vol. 29, no. 07

Osmotic and activity coefficients of aqueous solutions of the anesthetic drugs lidocaine-HCl and procaine-HCl at 298.15 K

2012-12-28T02:01:35Z

Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 7 Osmotic and activity coefficients were measured for aqueous solutions of Lidocaine-HCl and Procaine-HCl using the isopiestic method at 298.15 K. The results were fitted to the Pitzer equation and the parameters were calculated. A good correlation with the Pitzer model was found. The osmotic coefficients thus obtained were analyzed by comparing them with the Debye-Hückel limiting law. The results are discussed in terms of ion-solvent and ion-ion interactions.

Microscopic characters of the leaf and stem of Brunfelsia pilosa Plowman (solanaceae)

2012-12-28T02:01:37Z

Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 7 Species of Brunfelsia, whose flowers change colour progressively from violet to white, are popularly known as yesterday-today-tomorrow and used in folk medicine, mainly as anesthetic and diuretic. Based on ethnobotanical surveys, they have been investigated chemically and pharmacologically for expanding the knowledge on the native medicinal flora and for searching bioactive compounds. In order to contribute to pharmacognostic analyses, especially in distinguishing the species B. pilosa Plowman from the allied B. uniflora (Pohl) D. Don, this work has aimed to study the microscopic characters of the leaf and stem of the former. Mature leaves and young stem fragments were fixed in FAA, freehand sectioned transverse and longitudinally, and stained with astra blue and basic fuchsine. Microchemical tests and scanning electron analysis were also performed. The leaf is hypostomatic, having predominantly paracytic stomata. Multicellular non-glandular trichomes and capitate glandular ones are found on both surfaces. The mesophyll is dorsiventral and the midrib is traversed by a bicollateral vascular bundle in open arc. The stem, in incipient secondary growth, shows a uniseriate epidermis and the phellogen is formed in the sub-epidermal layers. The cortex has angular collenchyma, chlorenchyma and a starch sheath, and the vascular system shows external and internal phloem. Crystals of calcium oxalate are seen in the leaf and stem.

Intervenção farmacêutica em problemas relacionados com medicamentos em ambiente hospitalar: um estudo piloto realizado em um hospital do sul do Brasil

2012-12-28T02:01:37Z

Comunicacion Pharmaceutical intervention in medicine related problems in hospital: a pilot study performed in a hospital of south Brasil Latin American Journal of Pharmacy; vol. 29, no. 7 O objetivo deste estudo foi detectar problemas relacionados aos medicamentos (PRM) e avaliar a aceitabilidade das intervenções farmacêuticas pelos médicos. Este estudo foi realizado em um hospital geral do Sul de Santa Catarina, Brasil. Todos os pacientes (27) investigados tomaram mais de 5 medicamentos (média 8,3 ± 2,8). 27,5 % dos medicamentos utilizados foram agentes do sistema nervoso central, 25,7 % foram agentes cardiovasculares, 17,1 % dos medicamentos foram usados para afetar a coagulação do sangue e tratamento de anemias e 14,9 % medicamentos que atuam sobre o trato gastrointestinal. Foram realizadas 31 intervenções farmacêuticas relacionadas com PRM (87,1 %) e necessidade de exames ou diagnósticos complementares (12,9 %). 63,0 % dos PRM relacionados foram manifestados. 48,0 % das intervenções farmacêuticas aceitas foram relacionados a PRM. Ficou claro que os PRM em pacientes polimedicados podem ser identificados por farmacêuticos mostrando o seu papel no uso racional de medicamentos em ambiente hospitalar; The aim of this study was to detect medicine-related problems (MRP) and to evaluate physicians' acceptability of pharmaceutical interventions. This study was conducted in a general hospital in southern Santa Catarina, Brazil. All patients (27) investigated took more than 5 medications (mean 8.3 ± 2.8). 27.5 % of the medications used were central nervous system agents, 25.7 % were cardiovascular agents, 17.1 % were drugs used to affect blood clotting and agents used in anemia, and 14.9 % were drugs that act on the gastrointestinal tract. 31 pharmaceutical interventions were performed related to MRP (87.1 %) and to complementary diagnostic exams (12.9 %). 63.0 % of the listed MRP were reported. 48.0 % of the pharmaceutical interventions accepted by the physicians were related to MRP. It was clear that MRP in polymedicated patients can be identified by pharmacists, playing their role in promoting the rational use of medicines in hospital settings

Analgesic and anti-inflammatory activities of saponified fraction from Annona reticulata L. Bark

2012-12-28T02:01:38Z

Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 7 The saponified petroleum ether extract (SPE) of the Annona reticulata L. bark were studied for fatty acid composition by GC-MS analysis. Six fatty acids amounting 86.68% of the total contents were identified. The composition of saturated and unsaturated fatty acid was 22.10 % and 64.58 %, respectively. SPE at the doses of 12.5, 25 and 50 mg/kg body weight showed significant central as well as peripheral analgesic, along with anti-inflammatory activity.

Chemical composition and antibacterial activity of the essential oil from bark of Ocotea puberula (Rich.) Ness

2012-12-28T02:01:38Z

Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 7 Ocotea puberula (Rich.) Nees, known as canela-guaicá and canela-sebo, is a native woody species from Brazil. O. puberula has been used by indigenous communities to treat skin diseases and tumours. The aim of this work was to evaluate the chemical composition and antibacterial activity of the essential oil obtained by hydrodistillation from barks of O. puberula. Gas chromatography/mass spectrometry analysis showed spathulenol, β-pinene, bicyclogermacrene, germacrene D and α-pinene as the major volatile components. In the antibacterial activity, a very low response was demonstrated

Voltammetric determination of melatonin in tablet dosage forms and human serum

2012-12-28T02:01:38Z

Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 7 The electrochemical oxidation of melatonin is studied in Britton-Robinson buffer in the pH range 2.2-11.8 by cyclic voltammetry at glassy carbon electrode. Three irreversible, diffusion-controlled oxidation peaks were obtained. The utility of using differential pulse and square wave techniques for determination of melatonin was examined. Different parameters affecting the peak current were analylzed and at optimum conditions, linear calibration plots from 0.02-0.5 mM and 0.04 to 0.5 mM of melatonin were obtained applying the two techniques, respectively. The differential pulse mode was successfully applied to the determination of melatonin in commercial tablets containing about three-folds of vitamin B6 without previous separation. The same technique was also used for melatonin determination in human serum with acceptable accuracy.

Antioxidant, antimicrobial and cytotoxic activities of Corypha taliera Roxb

2012-12-28T02:01:39Z

Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 7 The methanol extract of Corypha taliera fruits as well as its n-hexane, carbon tetrachloride, dichloromethane and aqueous soluble fractions were subjected to screening for antioxidant, antimicrobial and cytotoxic activities. The methanolic crude extract exhibited the highest antioxidant activity (IC50 19.33 μg/ml as compared to 9.5 μg/ml for the standard agent, BHT). The crude methanol extract and its carbon tetrachloride, dichloromethane and aqueous soluble fractions showed mild to moderate inhibition of microbial growth against some of the tested organisms. All the extractives exhibited strong cytotoxic properties, among which the methanol extract revealed the strongest cytotixicity (LC50 = 0.43 μg/ml).

Validated spectrophotometric methods for simultaneous estimation of acetaminophen, chlorpheniramine maleate and cafeine in pure and tablet dosage form

2012-12-28T02:01:39Z

Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 7 Two methods for simultaneous estimation of acetaminophen, chlorpheniramine maleate and caffeine in pure and tablet dosage form have been developed. Method I employs formation and solving of simultaneous equation using 246.4 nm, 264.4 nm, and 272 nm as the λ_max of acetaminophen, chlorpheniramine maleate and caffeine respectively in 0.1N HCl. Method II is a multi-component spectrophotometric analysis in which the instrument is preprogrammed to collect and compile the spectral data from the scan of standards and produces the result by matrix calculations. These methods are validated for accuracy, precision, linearity, specificity and sensitivity as per ICH norms. Validation studies are statistically significant. Calibration curves are linear over the concentration ranges of 5-50 μg/mL for acetaminophen, 5-25 μg/mL for both chlorpheniramine maleate and caffeine. High recovery reveals the reliability of the methods for quantitative study in tablet formulation. The methods are rapid, cost-effective and can be used as quality-control tool for routine quantitative analysis of acetaminophen, chlorpheniramine maleate and caffeine in pure and tablet dosage form.

Development and physicochemical evaluation of bilayered floating tablet of diltiazem hydrochloride prepared from Plantago ovata seed husk

2012-12-28T02:01:39Z

Comunicacion Latin American Journal of Pharmacy; vol. 29, no. 7 The aim of the present study is to prepare bilayered floating tablets of diltiazem with different ratios of polymers like HPMC K4M, carbopol 934 P, sodium alginate, Plantago ovata seed husk (psyllium) and to carry out evaluation of the physicochemical parameters of tablets like hardness, friability, content uniformity, weight variation, in vitro buoyancy and in vitro dissolution profiles. In vivo X-ray study was done in human volunteers to determine the floating characteristics of the placebo tablets for a period of 12 h.

Evaluation of ethanol extracts of leaves and fruit of Piper sarmentosum for in vivo hepatoprotective activity

2012-12-28T02:01:39Z

Articulo Latin American Journal of Pharmacy; vol. 29, no. 7 The present study is aimed to describe hepatoprotective activity of extracts of a medicinal plant, Piper sarmentosum, in rats against CCl₄-induced toxicity. Seven groups of Sprague Dawley rats each containing six animals were treated as: group I (CCl₄), group II (control), group III and IV (fruit extract 500 and 250 mg/kg, respectively), group V and VI (leaf extract 500 and 250 mg/kg, respectively) and group VII (vitamin-E). The extracts and vitamin-E were administered orally for 14 days whilst equivalent amount of sample vehicle was administered to CCl₄ and control groups. Four hour following the last dose, a single dose of CCl4 (1.5 mg/kg, 1:1 olive oil) was administered orally to animals of all the groups except control. After 24 h blood was collected for the determination of hepatic function markers, and the animals were sacrificed to get liver for histology. Comparison of hepatic function markers and histology of pretreated and CCl₄ groups indicated that both the extracts in the two doses had protected liver from CCl₄ toxicity (P < 0.05). It is concluded from the present study that use of the plant as a vegetable or in the form of extracts may be valuable to protect liver from oxidative stress in hepatitis and long-term therapy

Therapeutic potential of Emblica officinalis L. fruit extract on ischemia reperfusion Injury induced acute renal failure in rat

2012-12-28T02:01:39Z

Articulo Latin American Journal of Pharmacy; vol. 29, no. 7 The present study was designed to explore the ameliorative effect of hydroalcoholic extract of Emblica officinalis (HAE) on renal ischemia reperfusion (I/R) injury induced acute renal failure (ARF). Rats were subjected to administration of HAE (250 and 500 mg/kg, p.o. for 10 days) before one hour of the ischemia (30 min) reperfusion (24 h) process on the 10th day of experiment. For evaluating the effect of HAE on acute renal failure, Blood urea nitrogen (BUN) and creatinine (Cr) were estimated in serum sample whereas, N-acetyl β-d-glucosaminidase (NAG) was estimated in urine sample. Further, renal tissue was used to evaluate the oxidative stress markers and histopathological changes. The results demonstrated that I/R caused marked changes in various biomarker levels. However, treatment with HAE significantly attenuated these changes. Histopathological evaluation also revealed protective role of HAE on renal cortex and tubular cells. These effects clearly indicated that HAE produced renoprotective effect against I/R induced acute renal failure

Sodium alginate microspheres containing multicomponent inclusion complex of domperidone

2012-12-28T02:01:39Z

Articulo Latin American Journal of Pharmacy; vol. 29, no. 7 Sodium alginate microspheres of domperidone for intranasal systemic delivery were developed to eliminate first pass metabolism, improve patient compliance and obtain improved therapeutic efficacy in treatment of migraine, gastro-esophageal reflux and chemotherapy induced nausea and vomiting. Domperidone was encapsulated as ternary inclusion complex with β-cyclodextrin and citric acid to improve solubility. The phase solubility studies were performed in order to select suitable acid and ternary inclusion complex was prepared by kneading method. The complex was characterized by differential scanning calorimetry, X-ray diffraction and Fourier transform infrared spectroscopy. In vitro dissolution study was carried out in simulated nasal electrolyte solution, pH 6.4. The microspheres of optimised ternary inclusion complex were prepared by emulsification-cross-linking method and were evaluated for particle size, encapsulation efficiency, equilibrium swelling degree, in vitro mucoadhesion and in vitro drug release. The effect of various formulation variables such as drug loading, polymer concentration, crosslinking agent concentration and cross-linking time on microsphere characteristics were studied. The microspheres size range was 57.63-65.3 µm, whereas the percentage drug encapsulation was within the range 15-50 %. All microspheres showed good bioadhesive properties. The formulation variables influenced the drug release profile. The treatment of in vitro release kinetics with kinetic equations indicated that the domperidone release followed Higuchi's matrix model.

Separation and purification of effective constituents of Rhizoma Paridis saponins by serum pharmacochemistry guiding

2012-12-28T02:01:39Z

Articulo Latin American Journal of Pharmacy; vol. 29, no. 7 Oral administration to rats of Rhizoma Paridis saponins (RPS) from Paris polyphylla var. yunnanensis extracts have been found to show strong anti-tumor activity, but the effective constituents were not known. To detail the effective components in RPS, we investigated the serum pharmacochemistry after oral administration of RPS and detected eight kinds of Paridis saponins in the rat serum. Then we purposefully purified a mixture (PM) from RPS to further research. By comparison of tumor weight, spleen index, antitumor rate and numbers of metastases, PM showed a considerable activity as RPS. In conclusion, the serum pharmacochemistry can help us purposefully to separate and purify RPS and to obtain a potential antitumor agent which may be better than parent drugs.

Comparison of the antioxidant effects of lipid extracts of Roystonea regia (D-004) and saw palmetto on blood oxidative variables of healthy men

2012-12-28T02:01:39Z

Articulo Latin American Journal of Pharmacy; vol. 29, no. 7 D-004, a lipid extract of Roystonea regia fruits that prevents testosterone-induced prostate hyperplasia in rodents, and saw palmetto (SP) lipid extract, used to treat benign prostate hyperplasia, have been shown antioxidant effects. This randomized, double-blind study compared their antioxidant effects in forty healthy men randomised to D-004 or SP (320 mg/day) capsules for 8 weeks. D-004 significantly (p < 0.001) reduced plasma malondialdehyde (MDA) (32.7 %), sulphydril groups (SH-G) (24.6 %) and (p < 0.01) total hydroxyperoxides (TOH) (26.5 %) values and increased (p < 0.001) total antioxidant status (TAS) (44.1 %) and catalase (CAT) (100.0 %) activity. Treatment with SP lowered (p < 0.001) MDA (26.6 %), SH-G (24.1 %), (p < 0.01) TOH (26.3 %) values, and raised (p < 0.001) TAS (57.4 %) and (p < 0.01) CAT (85.7 %) activity. Both treatments were similarly effective and well tolerated. Concluding, D- 004 and SP (320 mg/day) for 8 weeks similarly reduced plasma lipid peroxidation (MDA, TOH) and protein oxidation (SH-G) markers, increased TAS and CAT activity and were well tolerated in healthy men.

Preparation and pharmacokinetic studies of mucoadhesive oral multiple unit systems of metronidazole

2012-12-28T02:01:40Z

Articulo Latin American Journal of Pharmacy; vol. 29, no. 7 The objective of the present study was to investigate the applicability of matrix type chitosan treated alginate multiple unit systems (MUS) for sustained release of metronidazole prepared by ionotropic gelation method. Spherical MUS with 0.64 ± 0.95 to 0.75 ± 0.38 mm length and 0.63 ± 0.34 to 0.74 ± 0.28 mm breadth and 71.60 ± 0.42 to 82.15 ± 0.35 % entrapment efficiency were produced. The fluoroscopic study reveals that the MUS was retained in gastrointestinal tract (GIT) for more than 5 h and found to be distributed throughout the GIT. The in vivo evaluation in healthy human volunteers of the MUS and that of Flagyl® IR tablets each containing 400 mg drug revealed that the MUS showed improved pharmacokinetic parameters to Flagyl® producing a significantly different (p < 0.05) AUC. This study demonstrates that the MUS could be a good alternative to immediate release tablets to deliver metronidazole and expected to be less irritant to gastric and intestinal mucosa.

A quantitative method using one marker for simultaneous assay of steroidal saponins in rhizoma paridis

2012-12-28T02:01:40Z

Articulo Latin American Journal of Pharmacy; vol. 29, no. 7 Current quality control patterns are limited to industrial application, for most the natural chemical reference substances are expensive and unavailable. Here in, quantitative analysis of multi-components with single marker (QAMS) method, is established and validated to simultaneously determine five steroidal saponins (Paris-VII, Paris-H, Paris-II, Dioscin , Paris-I) in Rhizoma Paridis. Using Paris-I as the contrast, the relative correction factors (RCF) of the other four steroidal saponins are determined by HPLC-UV. With in the linear ranges, the values of RCF of Paris-I to Paris-VII, Paris-H, Paris-II and Dioscin are 0.877, 1.087, 0.975 and 1.127, respectively. The RCF has a good reproducibility in various instruments, chromatographic columns (RSD = 0.88 % ~ 4.52 %). According to their RCF, five steroidal saponins are simultaneously determined in Rhizoma Paridis by one marker.

In vitro antibacterial activities of silver (I) 4-substituted benzenesulfonate derivatives

2012-12-28T02:01:40Z

Articulo Latin American Journal of Pharmacy; vol. 29, no. 7 A new series of silver (I) 4-substitutedbenzenesulfonate derivatives (1-8) have been synthesized in order to search for new potential antibacterial agents. The antibacterial activity of 1-8 against various strains of bacteria has been determined. Compounds 2-4 (silver (I) 4-methylbenzenesulfonate (2), silver (I) 4-methoxybenzenesulfonate (3), and silver (I) 4-aminobenzenesulfonate (4)) showed broad spectrum of antibacterial activities against both Gram-positive (methicillin-resistant Staphylococcus aureus, Staphylococcus aureus, Bacillus subtilis, Enterococcus faecalis and vancomycin-resistant Enterococcus faecalis) and only one Gram-negative bacterium (Shigella sonnei). The Structure-Activity Relationship (SAR) has also been reported.

Inhibition of tumor cell proliferation and induction of apoptosis in 95-D lung cancer cells by drimartol A from hairy root cultures of Artemisia annua

2012-12-28T02:01:40Z

Articulo Latin American Journal of Pharmacy; vol. 29, no. 7 Drimartol A (DA), a sesquiterpene courmarin ether, was isolated from the cultured hairy roots of A. annua for the first time, and no biological activity of DA has ever been reported. In this work, DA was shown to possess interesting cytotoxic activities against the human tumor cell lines of HO8910 (ovary), 95-D (lung), QGY (liver) and HeLa (cervix) by MTT assay, whose IC50 values were ranged within 17.94-22.3 μM for 24h. Given that treatment of lung cancer is a priority of our interest, induction of apoptosis by DA in the human lung tumor cell line 95-D was focused. The 95-D cell growth was inhibited in a time dependent manner and its cell cycle was arrested in the G2 phase by DA. The apoptotic rate of the cells increased in a dose-dependent manner. DA also increased the activity of caspase-9 and -3 and caused a decrease in the mitochondrial membrane potential. These results revealed that DA could efficiently induce 95-D cell apoptosis through mitochondrial dependent pathway, and it may be a potential chemotherapeutic agent.

Synthesis of biodegradable microspheres of tramadol by simple phase separation technique and their in vitro evaluation

2012-12-28T02:01:41Z

Articulo Latin American Journal of Pharmacy; vol. 29, no. 7 Biodegradable microspheres of Tramadol Hydrochloride (TmH) were developed using simple phase separation technique. Poly lactide-co-glycolide (PLGA) was employed as a release controlling polymer. Simple phase separation method was adopted to prepare microspheres; Dichloromethane (DCM) and Liquid Paraffin (LP) were employed as solvent and non-solvent respectively. Five kinetic models were applied to assess and describe the mechanism and pattern of TmH release from biodegradable microspheres. Biodegradable microspheres were subjected to FTIR, DSC and XRD, to evaluate TmH-PLGA interaction. Retardation in the release of TmH was observed as PLGA concentration was increased. Kinetics of drug release was following higuchi model. The microspheres exhibited no interaction between TmH and PLGA. Biodegradable microspheres of TmH can be produced using phase separation method. Microspheres were stable with no drug-polymer interaction. The accelerated stability studies also ensured the physicochemical integrity as differences of release profile over the period of three months were insignificant.

Biphasic gastroretentive drug delivery system of acyclovir: formulation and in vitro evaluation

2012-12-28T02:01:41Z

Articulo Latin American Journal of Pharmacy; vol. 29, no. 7 A biphasic gastroretentive drug delivery system of acyclovir consisted of loading dose tablet and floating multiple matrix tablets was prepared by direct compression process. The delivery system was designed by hydroxy propyl methyl cellulose as retardant polymer with an effervescent component to get the desired buoyant and sustained release characteristics. All formulations compile within the limits. The FTIR studies did not show any evidence of an interaction between acyclovir and polymers. Dissolution studies revealed biphasic drug release pattern, with loading dose released within 30 min and floating multiple matrix tablets provided zero order sustained release profile for 12 h. It is concluded that floating multiple matrix tablets designed were particularly suitable as gastro retentive drug delivery system with anomalous non-fickian diffusion mechanism. The stability studies showed no significant change in dissolution profiles (f₂ value > 50).