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1.
Indian J Exp Biol ; 53(1): 31-5, 2015 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-25675709

RESUMO

Argemone mexicana (L.) has a role in the treatment of epileptic disorders in Indian traditional system of medicine. We studied its effect on induced status epilepticus (SE) and oxidative stress in rats. SE was induced in male albino rats by administration of pilocarpine (30 mg/kg, ip) 24 h after injection of lithium chloride (3 mEq/kg, ip). Different doses of the ethanol extract of A. mexicana were administered orally 1 h before the injection of pilocarpine. The severity of SE was observed and recorded every 15 min for 90 min and thereafter at every 30 min for another 90 min, using the Racine scoring system. In vivo lipid peroxidation of rat brain tissue was measured utilizing thiobarbiturate-reactive substances. Both in vitro free radical nitric oxide and 2,2-diphenyl-1-picryl hydrazyl scavenging activities of the extract were also determined. The SE severity was significantly reduced following oral administration of the extract at 250, 500 and 1000 mg/kg doses. None of the animals from groups 3 to 5 (with A. mexicana extract) have exhibited forelimb clonus of stage 4 seizure. The extract also exhibited both in vivo and in vitro antioxidant activities.


Assuntos
Argemone/química , Compostos de Lítio/toxicidade , Estresse Oxidativo/efeitos dos fármacos , Pilocarpina/toxicidade , Extratos Vegetais/farmacologia , Estado Epiléptico/prevenção & controle , Animais , Encéfalo/efeitos dos fármacos , Encéfalo/metabolismo , Peroxidação de Lipídeos/efeitos dos fármacos , Masculino , Ratos , Ratos Wistar , Estado Epiléptico/induzido quimicamente
2.
Acta Crystallogr Sect E Struct Rep Online ; 70(Pt 5): o553, 2014 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-24860361

RESUMO

In the title compound, C8H9N4S(+)·Cl(-)·H2O, the cation is approximately planar, with a dihedral angle of 7.71 (8)° between the mean planes of the benzo-imidazole ring system and the thio-urea unit. In the crystal, cations, anions and water molecules of crystallization are linked by O-H⋯Cl, N-H⋯O, N-H⋯Cl and N-H⋯S hydrogen bonds into a three-dimensional network. π-π stacking is observed between the benzene and imidazole rings of neighbouring mol-ecules, the centroid-centroid distance being 3.5774 (11) Å.

3.
Curr Drug Deliv ; 11(2): 172-8, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-23848354

RESUMO

Discovered in the 1920s, the biguanide metformin hydrochloride is still the first line drug in the management of Type 2 diabetes mellitus. Metformin hydrochloride is absorbed slowly and incompletely from the gastrointestinal tract. The present research work was undertaken with the aim of developing a fast dissolving film of metformin hydrochloride, suitable for oral trans mucosal administration. Fast dissolving films allow rapid drug dissolution in the oral cavity, ensuring bypass of first pass metabolism resulting in rapid absorption. Films of metformin were prepared by solvent casting method using Hydroxypropyl methylcellulose K15 (HPMC). Six formulations (F1-F6) of metformin hydrochloride were prepared and evaluated for their physical characteristics such as tackiness, thickness, tensile strength, elongation, weight variation, folding endurance, drug content and surface pH. The compatibility of the drug with HPMC was confirmed by FTIR studies. The formulations were subjected to disintegration, in-vitro drug release and the optimised formulation was evaluated for pharmacodynamic studies in diabetic rats. Among the formulations (F1-F6) F4 was found to be the best formulation which contained Hydroxypropyl methyl cellulose K15 at weight ratios of 1:4 and showed excellent film forming characteristics such as disintegration time at 42 sec and percentage drug release of 94.2% within 5 minutes. Pharmacodynamic assessment in diabetes induced rats demonstrated that the fast dissolving films of metformin had a quicker onset of action compared to conventional formulation.


Assuntos
Hipoglicemiantes/administração & dosagem , Metformina/administração & dosagem , Administração Oral , Sistemas de Liberação de Medicamentos , Humanos , Concentração de Íons de Hidrogênio , Derivados da Hipromelose/química , Metformina/análise , Metformina/química , Mucosa Bucal/metabolismo , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Resistência à Tração
4.
Curr Drug Discov Technol ; 11(2): 162-7, 2014 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-24295369

RESUMO

The aim of the investigation was to prepare nimesulide emulsion for incorporation in Aloe vera gel base to formulate 'nimesulide - Aloe vera transemulgel' (NAE) and to carryout in-vitro assessment and in-vivo anti-inflammatory studies of the product. Although the use of nimesulide is banned for oral administration, due to its potential for inducing hepatotoxicity and thrombocytopenia, the use of nimesulide for topical delivery is prominent in the treatment of many inflammatory conditions including rheumatoid arthritis. The drug loading capacity of transdermal gels is low for hydrophobic drugs such as nimesulide. Nimesulide can be effectively incorporated into emulgels (a combination of emulsion and gel). Aloe vera has a mild anti-inflammatory effect and in the present study Aloe vera gel was formulated and used as a gel base to prepare NAE. The emulgels thus prepared were evaluated for viscosity, pH, in-vitro permeation, stability and skin irritation test. In-vivo anti-inflammatory studies were performed using carrageenan induced hind paw edema method in Wistar rats. The results were compared with that of commercial nimesulide gel (CNG). From the in-vitro studies, effective permeation of nimesulide from NAE (53.04 %) was observed compared to CNG (44.72 %) at 30 min indicating better drug release from NAE. Topical application of the emulgel found no skin irritation. Stability studies proved the integrity of the formulation. The percentage of inhibition of edema was highest for the prepared NAE (67.4 % inhibition after 240 min) compared to CNG (59.6 %). From our results, it was concluded that the Aloe vera gel acts as an effective gel base to prepare nimesulide emulgel with high drug loading capacity (86.4 % drug content) compared to CNG (70.5 % drug content) with significant anti-inflammatory effect.


Assuntos
Anti-Inflamatórios não Esteroides , Preparações de Plantas , Sulfonamidas , Aloe , Animais , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacologia , Anti-Inflamatórios não Esteroides/uso terapêutico , Carragenina , Estabilidade de Medicamentos , Edema/induzido quimicamente , Edema/tratamento farmacológico , Géis , Concentração de Íons de Hidrogênio , Masculino , Preparações de Plantas/química , Preparações de Plantas/farmacologia , Preparações de Plantas/uso terapêutico , Ratos Wistar , Pele/efeitos dos fármacos , Sulfonamidas/química , Sulfonamidas/farmacologia , Sulfonamidas/uso terapêutico , Viscosidade
5.
J Indian Soc Pedod Prev Dent ; 31(2): 69-73, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-23886715

RESUMO

PURPOSE: This study was conducted to identify various factors in the development of rampant type of dental caries in South Kerala children, other than high sucrose intake and poor oral hygiene. This was done by comparing the salivary buffering capacity(BC), flow-rate(FR), resting pH and salivary immunoglobulin-A(s-IgA) levels in children who are caries resistant(CR) and who have rampant dental caries. MATERIALS AND METHODS: Two study groups, a rampant caries group(RC) with more than five active caries lesions in the early stages and a CR with no caries lesions were selected based on a specific criteria. Unstimulated whole mixed saliva was collected directly from the floor of the mouth for a period of 10 min and the FR was calculated. Resting pH of saliva was measured using color coded pH paper. BC was measured by calculating the amount of citric acid of pH2.5, required to lower the initial pH of saliva down to 3. s-IgA levels were also estimated by immunoturbidometric method after forming a precipitate of s-IgA with specific anti-IgA antibodies. RESULT: The salivary BC, FRs, pH and s-IgA levels were significantly lower in the RC group when compared to the CR group. CONCLUSION: This study showed that salivary BC, flow-rate, resting pH and levels of s-IgA in saliva are risk factors in the development of RC in children.


Assuntos
Suscetibilidade à Cárie Dentária/fisiologia , Cárie Dentária/metabolismo , Imunoglobulina A Secretora/análise , Saliva/fisiologia , Soluções Tampão , Pré-Escolar , Ácido Cítrico/química , Índice de Placa Dentária , Carboidratos da Dieta/administração & dosagem , Comportamento Alimentar , Humanos , Concentração de Íons de Hidrogênio , Higiene Bucal , Saliva/metabolismo , Taxa Secretória/fisiologia , Titulometria
6.
Acta Crystallogr Sect E Struct Rep Online ; 69(Pt 12): o1729, 2013 Nov 06.
Artigo em Inglês | MEDLINE | ID: mdl-24454191

RESUMO

In the title compound, C6H6BrNO, the Br atom is displaced from the pyridine ring mean plane by 0.0948 (3) Å, while the hydroxyl O atom and the methyl C atom are displaced by 0.0173 (19) and 0.015 (3) Å, respectively. In the crystal, mol-ecules are linked via O-H⋯N hydrogen bonds, forming chains propagating along the a-axis direction. These chains are linked by C-H⋯Br hydrogen bonds, forming corrugated two-dimensional networks lying parallel to the ac plane.

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