Cifuente, Diego A.; Gianello, José C.; María, Alejandra O.M.; Petenatti, Elisa M.; Petenatti, Marta E.; Del Vitto, Luis A.; Tonn, Carlos C.
Seveal Baccharis species known as "carquejas" are used in Argentinean folk medicine as phytotherapics. B. crispa, B. articulata, B. trimera, B. sagittalis and B. triangularis have been evaluated for their choleretic activity using Wistar rats. B. sagittalis and B. triangularis showed a significant choleretic activity (bile flow of 1.631 ± 0.089 and 1.598 ± 0.196 μl/min/g liver, respectively). B. crispa, B. trimera showed moderate activity and B. articulata exhibited the same choleretic property that the control. Only, B. articulata and B. crispa are informed as official drugs in the Argentinean Pharmacopoeia. In addition, phytochemical constituents and botanical characters are reported
Matias, Edinardo F.F.; Santos, Karla K. A.; Almeida, Thiago S.; Costa, José G.M. da; Coutinho, Henrique D.M.
Escherichia coli is known to produce enterotoxins whose properties and its role in diarrheal disease has been extensively investigated. Some species of Staphylococcus are often recognized as etiological agents of many animal and human opportunistic infections. This study is the first test of change in resistance of antibiotic activity by Cordia verbenacea DC. against multiresistant strains of Escherichia coli and Staphylococcus aureus. In this study, the hexane and methanol extract of Cordia verbenacea DC. were tested for antibacterial activity alone and in combination with aminoglycosides against bacterial strains. The synergy of the methanolic and hexane were verified by microdilution method....
Huri, Hasniza Z.; Wei, Amy T.-L.; Pendek, Rokiah; Sulaiman, Che Z.; Widodo, Riyanto T.
Sulphonylureas (SUs) are commonly prescribed in Malaysia and also worldwide. However, very limited information is available on their pattern of use and appropriateness of its utilization. Age, concurrent use of drugs such as beta blocker, salicylate and frusemide and also renal impairment were found to have influence on the selection of different types of SUs.
Yang, Xuezhi; Hu, Lufeng; Lin, Guanyang; Xu, Ren-ai; Zhang, Yu; Chen, Linzi; Zhu, Lihe; Zhao, Feng; Wang, Xianqin
A simple and sensitive LC-ESI-MS method for determination of norvancomycin in plasma
was developed and validated over the concentration range of 20-2,000 ng/mL. After addition of vancomycin
as internal standard (IS), protein precipitation with 5 % trichloroacetic acid was employed for
the sample preparation. Chromatographic separation was performed on a Zorbax SB-C18 (100 mm×2.1
mm, 3.5 μm) column with 10:90 (v/v) acetonitrile-0.1 % formic acid as mobile phase. The MS data acquisition
was accomplished by selective ions monitoring (SIM) mode with positive electrospray ionization
(ESI) interface. The limit of quantification (LOQ) was 20 ng/mL. For inter-day and intra-day tests, the
precision (RSD) for the entire validation was...
Mascotti, María L.; Bisogno, Fabricio; Lima, Beatriz; Kurina-Sanz, Marcela; Feresin, Gabriela E.; Enriz, Ricardo Daniel; Giannini, Fernando Angel
In this work, we present antibacterial activity of a 22 phenylpropanoids derived from cinnamic
acid, recently reported as antifungal agents by our group. Some of these compounds are commercial,
others are natural products and some of them were obtained by synthesis. Antibacterial activity was
determined in two stages. At first, a screening was made by an easy, economic and fast assay using a commercial
lyophilized of Gram (+) bacteria. Compounds that showed activity at the screening were tested
against Gram (+) and Gram (-) pathogens.
Khan, Shujaat A.; Ahmad, Mahmood; Shoaib, Harris M.; Murtaza, Ghulam; Aamir, Muhammad N.; Kousar, Rozina; Rasool, Fatima; Madni, Asadullah
A predictive in vitro-invivo correlation (IVIVC) can empower in vitro dissolution as a surrogate for in vivo bioavailability / bioequivalence. IVIVCs can decrease regulatory burden by decreasing the number of biostudies required in support of a drug product. The present study concerns the establishment of in vitro-in vivo correlation for three different sustained release nimesulide loaded ethylcellulose microparticulate formulations (M1, M2 and M3) and conventional tablet (100 mg Nimaran®-Novartis, Pakistan). In vitro dissolution study was conducted in phosphate buffer pH 6.8 stirred at 50 rpm and 37 ± 0.5ºC. A validated HPLC method was adopted to conduct bioavailability studies in...
Michelin, Daniele C.; Almeida, Glalber C. de; Galina, Karen Janaina; Lopes, Gisely C.; Nakamura, Celso Vataru; Dias Filho, Benedito Prado; Ueda Nakamura, Tânia; Salgado, Hérida R.N.; Mello, João Carlos Palazzo de
The high incidence of diarrhea in the population demands a search for new therapeutic options and easy access, mainly from plant-based sources. Leaves and bark of Guazuma ulmifolia Lam. (Sterculiaceae) are popularly employed against diarrhea. However, no information was found in the literature about this supposed property of the drug. In this study we evaluated in vivo antidiarrheal activity of stem bark extracts from G. ulmifolia in mice, and in vitro antimicrobial activity against Staphylococcus aureus, Escherichia coli, Bacillus subtilis, Salmonella sp., Shigella flexneri, and Pseudomonas aeruginosa by using the microdilution method. The n-BuOH semipurified fraction (GU#3) significantly reduced intestinal...
Rote, Ambadas R.; Niphade, Vaishali S.
A simple, rapid, sensitive and economical method has been developed for the simultaneous determination of montelukast sodium and levocetirizine dihydrochloride in combined tablet dosage form. The method was based on high performance liquid chromatography using zidovudine as an internal standard. The separation was carried out with a Eurosphere 100 C18 column (250×4.6 mm ID, 5 μm) and mobile phase 0.05 % orthophosphoric acid: methanol (10:90 v/v) at flow rate 1.2 ml/min. The UV detection was carried out at wavelength 225 nm.The method was validated statistically and by performing recovery study.
Takahashi, Andrea I.; Ferraz, Humberto G.
The purpose of this study was to attain and characterize ternary complexes of simvastatin, β-cyclodextrin (βCD) and different polymers, and then select those that lead to a greater increase in drug solubility. The complexes were prepared with the co-evaporation method and the polymers used were polyethylene glycol 1500, polyethylene glycol 4000, povidone, copovidone, crospovidone, maltodextrin and hydroxypropyl methyl cellulose. The characterization of complexes was carried out through aqueous solubility, DSC and TG. There was an increase in solubility for all the complexes prepared with βCD and the different polymers, but only when crospovidone and maltodextrin were used was there a...
Rajangam, Jayaraman; Thiyagarajan, Anitha; Joshi, Vishal D.; Palei, Narahari
Acorus calamus (Araceae) is commonly known in India as sweet flag and has been used in
traditional medicine as a remedy for pain, convulsion, inflammation, and ulcer. In the present work, the
methanolic extract of Acorus calamus roots (MEAC) was assessed for different psychopharmacological activities
in rats and mice by evaluation of general, exploratory behaviour, phenobarbitone sodium-induced
sleeping time and muscle relaxant activity. The extract at doses 100 mg/kg and above exhibited a reduction
in spontaneous activity and a decrease in exploratory behavioural pattern was observed. Also a significant
reduction in muscle relaxant activity and potentiated phenobarbitone sodium-induced sleeping time
in mice was noted in MEAC treated...
Leonardi, Gislaine R.; Rigon, Roberta B.; Cavallini, Míriam Elias; Polacow, María L. O.; Araújo, Marina R.; Andreollo, Nelson A.
This study evaluated the effect of Cordia verbenacea essential oil (CV) and glycolic acid 70 %
(GA), isolated and associated, on Wistar rats back skin. A base gel was added to 2 % of CV and/or 10 %
of GA, thus forming 4 formulations: 1) GA + CV, 2) CV, 3) GA, and 4) gel base. All formulation had their
final pH adjusted to 3,5 and were applied once daily, for 15 consecutive days, on 4 areas with 1 cm2, while
another area without application (control). Statistical analysis of biopsies showed no difference in epidermis
thickness and stratum corneum. Among fibroblast counts there was a...
Melquiades, Fábio; Appoloni, Carlos R.; Lonni, Audrey; Ferreira, Diego D.D.; Lopes, Fábio
Nowadays there are no official in vitro methods to determine TiO2, ZnO or other inorganic elements in sunscreen cosmetics. The objective of this work is to determine the concentration of several inorganic elements in sunscreen composition, without sample preparation, by employing a portable Energy Dispersive X-Ray Fluorescence (EDXRF) device. Particularly in the case of TiO2 and ZnO, the aim is also to estimate their Sun Protection Factor (SPF) due to the physical protection barrier. A sensitivity curve for the determination of inorganic elements in sunscreen, with atomic numbers ranging from 19 to 35, is presented. Fifteen commercial samples with different...
Nalawade, Pravin; Somvanshi, Amol; Dand, Neha; Kadam, Vilasrao; Hirlekar, Rajashree
The aim of the present investigation was to develop a modified release effervescent floating
drug delivery system of famotidine for 12 h dosage regimen to improve its bioavailability. Effervescent
floating tablets were prepared by direct compression method taking into account its advantages over wet
granulation by using directly compressible excipients like Carbopol® 71G and Cellactose® 80. The incorporation
of sodium bicarbonate aided in the buoyancy with effervescent approach. The prepared tablets
were evaluated for floating lag time (FLT), total floating time (TFT), in vitro drug release along with general
parameters. 23 factorial design was used for optimization. The tablets showed desired release of more
than 98 %...
Rasool, Fatima; Ahmad, Mahmood; Murtaza, Ghulam; Khan, Haji M. S.; Khan, Shujaat A.
This study introduced a novel phase separation technique for the microencapsulation of metoprolol tartrate as a model. Non-solvent addition coacervation technique was employed for the loading of drug into ethylcellulose, a hydrophobic plastic polymer. Dichloromethane (DCM) and paraffin oil were
employed as solvent and non-solvent, respectively. Microparticle batches abbreviated as M1, M2 and M3
were formulated by embedding 1 g of drug into 1 g, 2 g and 3 g of polymer, respectively followed by direct compression into tabletted microparticulate batches named a T1, T2 and T3, respectively. The drug and polymer remained intact in encapsulated form as confirmed by FTIR, XRD...
Higa, Valeria M.; Correa Salde, Viviana; Ravetti, Soledad; Arce Miranda, Julio E.; Fonsfría, Lucas D.; Palma, Santiago D.; Paraje, María Gabriela
Se analizaron las características de prescripción y dispensación de medicamentos en una población
de pacientes hipotiroideos, así como el conocimiento de los mismos sobre su terapia. Se trabajó con
un procedimiento normalizado analizando 948 prescripciones médicas en 42 farmacias comunitarias de
Córdoba (Argentina). Los laboratorios autorizados para elaborar medicamentos con levotiroxina fueron
siete, en 12 concentraciones distintas (desde 25 a 300 μg). En este estudio una sola marca abarcó el 59 %
de las prescripciones médicas. El 85 % de los usuarios fueron mujeres, principalmente entre 41-60 años.
En cuanto al uso del medicamento el 78 % manifestó tomar el mismo una vez al día y...
Kumar, Suresh; Bawa, Sandhya; Drabu, Sushma; Kumar, Rajiv; Panda, Bibhu P.
A series of N-[(2-chloro-7-methylquinolin-3-yl)methyl]-(substituted)-aniline/butan-1-amine/cyclohexamine
derivatives (4a-n) & N-benzyl-1-(2-chloro-7-methylquinolin-3-yl)methanamine (4o) was designed and
synthesized based on the structural requirements essential for allylamine / benzylamine antimycotics. Compounds
(4a-o) were synthesized by nucleophilic substitution reaction of 2-chloro-3-(chloromethyl)-7-
methylquinoline with substituted aromatic/aliphatic primary amine in absolute ethanol in presence of triethylamine.
The structures of all new products were confirmed by IR, 1H & 13C-NMR and mass spectral data. The
newly synthesized compounds were screened in-vitro for their antifungal activity against Aspergillus niger
MTCC 281, Aspergillus flavus MTCC 277, Monascus purpureus MTCC 369 and Penicillium citrinum NCIM
768 by cup plate method. Preliminary screening of compounds (4a-o) revealed that compounds viz. 4a, 4b,...
Ravanello, Aline; Dadalt, Gabriele; Torres, Bruna G. S.; Hurtado, Felipe K.; Marcolino, Ana I. P.; Rolim, Clarice M. B.
A simple UV-spectrophotometric method was developed and validated for the analysis and dissolution studies of sitagliptin phosphate in tablets. Specificity test indicated an adequate UV detection at 267 nm. The method was validated regarding Specificity/accuracy/precision (RSD < 2 %), linearity (r2 = 0.9999), and partial robustness. Tablets uniformity was 102.52 % (RSD = 2.54 %). The method was applied for the determination of the drug in commercial tablet preparations and proved to be reliable for quantification It was also used for the comparison of dissolution profiles of sitagliptin tablets. After dissolution tests comparing eight different conditions through dissolution efficiency (DE),...
Huang, Lijing; Gao, Wenyuan; Li, Xia; Man, Shuli; Zhang, Yanjun; Huang, Luqi; Liu, Changxiao
The combination of the bulb of Fritillaria ussuriensis Maxim. (Bulbus Fritillariae ussuriensis, BFU) and the fruit of Pyrus bretschneideri Rehd. (Xuehua pear, PBR), as folk medicine, is widely used in treatment with respiratory disease. In this study, three acute inflammatory models were used to estimate
the anti-inflammatory activities and cooperative interactions of them. The data were dealt with the Tallarida's improved contouring method and the Q value method to evaluate the cooperative interactions of BFU and PBR more directly. All the treated groups showed well preventive effects on xylene-induced mouse auricular edema, acetic acid-induced mouse vascular permeation and carrageenin-induced rat paw
Puri, Dinesh; Bhalekar, Mangesh R.; Sethi, Sunny S.
The purpose of this research was to formulate fast-disintegrating tablets of famotidine by using
tasteless complex of famotidine. Famotidine is a commonly used antiulcer drug but major disadvantage
is its bitterness and low bioavailability. A fast-disintegrating dosage form has been developed as a user-
friendly formulation that disintegrates in the mouth immediately. In this study the bitter taste of famotidine
was masked by making complex with ion exchange resin Indion 214. The drug-resin complexes were
characterized by infrared spectroscopy and thermal analysis. Famotidine oral fast disintegrating tablets
were prepared by direct compression method by using different superdisintegrants. The prepared tablets
were found to comply with various official...
Santos, Rodolfo I.; Pereira, Daniel F. A.; Teodoro, Guilherme R.; Del Ciampo, Jose Orestes; Ogasawara, Mario S.; Canettieri, Antonio C.V.; Khouri, Sonia; Salvador, Marcos J.
O objetivo deste estudo foi avaliar in vitro o efeito do óleo essencial de Thymus vulgaris (tomilho)
puro ou incorporado em uma formulação farmacêutica de uso oral (enxaguatório bucal), frente ao
Streptococcus mutans (ATCC 25175), determinando-se sua concentração inibitoria minima (CIM) e o efeito
na formação da placa bacteriana. A CIM obtida para o óleo essencial de tomilho foi de 100 μg/mL (1
%). Procedeu-se o desenvolvimento de enxaguatório bucal com efeito antiplaca contendo o óleo essencial
comercial de tomilho. As análises da formação da placa bacteriana (ensaios microbiológicos, análise macroscópica
de aderência e análises por MEV) confirmaram a eficácia destas novas formulações de enxaguatórios,