Prolonged-release lipid microparticles prepared with decyl oleate and hydrogenated castor oil of ibuprofen.

Ibuprofen is one of the most important non-steroidal anti-inflammatory drugs used in the treatment of inflammatory diseases. In its pure state, ibuprofen presents poor physical and mechanical characteristics and its use in solid dosage forms needs the addition of excipients that improve these properties. The selection of the best excipients and the most suitable pharmaceutical dosage form to carry ibuprofen is very important for the industrial success of this drug. Given these factors, lipid microparticles of ibuprofen with decyl oleate and hydrogenated castor oil were prepared. This formulation was intended to improve the content of ibuprofen in preparation and to sustain the release of this drug. Lipid microparticles were submitted to determination of ibuprofen content using UV-VIS spectrophotometry and, gelatin capsules filled with lipid microparticles and tablets prepared with these microparticles were submitted to dissolution tests in order to study the influence of the prepared system in the release profiles of ibuprofen. The improvement of the content of ibuprofen and prolonged release of this drug was achieved with the lipid microparticles prepared with this mixture of excipients.

Prolonged-release solid dispersions of ibuprofen.

Ibuprofen (IB) is one of the most important non-steroidal anti-inflammatory drugs used in the treatment of inflammatory chronic diseases. This drug presents, in the pure state, poor physical and mechanical characteristics and their use in solid dosage forms needs the addition of excipients which improve these properties. The selection of the best excipients and the suitable pharmaceutical dosage form to carry ibuprofen are very important for the industrial success of this drug. Thus, in this work, solid dispersions of ibuprofen in cethyl alcohol (SD CA), stearic acid (SD SA) and hydrogenated castor oil (SD HCO) were prepared in order to improve physical and mechanical characteristics of this drug. Physical mixtures with the same composition of solid dispersions were also prepared. Solid dispersions of ibuprofen with stearic acid and hydrogenated castor oil showed better flow characteristics than pure ibuprofen and the respective physical mixtures. Gelatin capsules filled with solid dispersions were submitted to dissolution tests in order to study the influence of the prepared systems in the release profiles of ibuprofen. Prolonged-release of ibuprofen was achieved with the solid dispersions prepared with the different types of excipients.

Comparative study of sustained-release lipid microparticles and solid dispersions containing ibuprofen

Ibuprofen is one of the most important non-steroidal anti-inflammatory drugs used in the treatment of inflammatory diseases. In its pure state, ibuprofen presents poor physical and mechanical characteristics and its use in solid dosage forms needs the addition of excipients that improve these properties. The selection of the best excipients and the most suitable pharmaceutical dosage form to carry ibuprofen is very important for the industrial success of this drug. Given these factors, lipid microparticles and solid dispersions of ibuprofen with cetyl alcohol, stearic acid, and hydrogenated castor oil were prepared. These formulations were intended to improve the physical and mechanical characteristics and to sustain the release of this drug. Physical mixtures were also prepared with the same ingredients in similar proportions. The solid dispersions of ibuprofen/stearic acid and ibuprofen/hydrogenated castor oil showed the best flow characteristics compared with pure ibuprofen. Further, gelatin capsules filled with lipid microparticles and solid dispersions were submitted to dissolution tests in order to study the influence of the prepared systems in the release profiles of ibuprofen. Prolonged release of ibuprofen was achieved with the lipid microparticles and solid dispersions prepared with the different types of excipients.

O ibuprofeno é um dos antiinflamatórios não esteróides mais utilizados no tratamento de patologias associadas a processos inflamatórios. Este fármaco, quando no seu estado puro, apresenta características físicas e mecânicas pouco satisfatórias e a sua utilização em formas sólidas só é possível se forem adicionados excipientes que permitam melhorar estas propriedades. A seleção dos excipientes ideais e da forma farmacêutica mais adequada para veicular o ibuprofeno é fundamental para o sucesso industrial deste fármaco. Tendo em conta estes fatores, prepararam-se micropartículas lipídicas e dispersões sólidas de ibuprofeno com cada um dos seguintes excipientes: álcool cetílico, ácido esteárico e óleo de rícino hidrogenado. Estas formulações tinham por finalidade melhorar as características físicas e mecânicas e prolongar a liberação deste fármaco. Foram, também, preparadas misturas físicas do ibuprofeno com os mesmos excipientes e nas mesmas proporções. As dispersões sólidas de ibuprofeno/ácido esteárico e as dispersões sólidas de ibuprofeno/óleo de rícino hidrogenado foram aquelas que apresentaram melhores características de escoamento comparativamente com o ibuprofeno puro. Por outro lado, foram preparadas cápsulas de gelatina com as diferentes micropartículas lipídicas e dispersões sólidas e submetidas a ensaios de dissolução com o objetivo de estudar a influência dos sistemas preparados nos perfis de liberação do ibuprofeno. A liberação prolongada do ibuprofeno foi conseguida nas diferentes micropartículas lipídicas e dispersões sólidas preparadas com os diferentes excipientes.