vol. 30, no. 02

Effect of monocrotaline on blood-brain barrier permeability in rats

2019-07-01T04:03:35Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 2 We studied if monocrotaline (MCT) portal hypertensive model modifies blood-brain barrier (BBB) condition. Male Wistar rats were used: Group MCT injected i.p. with MCT (60 mg/kg of body weight) and Group Sham (GS) with saline. Forty-four days after injection rats were sacrificed. Trypan blue and Evans blue tests were performed to evaluate BBB integrity in both groups. In cerebrospinal fluid (CF), protein and glucose were determined. Alanine aminotransferase (ALT), aspartate aminotransferase (AST), and alkaline phosphatase (AP) were measured in serum samples. Portal pressure rose after MCT injection. Trypan blue diffused into hippocampus, Evans blue increased concentrations in brain of Group MCT and CF showed an increase in protein and glucose content in Group MCT. Serum AST, ALT and AP activities were significantly increased in Group MCT rats. It is suggested that liver damage and vasoconstrictor substances could produce portal hypertension, associated to toxic effects on brain and modifying thereby the BBB permeability.

Docking studies of few substituted 5-benzyl-2, 4-thiazolidinedione with PPAR-γ for antidiabetic activity

2019-07-01T04:03:34Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 2 Docking studies of few substituted 5-benzyl-2, 4-thiazolidinedione moiety, which acts as peroxisome proliferator-activated receptor γ agonist was performed by using Glide v4.5. The docking studies reveal hydrogen bond formation to Thr241 with Gscore -7.22 and energy -62.2 kcal/mole. We found hydrogen bond formation of most of compounds with good Gscore and low energy as compared to the most active rosiglitazone.

Effect of Tephrosia purpurea roots extracts on acetic acid induced colitis in mice

2019-07-01T04:03:32Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 2 Tephrosia purpurea L. (Leguminosae), commonly known as Unhali in Marathi is a copiously branched perennial herb. Traditionally the roots of this plant are used in the treatment of ulcer and colic pain. So the present work was undertaken to validate its use in the treatment of ulcerative colitis by using suitable scientific methods. Shade dried and coarsely powdered roots were subjected to successive extraction with ethanol and water. The dried extracts (100 and 200 mg/kg) were screened for ulcerative colitis using the method acetic acid induced ulcerative colitis in mice. Macroscopical study of the colon, level of myeloperoxidase in colon and histopathology of the colon tissue were studied for the assessment of the activity. Results showed that aqueous extract was significantly effective in the treatment of ulcerative colitis at dose of 200 mg/kg. It can be concluded that the polar constituents of T. purpurea L. may be useful in the treatment of ulcerative colitis.

Cardioprotective effect of rutin considering cardiac enzyme level in induced myocardial infarction

2019-07-01T04:03:30Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 2 The present study was designed to investigate effects of rutin on isoproterenol induced myocardial infarction (MI) by considering enzyme level in rats. Rats were treated with rutin contineously for 10 days (10 mg/kg/day, i.p.,); MI were induced by treating rats with isoproterenol for last 2 consecutive days (5.25 and 8 mg/kg, i.p). Protein kinase C (PKC), malonylaldehyde (MAL), Glutathione (GSH), superoxide dismutase (SOD) and survival rate were evaluated. Rutin enhanced survival rate evaluated at the end of experiment. Result shows significant decrease in level of PKC (P < 0.001) and MAL enzyme (P < 0.01) while elevation of GSH (P < 0.001) and SOD (P < 0.001) level in pretreated rutin + isoproterenol group and pretreated rutin group as compared to isoproterenol treated group indicates cardioprotective effect of rutin. The results indicate that Rutin significantly reduces myocardial infarction and emphasize the beneficial action in prevention of MI.

Isolation of a bromotyrosine derivative compound of a bioactive fraction from the marine sponge Iotrochota birotulata from the Urabá Gulf (Colombia)

2019-07-01T04:03:28Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 2 Ethanol and dichloromethane extracts from the marine sponge Iotrochota birotulata collected in the Urabá Gulf (Colombia) were tested against three human tumor cellular lines, including lung (A- 549), colon (HT29) and breast (MDA-MB-231), at 1 µg/mL, 5 µg/mL and 25 µg/mL. The most bioactive extract (ethanol), was separated by flash column chromatography obtaining six fractions which biological activity was evaluated on the same cellular lines A-549, HT29 and MDA-MB-231, at 1µg/mL, 5 µg/mL and 25 µg/mL. The bioassay results showed that both extracts and two of the fractions totally inhibited the growing of the cellular line A549 at 25 µg/mL, while the most active fraction showed total inhibition of the growing of the three tumor cell lines on the three evaluated concentrations. The most active fraction was separated by reversed phase HPLC which allowed isolating and then characterizing by mono- and bidimensional NMR, a halogenated compound derived from the bromotyrosine.

Syntheses and antimicrobial activities of 2, 3-disubstituted-4-thiazolidinone derivatives

2019-07-01T04:03:27Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 2 Ten new 4-thiazolidinone derivatives have been synthesized from the alkanoic acids. Alkanoic acid hydrazides (I) on refluxing with aromatic aldehydes in the presence of a catalytic amount of glacial acetic acid in methanol furnish corresponding hydrazones (II). Thioglycolic acid react with (II) in methanol yield the title compounds (III). These 4-thiazolidinone derivatives were characterized by CHN analysis, IR and 1H NMR spectral data. All the compounds were evaluated for their in vitro antimicrobial activity against two Gram negative strains (Escherichia coli and Pseudomonas aeruginosa) and two Gram positive strains (Bacillus subtilis and Staphylococcus aureus) and fungal strain Candida albicans and Aspergillus niger. All newly synthesized compounds exhibited promising results.

Histological evaluation on Brazilian green propolis effect in tissue repair of Wistar rats cutaneous wounds

2019-07-01T04:03:25Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 2 This study aimed to evaluate the action of Brazilian green propolis (5%) topic use on cutaneous wound healing in rats, by inflammatory cell counting. Ten Wistar rats were separated in groups 24 h and 72 h, were trichotomized under anesthesia on cervical-dorsal region, and 2 wounds were provoked with a biopsy punch (5 mm diameter). Left wound underwent Brazilian green propolis topic treatment, and right wounds received nothing. Tissue samples were processed for light microscopy with hematoxilineosin., and leucocytes, macrophages and fibroblasts were counted using a histometric reticule in ocular lens. In both groups, within 24 and 72 h evolution, treated wounds demonstrated significant bigger means for leucocytes, macrophages and fibroblasts. Brazilian green propolis resulted in inflammatory cell quantity increase, suggesting its action on tissue repair process.

Determination of the anti-diabetic effect of methanolic extract of Sphaeranthus indicus L. on alloxan induced diabetic rabbits

2019-07-01T04:03:24Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 2 The aim of present study was to determine the anti-diabetic effect of methanolic extract of Sphaeranthus indicus L. (SMe) in alloxan induced diabetic rabbits. It was further aimed to determine the effect of SMe on various biochemical parameters, namely blood glucose levels, total cholesterol, lipoproteins (HDL and LDL), liver functions (SGOT and SGPT), serum creatinine and urea level in alloxan induced diabetic rabbits. Rabbits were divided into five groups: one non-diabetic control, treated with vehicle and four experimental (diabetic) groups. The experimental groups can be described as diabetic negative control, treated with vehicle, diabetic positive control, treated with 80 mg/kg of diamicron, a reference drug; and diabetic treated with 150 or 300 mg/kg of SMe. Pre- and post-experimental lipid profile, liver function and kidney function of rabbits was determined. The SMe at the dose of 300 mg/Kg body weight significantly (p < 0.05) reduced the blood glucose level, plasma total cholesterol, triglycerides and LDL in treated rabbits as compared to diabetic rabbits. This dose significantly increased the level of HDL (36.95 ± 2.95) in treated group as compared to diabetic group. The activity of SGOT and SGPT also significantly (p < 0.05) decreased in treated diabetic rabbits. The effect of SMe treatment on serum creatinine values was non-significant (p > 0.05).

Determination of tetramethylpyrazine in rat plasma by liquid chromatography/electrospray mass spectrometry

2019-07-01T04:03:21Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 2 A sensitive and selective liquid chromatography/electrospray mass spectrometry (LC-ESIMS) method for determination of tetramethylpyrazine in rat plasma was developed. After addition of phenacetin as internal standard, protein precipitation by acetonitrile was used as sample preparation. Chromatographic separation was achieved on a Zorbax SB-C18 (2.1 mm×150 mm, 5 µm) column with (40:60, v/v) acetonitrile-water containing 0.1 % formic acid as mobile phase. Electrospray ionization (ESI) source was applied and operated in positive ion mode; selected ion monitoring (SIM) mode was used to quantify tetramethylpyrazine using target fragment ions m/z 136.9 for tetramethylpyrazine and m/z 179.8 for the IS. Calibration plots were linear over the range of 20-4000 ng/mL for tetramethylpyrazine in plasma. Lower limit of quantitation (LLOQ) for tetramethylpyrazine was 20 ng/mL. Mean recovery of tetramethylpyrazine from plasma was in the range 95.4-97.2 %. RSD of intra-day and inter-day precision were less than 9 %, respectively. This method is simple, sensitive and fast enough to be used in pharmacokinetic research for determination of tetramethylpyrazine in rat plasma.

Effects of oral treatment (60 Days) with D-004, a lipid extract from Roystonea regia fruits, on rat prostate hyperplasia and oxidative markers

2019-07-01T04:03:17Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 2 Short-term (14 days) treatment with D-004, a lipid extract from Roystonea regia fruits, has been shown to prevent testosterone (T)-induced prostate hyperplasia (PH) and increased oxidative stress in rat prostate, but no study has documented if such effects persist after longer treatment. This study investigated the persistence of the effects of D-004 orally given for 60 days for preventing prostate enlargement and increase of oxidative markers in rats with T-induced PH. Rats were randomized into three groups: a negative control and two T-injected that received orally vehicle (positive control) or D-004 (400 mg/kg/day), respectively. Prostate weights of positive controls significantly and markedly increased over the time, while persistent and significant reductions of such increases were seen in D-004-treated rats. Also, D-004 significantly reduced the T-induced increase of prostate conjugated diene generation and sulphydril groups concentrations, achieving a complete reduction from the day 30 after starting the treatment. Concluding, the effects of oral treatment with D-004 (400 mg/kg/day) on T-induced prostate enlargement and increased prostate oxidative markers persisted over 60 days of treatment.

Anti-anaphylactic and mast cell stabilizing effect of Calotropis gigantea extract

2019-07-01T04:03:15Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 2 Calotropis gigantea (Linn.) R.Br. (Asclepiadaceae), commonly known as milkweed or swallow- wort, is found chiefly in wasteland throughout India. It has been reported as a traditional folkloric medicine in treatment of asthma in the Indian literature. Roots containing α-and β-amyrin are reported to possess anti-lipoxygenase activity. Hence, our objective was to evaluate the effect of the methanolic extract of Calotropis gigantea (CG) root on egg albumin induced passive paw anaphylaxis and compound 48/80 induced mast cell degranulation in rats. CG were given at doses of 100, 200, 400 mg/kg, p.o., to rats. We found that CG significantly increases percentage inhibition of paw edema volume at all doses but shows significant percentage protection of the mast cells at 400 mg/kg. p.o., to rats. Hence, the present investigation confirm the use of CG as anti-anaphylactic and mast cell stabilizing in treatment of asthma.

Inhibitory potential against methicillin-resistant staphylococcus aureus (MRSA) of Dolichandrone spathacea, a mangrove tree species of Malaysia

2019-07-01T04:03:14Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 2 In this study, methanol extracts from the leaf and stem of Dolichandrone spathacea (L.f) K. Schum., a lesser-known local mangrove tree species, was evaluated using disc diffusion and minimum inhibitory concentration (MIC) value determination assays against six strains of local MRSA clinical isolates and one ATCC MRSA reference strain. The stem extract exhibited a higher zone of inhibition as compared with the leaf extract against the tested isolates. Further qualitative evaluation of the stem extract showed MIC values between 1.25 to 1.88 mg/ml against three selected MRSA clinical isolates. Phytochemical screening revealed that the triterpene and saponin compounds might be responsible for the better inhibitory activity from the stem extract as compared to the leaf extract. This study is the first report of the phytochemical screening and the inhibitory activity of D. spathacea leaves and stems methanolic extracts against MRSA clinical isolates.

Anxiolytic-like effects of Tilia petiolaris DC: Inflorescences Infusion

2019-07-01T04:03:12Z

Comunicacion Latin American Journal of Pharmacy; vol. 30, no. 2 Infusions of the inflorescences of Tilia are widely used for their tranquilizing properties around the world and have been regarded as non-toxic. Despite the widespread use of the tea of silver Linden in folk medicine, the number of scientific studies for the evaluation of its therapeutic utilization is limited. In an attempt to add experimental confirmation to its popular medicinal use, the central nervous system related effects of the chronic ingestion of the infusion of Tilia petiolaris DC. inflorescences were evaluated in the holeboard, locomotor activity and light-dark tests in mice. The infusion induced significant increases in the exploration of holes and in the time spent head-dipping in the holeboard assay. Moreover, it significantly increased the time spent in the light area in the light-dark test. These results suggest that the infusion of Tilia petiolaris DC. inflorescences exerts an anxiolytic-like activity in mice.

Adverse drug reaction as cause of hospital admission of elderly people: a pilot study

2019-07-01T04:03:10Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 2 The objective of this study was to estimate the prevalence of adverse drug reactions (ADR) related to hospital admission of elderly people, identifying the use of potentially inappropriate medication (PIM) , the ADR and the risk factors associated with the hospitalization. A cross-sectional study was conducted in a private hospital of São Paulo State, Brazil. All patients aged ≥ 60 years, admitted in the general practice ward in May 2006 were interviewed about the drugs used and the symptoms/complaints that resulted in hospitalization. More than a half (54.5 %) of elderly hospitalizations were related with ADR. The therapeutic classes involved with ADR were: cardiovascular (37.7 %), central nervous (34.6 %) and respiratory (5.7 %). The ADR observed were disorders in circulatory (28.4 %), digestive (20.0 %) and respiratory (18.9 %) tracts. 27 elderly had made PIM and in 20 of them this was the cause of hospitalization. Polypharmacy was an ADR risk factor (p = 0.021).These data allows the healthcare professionals upgrade, qualifying them in pharmcovigilance.

RP-HPLC method for simultaneous estimation of amlodipine and valsartan in tablet formulation and validation as per ICH guidelines

2019-07-01T04:03:07Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 2 A simple, specific, sensitive and validated RP-HPLC method for the simultaneous estimation of amlodipine (AMB) and valsartan (VAL) in marketed tablet formulation was developed. The analysis was carried out on a phenomenex C18 (250 x 4.6 mm, 5 µm) column using a mobile phase of 0.1% ortho phosphoric acid solution: acetonitrile (35:65 v/v, pH 3.0). The flow rate of the mobile phase was adjusted to 1.0 ml/min and was detected at 238 nm. The retention time obtained from the analysis was 1.995 min and 4.910 min for AMB and VAL respectively. The developed method was validated as per ICH guidelines. In order to find out the linearity, the concentrations ranging 2-10 µg/ml for AMB and 64-320 µg/ml for VAL was used. The squared correlation co-efficient (r 2 value) derived from the equation for AMB and VAL was 0.9979 and 0.9994, respectively. The percentage recoveries calculated for AMB and VAL ranges from 96.93 to 99.63 %. The estimated drug in the tablet formulation was 100.13 % and 99.99 % for AMB and VAL respectively. The results of analysis shows that method can be used for the estimation of AMB and VAL in the tablet dosage form without further separation in the quality control laboratories.

Utility of inorganic oxidants for the spectrophotometric determination of ganciclovir in dosage forms

2019-07-01T04:03:05Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 2 Eight direct spectrophotometric methods for determination of ganciclovir has been developed and validated. These methods were based on the oxidation of the drug by different inorganic oxidants: ceric ammonium sulphate, potassium permanganate, ammonium molybdate, ammonium metavanadate, chromium trioxide, potassium dichromate, potassium iodate and potassium periodate. The oxidation reaction were performed in perchloric acid medium for ceric ammonium sulphate and in sulfuric acid medium for the other reagents. Different variables affecting the reaction conditions were carefully studied and optimized. Under the optimum conditions, linear relationships with good correlation coefficients (0.9987- 0.9993) were found between the reading and the corresponding concentration of the drug in the ranges of 2.0-1500 μg.mL–1 The limits of detection ranged from 0.26-18.25 μg mL–1 . The precision of the methods . was satisfactory; the values of relative standard deviations did not exceed 2.0 %. The proposed methods were successfully applied to the analysis of ganciclovir in dosage forms with good accuracy and precisions; the label claim percentages ranged from 99.9–100.4 ± 0.62–1.05 %.

Gastroretentive drug delivery system of captopril and hydrochlorothiazide bilayer tablet: formulation, optimization and in vivo evaluation

2019-07-01T04:03:02Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 2 The purpose of the present study was to develop and optimize floating-bioadhesive bilayer gastroretentive drug delivery system (GRDDS) exhibiting a unique combination of floatation and bioadhesion to prolong residence in the stomach using captopril (CP) and hydrochlorothiazide (HCTZ) as a model drug. Captopril being unstable in intestinal pH and HCTZ has specific absorption from duodenum and the first part of the jejunum and to a small extent in the stomach are suitable candidate for GRDDS. 32 factorial design was employed in formulating and optimizing the GRDDS for bilayer tablet of CP and HCTZ matrix tablet. The main effect and interaction terms were quantitatively evaluated using a mathematical model. The gastroretentive ability of the tablets was evaluated by X-radiographic studies in healthy human volunteer. The tablet releases CP and HCTZ for extended period up to 24 h in controlled manner. The predicted values agreed well with the experimental values and the results demonstrate the feasibility of the optimization methodology in the development of GRDDS. The tablet was buoyant for up to 16 h in human stomach. Development of once a day gastroretentive formulation of CP and HCTZ improves the patience compliance and bioavailability of drugs.

In vitro/in vivo assessment of flurbiprofen-matrix type transdermal delivery system

2019-07-01T04:02:59Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 2 In this study, matrix type patch formulations of flurbiprofen using certain skin permeation enhancers [isopropyl myristate (IPM), isopropyl palmitate (IPP) and Tween 80] were formulated, evaluated and compared. The cumulative amounts permeated and the permeation rates were higher for the prepared formulations as compared to the controls (without enhancers). The results also revealed better skin permeation characteristics of flurbiprofen using IPM than other enhancers. The pharmacokinetic parameters of the optimized formulation (F7), calculated from the blood levels of the drug, revealed a profile with the ability to maintain adequate plasma levels for 24 h (i.e. up to the next application): AUC_(0-24) 10.406 ± 1.34ng.h/ml, T_max 1.5 ± 0.91 and C_max 1.3049 ± 0.21 µg.ml^-1-. The amount of drug bioavailable for targeting the site of action is comparable to that of market control. Based on experimental results, preparation of 10 % flurbiprofen matrix type patch formulation containing IPM is promising

Pharmacobotanical study of Baccharis singularis (Vell.) G.M. Barroso, Asteraceae

2019-07-01T04:02:55Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 2 Baccharis is an important genus of Asteraceae and it comprehends approximately 400 species, many of which are frequently used in folk medicine as analgesic, diuretic, spasmolytic, antidiabetic, antiseptic and stomachic. Baccharis singularis belongs to the Singularis group and is popularly known as cambará-de-praia and cambará-da-serra. It is a shrub which occurs in Brazil, from Bahia to Rio Grande do Sul. The present study has aimed to investigate the morpho-anatomy of the aerial vegetative parts of this species for pharmacognostic purposes. The plant material was processed according to standard methods of light and scanning electron microscopy. Non-glandular trichomes, flagelliform, simple and uniseriate, secretory ducts located near the phloem, calcium oxalate crystals in the perimedullary region of the stem and in the ground parenchyma of the petiole are valued characters which contribute to the species identification.

Spectrophotometric analysis of Cabergoline in pharmaceutical preparations

2019-07-01T04:02:54Z

Articulo Latin American Journal of Pharmacy; vol. 30, no. 2 Cabergoline (CAB) is a synthetic ergoline dopamine agonist with high affinity to D₂ receptors, thus used for the treatment of Parkinson's patients and hyperprolactinemia disorders. In this study, simple, fast, reliable and validated UV-VIS and 2nd order derivative spectrophotometric methods for determination of CAB in pharmaceutical preparations were developed without any previous sample preparation step. Determination of CAB was performed at 280 nm wavelength by UV-VIS spectrophotometry and in the range of 227-232 nm by 2nd order derivative spectrophotometry. Developed both spectrophotometric methods were linear over the range of CAB concentrations from 1 to 125 µg mL^-1-. The highest relative error and relative standard deviation in within-day and day-to-day study for UV-VIS spectrophotometry were found to be 1.10% and 0.63%, respectively. The relative error and relative standard deviation in within-day and day-to-day study for 2nd order derivative spectrophotometry were not higher than 1.10% and 0.70%, respectively.