Design of Cáscara sagrada tablets by direct compression using spray dryed extract.

GALLO LOREANA; PORRAS MAURICIO; LLABOT JUAN MANUEL; BUCALÁ VERÓNICA; PIÑA JULIANA; ALLEMANDI DANIEL

Córdoba

Congreso; 1ª Reunión Internacional de Ciencias Farmacéuticas.; 2010

Dpto. Farmacia. Univ. Nac. de Córdoba.

Introduction. Pharmaceutical tablets are the principal dosage form for drug delivery, occuping two-thirds of the global market. Generally, direct compression (DC) is one of the most advantageous process for tablet manufacture; it offers several advantages such as simplicity, low processing time and power consumption. On the other hand, the DC primary limitations are good flow properties and compressibility requirements.In the case of phytomedicine tablets, the active component is a dry plant extract (DPE). Usually, DPE have poor flow properties and compactability and consequently they cannot be utilized for DC.Spray dryers are the most common technique used in the herbal processing induestries. One of the main reasons is the ability to generate a product with precise quality specifications in continuos operations. The most normally requiere product specifications are moisture content, flow properties and hygroscopicity. The goal of this study was to optimize the attaiment of a vegetal solid extract (SDE) with suitable flow and compression characteristics in order to develop tablets containg Cáscara sagrada solid extract as active component. The spray drying process was selected as method for the SDE attaiment and the composition of the tablet formulae was proposed. The pharmaceutical performance of the formulation was evaluted. Materials and methods. The extract was spray dry in a  Mini Spray Dryer Buchi B-290 utilizing colloidal silicon dioxide as drying aid. The most efficient experimental conditions for spray drying was previously determinated from a 2 ^ (5-1) fractional factorial design. Such conditions were: drying air inlet temperature 130º C, atomization air volumetric flow rate 400 l/h, feed volumetric flow rate 15% (expressed as % of the maximum pump rate) drying air volumetric flowrate 100% (given as maximun aspiration rate) and dispersion concentration 7.32% /w/w) with 1:1 colloidal silicon dioxide:solid residue ratio. The quantitative determination of the actives components (hydroxyanthracene derivatives and cascarosides) was assayed by spectrophotometric meansurements and High Performance Liquid Cromatography.Four solid pharamceutical formulations, containing the SDE and common excipients for DC, were formulated by means of a 2^2 factorial experimental design. Th fluidity and compressibility, hardness, friability, desintegration time and dissolution rate were evaluated. Results. The four formualtions presented good flow properties and acceptable hardness, friability and disintegration time. The dissolution test indicated, for some formulations, a rapid release of the active components. Two of the four formulations, one constituted by SDE (146 mg), Lactose CD (70 mg), Avicel PH 101 (70 mg), Acdisol (70 mg) and magnesium stearate (4 mg) and another containg SDE (146 mg), Lactose CD (70 mg), Emcompress (70 mg), Acdisol (70 mg) and magnesium stearate (4 mg) showed the best pharmaceutical performance. The presece of Acdisol lead to the lowest disintegration time and highets extract release. Conclusions. The spray dry technology allowed the production of a SDE with good flowability for the formulation of phytomedicine tablets by DC. The manufacture of tablets by a 2^2 factorial design was a strategy to evaluated the influence of different excipients and their proportions on the analyzed responses.