Rapidly absorbed orodispersible tablet containing molecularly dispersed felodipine for management of hypertensive crisis: Development, optimization andin vitro/in vivostudies

Abstract

A liquisolid orodispersible tablet of felodipine, a BCS Class II drug, was developed to improve drug dissolution and absorption through the buccal mucosa for management of hypertensive crisis. A 24 full-factorial design was applied to optimize felodipine liquisolid systems (FLSs) having acceptable flow properties and possessing enhanced drug dissolution rates. Four formulation variables; The liquid type, X1 (PG or PEG), drug concentration, X2 (10% and 20%), type of coat, X3 (Aerosil® and Aeroperl®) and excipients ratio, X4 (10 and 20) were included in the design. The systems were assessed for dissolution and flow properties. Following optimization, the formulation components (X1, X2, X3 and X4) were PEG, 10%, Aerosil® and 20, respectively. The optimized FLS was compressed into felodipine liquisolid orodispersible tablet using Prosolv® as carrier material (FLODT-2). The in vitro and in vivo disintegration times of FLODT-2 were 9 and 7 s, respectively. The in vivo pharmacokinetic study using human volunteers showed a significant increase in dissolution and absorption rates of the formulation of FLODT-2 compared to soft gelatin capsules filled with felodipine solution in PEG under the same conditions. Our results proposed that the optimized FLODT formulation could be promising to manage hypertensive crisis.

Supercritical impregnation of polymer matrices spatially confined in microcontainers for oral drug delivery: Effect of temperature, pressure and time

“…As a result, stabilization of amorphous forms is necessary in order to preserve the above-mentioned advantages [3]. amorphous form can be achieved by the addition of a polymeric carrier wherein the drug is confined in supramolecular domains or even molecularly dispersed [4]. Together with the solid state properties, the solubility and dissolution rate can be improved by reducing the particle size of the formulation [5].…”

Orally Disintegrating Tablets: General Overview and Quality by Design Approach: Review

“…Faktöriyel tasarım kullanımının majör yararı bütün tahmin edilen etki ve etkileşimlerin diğer faktörlerin etkisi ile bağımlı olduğunu göstermesidir. 60 Bunun için farklı çalışmalar yapılır. Bunlar; ADT'lerde CQA olan dağılma zamanı, sertlik, friabilite ve çözünme hızı üzerine dağıtıcı miktarı, türünün etkisi, dağılma süresi ve çözünme hızı üzerine kaydırıcı dü-zeyinin etkisi, tablet basım proçesinin CQA'lar üzerine etkisi ve kritik proçes parametrelerinin risk analizi olarak düşünülmektedir (Tablo 5).…”

Stress-Dependent Particle Interactions of Magnesium Aluminometasilicates as Their Performance Factor in Powder Flow and Compaction Applications

“…Colloidal silica (Aerosil ® , Cab-O-Sil ® ) belongs among ones exhibiting this characteristic [28,29]. Amorphous silica gel (Syloid ® , Sylysia ® ), granulated silicon dioxide (Aeroperl ® (Evonik Industries AG, North Rhine-Westphalia, Essen, Germany)), Silica Aerogel, calcium silicate (Florite ® (Tomita Pharmaceutical Co., Ltd., Tokushima, Japan)), and ordered mesoporous silicate can be also taken into consideration for application [30][31][32].…”