influenza virus H1N1: Pharmacosurveillance of adverse reactions in health staff at Hospital San Luis, Argentina

Sat, 01 Jan 2011 00:00:00 GMT

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 8 In March 2010, the Immunization Program of San Luis Province began a vaccination campaign against influenza A H1N1 with monovalent and trivalent vaccines. Being this the first year that this vaccine is used, and following the recommendations of WHO, we decided to develop pharmacovigilance actions in order to assess its safety. Our objective was to identify, describe and analyze adverse reactions associated with the vaccine against pandemic influenza occurring in health personnel of the Hospital San Luis, through active monitoring of vaccinated employees. An epidemiological descriptive and transversal study was carried out from March to June 2010. We found that 67 % (n = 809) reported adverse reactions associated with the vaccine. Main adverse reactions reported included: pain at injection site (54 %), fatigue, swelling and redness, malaise, headache and fever. The most frequent adverse reactions that have been reported were non-serious and within expectations.

Single RP-HPLC method for simultaneous estimation of pioglitazone, glibenclamide and glibenclamide impurities from a combination drug product

Sat, 01 Jan 2011 00:00:00 GMT

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 8 A simple reversed phase HPLC method was developed for simultaneous estimation of pioglitazone, glibenclamide, and glibenclamide impurities A and B from a combination drug product. The drugs and impurities are well separated using a reverse phase liquid chromatography with C-8 column. The isocratic mobile phase comprising phosphate buffer (pH 5.0): acetonitrile in the ratio of 75:25 (v/v) at 1.0 mL/min flow rate, UV detection at 250 nm, column temperature was maintained at 30 °C and the injection volume was used 150 μL. The proposed method was validated according to the ICH guidelines and proved suitable for routine analysis and quality control testing of these drugs in pharmaceutical preparations.

Anti-inflammatory activity and effect on locomotion of Polygonum persicaria L. (Polygonaceae) extract in rats

Sat, 01 Jan 2011 00:00:00 GMT

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 8 Several species of the Polygonum genera are collectively known in Brazil under the name "erva-de-bicho". In tradicional medicine, these species often mistaken for each other and are probably used for the same therapeutic purpose. In this study, the hydroalcoholic extract of the aerial parts of Polygonum persicaria was isolated, and the phytochemical composition was examined. In addition, the anti-inflammatory activity was tested in rats by paw edema inhibition analysis. The effects on locomotion were tested in rats, using the open field test. Flavonoids, mucilage, saponins, tannins and essential oils were detected. The extract showed anti-inflammatory and decreased locomotion after intraperitoneal administration to rats.

Anticholinesterasic activity of Manilkara subsericea (Mart.) Dubard triterpenes

Sat, 01 Jan 2011 00:00:00 GMT

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 8 Manilkara subsericea (Mart.) Dubard (Sapotaceae) is popularly known in Brazil as "guracica". The species from the genus Manilkara have been studied and several substances were found, including triterpenes. In the present study, we describe the anticholinesterasic activity of an extract of M. subsericea containg beta-amyrin acetate (76.3 %) and alpha-amyrin acetate (23.7 %) using a TLC bioassay.

Glycyrrhizic acid-phospholipid complex: preparation process optimization and therapeutic and pharmacokinetic evaluation in rats

Sat, 01 Jan 2011 00:00:00 GMT

Articulo Latin American Journal of Pharmacy; vol. 30, no. 8 The purpose of the present study was to prepare glycyrrhizic acid-phospholipid complex (GL-PLC) as to improve the oral bioavailability of glycyrrhizic acid (GL), enhance the drug efficacy and reduce the side effects. The uniform experimental design approach was utilized for the process optimization in order to obtain the satisfactory complex. The results of comparison between GL-PLC and free GL indicated that the anti-inflammatory activity of the phospholipid complex was significantly higher than that of free GL at the same dose. The results of pharmacokinetic study displayed that the plasma concentration of glycyrrhetic acid, the metabolite of GL in vivo, increased after oral administration of GL-PLC. The Cmax of GL-PLC was 2.14 times higher than that of free glycyrrhizic acid, while the AUC of GL-PLC was 1.74 times higher than that of free GL. The results proved that GL-PLC improved the lipophilic property of GL, increased the bioavailability and anti-inflammatory activity.

Curcumin inhibits proliferation and metastasis of human hypopharyngeal carcinoma cells

Sat, 01 Jan 2011 00:00:00 GMT

Articulo Latin American Journal of Pharmacy; vol. 30, no. 8 The present study was designed to investigate the effects of curcumin, a natural product derived from turmeric of the herb Curcuma longa, on proliferation, metastasis of FaDu cells, and the relevant mechanisms. Results showed that curcumin could inhibit the proliferation, induce apoptosis of FaDu cells, and arrest the cell-cycle at S phases in a dose-dependent manner. The ability of FaDu cells in migration and invasion was declined significantly after treated with curcumin. Additionally, caspase-9 and caspase-3 were activated, and the expression of Bax and E-cadherin were up-regulated, whereas, the expressions of Bcl-2, MMP-2 and MMP-9 were down-regulated in response to curcumin. In conclusion, these data suggested that curcumin can effectively suppress proliferation and inhibit the invasion and metastasis of FaDu cells via the induction of apoptosis, the blockage of cell cycle as well as the modulation of certain relevant genes.

Molecular research on a hypotensive herb formula and PPARα activation

Sat, 01 Jan 2011 00:00:00 GMT

Articulo Latin American Journal of Pharmacy; vol. 30, no. 8 Surflex-dock method was explored to study interactions between Qingxuanjiangya decoction (QXJYD in abbreviation, a famous hypotensive herb formula from Traditional Chinese Medicine prescription) and Peroxisome proliferators activated receptor-alpha (PPARα) for detecting its pharmacological effects as well as to screen out PPARα agonists. First, 28 compounds with values of PPARα EC50 from reported were introduced as a test set to evaluate the docking accuracy according to the good validation between experimental values and surflex-dock scores (correlation coefficient R = 0.866, RMSD = 1.169 Å, similarity = 0.804). And then, 739 molecules from QXJYD were docked to PPARα by the validated way. The result showed 200 compounds from QXJYD had activity with PPARα and discovered that a flavones compound (moralbanone, extracted from folium mori) with an excellent docking score might be considered as a guide to design a new scaffold of PPARα agonists in the further study.

Evaluation of cisplatin, doxorubicin and paclitaxel inactivation using asepto 75^TM 0.5 %, sodium hypochloride 10 % and sodium thiosulfate 10 % by high performance liquid chromatography (HPLC) and in vitro cytotoxicity test

Sat, 01 Jan 2011 00:00:00 GMT

Articulo Latin American Journal of Pharmacy; vol. 30, no. 8 Antineoplastic agents are considered risk drugs; that is, they can cause harmful effects, such as genotoxicity, carcinogenicity, teratogenicity, as well as fertility alterations, therefore being the exposure of health professionals to these substances considerably worrying. These medicaments must be submitted to physical, chemical and biological analyses, what generates a considerable volume of residues, what also requires treatment. The aim of this work was to evaluate the efficacy of different methods of inactivation concerning cisplatin, doxorubicin and paclitaxel, using high performance liquid chromatography and in vitro cytotoxicity test. The results demonstrated that Asepto 75TM is efficient for chemical and biological inactivation of the three drugs, being the exposure time determinant for cisplatin chemical degradation. Cytotoxicity levels varied from none to slight. In spite of its own degree of cytotoxicity, sodium hypochloride was also effective in the chemical inactivation of the three drugs. Sodium thiosulfate degrader, however, was only effective concerning cisplatin chemical inactivation, presenting no effect on doxorubicin or paclitaxel. The results of the in vitro tests were compatible with those from the chemical evaluation. It can therefore be concluded that the inactivation of cytotoxic drugs prior to waste effectively reduces occupational and environmental risks.

Simultaneous determination of cortisone and cortisol in serum by HPLC-DAD and application for pharmacokinetics

Sat, 01 Jan 2011 00:00:00 GMT

Articulo Latin American Journal of Pharmacy; vol. 30, no. 8 To develop a high performance liquid chromatography method for the simultaneous determination of cortisone and cortisol in rat serum and apply it for pharmacokinetics. After addition of pirfenidone as internal standard (IS), a liquid-liquid extraction with ethylacetate was employed for the sample preparation. Samples were separated on Zorbax SB-C18 column at 25 ºC using mobile phase consisting of acetonitrile-water-0.1 % trifluoroacetic acid with flow rate of 0.9 mL/min, utilizing DAD detection at 246 nm. Excellent liner relationships of the cortisone and cortisol concentrations were obtained from 50 to 6000 ng/mL, with r = 0.9997, 0.9999 respectively, and the lower limit of quantitation (LLOQ) were both 50 ng/mL. The developed method was successfully applied to pharmacokinetic studies of cortisone and cortisol in rats following single dose of 20 mg/kg via intraperitoneal injection.

Optimization and pharmacodynamic evaluation of solid dispersion of gliclazide for dissolution rate enhancement

Sat, 01 Jan 2011 00:00:00 GMT

Articulo Latin American Journal of Pharmacy; vol. 30, no. 8 The present study utilizes approach of solid dispersions (SDs) to improve dissolution rate of Gliclazide (GLZ); a poorly water soluble anti-diabetic drug. Formulations were prepared by solvent evaporation and melt dispersion techniques using poloxamer as hydrophilic carriers. SDs and physical mixtures (PM) were characterized by thin layer chomatography, FTIR spectroscopy, X-Ray Diffractometry, and Differential Scanning Calorimetry. TLC was used to identify any possibility of degradation during preparation and optimize melting temperature for melt dispersion batches, which was supported by FTIR and DSC, showing absence of chemical interaction between the drug and carrier. XRD showed that GLZ was converted to amorphous form. Enhancement in dissolution was found more prominent with melt dispersions compared to solvent evaporation and physical mixtures. In vivo pharmacodynamic bioavailability study was performed for 28 days on alloxan induced diabetic wistar rats. Blood glucose levels were evidently lowered and controlled by SD compared to GLZ alone.

Oral bioavailability of novel genistein sulfonates and their pre-clinical pharmacokinetics

Sat, 01 Jan 2011 00:00:00 GMT

Articulo Latin American Journal of Pharmacy; vol. 30, no. 8 The oral bioavailability of genistein (GE) in its benzensulfonates was studied in search for new drugs or food functional ingredients. The plasma were collected at different points of time after the intragastric or intravenous administration of genistein benzensulfonate (GBS) 40 mg/kg to rats. The GBS and GE contents in plasma were determined by HPLC. The compartment model was fitted and pharmacokinetic parameters were calculated by DAS 2.1.1. The result indicated that the dynamic process of GE was consistent with two compartment model after intragastric or intravenous administration of two GBS prodrugs to rats. The relative oral bioavailability of GE in two prodrugs GBS1 and GBS2 were 159.2 and 253.8 %, respectively. In conclusion, the above results demonstrated that the oral bioavailability of GE in two prodrugs had been improved. Meanwhile, GBS2 was proven to have a higher relative bioavailability prodrug of GE than GBS1.

Effect of Sutherlandia frutescens and Hypoxis hemerocallidea extracts on inflammatory markers in vitro

Sat, 01 Jan 2011 00:00:00 GMT

Articulo Latin American Journal of Pharmacy; vol. 30, no. 8 Immunomodulating effects of Hypoxis hemerocallidea, Sutherlandia frutescens and standard compounds found in these plants were determined. Neither of the extracts, nor the standard compounds were cytotoxic to THP-1 and U937 macrophages. Antioxidant activity of H. hemerocallidea was equivalent to 0.2 mg/mL Trolox. Canavanine showed antioxidant activity comparable to that of curcumin (positive control). Curcumin (9.2 μg/mL) and beta-sitosterol (12.5 μg/mL) reduced IL-1β and IL-8 production significantly (p < 0.05) and decreased the production of TNF-α. Beta-sitosterol (25 μg/mL) and pinitol (50 μg/mL) significantly (p<0.01) decreased extracellular PGE2 levels in U937 macrophages by 12 % and 14 %, respectively. From the current results it would appear that the standard compounds present in the plants are far more effective in modulating the immune system than the extracts.

Synthesis, anti-toxoplasma gondii and antimicrobial activities of 2-hydrazolyl-3-phenyl-5-(4-nitrobenzylidene)-4-thiazolidinone substituted derivatives

Sat, 01 Jan 2011 00:00:00 GMT

Articulo Latin American Journal of Pharmacy; vol. 30, no. 8 A novel series of 2-hydrazolyl-3-phenyl-5-(4-nitrobenzylidene)-4-thiazolidinone substituted (3a-p) has been synthesized. The intermediates 2-hydrazolyl-3-phenyl-4-thiazolidinone substituted (2a-p) were prepared by condensation of benzaldehyde 4-phenyl-3-thiosemicarbazone substituted (1a-p) with ethyl chloroacetate. Theses intermediates were submitted to reaction with ethyl 2-cyano-3-(4-nitrophenyl)-acetate to give the title compounds. The 4-thiazolidinones were screened for their anti-Toxoplasma gondii, and all derivatives promoted decrease of percentage of infection of Vero cells, with elimination of intracellular tachyzoites. The LD50 ranged around 0.5 mM for the intracellular parasites and were higher than 10 mM for Vero cells. According to results of antimicrobial activity, only two compounds showed significant inhibition against M. luteus, but demonstrated higher values of MIC and MBC when compared with standard drug.

Comparative morpho-anatomical study of Baccharis curitybensis Heering ex Malme and Baccharis spicata (Lam.) Baill.

Sat, 01 Jan 2011 00:00:00 GMT

Articulo Latin American Journal of Pharmacy; vol. 30, no. 8 The genus Baccharis L. belongs to Asteraceae and comprises several medicinal species. Both Baccharis spicata (Lam.) Baill. and Baccharis curitybensis Heering ex Malme are traditionally known as "vassoura" (broom) in Brazil. The species B. spicata has antibacterial, antioxidant and trypanocidal activities. Despite of B. curitybensis shows an external morphology quite similar to B. spicata, no chemical and pharmacological study is available about B. curitybensis. Therefore some confusion and/or problems can occur during popular use. In order to differentiate these taxa, the morpho-anatomy of their leaves and stems were investigated according to the usual light and scanning electron microtechniques. The species B. curitybensis reveals smooth and revolute margin, alternate leaf arrangement and non-capitate uniseriate glandular trichomes. Otherwise, dentate and flat margin, opposite leaf arrangement and uniseriate flagelliform non-glandular trichomes are observed in B. spicata. Morphological and anatomical data can be useful for differentiating B. curitybensis and B. spicata.

Chemical composition and anti-inflammatory activity of the essential oil of Schinus terebinthifolius Raddi (Anacardiaceae) fruits

Sat, 01 Jan 2011 00:00:00 GMT

Articulo Latin American Journal of Pharmacy; vol. 30, no. 8 Traditional usage of Schinus terebinthifolius Raddi, popularly known as Brazilian pepper, includes the treatment of inflammatory diseases. Chemical composition of the essential oil extracted of fruits of S. terebinthifolius collected in Mato Grosso do Sul was investigated and the anti-inflammatory activity was evaluated. The essential oil (EOST) obtained in Clevenger and analyzed by GC-MS, exhibited predominance of monoterpenes. The oral administration of EOST significantly inhibited, in dose dependent manner, the carrageenan (Cg) induced rat paw oedema. The observed inhibitions after two hours of Cginjection were 57 ± 8% (100 mg kg-1) for EOST and 66 ± 6% for dexamethasone (DEXA). In another model of inflammation, the oral administration of EOST (100 mg kg-1) reduced 56 ± 11% while DEXA inhibited about 91 ± 5% the Cg-induced leukocyte migration in the air pouch model. Finally, in the persistent inflammation induced by complete Freund's adjuvant (CFA), the daily oral treatment with EOST (200 mg/kg) inhibited 33 ± 6% in 4 days after injection of CFA. The essential oil (EOST) exhibited a marked anti-inflammatory activity and these response profiles differ from others oils collected in different places.

Pharmaceutical development of paracetamol oral suspension

Sat, 01 Jan 2011 00:00:00 GMT

Articulo Latin American Journal of Pharmacy; vol. 30, no. 8 The aims of this work are obtaining and evaluating paracetamol oral suspension 32 mg/mL by qualitative and quantitative planning of the ingredients. The observations of the physical-chemical formulations were based in comparison with the specifications of paracetamol solution contained in the Brazilian Pharmacopoeia and editing with some analysis on the same reference drug (Tylenol® child 32 mg / mL). We sought to develop a low cost and good quality formulation, acceptable to the children's market, since the suspension dosage form is characterized by disguising the unpleasant taste of drugs. The chosen formulation showed good rheology properties, excellent sensory and values of pH, viscosity, density and content within the pharmacopoeia specifications. We obtained a satisfactory formulation, with smaller amount of excipients in relation to the reference product, which can be used by diabetics and is compatible with the official specifications, with respect to physical-chemical tests performed.

vol. 30, no. 08

Short and stereoselective synthesis of α-methylene-β-hydroxy-γ-butyrolactone diastereomers: Structures revised by theoretical investigations

Antidiabetic principle from Eclipta prostrata

Simultaneous determination of caffeic acid and rosmarinic acid in Ziziphora clinopodioides Lam. from different sources in Xinjiang by a novel rapid resolution liquid chromatography method

Improvement of anti inflammatory activity of quercetin with cyclodextrin complexes

New vaccine for influenza virus H1N1: Pharmacosurveillance of adverse reactions in health staff at Hospital San Luis, Argentina

Single RP-HPLC method for simultaneous estimation of pioglitazone, glibenclamide and glibenclamide impurities from a combination drug product

Anti-inflammatory activity and effect on locomotion of Polygonum persicaria L. (Polygonaceae) extract in rats

Anticholinesterasic activity of Manilkara subsericea (Mart.) Dubard triterpenes

Glycyrrhizic acid-phospholipid complex: preparation process optimization and therapeutic and pharmacokinetic evaluation in rats

Curcumin inhibits proliferation and metastasis of human hypopharyngeal carcinoma cells

Molecular research on a hypotensive herb formula and PPARα activation

Evaluation of cisplatin, doxorubicin and paclitaxel inactivation using asepto 75TM 0.5 %, sodium hypochloride 10 % and sodium thiosulfate 10 % by high performance liquid chromatography (HPLC) and in vitro cytotoxicity test

Simultaneous determination of cortisone and cortisol in serum by HPLC-DAD and application for pharmacokinetics

Optimization and pharmacodynamic evaluation of solid dispersion of gliclazide for dissolution rate enhancement

Oral bioavailability of novel genistein sulfonates and their pre-clinical pharmacokinetics

Effect of Sutherlandia frutescens and Hypoxis hemerocallidea extracts on inflammatory markers in vitro

Synthesis, anti-toxoplasma gondii and antimicrobial activities of 2-hydrazolyl-3-phenyl-5-(4-nitrobenzylidene)-4-thiazolidinone substituted derivatives

Comparative morpho-anatomical study of Baccharis curitybensis Heering ex Malme and Baccharis spicata (Lam.) Baill.

Chemical composition and anti-inflammatory activity of the essential oil of Schinus terebinthifolius Raddi (Anacardiaceae) fruits

Pharmaceutical development of paracetamol oral suspension

Evaluation of cisplatin, doxorubicin and paclitaxel inactivation using asepto 75^TM 0.5 %, sodium hypochloride 10 % and sodium thiosulfate 10 % by high performance liquid chromatography (HPLC) and in vitro cytotoxicity test