CinÃtica de difusÃo in vitro e atividade in vivo de preparaÃÃes magistrais de cetoprofeno

AUTOR(ES)
DATA DE PUBLICAÇÃO

2007

RESUMO

The Ketoprofen is a nonsteroidal antiinflammatory drug (NSAID) used in the symptomatic treatment for rheumatoid arthritis. The oral administration, for a long period can cause gastric disorders, as stomach upset, pains and ulceration. The emulgel studied in this work was based on PLO (Pluronic Lecithin Organogel) and was developed with the aim of reaching systemic circulation while avoiding stomach contact. This vehicle has been used en compounding pharmacies in Brazil and the U.S.A. The goal of this work was to evaluate the in vitro diffusion kinetics and preliminary in vivo activity in galenic ketoprofen formulations based on PLO. Initially, a ketoprofen quantification method for the emulgel formulation was developed by high performance liquid chromatography (HPLC) and applied to the determination of ketoprofen in the in vitro diffusion kinetics experiments. The method used HPLC with uv detection at 254nm. Separation was carried out with a C-18 reversed phase column (150 x 4,6, 5μ) with a mobile phase contisting of 20mm sodium phosphate buffer pH 3 and acetonitrile (50:50). The method was validated and proved to be linear (5 a 60μg.mL-Â), sensitive, precise and accurate. The realease profile of ketoprofen from the emulgel formulation was studied in vitro using franz diffusion cells with cellulose acetate membrane. The results indicated that all formulations tested have similar diffusion profiles and the effect of permeation promoter (Transcutol CG) could not be demonstrated in the in vitro realease studies. The formulations used F3 e F8 showed the highesr flow (μg/cmÂ. h-Â). Finally a preliminary antiinflamatory activity study was carried out with the formulation using the carragenin â induced paw edema in rats, with topical administrationof 1 g (25mg/g emulgel) in the dorsal region. The formulation F3 e F8 was tested againt their respective placebos formulations. In the anti-inflammatory assay, formulation F3 and its placebo did not differ significantly in relation to edema inhibition showing that this formulation did not produce sufficient drug permeation up to 6 hours. The formulation F8 showed a 47, 17% reduction of paw edema after 06 hours, a reduction that the F8 formulation with transcutol CGÂ, promoted ketoprofen permeation when applied in the animalâs dorsal region

ASSUNTO(S)

emulgel atividade antiinflamatÃria validaÃÃo antiinflammatory activity farmacia emulgel ketoprofen validation in vitro diffusion kinetic cetoprofeno cinÃtica de difusÃo in vitro

ACESSO AO ARTIGO

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