Background:
In many countries, the hypertension in the pediatric population is considered an important risk of
mortality and morbidity. In this sense, it is important to design and develop new pharmaceutical forms for pediatric
patients with hypertension. The development of orodispersible mini-tablets (ODMTs) for paediatric use has gained
importance within recent years the WHO authorities set up regulations for developing suitable and palatable dosage forms
for paediatric patients.
Objective:
The aim of this study was to design and develop orodispersible mini tablets of enalapril maleate for pediatric
use.
Methods:
Five pharmaceutical formulations were designed. The effects of different co-processed excipients and active
pharmaceuthical ingredient at different doses were study. Lactose co-processed excipients selected were Tablettose® 80,
MicroceLac® 100 and StarLac®. The micromeritic properties were evaluated for all the physical mixtures. The mini
tablets were obtained by direct compression and quality control parameters were determined in accordance with United
States Pharmacopeia.
Results:
Three OMDTs with StarLac® provide good results of hardness, flowability and fast disintegration. One of them,
with 0.1 mg of enalapril maleate, showed the best results for the official parameters of hardness (4.0 kp), friability (< 1%),
disintegration time (28 s), drug content uniformity (103.6 %) and the best wetting time (23 s).
Conclusion:
The orodispersible mini tablets with StarLac® showed good officially quality parameters. One
of them showed the best wetting time and doses for pediatric patients. This formulation could be considered
eligible to be elaborated on an industrial scale.
The search for new compounds with trypanocidal activity is crucial for the treatment of Chagas' disease. Previous in vitro studies have shown that the diterpene 5-epi-icetexone (ICTX) is active against Trypanosoma cruzi. The aim of this work was to evaluate the effect of ICTX on the parasites in infected mice, in an experimental model that mimics the acute phase of the disease. Swiss albino mice were infected with T. cruzi and treated daily with 10mg/kg/day ICTX (i.p.). Infected mice and mice injected with either saline or the vehicle DMSO were used as controls. Animals' survival and parasitemia were monitored once a week and histological studies were made at necropsy by the 5th week after infection. It was observed that the administration of ICTX increased the survival of mice infected, and induced a significant decrease in the parasitemia, as compared to controls. A similar protective effect was observed when animals were treated orally with benznidazole (BZN, used as a control of antiparasitic effect). By the 5th week post-infection, the presence of amastigote nests was observed within the fibers of the cardiac and skeletal muscle in controls, but not in animals treated with either ICTX or BZN. In addition, inflammatory infiltrates were observed in the tissues of controls, but not in animals treated with the drugs. We conclude that ICTX has an antiparasitic effect against T. cruzi, thus constituting an interesting option for the treatment of Chagas' disease, alone or combined with other drugs.
The antiinflammatory activities of ten organic extracts from the aerial parts of Baccharis medullosa DC., Baccharis rufescens S. and Laennecia sophiifolia (Kunth) G. L. Nesom were investigated in mice subjected to carrageenan induced paw oedema. Intraperitoneally administered organic extracts given at doses equivalent to 80 mg/kg of material inhibited the acute phases of inflammation in this model. Our results indicate that the most effective extracts were: n-hexane (I) from B. medullosa, acetone (V) and chloroform (VII) from L. sophiifolia, and acetone (VIII) and chloroform (X) from B. rufescens. All exerted the strongest effect at 5 h after injection of the phlogistic agent.
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